Ligand source activities (1 row/activity)



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 DOI
1185 10473 38 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
3038517 10473 38 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL22055 10473 38 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
DB06494 10473 38 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
1185 10473 38 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
3038517 10473 38 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
CHEMBL22055 10473 38 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
DB06494 10473 38 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
53386917 70293 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800156 70293 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53388960 70342 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 682 11 2 9 6.0 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800663 70342 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 682 11 2 9 6.0 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
11512905 145196 0 None 1778 2 Human 10.2 pIC50 = 10.2 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL377396 145196 0 None 1778 2 Human 10.2 pIC50 = 10.2 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
9961721 175258 0 None 60 2 Human 10.2 pIC50 = 10.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL435167 175258 0 None 60 2 Human 10.2 pIC50 = 10.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
53388958 70340 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 668 10 2 9 5.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800661 70340 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 668 10 2 9 5.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
18324807 70347 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800668 70347 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
20691661 86388 0 None 138 2 Human 10.0 pIC50 = 10 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211485 86388 0 None 138 2 Human 10.0 pIC50 = 10 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
10100930 70292 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800155 70292 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386915 70290 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800153 70290 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53389117 70345 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 688 11 2 9 4.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN2CCCC2=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800666 70345 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 688 11 2 9 4.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN2CCCC2=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53389115 70343 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 698 11 3 10 5.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2cccc(CO)n2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800664 70343 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 698 11 3 10 5.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2cccc(CO)n2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53387071 70294 5 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800157 70294 5 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
10371708 70295 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800158 70295 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53389118 70346 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 712 12 2 10 4.2 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN(C)S(C)(=O)=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800667 70346 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 712 12 2 10 4.2 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN(C)S(C)(=O)=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53386756 70348 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 617 13 2 10 3.6 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CCOC)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800669 70348 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 617 13 2 10 3.6 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CCOC)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
44293301 195284 0 None - 1 Rat 9.5 pIC50 = 9.5 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50283 195284 0 None - 1 Rat 9.5 pIC50 = 9.5 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
16221494 168731 0 None 8 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL415659 168731 0 None 8 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
10348973 10086 58 None -1 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 10086 58 None -1 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 10086 58 None -1 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 10086 58 None -1 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 10086 58 None -1 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
53386757 70349 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 631 14 2 10 4.0 CCOCCn1c(=O)c2c(CN(C)CCOC)c(-c3ccc(NC(=O)NOC)cc3)sc2n(Cc2c(F)cccc2F)c1=O 10.1021/jm200216q
CHEMBL1800670 70349 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 631 14 2 10 4.0 CCOCCn1c(=O)c2c(CN(C)CCOC)c(-c3ccc(NC(=O)NOC)cc3)sc2n(Cc2c(F)cccc2F)c1=O 10.1021/jm200216q
10100930 70292 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800155 70292 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386917 70293 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800156 70293 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
11421412 185520 15 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL468551 185520 15 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
11477988 97785 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
CHEMBL23969 97785 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
16155709 175254 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1661 42 17 19 1.7 CONC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL435141 175254 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1661 42 17 19 1.7 CONC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16155709 175254 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1661 42 17 19 1.7 CONC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL435141 175254 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1661 42 17 19 1.7 CONC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL262747 217325 9 None 1 2 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
101755083 8141 47 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
16136245 8141 47 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
4379 8141 47 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
5585 8141 47 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
CHEMBL415606 8141 47 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
DB06699 8141 47 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
101755083 8141 47 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
16136245 8141 47 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
4379 8141 47 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
5585 8141 47 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
CHEMBL415606 8141 47 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
DB06699 8141 47 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
44293163 195479 0 None - 1 Rat 9.2 pIC50 = 9.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50433 195479 0 None - 1 Rat 9.2 pIC50 = 9.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL407661 219454 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
11262242 195517 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 645 13 2 7 6.1 Cc1c(-c2cccc(OCCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL505033 195517 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 645 13 2 7 6.1 Cc1c(-c2cccc(OCCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
16221267 148780 0 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
CHEMBL387499 148780 0 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
23656390 168462 0 None 4 2 Rat 9.2 pIC50 = 9.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL413245 168462 0 None 4 2 Rat 9.2 pIC50 = 9.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
1184 10505 36 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of LHRH-stimulated arachidonic acid (AA) release from CHO cells expressing human Leutinizing releasing hormone receptorInhibition of LHRH-stimulated arachidonic acid (AA) release from CHO cells expressing human Leutinizing releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
9874838 10505 36 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of LHRH-stimulated arachidonic acid (AA) release from CHO cells expressing human Leutinizing releasing hormone receptorInhibition of LHRH-stimulated arachidonic acid (AA) release from CHO cells expressing human Leutinizing releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
CHEMBL71917 10505 36 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of LHRH-stimulated arachidonic acid (AA) release from CHO cells expressing human Leutinizing releasing hormone receptorInhibition of LHRH-stimulated arachidonic acid (AA) release from CHO cells expressing human Leutinizing releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
1184 10505 36 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
9874838 10505 36 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
CHEMBL71917 10505 36 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
CHEMBL407661 219454 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL262747 217325 9 None 1 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL262747 217325 9 None 1 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL434380 220433 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@@H](C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)cc1 10.1021/jm060240a
44395623 131435 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 551 7 3 8 5.3 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL364167 131435 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 551 7 3 8 5.3 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL434380 220433 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@@H](C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)cc1 10.1021/jm060240a
16221104 92333 0 None 6 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)Sc2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL227861 92333 0 None 6 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)Sc2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
87285768 177274 3 None 158 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assayAntagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 177274 3 None 158 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assayAntagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
22129998 108052 0 None - 1 Rat 9.1 pIC50 = 9.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL296321 108052 0 None - 1 Rat 9.1 pIC50 = 9.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
16156699 173345 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1647 41 18 19 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NO)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL427976 173345 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1647 41 18 19 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NO)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16221266 173138 0 None 2 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
CHEMBL427438 173138 0 None 2 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
44395435 130590 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 523 7 3 8 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL362371 130590 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 523 7 3 8 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
16221495 92298 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL227451 92298 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
16156699 173345 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1647 41 18 19 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NO)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL427976 173345 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1647 41 18 19 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NO)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
10348973 10086 58 None -1 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 10086 58 None -1 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 10086 58 None -1 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 10086 58 None -1 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 10086 58 None -1 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
9895596 70289 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800152 70289 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
16221556 175128 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1580 41 14 17 2.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@@H](C(N)=O)[S+](C)[O-])cc1 10.1021/jm0613931
CHEMBL434371 175128 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1580 41 14 17 2.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@@H](C(N)=O)[S+](C)[O-])cc1 10.1021/jm0613931
CHEMBL429527 220315 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NO)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
155531714 182970 0 None 501 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assayAntagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL4593521 182970 0 None 501 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assayAntagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL429527 220315 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NO)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16221496 149525 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1580 41 14 17 2.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C(N)=O)[S+](C)[O-])cc1 10.1021/jm0613931
CHEMBL389248 149525 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1580 41 14 17 2.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C(N)=O)[S+](C)[O-])cc1 10.1021/jm0613931
16156573 175655 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1747 48 17 20 2.2 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL438239 175655 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1747 48 17 20 2.2 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16156573 175655 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1747 48 17 20 2.2 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL438239 175655 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1747 48 17 20 2.2 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
10649568 21338 0 None 4 2 Human 9.1 pIC50 = 9.1 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL120432 21338 0 None 4 2 Human 9.1 pIC50 = 9.1 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL219061 216183 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL219061 216183 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
53387071 70294 5 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800157 70294 5 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
10371708 70295 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800158 70295 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
10649568 21338 0 None 4 2 Human 9.0 pIC50 = 9 Functional
Activity at human GnRH receptor by inositol phosphate functional assayActivity at human GnRH receptor by inositol phosphate functional assay
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm701249f
CHEMBL120432 21338 0 None 4 2 Human 9.0 pIC50 = 9 Functional
Activity at human GnRH receptor by inositol phosphate functional assayActivity at human GnRH receptor by inositol phosphate functional assay
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm701249f
53386916 70291 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 654 11 2 10 4.5 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(F)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800154 70291 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 654 11 2 10 4.5 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(F)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
10649568 21338 0 None 4 2 Human 9.0 pIC50 = 9 Functional
Functional antagonism at the human GnRH receptor (PI turnover)Functional antagonism at the human GnRH receptor (PI turnover)
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 21338 0 None 4 2 Human 9.0 pIC50 = 9 Functional
Functional antagonism at the human GnRH receptor (PI turnover)Functional antagonism at the human GnRH receptor (PI turnover)
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
44321052 213050 0 None - 1 Human 9.0 pIC50 = 9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 578 9 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(O)nc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86912 213050 0 None - 1 Human 9.0 pIC50 = 9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 578 9 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(O)nc2)c1 10.1016/s0960-894x(01)00512-1
16155593 165216 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1767 53 17 21 2.2 CONC(=O)NCCOCCOCCOCCC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL409044 165216 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1767 53 17 21 2.2 CONC(=O)NCCOCCOCCOCCC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16155593 165216 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1767 53 17 21 2.2 CONC(=O)NCCOCCOCCOCCC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL409044 165216 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1767 53 17 21 2.2 CONC(=O)NCCOCCOCCOCCC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL409043 219522 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL409043 219522 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16221433 148941 0 None 1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1548 40 13 16 4.7 CS[C@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
CHEMBL388369 148941 0 None 1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1548 40 13 16 4.7 CS[C@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
16221211 176041 0 None 2 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1566 40 14 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
CHEMBL441211 176041 0 None 2 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1566 40 14 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
44432651 93478 0 None 21 2 Rat 8.9 pIC50 = 8.9 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 632 9 3 4 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231760 93478 0 None 21 2 Rat 8.9 pIC50 = 8.9 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 632 9 3 4 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
53386915 70290 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800153 70290 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
44395650 176100 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 537 7 3 8 4.9 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL441676 176100 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 537 7 3 8 4.9 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL2105773 219520 8 None -1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
CHEMBL409018 219520 8 None -1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
16155157 103223 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1622 44 16 18 3.6 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL262180 103223 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1622 44 16 18 3.6 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398152 166994 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1675 42 17 20 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL410967 166994 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1675 42 17 20 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16155157 103223 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1622 44 16 18 3.6 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL262180 103223 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1622 44 16 18 3.6 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL2105773 219520 8 None -1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL409018 219520 8 None -1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
18324807 70347 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800668 70347 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL2105773 219520 8 None 1 2 Rat 8.9 pIC50 = 8.9 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
CHEMBL409018 219520 8 None 1 2 Rat 8.9 pIC50 = 8.9 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
44321964 103194 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL261979 103194 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
16156328 103427 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1592 43 16 17 3.4 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL263691 103427 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1592 43 16 17 3.4 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398047 103688 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1645 41 16 18 1.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL265879 103688 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1645 41 16 18 1.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16156328 103427 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1592 43 16 17 3.4 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL263691 103427 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1592 43 16 17 3.4 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL376654 219032 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)NCC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL376654 219032 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)NCC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398065 162492 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1671 41 17 18 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC1CCCCC1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL405273 162492 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1671 41 17 18 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC1CCCCC1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
11250647 8327 46 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
5293 8327 46 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
8362 8327 46 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
CHEMBL1208155 8327 46 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
DB11979 8327 46 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
44449120 102008 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL256109 102008 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL262747 217325 9 None -1 2 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
44380487 174358 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]ncc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL430069 174358 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]ncc3c2)c1 10.1016/s0960-894x(02)00026-4
23656390 168462 0 None -4 2 Human 8.8 pIC50 = 8.8 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL413245 168462 0 None -4 2 Human 8.8 pIC50 = 8.8 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL219562 216196 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=O)CNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL219562 216196 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=O)CNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
44398064 173789 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1647 40 17 20 -0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL428825 173789 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1647 40 17 20 -0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
145957953 168909 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 633 9 1 9 4.3 COc1ccccc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4161566 168909 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 633 9 1 9 4.3 COc1ccccc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
44398063 168588 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1661 41 17 20 0.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL414347 168588 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1661 41 17 20 0.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
58239302 168769 0 None 616 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 577 12 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(C)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4159247 168769 0 None 616 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 577 12 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(C)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44395462 175002 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 551 7 3 8 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL433594 175002 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 551 7 3 8 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
16155358 144914 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1778 49 18 21 1.9 CCOCCOCCNC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL376728 144914 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1778 49 18 21 1.9 CCOCCOCCNC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398043 168476 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1603 37 17 18 -0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(=O)NC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL413450 168476 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1603 37 17 18 -0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(=O)NC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16155358 144914 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1778 49 18 21 1.9 CCOCCOCCNC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL376728 144914 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1778 49 18 21 1.9 CCOCCOCCNC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
101755083 8141 47 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None None 10.1021/jm050134t
16136245 8141 47 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None None 10.1021/jm050134t
4379 8141 47 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None None 10.1021/jm050134t
5585 8141 47 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None None 10.1021/jm050134t
CHEMBL415606 8141 47 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None None 10.1021/jm050134t
DB06699 8141 47 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None None 10.1021/jm050134t
16156341 168510 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1929 63 17 25 2.5 CONC(=O)NCCOCCOCCOCCOCCOCCOCCC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)NOC)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL413688 168510 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1929 63 17 25 2.5 CONC(=O)NCCOCCOCCOCCOCCOCCOCCC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)NOC)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16156341 168510 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1929 63 17 25 2.5 CONC(=O)NCCOCCOCCOCCOCCOCCOCCC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)NOC)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL413688 168510 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1929 63 17 25 2.5 CONC(=O)NCCOCCOCCOCCOCCOCCOCCC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)NOC)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16155098 167444 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1656 43 19 19 0.1 CONC(=O)NCC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL411337 167444 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1656 43 19 19 0.1 CONC(=O)NCC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16155098 167444 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1656 43 19 19 0.1 CONC(=O)NCC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL411337 167444 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1656 43 19 19 0.1 CONC(=O)NCC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16221267 148780 0 None -2 2 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
CHEMBL387499 148780 0 None -2 2 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
16221266 173138 0 None -2 2 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
CHEMBL427438 173138 0 None -2 2 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
44398150 103476 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1617 40 17 18 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL264090 103476 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1617 40 17 18 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44398066 103921 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1701 41 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCNC(C(=O)O)C1CCCCC1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL267873 103921 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1701 41 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCNC(C(=O)O)C1CCCCC1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44398045 168745 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1715 40 19 20 -1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=O)[C@H]1CC(=O)NC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL415820 168745 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1715 40 19 20 -1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=O)[C@H]1CC(=O)NC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44293111 107995 0 None -5 2 Rat 8.7 pIC50 = 8.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295917 107995 0 None -5 2 Rat 8.7 pIC50 = 8.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44398151 168729 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1689 43 17 20 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL415595 168729 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1689 43 17 20 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44398046 168105 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1645 41 16 18 1.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N(C)[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL412500 168105 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1645 41 16 18 1.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N(C)[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
1185 10473 38 None -5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
3038517 10473 38 None -5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL22055 10473 38 None -5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
DB06494 10473 38 None -5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
44320921 113946 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 548 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL316362 113946 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 548 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44398135 103579 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1675 41 16 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CN(C)CCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL265020 103579 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1675 41 16 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CN(C)CCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44398001 175734 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1661 41 17 20 0.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CNCCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL438905 175734 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1661 41 17 20 0.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CNCCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
10004181 107863 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL294910 107863 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44292974 108172 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 544 7 4 5 7.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL297238 108172 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 544 7 4 5 7.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44460342 174701 0 None - 1 Human 8.0 pIC50 = 8 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 9 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL431402 174701 0 None - 1 Human 8.0 pIC50 = 8 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 9 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
16656823 135441 0 None - 1 Human 8.0 pIC50 = 8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 468 5 2 6 4.3 CC(C)(C(=O)c1ccc(Cl)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1)c1ccccc1 nan
CHEMBL3668011 135441 0 None - 1 Human 8.0 pIC50 = 8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 468 5 2 6 4.3 CC(C)(C(=O)c1ccc(Cl)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1)c1ccccc1 nan
11191675 70156 0 None - 1 Human 8.0 pIC50 = 8 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL179600 70156 0 None - 1 Human 8.0 pIC50 = 8 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL3085404 70156 0 None - 1 Human 8.0 pIC50 = 8 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
1185 10473 38 None -5 2 Human 8.0 pIC50 = 8 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
3038517 10473 38 None -5 2 Human 8.0 pIC50 = 8 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
CHEMBL22055 10473 38 None -5 2 Human 8.0 pIC50 = 8 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
DB06494 10473 38 None -5 2 Human 8.0 pIC50 = 8 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
44380317 175268 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL435262 175268 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
44359191 18978 0 None 173 2 Human 8.0 pIC50 = 8.0 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184298 18978 0 None 173 2 Human 8.0 pIC50 = 8.0 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL343396 18978 0 None 173 2 Human 8.0 pIC50 = 8.0 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44398121 103408 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1655 41 18 19 0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
77232195 103408 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1655 41 18 19 0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL263507 103408 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1655 41 18 19 0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16145131 166259 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1628 41 16 20 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)c3cc(O)nc(O)n3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361540 166259 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1628 41 16 20 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)c3cc(O)nc(O)n3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL410165 166259 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1628 41 16 20 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)c3cc(O)nc(O)n3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361888 148554 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL386105 148554 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL2369138 216376 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CNC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44380222 64369 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 614 10 2 5 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166778 64369 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 614 10 2 5 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
44293010 181026 0 None - 1 Rat 7.0 pIC50 = 7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 472 7 2 8 5.0 O=[N+]([O-])c1cccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL45490 181026 0 None - 1 Rat 7.0 pIC50 = 7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 472 7 2 8 5.0 O=[N+]([O-])c1cccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
1179 7748 36 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
9957278 7748 36 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
CHEMBL494803 7748 36 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
44434414 95301 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 709 14 3 9 4.6 C#CCNC(=O)CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCC)cc2)nc2n(Cc3c(F)cccc3F)cc(C(=O)OCC)c(=O)n12 10.1016/j.bmc.2007.04.065
CHEMBL235179 95301 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 709 14 3 9 4.6 C#CCNC(=O)CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCC)cc2)nc2n(Cc3c(F)cccc3F)cc(C(=O)OCC)c(=O)n12 10.1016/j.bmc.2007.04.065
44293594 108344 0 None -10 2 Rat 6.0 pIC50 = 6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298497 108344 0 None -10 2 Rat 6.0 pIC50 = 6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293349 190903 0 None - 1 Rat 6.0 pIC50 = 6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL48273 190903 0 None - 1 Rat 6.0 pIC50 = 6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
145993478 174099 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 602 8 3 9 4.4 CC(C)(C)OC(=O)N[C@@H](Cn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1)C(=O)O 10.1039/C7MD00320J
CHEMBL4294163 174099 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 602 8 3 9 4.4 CC(C)(C)OC(=O)N[C@@H](Cn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1)C(=O)O 10.1039/C7MD00320J
44577102 185305 0 None - 1 Human 5.0 pIC50 = 5 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 303 5 1 4 4.1 CCSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1021/jm701249f
CHEMBL466735 185305 0 None - 1 Human 5.0 pIC50 = 5 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 303 5 1 4 4.1 CCSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1021/jm701249f
118098039 135435 0 None - 1 Human 7.0 pIC50 = 7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 461 4 1 6 3.5 Cc1cccc(N(C)S(=O)(=O)c2ccc(Cl)c(-n3c(=O)[nH]c4sccc4c3=O)c2)c1 nan
CHEMBL3668005 135435 0 None - 1 Human 7.0 pIC50 = 7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 461 4 1 6 3.5 Cc1cccc(N(C)S(=O)(=O)c2ccc(Cl)c(-n3c(=O)[nH]c4sccc4c3=O)c2)c1 nan
44380681 65548 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 669 9 3 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(F)(F)F)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168726 65548 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 669 9 3 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(F)(F)F)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44341198 119835 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 620 10 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL331144 119835 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 620 10 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
145959547 169062 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 604 9 1 9 3.9 Cc1ccccc1C(N)Cn1c(=O)c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4164102 169062 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 604 9 1 9 3.9 Cc1ccccc1C(N)Cn1c(=O)c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
44359191 18978 0 None -173 2 Rat 6.0 pIC50 = 6.0 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184298 18978 0 None -173 2 Rat 6.0 pIC50 = 6.0 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL343396 18978 0 None -173 2 Rat 6.0 pIC50 = 6.0 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
11467552 179490 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium fluxAntagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium flux
ChEMBL 603 11 2 6 5.7 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL450471 179490 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium fluxAntagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium flux
ChEMBL 603 11 2 6 5.7 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44561397 196603 0 None 4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL516479 196603 0 None 4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44341197 115812 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 587 9 2 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C#N)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL321258 115812 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 587 9 2 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C#N)c2)c1 10.1016/s0960-894x(02)00751-5
44321394 113716 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 10 2 4 7.5 COc1ccc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)cn1 10.1016/s0960-894x(01)00512-1
CHEMBL314860 113716 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 10 2 4 7.5 COc1ccc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)cn1 10.1016/s0960-894x(01)00512-1
44395677 73512 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 565 7 2 8 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185738 73512 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 565 7 2 8 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44380538 65859 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 619 9 2 5 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3nsnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169620 65859 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 619 9 2 5 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3nsnc3c2)c1 10.1016/s0960-894x(02)00026-4
44380318 127157 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL353308 127157 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
44293151 107951 0 None 23 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 510 12 2 3 6.9 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C(C)C 10.1016/s0960-894x(01)00275-x
CHEMBL295595 107951 0 None 23 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 510 12 2 3 6.9 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C(C)C 10.1016/s0960-894x(01)00275-x
44432638 93559 0 None 10 2 Rat 7.0 pIC50 = 7.0 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 506 9 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232151 93559 0 None 10 2 Rat 7.0 pIC50 = 7.0 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 506 9 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
44451397 102678 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 856 16 4 10 5.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL259220 102678 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 856 16 4 10 5.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44444665 100976 0 None -2 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 8 1 5 6.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249772 100976 0 None -2 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 8 1 5 6.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44432638 93559 0 None -10 2 Human 6.0 pIC50 = 6.0 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 506 9 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232151 93559 0 None -10 2 Human 6.0 pIC50 = 6.0 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 506 9 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
10208964 73456 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 536 7 2 7 7.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCC2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185438 73456 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 536 7 2 7 7.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCC2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44444676 161717 0 None -1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 646 9 1 6 5.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(OCC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401080 161717 0 None -1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 646 9 1 6 5.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(OCC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44444628 101094 0 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 722 8 2 5 8.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250568 101094 0 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 722 8 2 5 8.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
44340929 120279 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 604 10 2 4 7.7 CC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL332049 120279 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 604 10 2 4 7.7 CC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
44293591 108373 0 None 1 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298700 108373 0 None 1 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44572286 187580 0 None -6 2 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475650 187580 0 None -6 2 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
11237922 72294 0 None 1 2 Human 6.9 pIC50 = 6.9 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1021/jm701249f
CHEMBL183066 72294 0 None 1 2 Human 6.9 pIC50 = 6.9 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1021/jm701249f
44293194 193214 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 14 3 4 6.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)C 10.1016/s0960-894x(01)00274-8
CHEMBL48763 193214 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 14 3 4 6.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)C 10.1016/s0960-894x(01)00274-8
44292919 107922 0 None -2 2 Human 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295376 107922 0 None -2 2 Human 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
25193798 176977 0 None 2 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 562 6 2 5 6.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL444509 176977 0 None 2 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 562 6 2 5 6.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44293802 108809 0 None -1 2 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 11 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL301802 108809 0 None -1 2 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 11 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293273 168871 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL416102 168871 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44293164 174610 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 482 11 3 3 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)NC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL430763 174610 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 482 11 3 3 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)NC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44321496 112740 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 657 13 2 5 6.3 CCS(=O)(=O)N1CCN(C(=O)C(C)(C)c2ccc3[nH]c(-c4cc(C)cc(C)c4)c([C@H](C)CNCCCCc4ccncc4)c3c2)CC1 10.1016/s0960-894x(01)00512-1
CHEMBL312995 112740 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 657 13 2 5 6.3 CCS(=O)(=O)N1CCN(C(=O)C(C)(C)c2ccc3[nH]c(-c4cc(C)cc(C)c4)c([C@H](C)CNCCCCc4ccncc4)c3c2)CC1 10.1016/s0960-894x(01)00512-1
145980339 173366 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 380 4 1 3 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCF)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4280124 173366 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 380 4 1 3 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCF)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
44359333 18402 0 None -151 2 Rat 5.9 pIC50 = 5.9 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180707 18402 0 None -151 2 Rat 5.9 pIC50 = 5.9 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138999 18402 0 None -151 2 Rat 5.9 pIC50 = 5.9 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44361524 175373 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1623 40 15 17 3.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL435925 175373 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1623 40 15 17 3.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
44444632 101095 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 622 7 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250569 101095 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 622 7 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
9895596 70289 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800152 70289 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
16221557 172795 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1546 41 15 17 1.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
CHEMBL425486 172795 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1546 41 15 17 1.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
44573276 194195 0 None 4 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 484 6 1 5 5.9 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)n1CC 10.1016/j.bmcl.2009.02.043
CHEMBL493731 194195 0 None 4 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 484 6 1 5 5.9 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)n1CC 10.1016/j.bmcl.2009.02.043
44321100 113870 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC(CC5)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL315909 113870 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC(CC5)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44380394 126726 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 601 9 3 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL349638 126726 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 601 9 3 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44398117 168744 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1649 43 19 19 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCNc1ncc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL415813 168744 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1649 43 19 19 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCNc1ncc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44358957 18916 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184158 18916 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL336039 18916 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293070 172874 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 15 3 4 7.0 CCN(CC)C(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL42592 172874 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 15 3 4 7.0 CCN(CC)C(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
18914248 194510 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 15 3 4 6.4 CCN(CC)C(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL49542 194510 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 15 3 4 6.4 CCN(CC)C(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293335 179406 0 None 1 2 Rat 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL449351 179406 0 None 1 2 Rat 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293195 192071 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL48592 192071 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44293165 108470 0 None -7 2 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 556 16 2 5 5.7 COCCN(CCOC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL299392 108470 0 None -7 2 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 556 16 2 5 5.7 COCCN(CCOC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44380212 64392 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166843 64392 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
44434437 157752 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1663 42 6 27 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL395826 157752 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1663 42 6 27 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44359254 18404 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 561 8 3 8 5.8 COc1nccc(NC(=O)c2cc3c(OCCC4CCCCN4)c(-c4cc(C)cc(C)c4)c(O)nc3cc2Cl)n1 10.1016/s0960-894x(00)00024-x
CHEMBL1180716 18404 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 561 8 3 8 5.8 COc1nccc(NC(=O)c2cc3c(OCCC4CCCCN4)c(-c4cc(C)cc(C)c4)c(O)nc3cc2Cl)n1 10.1016/s0960-894x(00)00024-x
CHEMBL139292 18404 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 561 8 3 8 5.8 COc1nccc(NC(=O)c2cc3c(OCCC4CCCCN4)c(-c4cc(C)cc(C)c4)c(O)nc3cc2Cl)n1 10.1016/s0960-894x(00)00024-x
44434412 168556 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1565 39 4 26 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL414045 168556 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1565 39 4 26 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44572236 178678 0 None 6 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL446978 178678 0 None 6 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
11496945 183254 0 None 17 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459659 183254 0 None 17 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
24825725 199406 0 None 7 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL521674 199406 0 None 7 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
44321510 113916 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 608 15 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL316159 113916 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 608 15 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
9983568 105758 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL279885 105758 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
44215053 192399 0 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48641 192399 0 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44359285 18399 0 None 17 2 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180695 18399 0 None 17 2 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138747 18399 0 None 17 2 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44572287 187582 0 None 9 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6cccnc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475660 187582 0 None 9 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6cccnc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44292990 107975 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 16 3 4 7.2 CCCN(CCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL295731 107975 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 16 3 4 7.2 CCCN(CCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293348 107268 0 None 1 2 Rat 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL290991 107268 0 None 1 2 Rat 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293487 108411 0 None -2 2 Rat 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL299006 108411 0 None -2 2 Rat 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
9936150 195515 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50500 195515 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
145952400 169514 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 608 9 1 9 3.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(CC(N)c2ccccc2F)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4171296 169514 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 608 9 1 9 3.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(CC(N)c2ccccc2F)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
145950534 169584 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 608 9 1 9 3.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(CC(N)c2cccc(F)c2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4172405 169584 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 608 9 1 9 3.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(CC(N)c2cccc(F)c2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
44293605 107950 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295591 107950 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
10209293 107979 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295791 107979 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
24825725 199406 0 None 7 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL521674 199406 0 None 7 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
12283 9103 17 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 508 7 2 8 3.5 COc1c(c(c(cc1)F)F)COc1c(cc(c(c1)n1c(=O)c2c(scc2[nH]c1=O)C(=O)O)F)OC nan
16656889 9103 17 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 508 7 2 8 3.5 COc1c(c(c(cc1)F)F)COc1c(cc(c(c1)n1c(=O)c2c(scc2[nH]c1=O)C(=O)O)F)OC nan
CHEMBL3668014 9103 17 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 508 7 2 8 3.5 COc1c(c(c(cc1)F)F)COc1c(cc(c(c1)n1c(=O)c2c(scc2[nH]c1=O)C(=O)O)F)OC nan
16656891 135444 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 522 9 2 8 3.5 COCCOc1ccc(F)c(F)c1COc1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
CHEMBL3668015 135444 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 522 9 2 8 3.5 COCCOc1ccc(F)c(F)c1COc1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
10438167 107959 0 None 15 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 578 12 2 3 8.6 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL295641 107959 0 None 15 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 578 12 2 3 8.6 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCCCC1 10.1016/s0960-894x(01)00275-x
44293803 195661 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50721 195661 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
20691661 86388 0 None 138 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing monkey LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing monkey LHRH receptor
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211485 86388 0 None 138 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing monkey LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing monkey LHRH receptor
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
145953549 169196 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 619 8 2 9 4.0 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4166067 169196 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 619 8 2 9 4.0 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
44293054 108272 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 603 14 3 5 6.8 CCOC(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL297927 108272 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 603 14 3 5 6.8 CCOC(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292919 107922 0 None 2 2 Rat 6.8 pIC50 = 6.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295376 107922 0 None 2 2 Rat 6.8 pIC50 = 6.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
15602808 14881 0 None -5 2 Rat 5.8 pIC50 = 5.8 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091580 14881 0 None -5 2 Rat 5.8 pIC50 = 5.8 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44561368 183593 0 None -42 2 Rat 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL460892 183593 0 None -42 2 Rat 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44434435 95337 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1575 36 6 25 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL235361 95337 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1575 36 6 25 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44572286 187580 0 None 6 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475650 187580 0 None 6 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44293222 182739 0 None 100 2 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138464 182739 0 None 100 2 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL45883 182739 0 None 100 2 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
9958318 97002 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23830 97002 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
44293348 107268 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL290991 107268 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44432653 93479 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 650 9 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cc4nn[nH]c4cc2F)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231761 93479 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 650 9 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cc4nn[nH]c4cc2F)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44380146 127055 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 627 10 2 4 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352565 127055 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 627 10 2 4 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
44293062 193486 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 461 6 2 6 5.7 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)cc3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL48853 193486 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 461 6 2 6 5.7 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)cc3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44577104 185525 0 None -7 2 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL468565 185525 0 None -7 2 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
145973813 169802 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 604 9 1 9 3.9 Cc1cccc(C(N)Cn2c(=O)c(N3CCN(Cc4cccc([N+](=O)[O-])c4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.ejmech.2017.12.095
CHEMBL4175816 169802 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 604 9 1 9 3.9 Cc1cccc(C(N)Cn2c(=O)c(N3CCN(Cc4cccc([N+](=O)[O-])c4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.ejmech.2017.12.095
44293053 108269 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 13 3 4 6.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL297918 108269 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 13 3 4 6.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293803 195661 0 None -1 2 Rat 6.8 pIC50 = 6.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50721 195661 0 None -1 2 Rat 6.8 pIC50 = 6.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293651 169893 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL417726 169893 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44432656 165937 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 645 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL409825 165937 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 645 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44444641 161748 0 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 601 7 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401212 161748 0 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 601 7 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67143420 169687 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4173938 169687 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
44359458 18919 0 None -15 2 Rat 6.8 pIC50 = 6.8 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184171 18919 0 None -15 2 Rat 6.8 pIC50 = 6.8 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL336884 18919 0 None -15 2 Rat 6.8 pIC50 = 6.8 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
145955260 169313 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 608 9 1 9 3.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccc(F)cc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4167957 169313 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 608 9 1 9 3.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccc(F)cc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
16656887 135442 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 504 6 2 7 4.8 COc1ccc(F)cc1C(C)(C)Sc1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
CHEMBL3668012 135442 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 504 6 2 7 4.8 COc1ccc(F)cc1C(C)(C)Sc1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
44380551 65532 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168649 65532 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
145955571 169438 0 None -131 2 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 721 13 2 9 5.2 Cc1cc(F)cc([C@H](Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)NCCCC(=O)O)c1 10.1016/j.ejmech.2017.12.095
CHEMBL4169891 169438 0 None -131 2 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 721 13 2 9 5.2 Cc1cc(F)cc([C@H](Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)NCCCC(=O)O)c1 10.1016/j.ejmech.2017.12.095
44293555 107987 0 None -141 2 Human 6.8 pIC50 = 6.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 574 11 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C4(C(=O)N5C6CCC5CC6)CCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295897 107987 0 None -141 2 Human 6.8 pIC50 = 6.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 574 11 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C4(C(=O)N5C6CCC5CC6)CCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44444649 161784 0 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 646 10 3 7 4.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(O)CN3CCNCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401418 161784 0 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 646 10 3 7 4.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(O)CN3CCNCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44398149 168073 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1621 40 18 19 0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL412212 168073 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1621 40 18 19 0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44293041 108117 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 455 6 2 6 5.7 Cc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
CHEMBL296819 108117 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 455 6 2 6 5.7 Cc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
44292833 108317 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 480 7 2 7 5.5 Cc1cc(CC#N)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL298278 108317 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 480 7 2 7 5.5 Cc1cc(CC#N)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44292733 183562 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 548 7 4 5 6.8 O=C(Nc1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)c(Cl)c3)c(O)nc2cc1Cl)NC1CC1 10.1016/s0960-894x(00)00318-8
CHEMBL46060 183562 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 548 7 4 5 6.8 O=C(Nc1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)c(Cl)c3)c(O)nc2cc1Cl)NC1CC1 10.1016/s0960-894x(00)00318-8
10348973 10086 58 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 10086 58 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 10086 58 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 10086 58 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 10086 58 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
44577104 185525 0 None 7 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL468565 185525 0 None 7 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
44293249 192222 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL48616 192222 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
10077523 129492 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 613 7 3 7 7.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL360429 129492 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 613 7 3 7 7.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44395463 133553 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 627 7 2 7 7.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL365366 133553 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 627 7 2 7 7.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44215055 108067 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 576 11 1 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(C)CCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL296442 108067 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 576 11 1 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(C)CCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293249 192222 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48616 192222 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
21899433 161481 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 631 8 1 6 5.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399772 161481 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 631 8 1 6 5.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44341081 174843 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 590 10 2 3 8.0 CCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL432450 174843 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 590 10 2 3 8.0 CCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
16656822 135440 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 455 4 2 6 3.4 CN(C(=O)c1ccc(Cl)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1)c1ccccc1 nan
CHEMBL3668010 135440 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 455 4 2 6 3.4 CN(C(=O)c1ccc(Cl)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1)c1ccccc1 nan
44359333 18402 0 None 151 2 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180707 18402 0 None 151 2 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138999 18402 0 None 151 2 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293347 169890 0 None 4 2 Rat 6.7 pIC50 = 6.7 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 11 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL417720 169890 0 None 4 2 Rat 6.7 pIC50 = 6.7 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 11 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293592 169669 0 None -4 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL417363 169669 0 None -4 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44434434 154852 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1531 33 6 24 8.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL393486 154852 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1531 33 6 24 8.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44434392 175777 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1389 27 4 22 9.4 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL439200 175777 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1389 27 4 22 9.4 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44444652 101277 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 588 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL251578 101277 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 588 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44293111 107995 0 None -5 2 Rat 5.7 pIC50 = 5.7 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295917 107995 0 None -5 2 Rat 5.7 pIC50 = 5.7 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44444642 101145 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 629 8 1 6 5.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250770 101145 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 629 8 1 6 5.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
58022100 135433 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 473 3 1 6 3.5 O=c1[nH]c2ccsc2c(=O)n1-c1cc(S(=O)(=O)N2CCCc3ccccc32)ccc1Cl nan
CHEMBL3668003 135433 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 473 3 1 6 3.5 O=c1[nH]c2ccsc2c(=O)n1-c1cc(S(=O)(=O)N2CCCc3ccccc32)ccc1Cl nan
138978203 173479 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 639 7 3 11 3.1 Cc1cn([C@H]2C[C@@H](n3cc(CN4CCN(c5cccc6[nH]c(-c7ccc(C(C)(C)C)cc7)nc56)CC4)nn3)[C@@H](CO)O2)c(=O)[nH]c1=O 10.1039/C7MD00320J
CHEMBL4282476 173479 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 639 7 3 11 3.1 Cc1cn([C@H]2C[C@@H](n3cc(CN4CCN(c5cccc6[nH]c(-c7ccc(C(C)(C)C)cc7)nc56)CC4)nn3)[C@@H](CO)O2)c(=O)[nH]c1=O 10.1039/C7MD00320J
145984647 173195 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 509 5 1 6 5.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6ccc(F)cc6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4277116 173195 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 509 5 1 6 5.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6ccc(F)cc6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
138978207 173932 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 372 3 1 3 4.3 C#CCN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1039/C7MD00320J
CHEMBL4290761 173932 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 372 3 1 3 4.3 C#CCN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1039/C7MD00320J
16657781 135436 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 517 4 2 7 3.2 O=C(O)c1scc2[nH]c(=O)n(-c3cc(S(=O)(=O)N4CCCc5ccccc54)ccc3Cl)c(=O)c12 nan
CHEMBL3668006 135436 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 517 4 2 7 3.2 O=C(O)c1scc2[nH]c(=O)n(-c3cc(S(=O)(=O)N4CCCc5ccccc54)ccc3Cl)c(=O)c12 nan
44380798 66100 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 3 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL170606 66100 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 3 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
44380537 103336 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL263004 103336 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL2371821 216908 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CN[C@H](C(=O)O)C1CCCCC1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL438629 220562 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NCCOCCOCC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL438629 220562 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NCCOCCOCC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL2371822 216909 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None C#C[C@H](NC(=O)[C@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16156049 103558 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1689 44 17 19 2.5 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL264781 103558 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1689 44 17 19 2.5 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16156049 103558 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1689 44 17 19 2.5 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL264781 103558 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1689 44 17 19 2.5 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
102090748 168586 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
16138575 168586 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL414344 168586 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
44395491 130628 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 531 7 3 7 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL362544 130628 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 531 7 3 7 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
10053165 190778 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL48192 190778 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44398044 162010 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1617 38 17 18 0.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)NC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL402683 162010 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1617 38 17 18 0.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)NC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16221433 148941 0 None -1 2 Rat 8.6 pIC50 = 8.6 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1548 40 13 16 4.7 CS[C@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
CHEMBL388369 148941 0 None -1 2 Rat 8.6 pIC50 = 8.6 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1548 40 13 16 4.7 CS[C@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
16221494 168731 0 None -8 2 Rat 8.6 pIC50 = 8.6 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL415659 168731 0 None -8 2 Rat 8.6 pIC50 = 8.6 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
9873212 64350 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166649 64350 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
10008768 65508 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168563 65508 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL268450 217534 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@H](Cc2ccc(NC(=O)NCCOCCOCC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL268450 217534 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@H](Cc2ccc(NC(=O)NCCOCCOCC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
11365653 180969 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 631 12 2 7 5.7 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL454774 180969 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 631 12 2 7 5.7 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44448991 162120 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL403234 162120 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL556355 162120 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
44320895 171041 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccnc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL421160 171041 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccnc2)c1 10.1016/s0960-894x(01)00512-1
44380626 65501 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 587 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168539 65501 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 587 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
16155654 172857 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 20 19 -0.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CCNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL425813 172857 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 20 19 -0.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CCNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16155654 172857 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 20 19 -0.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CCNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL425813 172857 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 20 19 -0.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CCNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398178 168608 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1660 43 18 19 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CNCc1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL414507 168608 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1660 43 18 19 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CNCc1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44361795 175277 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1574 40 15 18 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL435322 175277 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1574 40 15 18 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL269711 217580 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
21036877 180429 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 627 13 2 7 5.9 Cc1c(-c2cccc(OCCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL453441 180429 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 627 13 2 7 5.9 Cc1c(-c2cccc(OCCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
11167850 9518 28 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
1178 9518 28 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
1187 9518 28 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
CHEMBL179691 9518 28 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
44321101 103623 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL265288 103623 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
9960399 57316 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 603 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3nnnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL157412 57316 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 603 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3nnnc-3c2)c1 10.1016/s0960-894x(02)00026-4
44398040 175590 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1681 41 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL437672 175590 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1681 41 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL264779 217409 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL268813 217544 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL264779 217409 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL268813 217544 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44293195 192071 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL48592 192071 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
15602804 14853 0 None 70 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091209 14853 0 None 70 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44340928 16516 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 10 3 4 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL113432 16516 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 10 3 4 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
16656888 135443 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 488 5 2 7 3.3 CC(C)(c1ccccc1)S(=O)(=O)c1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
CHEMBL3668013 135443 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 488 5 2 7 3.3 CC(C)(c1ccccc1)S(=O)(=O)c1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
44293058 108770 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 483 6 2 6 6.4 CC(C)(C)c1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1 10.1016/s0960-894x(00)00318-8
CHEMBL301552 108770 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 483 6 2 6 6.4 CC(C)(C)c1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1 10.1016/s0960-894x(00)00318-8
24825725 199406 0 None -7 2 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL521674 199406 0 None -7 2 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
44293484 103491 0 None -64 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 604 12 1 3 8.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)C(C)C)c1 10.1016/s0960-894x(01)00275-x
CHEMBL264193 103491 0 None -64 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 604 12 1 3 8.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)C(C)C)c1 10.1016/s0960-894x(01)00275-x
44214069 108095 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 575 14 3 5 6.1 CCOC(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL296644 108095 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 575 14 3 5 6.1 CCOC(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
16221614 143326 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1562 41 15 18 0.8 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)S(=O)(=O)C(C)C)cc1 10.1021/jm0613931
CHEMBL373725 143326 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1562 41 15 18 0.8 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)S(=O)(=O)C(C)C)cc1 10.1021/jm0613931
44432646 154012 0 None 2 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 581 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCC2CCOCC2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL392843 154012 0 None 2 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 581 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCC2CCOCC2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44444639 161746 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 589 8 1 5 5.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N(C)C)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401193 161746 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 589 8 1 5 5.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N(C)C)CC2)c1 10.1016/j.bmcl.2007.09.099
44321498 213084 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL87099 213084 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44359471 18970 0 None 67 2 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184266 18970 0 None 67 2 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL341717 18970 0 None 67 2 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44444672 176181 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 8 1 5 6.4 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL442283 176181 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 8 1 5 6.4 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
44293074 194562 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 612 12 3 4 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49578 194562 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 612 12 3 4 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44561108 193209 0 None 4 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 468 3 2 4 4.8 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL487627 193209 0 None 4 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 468 3 2 4 4.8 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44444670 101254 0 None -6 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 7 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCCC(O)C3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL251388 101254 0 None -6 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 7 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCCC(O)C3)CC2)c1 10.1016/j.bmcl.2007.09.099
44444673 101058 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 644 8 1 5 6.8 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL250389 101058 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 644 8 1 5 6.8 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
145954439 169435 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 622 9 1 9 4.0 Cc1cc(F)cc([C@@H](N)Cn2c(=O)c(N3CCN(Cc4cccc([N+](=O)[O-])c4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.ejmech.2017.12.095
CHEMBL4169864 169435 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 622 9 1 9 4.0 Cc1cc(F)cc([C@@H](N)Cn2c(=O)c(N3CCN(Cc4cccc([N+](=O)[O-])c4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.ejmech.2017.12.095
44341046 16848 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 634 11 2 5 7.5 CC(=O)OCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL115365 16848 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 634 11 2 5 7.5 CC(=O)OCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
44359301 18408 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nncs4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180754 18408 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nncs4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL141221 18408 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nncs4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293488 108331 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL298366 108331 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293335 179406 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL449351 179406 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44432657 156246 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 635 10 3 3 7.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(C(=O)O)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL394613 156246 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 635 10 3 3 7.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(C(=O)O)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44398396 168702 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1737 44 17 20 2.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCN(c1ccccn1)c1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL415328 168702 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1737 44 17 20 2.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCN(c1ccccn1)c1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
9845762 193605 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 433 6 2 7 5.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccs3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL48938 193605 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 433 6 2 7 5.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccs3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44444675 161501 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)C(C)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399857 161501 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)C(C)C2)c1 10.1016/j.bmcl.2007.09.099
44321497 104869 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 665 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCN(C(=O)OC(C)(C)C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL273390 104869 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 665 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCN(C(=O)OC(C)(C)C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44293076 108598 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 600 12 3 4 6.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL300268 108598 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 600 12 3 4 6.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293222 182739 0 None -100 2 Rat 5.7 pIC50 = 5.7 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138464 182739 0 None -100 2 Rat 5.7 pIC50 = 5.7 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL45883 182739 0 None -100 2 Rat 5.7 pIC50 = 5.7 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293126 169095 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 467 6 2 7 5.8 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)s3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL416459 169095 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 467 6 2 7 5.8 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)s3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44292747 194719 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 494 7 4 5 5.8 Cc1cccc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL49695 194719 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 494 7 4 5 5.8 Cc1cccc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44587394 179252 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 599 11 2 7 5.1 Cc1c(-c2cccc(OCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL448253 179252 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 599 11 2 7 5.1 Cc1c(-c2cccc(OCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44573110 193973 0 None 2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 442 4 1 5 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL492327 193973 0 None 2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 442 4 1 5 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
71449058 91181 0 None -10 2 Rat 7.6 pIC50 = 7.6 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2111955 91181 0 None -10 2 Rat 7.6 pIC50 = 7.6 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2219718 91181 0 None -10 2 Rat 7.6 pIC50 = 7.6 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
25193700 180061 0 None 7 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 534 7 2 5 5.9 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL452547 180061 0 None 7 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 534 7 2 5 5.9 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44293163 195479 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50433 195479 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44444668 161058 0 None -2 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 7 1 6 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL398648 161058 0 None -2 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 7 1 6 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44434389 175683 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 838 21 2 14 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL438504 175683 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 838 21 2 14 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44292661 108566 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 495 6 2 6 6.4 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cc(Cl)cc(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL300048 108566 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 495 6 2 6 6.4 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cc(Cl)cc(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44561369 197247 0 None 15 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL517881 197247 0 None 15 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44341082 16549 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 590 9 2 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)nc(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL113574 16549 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 590 9 2 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)nc(C)c2)c1 10.1016/s0960-894x(02)00751-5
11620431 186148 0 None -21 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL473807 186148 0 None -21 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
11496945 183254 0 None -17 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459659 183254 0 None -17 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
10258659 18971 0 None -46 2 Rat 6.6 pIC50 = 6.6 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184268 18971 0 None -46 2 Rat 6.6 pIC50 = 6.6 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL341809 18971 0 None -46 2 Rat 6.6 pIC50 = 6.6 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293208 177922 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 16 3 4 7.2 CCCCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL445848 177922 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 16 3 4 7.2 CCCCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292940 108041 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296244 108041 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293511 108063 0 None 3 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296426 108063 0 None 3 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44293377 108680 0 None 2 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 576 12 2 3 7.8 CCC(C)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL300865 108680 0 None 2 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 576 12 2 3 7.8 CCC(C)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293236 181658 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 560 13 4 4 5.7 CCNC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL45639 181658 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 560 13 4 4 5.7 CCNC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
54584354 68029 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at GnRH receptor by GnRHAntagonist activity at GnRH receptor by GnRH
ChEMBL 515 7 2 6 6.1 Cc1cc(C)cc(-c2cnc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766108 68029 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at GnRH receptor by GnRHAntagonist activity at GnRH receptor by GnRH
ChEMBL 515 7 2 6 6.1 Cc1cc(C)cc(-c2cnc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
44293112 194074 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cncnc4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL49293 194074 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cncnc4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
16221434 103962 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1548 40 13 16 4.7 CS[C@@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
CHEMBL268297 103962 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1548 40 13 16 4.7 CS[C@@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
44593424 182912 0 None -4 2 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL459215 182912 0 None -4 2 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44593424 182912 0 None -4 2 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459215 182912 0 None -4 2 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44341199 119836 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 620 10 2 5 7.2 COC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL331145 119836 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 620 10 2 5 7.2 COC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
44398119 104034 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1646 41 18 19 -0.4 CNC(=O)C[C@H](NC(=O)[C@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL268829 104034 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1646 41 18 19 -0.4 CNC(=O)C[C@H](NC(=O)[C@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44359252 18403 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 571 8 3 7 6.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C5CC5)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180715 18403 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 571 8 3 7 6.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C5CC5)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL139291 18403 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 571 8 3 7 6.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C5CC5)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44432628 94530 0 None 13 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 484 8 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2CCCC2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL233762 94530 0 None 13 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 484 8 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2CCCC2)CC3)c1 10.1016/j.bmcl.2007.05.009
44448991 162120 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL403234 162120 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL556355 162120 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
44293223 181080 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 545 8 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(CC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL45501 181080 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 545 8 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(CC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44434387 159554 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 750 15 2 12 5.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL397360 159554 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 750 15 2 12 5.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44587393 179413 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 613 12 2 7 5.5 Cc1c(-c2cccc(OCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL449468 179413 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 613 12 2 7 5.5 Cc1c(-c2cccc(OCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44341164 16336 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2C)c1 10.1016/s0960-894x(02)00751-5
CHEMBL112378 16336 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2C)c1 10.1016/s0960-894x(02)00751-5
44432651 93478 0 None -21 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 632 9 3 4 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231760 93478 0 None -21 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 632 9 3 4 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
15602805 14879 0 None -11 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
CHEMBL1091579 14879 0 None -11 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
44293376 108452 0 None 1 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 590 13 2 3 8.2 CCC(CC)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL299301 108452 0 None 1 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 590 13 2 3 8.2 CCC(CC)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293594 108344 0 None 10 2 Human 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298497 108344 0 None 10 2 Human 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293131 195618 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 520 10 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50663 195618 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 520 10 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293650 169108 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL416470 169108 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44432641 174282 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 540 9 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2Cl)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL429976 174282 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 540 9 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2Cl)CC3)c1 10.1016/j.bmcl.2007.05.009
44292878 181749 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 441 6 2 6 5.4 Cc1cccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL45661 181749 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 441 6 2 6 5.4 Cc1cccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
25156400 195638 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 581 12 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL506877 195638 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 581 12 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
11214860 91546 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
CHEMBL22314 91546 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
44380483 65849 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 635 9 4 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2F)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169569 65849 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 635 9 4 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2F)c1 10.1016/s0960-894x(02)00026-4
44292835 188034 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 526 10 2 7 6.2 CCN(CC)Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL47618 188034 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 526 10 2 7 6.2 CCN(CC)Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
1185 10473 38 None -5 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
3038517 10473 38 None -5 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL22055 10473 38 None -5 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
DB06494 10473 38 None -5 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
18914272 176460 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 588 14 3 4 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL443768 176460 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 588 14 3 4 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44432640 161752 0 None 1 2 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 524 9 2 3 5.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL401226 161752 0 None 1 2 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 524 9 2 3 5.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2F)CC3)c1 10.1016/j.bmcl.2007.05.009
16656819 135438 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 530 4 2 7 2.9 CNC(=O)c1scc2[nH]c(=O)n(-c3cc(S(=O)(=O)N4CCCc5ccccc54)ccc3Cl)c(=O)c12 nan
CHEMBL3668008 135438 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 530 4 2 7 2.9 CNC(=O)c1scc2[nH]c(=O)n(-c3cc(S(=O)(=O)N4CCCc5ccccc54)ccc3Cl)c(=O)c12 nan
145949496 169637 0 None -165 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 685 13 2 9 4.9 Cc1cccc(F)c1Cn1c(C)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4173065 169637 0 None -165 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 685 13 2 9 4.9 Cc1cccc(F)c1Cn1c(C)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.ejmech.2017.12.095
11496610 10847 13 None 8 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
5582 10847 13 None 8 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
CHEMBL474991 10847 13 None 8 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
11496610 10847 13 None 8 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
5582 10847 13 None 8 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
CHEMBL474991 10847 13 None 8 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
44432653 93479 0 None -1 2 Rat 7.6 pIC50 = 7.6 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 650 9 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cc4nn[nH]c4cc2F)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231761 93479 0 None -1 2 Rat 7.6 pIC50 = 7.6 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 650 9 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cc4nn[nH]c4cc2F)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44444647 161780 0 None -1 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 688 10 2 7 4.6 CC(=O)N1CCN(CC(O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL401352 161780 0 None -1 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 688 10 2 7 4.6 CC(=O)N1CCN(CC(O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
44432640 161752 0 None -1 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 524 9 2 3 5.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL401226 161752 0 None -1 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 524 9 2 3 5.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2F)CC3)c1 10.1016/j.bmcl.2007.05.009
25194090 195707 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 484 6 3 5 5.3 Cc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL507973 195707 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 484 6 3 5 5.3 Cc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44292983 108013 0 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 495 6 2 6 6.4 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)c(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL296084 108013 0 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 495 6 2 6 6.4 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)c(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44444635 161483 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 637 7 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399779 161483 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 637 7 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
16656821 135439 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 474 6 2 7 3.9 COc1cccc(F)c1C(C)Oc1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
CHEMBL3668009 135439 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 474 6 2 7 3.9 COc1cccc(F)c1C(C)Oc1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
16656892 135446 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 491 6 2 7 3.5 COc1cc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)cc1CN(C)c1c(F)cccc1F nan
CHEMBL3668017 135446 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 491 6 2 7 3.5 COc1cc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)cc1CN(C)c1c(F)cccc1F nan
44293305 108238 0 None 1 2 Rat 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL297703 108238 0 None 1 2 Rat 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
10032223 18975 0 None -81 2 Rat 6.5 pIC50 = 6.5 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184284 18975 0 None -81 2 Rat 6.5 pIC50 = 6.5 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL342822 18975 0 None -81 2 Rat 6.5 pIC50 = 6.5 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
16146022 176898 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1631 41 17 18 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL444381 176898 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1631 41 17 18 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
9918188 161500 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 708 8 2 5 8.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399856 161500 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 708 8 2 5 8.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
44444626 161662 0 None -1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 680 7 2 5 7.6 COC(=O)/N=C(/NC[C@@H](C)c1c(-c2cc(C)cc(C)c2)[nH]c2sc(C(C)(C)C(=O)N3C4CCC3CC4)cc12)N1CCC(c2ccncc2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL400739 161662 0 None -1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 680 7 2 5 7.6 COC(=O)/N=C(/NC[C@@H](C)c1c(-c2cc(C)cc(C)c2)[nH]c2sc(C(C)(C)C(=O)N3C4CCC3CC4)cc12)N1CCC(c2ccncc2)C1 10.1016/j.bmcl.2007.09.099
16221212 173110 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1566 40 14 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
CHEMBL427269 173110 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1566 40 14 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
145954419 169408 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 651 9 1 9 4.4 COc1ccc(F)cc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4169486 169408 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 651 9 1 9 4.4 COc1ccc(F)cc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
16156517 167506 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 19 19 -0.3 CONC(=O)NC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL411381 167506 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 19 19 -0.3 CONC(=O)NC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL219532 216195 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16156517 167506 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 19 19 -0.3 CONC(=O)NC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL411381 167506 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 19 19 -0.3 CONC(=O)NC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL219532 216195 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
54582417 68027 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at GnRH receptor by GnRHAntagonist activity at GnRH receptor by GnRH
ChEMBL 488 6 2 5 5.8 Cc1cc(C)cc(-c2c(OCCC3CCCCN3)c3cc(-c4ccncn4)c(Cl)cc3[nH]c2=O)c1 10.1021/jm101501b
CHEMBL1766106 68027 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at GnRH receptor by GnRHAntagonist activity at GnRH receptor by GnRH
ChEMBL 488 6 2 5 5.8 Cc1cc(C)cc(-c2c(OCCC3CCCCN3)c3cc(-c4ccncn4)c(Cl)cc3[nH]c2=O)c1 10.1021/jm101501b
25156943 195216 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 597 12 2 7 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL502341 195216 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 597 12 2 7 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
16221211 176041 0 None -2 2 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1566 40 14 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
CHEMBL441211 176041 0 None -2 2 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1566 40 14 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
CHEMBL2370890 216724 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](CCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
44449681 102820 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 551 8 1 6 5.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL259906 102820 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 551 8 1 6 5.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
9872676 84970 0 None 2 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human recombinant GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulationAntagonist activity at human recombinant GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulation
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
CHEMBL210514 84970 0 None 2 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human recombinant GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulationAntagonist activity at human recombinant GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulation
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
9893269 73070 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 532 7 2 7 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL184819 73070 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 532 7 2 7 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
16155218 173601 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1628 41 20 19 -0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL428484 173601 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1628 41 20 19 -0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16155218 173601 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1628 41 20 19 -0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL428484 173601 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1628 41 20 19 -0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398182 168725 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1635 42 19 19 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CNc1ncc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL415549 168725 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1635 42 19 19 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CNc1ncc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
1188 7007 48 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
16131215 7007 48 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
35 7007 48 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
CHEMBL1252 7007 48 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
DB00106 7007 48 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
CHEMBL1251 215440 27 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC/N=C(\NCC)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCN/C(=N/CC)NCC)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL5314377 215440 27 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC/N=C(\NCC)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCN/C(=N/CC)NCC)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
44398179 168587 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1674 44 18 19 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCNCc1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL414346 168587 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1674 44 18 19 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCNCc1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44321963 112718 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 622 11 2 5 6.8 COCn1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccc1=O 10.1016/s0960-894x(01)00512-1
CHEMBL312864 112718 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 622 11 2 5 6.8 COCn1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccc1=O 10.1016/s0960-894x(01)00512-1
44380536 127169 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 602 9 2 4 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL353395 127169 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 602 9 2 4 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
44293378 108670 0 None -37 2 Human 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 618 13 1 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)CC(C)C)c1 10.1016/s0960-894x(01)00275-x
CHEMBL300792 108670 0 None -37 2 Human 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 618 13 1 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)CC(C)C)c1 10.1016/s0960-894x(01)00275-x
10985312 85521 0 None 91 2 Human 6.5 pIC50 = 6.5 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21126 85521 0 None 91 2 Human 6.5 pIC50 = 6.5 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44434390 158422 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 882 24 2 15 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL396385 158422 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 882 24 2 15 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44434438 152973 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1707 45 6 28 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL392008 152973 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1707 45 6 28 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44321458 112742 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 658 11 2 3 9.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCCC5C5CCCCC54)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL313004 112742 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 658 11 2 3 9.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCCC5C5CCCCC54)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44380192 64221 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL165534 64221 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
44434402 153529 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1433 30 4 23 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL392433 153529 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1433 30 4 23 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
145958075 169091 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 10 1 10 3.7 COc1ccc(F)cc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4164522 169091 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 10 1 10 3.7 COc1ccc(F)cc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
10258643 108160 0 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 644 16 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL297151 108160 0 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 644 16 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44395502 172677 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 553 7 3 9 5.0 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2COCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL424991 172677 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 553 7 3 9 5.0 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2COCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44432647 93515 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 622 9 2 4 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(=O)n(C)c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231954 93515 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 622 9 2 4 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(=O)n(C)c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
11496610 10847 13 None -8 2 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
5582 10847 13 None -8 2 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
CHEMBL474991 10847 13 None -8 2 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
44292838 108294 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 574 13 3 4 5.6 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL298074 108294 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 574 13 3 4 5.6 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44359264 18400 0 None 11 2 Human 7.5 pIC50 = 7.5 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180700 18400 0 None 11 2 Human 7.5 pIC50 = 7.5 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138866 18400 0 None 11 2 Human 7.5 pIC50 = 7.5 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44292974 108172 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 544 7 4 5 7.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL297238 108172 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 544 7 4 5 7.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44380796 65977 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 598 9 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL170159 65977 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 598 9 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
44293804 108576 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Compound tested for the inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsCompound tested for the inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL300095 108576 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Compound tested for the inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsCompound tested for the inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44214098 108071 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL296483 108071 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
15602807 14992 0 None -8 2 Rat 5.5 pIC50 = 5.5 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1092245 14992 0 None -8 2 Rat 5.5 pIC50 = 5.5 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44561141 200581 0 None 37 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 432 3 3 4 4.4 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL527422 200581 0 None 37 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 432 3 3 4 4.4 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44577069 185495 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3ccccc3OC)ccc2n1Cc1ccccc1 10.1021/jm701249f
CHEMBL468348 185495 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3ccccc3OC)ccc2n1Cc1ccccc1 10.1021/jm701249f
44432628 94530 0 None -13 2 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 484 8 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2CCCC2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL233762 94530 0 None -13 2 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 484 8 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2CCCC2)CC3)c1 10.1016/j.bmcl.2007.05.009
10649568 21338 0 None 4 2 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism at gonadotropin-releasing hormone receptor in dog (PI turnover)Functional antagonism at gonadotropin-releasing hormone receptor in dog (PI turnover)
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 21338 0 None 4 2 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism at gonadotropin-releasing hormone receptor in dog (PI turnover)Functional antagonism at gonadotropin-releasing hormone receptor in dog (PI turnover)
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
44293130 188671 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 482 11 3 3 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(N)=O)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL47791 188671 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 482 11 3 3 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(N)=O)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44434411 153531 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1521 36 4 25 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL392434 153531 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1521 36 4 25 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44444678 161718 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 618 12 1 5 7.3 CCN(CC)CCOC1CCN(CCc2c(-c3cc(C)cc(C)c3)[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc23)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL401081 161718 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 618 12 1 5 7.3 CCN(CC)CCOC1CCN(CCc2c(-c3cc(C)cc(C)c3)[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc23)CC1 10.1016/j.bmcl.2007.09.099
44293085 105091 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 461 6 2 6 5.7 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccccc3Cl)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL274952 105091 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 461 6 2 6 5.7 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccccc3Cl)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
11496610 10847 13 None -8 2 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
5582 10847 13 None -8 2 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
CHEMBL474991 10847 13 None -8 2 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
44359456 18976 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 572 8 3 6 7.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccc(N(C)C)cc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184286 18976 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 572 8 3 6 7.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccc(N(C)C)cc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL342908 18976 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 572 8 3 6 7.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccc(N(C)C)cc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293617 195454 0 None -23 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50380 195454 0 None -23 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293134 194180 0 None 1 2 Rat 5.4 pIC50 = 5.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49366 194180 0 None 1 2 Rat 5.4 pIC50 = 5.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44434388 96579 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 794 18 2 13 5.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL237729 96579 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 794 18 2 13 5.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44341186 16816 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 10 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(=O)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL115192 16816 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 10 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(=O)O)c2)c1 10.1016/s0960-894x(02)00751-5
22129998 108052 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL296321 108052 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
11477970 96274 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
CHEMBL23729 96274 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
44293377 108680 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 576 12 2 3 7.8 CCC(C)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL300865 108680 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 576 12 2 3 7.8 CCC(C)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293802 108809 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 11 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL301802 108809 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 11 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
145957253 168973 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 737 14 2 10 4.9 COc1ccc(F)cc1[C@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O)NCCCC(=O)O 10.1016/j.ejmech.2017.12.095
CHEMBL4162619 168973 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 737 14 2 10 4.9 COc1ccc(F)cc1[C@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O)NCCCC(=O)O 10.1016/j.ejmech.2017.12.095
44292888 181557 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 567 14 3 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45614 181557 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 567 14 3 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292918 178194 0 None 1 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL44627 178194 0 None 1 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44215908 101004 0 None -4 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 616 7 1 5 6.1 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249982 101004 0 None -4 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 616 7 1 5 6.1 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
16221329 143325 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1562 41 15 18 0.8 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)S(=O)(=O)C(C)C)cc1 10.1021/jm0613931
CHEMBL373724 143325 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1562 41 15 18 0.8 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)S(=O)(=O)C(C)C)cc1 10.1021/jm0613931
44449120 102008 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL256109 102008 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
16221613 173773 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1530 41 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL428795 173773 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1530 41 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
15602808 14881 0 None 5 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091580 14881 0 None 5 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44321146 113182 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC(C)(C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL313946 113182 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC(C)(C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44593425 183544 0 None 12 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
CHEMBL460480 183544 0 None 12 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
44593425 183544 0 None 12 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2009.02.043
CHEMBL460480 183544 0 None 12 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2009.02.043
44321410 113785 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL315325 113785 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321393 213049 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 606 9 2 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)c(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86911 213049 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 606 9 2 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)c(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
11226531 106296 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
CHEMBL283381 106296 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
10985312 85521 0 None 91 2 Human 8.4 pIC50 = 8.4 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21126 85521 0 None 91 2 Human 8.4 pIC50 = 8.4 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
16156639 144789 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1648 47 16 17 5.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL376466 144789 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1648 47 16 17 5.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16156639 144789 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1648 47 16 17 5.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL376466 144789 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1648 47 16 17 5.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
1190 7669 47 None 6025 3 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
25074887 7669 47 None 6025 3 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
583 7669 47 None 6025 3 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
CHEMBL1200490 7669 47 None 6025 3 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
DB00050 7669 47 None 6025 3 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
44398180 162806 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1696 42 18 19 2.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CNc1ccc2ccccc2n1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL406225 162806 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1696 42 18 19 2.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CNc1ccc2ccccc2n1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16147767 104134 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL269516 104134 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16221104 92333 0 None -6 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)Sc2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL227861 92333 0 None -6 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)Sc2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
44380625 65500 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168538 65500 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
9894997 127092 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352806 127092 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
16155412 167944 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1864 55 18 22 2.4 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL411749 167944 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1864 55 18 22 2.4 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16155412 167944 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1864 55 18 22 2.4 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL411749 167944 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1864 55 18 22 2.4 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16221150 168714 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 40 13 16 3.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)[S+](C)[O-])C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL415432 168714 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 40 13 16 3.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)[S+](C)[O-])C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
9938925 64365 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 616 11 3 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166763 64365 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 616 11 3 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
44380478 65529 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168637 65529 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
145955571 169438 0 None 131 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 721 13 2 9 5.2 Cc1cc(F)cc([C@H](Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)NCCCC(=O)O)c1 10.1016/j.ejmech.2017.12.095
CHEMBL4169891 169438 0 None 131 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 721 13 2 9 5.2 Cc1cc(F)cc([C@H](Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)NCCCC(=O)O)c1 10.1016/j.ejmech.2017.12.095
11331001 195801 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium fluxAntagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium flux
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL509075 195801 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium fluxAntagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium flux
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
16156572 173892 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1678 48 16 18 5.2 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL429016 173892 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1678 48 16 18 5.2 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
22130002 183481 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 505 6 2 6 5.8 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccc(Br)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL45990 183481 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 505 6 2 6 5.8 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccc(Br)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44292829 183658 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 471 7 2 7 5.4 COc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
CHEMBL46157 183658 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 471 7 2 7 5.4 COc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
44292621 183793 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 461 6 2 6 5.7 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccc(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL46288 183793 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 461 6 2 6 5.7 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccc(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
9959121 195138 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50120 195138 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
21254089 188436 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47761 188436 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293376 108452 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 590 13 2 3 8.2 CCC(CC)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL299301 108452 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 590 13 2 3 8.2 CCC(CC)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44292984 184180 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 455 6 2 6 5.7 Cc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c(C)c1 10.1016/s0960-894x(00)00318-8
CHEMBL46383 184180 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 455 6 2 6 5.7 Cc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c(C)c1 10.1016/s0960-894x(00)00318-8
11583756 196433 0 None 31 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL515123 196433 0 None 31 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
21254068 108565 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 12 3 5 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL300045 108565 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 12 3 5 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293488 108331 0 None -1 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL298366 108331 0 None -1 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293592 169669 0 None 4 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL417363 169669 0 None 4 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44293148 194265 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 524 12 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49412 194265 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 524 12 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
11532637 14486 0 None 4 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL1088866 14486 0 None 4 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
44561397 196603 0 None -4 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL516479 196603 0 None -4 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44292608 185168 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 427 6 2 6 5.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccccc3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL46550 185168 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 427 6 2 6 5.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccccc3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44577103 185524 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 530 10 4 9 4.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(O)NC)c21 10.1021/jm701249f
CHEMBL468564 185524 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 530 10 4 9 4.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(O)NC)c21 10.1021/jm701249f
44432645 93977 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 487 5 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CN)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232752 93977 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 487 5 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CN)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
16048665 135445 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 508 7 2 8 3.5 COc1cc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)cc1COc1c(OC)ccc(F)c1F nan
CHEMBL3668016 135445 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 508 7 2 8 3.5 COc1cc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)cc1COc1c(OC)ccc(F)c1F nan
18914263 103676 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 630 15 3 4 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL265774 103676 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 630 15 3 4 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
11532637 14486 0 None -4 2 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL1088866 14486 0 None -4 2 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
44380192 64221 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL165534 64221 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
11634198 194145 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
CHEMBL493344 194145 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
44380624 65912 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 587 8 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169873 65912 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 587 8 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
44293274 108033 0 None -9 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 12 1 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCN(C)CCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296199 108033 0 None -9 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 12 1 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCN(C)CCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
11604354 194303 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 428 4 2 4 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c[nH]1 10.1016/j.bmcl.2009.02.043
CHEMBL494400 194303 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 428 4 2 4 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c[nH]1 10.1016/j.bmcl.2009.02.043
44572235 196286 0 None -5 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
CHEMBL513998 196286 0 None -5 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
44359458 18919 0 None 15 2 Human 7.4 pIC50 = 7.4 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184171 18919 0 None 15 2 Human 7.4 pIC50 = 7.4 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL336884 18919 0 None 15 2 Human 7.4 pIC50 = 7.4 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44432654 166574 0 None -6 2 Rat 7.4 pIC50 = 7.4 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 660 10 3 6 6.1 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)nc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL410547 166574 0 None -6 2 Rat 7.4 pIC50 = 7.4 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 660 10 3 6 6.1 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)nc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44451342 103240 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 898 20 4 10 6.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL262334 103240 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 898 20 4 10 6.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
15602804 14853 0 None -70 2 Rat 5.4 pIC50 = 5.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091209 14853 0 None -70 2 Rat 5.4 pIC50 = 5.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44444630 161602 0 None -3 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 596 7 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4CCCC4)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL400390 161602 0 None -3 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 596 7 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4CCCC4)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
44293101 193897 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 513 8 2 8 5.5 CC(=O)OCc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL49162 193897 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 513 8 2 8 5.5 CC(=O)OCc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
145951481 169734 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 10 1 10 3.6 COc1ccccc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4174753 169734 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 10 1 10 3.6 COc1ccccc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
25193797 196444 0 None 4 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 548 7 2 5 6.4 CC(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL515200 196444 0 None 4 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 548 7 2 5 6.4 CC(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44593415 196158 0 None 20 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL512893 196158 0 None 20 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44444617 100920 0 None -3 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 656 8 2 5 7.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N(C)C)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249372 100920 0 None -3 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 656 8 2 5 7.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N(C)C)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
44380319 65524 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168615 65524 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
44451319 102950 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 882 15 3 10 6.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL260647 102950 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 882 15 3 10 6.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44451396 163452 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 842 16 4 10 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL406958 163452 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 842 16 4 10 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
25113693 168693 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 896 15 3 10 6.2 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3ccccc3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL415279 168693 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 896 15 3 10 6.2 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3ccccc3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44432639 93738 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 536 10 2 4 5.8 COc1ccccc1CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
CHEMBL232356 93738 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 536 10 2 4 5.8 COc1ccccc1CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
10209293 107979 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295791 107979 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44434431 95286 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 909 24 3 15 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL235132 95286 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 909 24 3 15 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
11331001 195801 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL509075 195801 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
44432642 160373 0 None 1 2 Rat 7.3 pIC50 = 7.3 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 574 9 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL398060 160373 0 None 1 2 Rat 7.3 pIC50 = 7.3 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 574 9 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44293591 108373 0 None -1 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298700 108373 0 None -1 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44432635 93558 0 None -5 2 Human 6.3 pIC50 = 6.3 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 512 8 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2C(C)(C)C2(C)C)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232150 93558 0 None -5 2 Human 6.3 pIC50 = 6.3 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 512 8 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2C(C)(C)C2(C)C)CC3)c1 10.1016/j.bmcl.2007.05.009
44341056 121312 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2C)c1 10.1016/s0960-894x(02)00751-5
CHEMBL333614 121312 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2C)c1 10.1016/s0960-894x(02)00751-5
44398120 163071 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1660 41 17 19 -0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(=O)N(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL406535 163071 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1660 41 17 19 -0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(=O)N(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44561369 197247 0 None -15 2 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL517881 197247 0 None -15 2 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44432646 154012 0 None -2 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 581 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCC2CCOCC2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL392843 154012 0 None -2 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 581 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCC2CCOCC2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44358962 18915 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 559 7 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)nc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184155 18915 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 559 7 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)nc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL335764 18915 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 559 7 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)nc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44395583 131124 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 524 7 2 8 5.8 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL363663 131124 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 524 7 2 8 5.8 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL268875 217550 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NCC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
15602805 14879 0 None 11 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
CHEMBL1091579 14879 0 None 11 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
44295755 199900 0 None 46 2 Human 8.3 pIC50 = 8.3 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2111956 199900 0 None 46 2 Human 8.3 pIC50 = 8.3 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL52278 199900 0 None 46 2 Human 8.3 pIC50 = 8.3 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44380513 126969 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 631 10 4 4 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(CO)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL351836 126969 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 631 10 4 4 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(CO)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44380147 127056 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352566 127056 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
1184 10505 36 None 2 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
9874838 10505 36 None 2 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
CHEMBL71917 10505 36 None 2 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
16156572 173892 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1678 48 16 18 5.2 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL429016 173892 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1678 48 16 18 5.2 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398395 103755 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1751 45 17 20 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CN(Cc1ccccn1)Cc1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL266444 103755 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1751 45 17 20 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CN(Cc1ccccn1)Cc1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44448991 162120 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL403234 162120 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL556355 162120 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
16146554 168238 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)CO 10.1021/jm0003900
CHEMBL412749 168238 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)CO 10.1021/jm0003900
10051739 92208 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL22653 92208 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
44398181 162461 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1710 43 18 19 2.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCNc1ccc2ccccc2n1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL404973 162461 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1710 43 18 19 2.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCNc1ccc2ccccc2n1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16147453 103892 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1645 42 17 18 1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL267622 103892 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1645 42 17 18 1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
9808288 118258 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL327704 118258 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
11421518 172075 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL423291 172075 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
9808288 118258 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL327704 118258 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(02)00026-4
44361796 90167 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1583 42 17 18 0.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL219461 90167 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1583 42 17 18 0.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
44395533 73572 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 577 7 2 8 6.5 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CC3CCN2CC3)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185986 73572 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 577 7 2 8 6.5 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CC3CCN2CC3)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44380148 127089 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352782 127089 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
9985901 117230 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL324654 117230 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
71449058 91181 0 None 10 2 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2111955 91181 0 None 10 2 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2219718 91181 0 None 10 2 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
145991962 173611 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 531 5 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6nc7ccccc7[nH]6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4285058 173611 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 531 5 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6nc7ccccc7[nH]6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
44292988 189220 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 586 12 3 4 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47862 189220 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 586 12 3 4 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293411 195547 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 494 10 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50552 195547 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 494 10 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44359287 18407 0 None -38 2 Rat 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180743 18407 0 None -38 2 Rat 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL139993 18407 0 None -38 2 Rat 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293163 195479 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50433 195479 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44398086 103810 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1645 41 16 18 1.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL266893 103810 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1645 41 16 18 1.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44451379 175759 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 884 17 4 10 6.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccccc2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL439076 175759 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 884 17 4 10 6.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccccc2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44359471 18970 0 None -67 2 Rat 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184266 18970 0 None -67 2 Rat 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL341717 18970 0 None -67 2 Rat 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44434428 153532 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 865 21 3 14 5.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL392435 153532 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 865 21 3 14 5.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44292606 108321 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 445 6 2 6 5.2 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccc(F)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL298300 108321 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 445 6 2 6 5.2 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccc(F)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44292862 188426 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 477 6 2 6 6.2 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc4ccccc4c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL47758 188426 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 477 6 2 6 6.2 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc4ccccc4c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44293486 194196 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 592 13 2 3 8.5 CCN(C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL49374 194196 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 592 13 2 3 8.5 CCN(C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44572287 187582 0 None -9 2 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6cccnc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475660 187582 0 None -9 2 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6cccnc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44293366 168990 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 511 12 3 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL416285 168990 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 511 12 3 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293250 108510 0 None -1 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 11 2 4 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL299615 108510 0 None -1 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 11 2 4 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44432636 94160 0 None -8 2 Human 6.3 pIC50 = 6.3 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 550 8 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C24CC5CC(CC(C5)C2)C4)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL233341 94160 0 None -8 2 Human 6.3 pIC50 = 6.3 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 550 8 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C24CC5CC(CC(C5)C2)C4)CC3)c1 10.1016/j.bmcl.2007.05.009
44460343 212124 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 11 2 4 7.6 COCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL79639 212124 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 11 2 4 7.6 COCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
44293301 195284 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50283 195284 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44432643 153545 0 None 1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 592 9 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL392446 153545 0 None 1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 592 9 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44293274 108033 0 None 9 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 510 12 1 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCN(C)CCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296199 108033 0 None 9 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 510 12 1 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCN(C)CCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
22100905 191045 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL48380 191045 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44593425 183544 0 None -12 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
CHEMBL460480 183544 0 None -12 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
44293250 108510 0 None 1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 552 11 2 4 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL299615 108510 0 None 1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 552 11 2 4 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
58239302 168769 0 None -616 2 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 577 12 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(C)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4159247 168769 0 None -616 2 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 577 12 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(C)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
11583756 196433 0 None -31 2 Rat 5.2 pIC50 = 5.2 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL515123 196433 0 None -31 2 Rat 5.2 pIC50 = 5.2 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44359193 18410 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 587 8 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)NCc4ccc5c(c4)OCO5)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180764 18410 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 587 8 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)NCc4ccc5c(c4)OCO5)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL141750 18410 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 587 8 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)NCc4ccc5c(c4)OCO5)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293323 107993 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ncccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295911 107993 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ncccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
22129993 185506 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 558 7 4 5 6.2 O=C(Nc1cc2c(OCCC3CCCCN3)c(-c3cccc(Br)c3)c(O)nc2cc1Cl)NC1CC1 10.1016/s0960-894x(00)00318-8
CHEMBL46844 185506 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 558 7 4 5 6.2 O=C(Nc1cc2c(OCCC3CCCCN3)c(-c3cccc(Br)c3)c(O)nc2cc1Cl)NC1CC1 10.1016/s0960-894x(00)00318-8
44292745 194693 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 508 7 4 5 6.1 Cc1ccc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
CHEMBL49667 194693 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 508 7 4 5 6.1 Cc1ccc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
16144515 162906 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1533 40 15 16 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL406337 162906 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1533 40 15 16 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
11249548 105866 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
CHEMBL280664 105866 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
16221328 92375 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1530 41 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL228197 92375 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1530 41 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
145949496 169637 0 None 165 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 685 13 2 9 4.9 Cc1cccc(F)c1Cn1c(C)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4173065 169637 0 None 165 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 685 13 2 9 4.9 Cc1cccc(F)c1Cn1c(C)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.ejmech.2017.12.095
44361802 175628 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1547 41 15 16 2.6 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](Cc2ccc(CNC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL438018 175628 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1547 41 15 16 2.6 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](Cc2ccc(CNC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44340906 16343 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 578 9 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL112400 16343 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 578 9 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2)c1 10.1016/s0960-894x(02)00751-5
44321291 213056 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 632 11 2 3 9.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5(C)CC4CC(C)(C)C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86950 213056 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 632 11 2 3 9.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5(C)CC4CC(C)(C)C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
10032223 18975 0 None 81 2 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184284 18975 0 None 81 2 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL342822 18975 0 None 81 2 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44432652 103916 0 None 1 2 Rat 8.2 pIC50 = 8.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 633 9 3 5 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cnc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL267838 103916 0 None 1 2 Rat 8.2 pIC50 = 8.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 633 9 3 5 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cnc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44380514 126990 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 645 10 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(=O)O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352051 126990 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 645 10 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(=O)O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL262747 217325 9 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44321292 213065 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCCC4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL87000 213065 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCCC4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44380797 66066 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL170499 66066 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL2105773 219520 8 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL409018 219520 8 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
16221151 150374 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 40 13 16 3.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)[S+](C)[O-])C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL389945 150374 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 40 13 16 3.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)[S+](C)[O-])C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
15602806 15068 0 None 7 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL1092638 15068 0 None 7 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
44432648 157006 0 None 1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 643 9 2 4 7.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4nccnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL395225 157006 0 None 1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 643 9 2 4 7.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4nccnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44292728 108014 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 487 8 2 8 5.1 COc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1OC 10.1016/s0960-894x(00)00318-8
CHEMBL296086 108014 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 487 8 2 8 5.1 COc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1OC 10.1016/s0960-894x(00)00318-8
44293305 108238 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL297703 108238 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293071 108378 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 589 14 3 5 6.6 CCOC(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL298748 108378 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 589 14 3 5 6.6 CCOC(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293165 108470 0 None 7 2 Human 6.2 pIC50 = 6.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 556 16 2 5 5.7 COCCN(CCOC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL299392 108470 0 None 7 2 Human 6.2 pIC50 = 6.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 556 16 2 5 5.7 COCCN(CCOC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44341080 117355 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 604 11 2 3 8.4 CCCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL325417 117355 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 604 11 2 3 8.4 CCCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
44293347 169890 0 None -4 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 11 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL417720 169890 0 None -4 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 11 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293617 195454 0 None 23 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50380 195454 0 None 23 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44432643 153545 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 592 9 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL392446 153545 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 592 9 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44293100 194045 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 485 7 3 7 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc(C(C)O)c1 10.1016/s0960-894x(00)00318-8
CHEMBL49276 194045 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 485 7 3 7 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc(C(C)O)c1 10.1016/s0960-894x(00)00318-8
44561368 183593 0 None 42 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL460892 183593 0 None 42 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44432636 94160 0 None 8 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 550 8 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C24CC5CC(CC(C5)C2)C4)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL233341 94160 0 None 8 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 550 8 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C24CC5CC(CC(C5)C2)C4)CC3)c1 10.1016/j.bmcl.2007.05.009
44432655 156265 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 675 11 3 6 6.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCOc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL394634 156265 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 675 11 3 6 6.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCOc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
11583756 196433 0 None 31 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL515123 196433 0 None 31 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
11712618 187005 0 None 22 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6ncccc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL474992 187005 0 None 22 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6ncccc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
25194091 195789 0 None 13 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 498 7 3 5 5.5 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL508898 195789 0 None 13 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 498 7 3 5 5.5 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44214108 107893 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 656 13 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL295152 107893 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 656 13 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
145952498 169655 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 719 14 2 10 4.8 COc1ccccc1[C@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O)NCCCC(=O)O 10.1016/j.ejmech.2017.12.095
CHEMBL4173316 169655 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 719 14 2 10 4.8 COc1ccccc1[C@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O)NCCCC(=O)O 10.1016/j.ejmech.2017.12.095
44321148 103583 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 622 11 2 5 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CC4)OCCO5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL265042 103583 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 622 11 2 5 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CC4)OCCO5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321509 212968 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CCCC[C@H]5C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86431 212968 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CCCC[C@H]5C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44292874 190619 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 13 3 4 7.2 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)(C)C 10.1016/s0960-894x(01)00274-8
CHEMBL48069 190619 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 13 3 4 7.2 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)(C)C 10.1016/s0960-894x(01)00274-8
10187208 73522 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 540 7 2 9 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2OCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185785 73522 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 540 7 2 9 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2OCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44434386 96583 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 638 11 2 8 5.1 C#CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL237734 96583 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 638 11 2 8 5.1 C#CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44434391 96863 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 926 27 2 16 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL238177 96863 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 926 27 2 16 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44293015 181816 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 530 7 4 5 6.6 O=C(Nc1cc2c(OCCC3CCCCN3)c(-c3ccc4ccccc4c3)c(O)nc2cc1Cl)NC1CC1 10.1016/s0960-894x(00)00318-8
CHEMBL45675 181816 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 530 7 4 5 6.6 O=C(Nc1cc2c(OCCC3CCCCN3)c(-c3ccc4ccccc4c3)c(O)nc2cc1Cl)NC1CC1 10.1016/s0960-894x(00)00318-8
44432648 157006 0 None -1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 643 9 2 4 7.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4nccnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL395225 157006 0 None -1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 643 9 2 4 7.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4nccnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44451356 103138 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 870 18 4 10 5.9 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL261649 103138 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 870 18 4 10 5.9 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44293129 188515 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL47772 188515 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
22129998 108052 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL296321 108052 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44572236 178678 0 None -6 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL446978 178678 0 None -6 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44293264 107991 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 560 12 3 4 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL295908 107991 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 560 12 3 4 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
16148338 168727 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL415573 168727 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
10649568 21338 0 None 4 2 Human 8.2 pIC50 = 8.2 Functional
Functional antagonism at the rhesus monkey gonadotropin-releasing hormone receptorFunctional antagonism at the rhesus monkey gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 21338 0 None 4 2 Human 8.2 pIC50 = 8.2 Functional
Functional antagonism at the rhesus monkey gonadotropin-releasing hormone receptorFunctional antagonism at the rhesus monkey gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
44321290 213185 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 548 9 2 3 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL87785 213185 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 548 9 2 3 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44432654 166574 0 None 6 2 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 660 10 3 6 6.1 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)nc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL410547 166574 0 None 6 2 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 660 10 3 6 6.1 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)nc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
9961721 175258 0 None 60 2 Human 8.2 pIC50 = 8.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL435167 175258 0 None 60 2 Human 8.2 pIC50 = 8.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
16144832 168558 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1533 40 15 16 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL414061 168558 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1533 40 15 16 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
10231401 8801 1 None 1 2 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1016/s0960-894x(01)00512-1
5584 8801 1 None 1 2 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1016/s0960-894x(01)00512-1
CHEMBL314260 8801 1 None 1 2 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1016/s0960-894x(01)00512-1
44572235 196286 0 None 5 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
CHEMBL513998 196286 0 None 5 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
44340888 117302 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 592 10 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(CO)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL325091 117302 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 592 10 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(CO)c2)c1 10.1016/s0960-894x(02)00751-5
44380552 65533 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168655 65533 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
44380643 65492 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 659 10 3 5 7.7 COC(=O)c1nc2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4ccc(C(C)(C)C(=O)N5CC6CCC5CC6)cc34)ccc2[nH]1 10.1016/s0960-894x(02)00026-4
CHEMBL168498 65492 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 659 10 3 5 7.7 COC(=O)c1nc2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4ccc(C(C)(C)C(=O)N5CC6CCC5CC6)cc34)ccc2[nH]1 10.1016/s0960-894x(02)00026-4
44361468 168511 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL413698 168511 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
16147757 168583 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1645 42 17 18 1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL414266 168583 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1645 42 17 18 1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
16144824 103622 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)CO 10.1021/jm0003900
CHEMBL265286 103622 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)CO 10.1021/jm0003900
44361351 167738 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 42 16 18 1.7 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@@H](Cc2ccc(CNC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL411565 167738 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 42 16 18 1.7 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@@H](Cc2ccc(CNC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361797 168582 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1659 42 17 18 1.5 CNC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL414249 168582 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1659 42 17 18 1.5 CNC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44293223 181080 0 None - 1 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 8 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(CC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL45501 181080 0 None - 1 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 8 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(CC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
9809394 127290 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 628 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL354524 127290 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 628 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
44293178 108199 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 658 17 3 4 7.9 CCCN(CCC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL297430 108199 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 658 17 3 4 7.9 CCCN(CCC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
9809382 107451 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 628 11 2 8 5.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL292291 107451 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 628 11 2 8 5.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44434373 96823 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 637 11 3 7 4.6 C#CCNC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL238160 96823 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 637 11 3 7 4.6 C#CCNC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44292820 107943 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 498 8 3 7 4.4 Cc1cc(CC(N)=O)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295556 107943 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 498 8 3 7 4.4 Cc1cc(CC(N)=O)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44293011 108032 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 563 6 2 6 7.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL296198 108032 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 563 6 2 6 7.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44573791 194167 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 484 7 1 5 6.2 CCCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493565 194167 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 484 7 1 5 6.2 CCCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
44215055 108067 0 None 1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 576 11 1 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(C)CCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL296442 108067 0 None 1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 576 11 1 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(C)CCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293249 192222 0 None -1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48616 192222 0 None -1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44292977 181016 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 14 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45489 181016 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 14 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44434415 95302 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 821 18 3 13 5.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL235180 95302 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 821 18 3 13 5.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44434432 95523 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 953 27 3 16 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL236221 95523 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 953 27 3 16 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44215053 192399 0 None 1 2 Rat 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48641 192399 0 None 1 2 Rat 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293485 108292 0 None 2 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 590 12 1 3 8.2 CCN(CCCCc1ccncc1)CCc1c(-c2cc(C)cc(C)c2)[nH]c2ccc(C(C)(C)C(=O)N3C4CCC3CC4)cc12 10.1016/s0960-894x(01)00275-x
CHEMBL298051 108292 0 None 2 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 590 12 1 3 8.2 CCN(CCCCc1ccncc1)CCc1c(-c2cc(C)cc(C)c2)[nH]c2ccc(C(C)(C)C(=O)N3C4CCC3CC4)cc12 10.1016/s0960-894x(01)00275-x
44444663 100975 0 None -4 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 645 8 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CNC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249771 100975 0 None -4 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 645 8 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CNC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44593415 196158 0 None -20 2 Rat 4.1 pIC50 = 4.1 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL512893 196158 0 None -20 2 Rat 4.1 pIC50 = 4.1 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44359287 18407 0 None 38 2 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180743 18407 0 None 38 2 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL139993 18407 0 None 38 2 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
22100905 191045 0 None 1 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL48380 191045 0 None 1 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44359303 18409 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 520 7 4 7 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nc[nH]n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180760 18409 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 520 7 4 7 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nc[nH]n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL141539 18409 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 520 7 4 7 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nc[nH]n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44359285 18399 0 None -17 2 Rat 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180695 18399 0 None -17 2 Rat 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138747 18399 0 None -17 2 Rat 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44576656 195025 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium fluxAntagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium flux
ChEMBL 571 10 2 7 4.2 N[C@@H](Cn1c(=O)c(-c2ccc(COCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL499588 195025 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium fluxAntagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium flux
ChEMBL 571 10 2 7 4.2 N[C@@H](Cn1c(=O)c(-c2ccc(COCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
138978204 173533 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 461 6 1 6 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(CCF)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4283577 173533 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 461 6 1 6 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(CCF)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
145992260 173713 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 744 10 2 14 3.3 CC(=O)N[C@@H]1[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](COC(C)=O)O[C@H]1n1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1 10.1039/C7MD00320J
CHEMBL4286937 173713 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 744 10 2 14 3.3 CC(=O)N[C@@H]1[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](COC(C)=O)O[C@H]1n1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1 10.1039/C7MD00320J
16147451 103789 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 41 15 18 2.3 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL266653 103789 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 41 15 18 2.3 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL2370894 216725 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)C[C@@H]3NC(=O)NC3=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16147765 168630 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1628 41 16 20 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)c3cnc(O)nc3O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361477 168630 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1628 41 16 20 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)c3cnc(O)nc3O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL414715 168630 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1628 41 16 20 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)c3cnc(O)nc3O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
10051739 92208 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL22653 92208 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
44321345 213021 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 596 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCC2CCC(=O)N(C)C2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86758 213021 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 596 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCC2CCC(=O)N(C)C2)c1 10.1016/s0960-894x(01)00512-1
10258659 18971 0 None 46 2 Human 8.1 pIC50 = 8.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184268 18971 0 None 46 2 Human 8.1 pIC50 = 8.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL341809 18971 0 None 46 2 Human 8.1 pIC50 = 8.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293487 108411 0 None 2 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL299006 108411 0 None 2 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
145973618 169864 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 635 8 1 8 4.7 Cc1cc(F)cc([C@@H](N)Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.ejmech.2017.12.095
CHEMBL4176683 169864 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 635 8 1 8 4.7 Cc1cc(F)cc([C@@H](N)Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.ejmech.2017.12.095
44380236 65495 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 641 11 2 4 8.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168506 65495 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 641 11 2 4 8.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
16144222 103797 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL266728 103797 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44341113 16693 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL114438 16693 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C)c2)c1 10.1016/s0960-894x(02)00751-5
44321411 113786 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@@H]5CC[C@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL315326 113786 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@@H]5CC[C@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
101755083 8141 47 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
16136245 8141 47 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
4379 8141 47 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
5585 8141 47 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
CHEMBL415606 8141 47 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
DB06699 8141 47 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
44361587 168090 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1602 41 16 17 2.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(CNC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O 10.1021/jm0003900
CHEMBL412336 168090 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1602 41 16 17 2.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(CNC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O 10.1021/jm0003900
9872676 84970 0 None -2 2 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity at rat pituitary GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulationAntagonist activity at rat pituitary GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulation
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
CHEMBL210514 84970 0 None -2 2 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity at rat pituitary GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulationAntagonist activity at rat pituitary GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulation
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
44321412 213031 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 590 11 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86805 213031 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 590 11 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
16144865 90215 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1648 43 18 18 1.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)C(NC(N)=O)NC(N)=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL219799 90215 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1648 43 18 18 1.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)C(NC(N)=O)NC(N)=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
53239183 169622 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 603 8 1 8 4.3 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4172886 169622 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 603 8 1 8 4.3 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
58022331 135434 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 473 3 1 6 3.5 O=c1[nH]c2sccc2c(=O)n1-c1cc(S(=O)(=O)N2CCCc3ccccc32)ccc1Cl nan
CHEMBL3668004 135434 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 473 3 1 6 3.5 O=c1[nH]c2sccc2c(=O)n1-c1cc(S(=O)(=O)N2CCCc3ccccc32)ccc1Cl nan
44292918 178194 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL44627 178194 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
9936667 107294 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 525 10 3 4 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL291201 107294 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 525 10 3 4 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44432627 154907 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 430 7 2 3 4.5 CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
CHEMBL393540 154907 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 430 7 2 3 4.5 CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
10649568 21338 0 None -4 2 Rat 7.1 pIC50 = 7.1 Functional
Functional antagonism at GnRH receptor in rat (PI turnover)Functional antagonism at GnRH receptor in rat (PI turnover)
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 21338 0 None -4 2 Rat 7.1 pIC50 = 7.1 Functional
Functional antagonism at GnRH receptor in rat (PI turnover)Functional antagonism at GnRH receptor in rat (PI turnover)
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
44293177 181482 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 644 13 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45597 181482 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 644 13 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
10438167 107959 0 None -15 2 Rat 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 578 12 2 3 8.6 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL295641 107959 0 None -15 2 Rat 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 578 12 2 3 8.6 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCCCC1 10.1016/s0960-894x(01)00275-x
44321695 112758 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccn(C)c2=O)c1 10.1016/s0960-894x(01)00512-1
CHEMBL313086 112758 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccn(C)c2=O)c1 10.1016/s0960-894x(01)00512-1
44292979 194968 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 483 10 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49893 194968 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 483 10 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
11712618 187005 0 None -22 2 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6ncccc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL474992 187005 0 None -22 2 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6ncccc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44293151 107951 0 None -23 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 12 2 3 6.9 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C(C)C 10.1016/s0960-894x(01)00275-x
CHEMBL295595 107951 0 None -23 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 12 2 3 6.9 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C(C)C 10.1016/s0960-894x(01)00275-x
44560995 185932 0 None -9 2 Rat 4.1 pIC50 = 4.1 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL472117 185932 0 None -9 2 Rat 4.1 pIC50 = 4.1 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44434433 95524 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 997 30 3 17 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL236222 95524 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 997 30 3 17 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44434436 157751 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1619 39 6 26 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL395825 157751 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1619 39 6 26 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
16221379 168710 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1546 41 15 17 1.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
CHEMBL415380 168710 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1546 41 15 17 1.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
58022131 135437 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 442 5 2 6 4.0 Cc1ccccc1COc1ccc(Cl)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
CHEMBL3668007 135437 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 442 5 2 6 4.0 Cc1ccccc1COc1ccc(Cl)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
44432642 160373 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 574 9 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL398060 160373 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 574 9 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44432649 93474 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 645 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]c(C)nc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231739 93474 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 645 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]c(C)nc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44359264 18400 0 None -11 2 Rat 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180700 18400 0 None -11 2 Rat 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138866 18400 0 None -11 2 Rat 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44185958 161777 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 615 8 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401349 161777 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 615 8 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
145956692 168852 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 606 9 2 10 3.3 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4160698 168852 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 606 9 2 10 3.3 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
44380488 65790 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ocnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169238 65790 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ocnc3c2)c1 10.1016/s0960-894x(02)00026-4
44432652 103916 0 None -1 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 633 9 3 5 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cnc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL267838 103916 0 None -1 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 633 9 3 5 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cnc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
16146884 103945 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1602 41 16 17 2.1 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CNC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL268146 103945 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1602 41 16 17 2.1 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CNC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44398118 174076 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1632 41 18 19 -0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL429378 174076 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1632 41 18 19 -0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44593424 182912 0 None 4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL459215 182912 0 None 4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44593424 182912 0 None 4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459215 182912 0 None 4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
16156706 143879 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1745 48 17 19 4.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL374747 143879 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1745 48 17 19 4.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16144863 103650 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL265556 103650 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16156706 143879 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1745 48 17 19 4.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL374747 143879 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1745 48 17 19 4.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
11620431 186148 0 None 21 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL473807 186148 0 None 21 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
15602807 14992 0 None 8 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1092245 14992 0 None 8 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44293485 108292 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 590 12 1 3 8.2 CCN(CCCCc1ccncc1)CCc1c(-c2cc(C)cc(C)c2)[nH]c2ccc(C(C)(C)C(=O)N3C4CCC3CC4)cc12 10.1016/s0960-894x(01)00275-x
CHEMBL298051 108292 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 590 12 1 3 8.2 CCN(CCCCc1ccncc1)CCc1c(-c2cc(C)cc(C)c2)[nH]c2ccc(C(C)(C)C(=O)N3C4CCC3CC4)cc12 10.1016/s0960-894x(01)00275-x
44292837 108249 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 433 6 2 7 5.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccsc3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL297768 108249 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 433 6 2 7 5.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccsc3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44292683 193736 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 537 7 2 6 7.4 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(-c4ccccc4)c(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL49028 193736 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 537 7 2 6 7.4 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(-c4ccccc4)c(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44293134 194180 0 None -1 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49366 194180 0 None -1 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44432650 93546 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 703 10 3 5 6.5 CCn1c(=O)[nH]c2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4c3CN(C(=O)Cc3c(F)cccc3C(F)(F)F)CC4)ccc2c1=O 10.1016/j.bmcl.2007.05.009
CHEMBL232097 93546 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 703 10 3 5 6.5 CCn1c(=O)[nH]c2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4c3CN(C(=O)Cc3c(F)cccc3C(F)(F)F)CC4)ccc2c1=O 10.1016/j.bmcl.2007.05.009
15602806 15068 0 None -7 2 Rat 6.0 pIC50 = 6.0 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL1092638 15068 0 None -7 2 Rat 6.0 pIC50 = 6.0 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
44560995 185932 0 None 9 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL472117 185932 0 None 9 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44321147 170259 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 618 11 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CCCC5)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL420051 170259 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 618 11 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CCCC5)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44293443 190830 0 None - 1 Rat 6.0 pIC50 = 6.0 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48224 190830 0 None - 1 Rat 6.0 pIC50 = 6.0 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293511 108063 0 None -3 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296426 108063 0 None -3 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44444645 161779 0 None -5 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 672 9 2 6 4.8 CC(=O)NC1CCN(C(=O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL401351 161779 0 None -5 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 672 9 2 6 4.8 CC(=O)NC1CCN(C(=O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
44293075 97439 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 614 12 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL239108 97439 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 614 12 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292827 194967 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49891 194967 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44434404 173347 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1477 33 4 24 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL427981 173347 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1477 33 4 24 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44432635 93558 0 None 5 2 Rat 7.0 pIC50 = 7.0 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 512 8 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2C(C)(C)C2(C)C)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232150 93558 0 None 5 2 Rat 7.0 pIC50 = 7.0 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 512 8 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2C(C)(C)C2(C)C)CC3)c1 10.1016/j.bmcl.2007.05.009
44295755 199900 0 None -46 2 Rat 7.0 pIC50 = 7.0 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2111956 199900 0 None -46 2 Rat 7.0 pIC50 = 7.0 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL52278 199900 0 None -46 2 Rat 7.0 pIC50 = 7.0 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293486 194196 0 None 1 2 Rat 6.0 pIC50 = 6.0 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 592 13 2 3 8.5 CCN(C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL49374 194196 0 None 1 2 Rat 6.0 pIC50 = 6.0 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 592 13 2 3 8.5 CCN(C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293222 182739 0 None -100 2 Rat 7.0 pIC50 = 7.0 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL138464 182739 0 None -100 2 Rat 7.0 pIC50 = 7.0 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL45883 182739 0 None -100 2 Rat 7.0 pIC50 = 7.0 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44359289 18923 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 547 8 3 7 6.3 CCn1nccc1NC(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
CHEMBL1184180 18923 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 547 8 3 7 6.3 CCn1nccc1NC(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
CHEMBL337323 18923 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 547 8 3 7 6.3 CCn1nccc1NC(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
44361351 167738 0 None - 1 Human 9.5 pKd = 9.5 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 42 16 18 1.7 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@@H](Cc2ccc(CNC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL411565 167738 0 None - 1 Human 9.5 pKd = 9.5 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 42 16 18 1.7 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@@H](Cc2ccc(CNC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16144515 162906 0 None - 1 Human 9.3 pKd = 9.3 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1533 40 15 16 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL406337 162906 0 None - 1 Human 9.3 pKd = 9.3 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1533 40 15 16 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL1251 215440 27 None - 1 Human 9.3 pKd = 9.3 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CC/N=C(\NCC)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCN/C(=N/CC)NCC)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL5314377 215440 27 None - 1 Human 9.3 pKd = 9.3 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CC/N=C(\NCC)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCN/C(=N/CC)NCC)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL2370890 216724 0 None - 1 Human 9.3 pKd = 9.3 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](CCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
101755083 8141 47 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
16136245 8141 47 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
4379 8141 47 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
5585 8141 47 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
CHEMBL415606 8141 47 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
DB06699 8141 47 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
16146884 103945 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1602 41 16 17 2.1 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CNC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL268146 103945 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1602 41 16 17 2.1 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CNC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361587 168090 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1602 41 16 17 2.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(CNC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O 10.1021/jm0003900
CHEMBL412336 168090 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1602 41 16 17 2.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(CNC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O 10.1021/jm0003900
16146554 168238 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)CO 10.1021/jm0003900
CHEMBL412749 168238 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)CO 10.1021/jm0003900
44361802 175628 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1547 41 15 16 2.6 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](Cc2ccc(CNC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL438018 175628 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1547 41 15 16 2.6 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](Cc2ccc(CNC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
1188 7007 48 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
16131215 7007 48 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
35 7007 48 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
CHEMBL1252 7007 48 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
DB00106 7007 48 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
44361796 90167 0 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1583 42 17 18 0.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL219461 90167 0 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1583 42 17 18 0.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
16147451 103789 0 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 41 15 18 2.3 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL266653 103789 0 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 41 15 18 2.3 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361797 168582 0 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1659 42 17 18 1.5 CNC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL414249 168582 0 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1659 42 17 18 1.5 CNC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16144824 103622 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)CO 10.1021/jm0003900
CHEMBL265286 103622 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)CO 10.1021/jm0003900
16144863 103650 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL265556 103650 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16144222 103797 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL266728 103797 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361888 148554 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL386105 148554 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
44361468 168511 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL413698 168511 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
1190 7669 47 None 6025 3 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
25074887 7669 47 None 6025 3 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
583 7669 47 None 6025 3 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
CHEMBL1200490 7669 47 None 6025 3 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
DB00050 7669 47 None 6025 3 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
16147453 103892 0 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1645 42 17 18 1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL267622 103892 0 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1645 42 17 18 1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
16147767 104134 0 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL269516 104134 0 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL268875 217550 0 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NCC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
9854500 109049 0 None - 0 Rat 8.8 pKd = 8.8 Functional
Antagonist activity at rat GnRH receptor assessed as luteinizing hormone release in rat pituitary cellsAntagonist activity at rat GnRH receptor assessed as luteinizing hormone release in rat pituitary cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm701249f
CHEMBL303274 109049 0 None - 0 Rat 8.8 pKd = 8.8 Functional
Antagonist activity at rat GnRH receptor assessed as luteinizing hormone release in rat pituitary cellsAntagonist activity at rat GnRH receptor assessed as luteinizing hormone release in rat pituitary cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm701249f
16148338 168727 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL415573 168727 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16146022 176898 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1631 41 17 18 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL444381 176898 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1631 41 17 18 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL269711 217580 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL2105773 219520 8 None -1 2 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL409018 219520 8 None -1 2 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
44361795 175277 0 None - 1 Human 8.7 pKd = 8.7 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1574 40 15 18 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL435322 175277 0 None - 1 Human 8.7 pKd = 8.7 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1574 40 15 18 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL262747 217325 9 None 1 2 Human 8.6 pKd = 8.6 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
10394119 121225 0 None - 0 Rat 8.3 pKd = 8.3 Functional
Competitive inhibition of GnRH-stimulated extracellular acidification in cells expressing recombinant rat GnRH receptorCompetitive inhibition of GnRH-stimulated extracellular acidification in cells expressing recombinant rat GnRH receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333345 121225 0 None - 0 Rat 8.3 pKd = 8.3 Functional
Competitive inhibition of GnRH-stimulated extracellular acidification in cells expressing recombinant rat GnRH receptorCompetitive inhibition of GnRH-stimulated extracellular acidification in cells expressing recombinant rat GnRH receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
1184 10505 36 None 2 2 Human 10.0 pKi = 10 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
9874838 10505 36 None 2 2 Human 10.0 pKi = 10 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
CHEMBL71917 10505 36 None 2 2 Human 10.0 pKi = 10 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
145991962 173611 0 None - 1 Human 7.0 pKi = 7.0 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 531 5 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6nc7ccccc7[nH]6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4285058 173611 0 None - 1 Human 7.0 pKi = 7.0 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 531 5 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6nc7ccccc7[nH]6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
11583756 196433 0 None 31 2 Human 7.9 pKi = 7.9 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL515123 196433 0 None 31 2 Human 7.9 pKi = 7.9 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
138978204 173533 0 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 461 6 1 6 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(CCF)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4283577 173533 0 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 461 6 1 6 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(CCF)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
145992260 173713 0 None - 1 Human 6.8 pKi = 6.8 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 744 10 2 14 3.3 CC(=O)N[C@@H]1[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](COC(C)=O)O[C@H]1n1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1 10.1039/C7MD00320J
CHEMBL4286937 173713 0 None - 1 Human 6.8 pKi = 6.8 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 744 10 2 14 3.3 CC(=O)N[C@@H]1[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](COC(C)=O)O[C@H]1n1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1 10.1039/C7MD00320J
145993478 174099 0 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 602 8 3 9 4.4 CC(C)(C)OC(=O)N[C@@H](Cn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1)C(=O)O 10.1039/C7MD00320J
CHEMBL4294163 174099 0 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 602 8 3 9 4.4 CC(C)(C)OC(=O)N[C@@H](Cn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1)C(=O)O 10.1039/C7MD00320J
1179 7748 36 None - 1 Human 7.7 pKi = 7.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
9957278 7748 36 None - 1 Human 7.7 pKi = 7.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
CHEMBL494803 7748 36 None - 1 Human 7.7 pKi = 7.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
145980339 173366 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 380 4 1 3 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCF)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4280124 173366 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 380 4 1 3 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCF)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
138978203 173479 0 None - 1 Human 7.4 pKi = 7.4 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 639 7 3 11 3.1 Cc1cn([C@H]2C[C@@H](n3cc(CN4CCN(c5cccc6[nH]c(-c7ccc(C(C)(C)C)cc7)nc56)CC4)nn3)[C@@H](CO)O2)c(=O)[nH]c1=O 10.1039/C7MD00320J
CHEMBL4282476 173479 0 None - 1 Human 7.4 pKi = 7.4 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 639 7 3 11 3.1 Cc1cn([C@H]2C[C@@H](n3cc(CN4CCN(c5cccc6[nH]c(-c7ccc(C(C)(C)C)cc7)nc56)CC4)nn3)[C@@H](CO)O2)c(=O)[nH]c1=O 10.1039/C7MD00320J
138978207 173932 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 372 3 1 3 4.3 C#CCN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1039/C7MD00320J
CHEMBL4290761 173932 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 372 3 1 3 4.3 C#CCN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1039/C7MD00320J
145984647 173195 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 509 5 1 6 5.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6ccc(F)cc6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4277116 173195 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 509 5 1 6 5.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6ccc(F)cc6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
3860 7531 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
NoneNone
Drug Central None None None None None
436 7531 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
NoneNone
Drug Central None None None None None
50225 7531 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
NoneNone
Drug Central None None None None None
CHEMBL2110824 7531 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
NoneNone
Drug Central None None None None None
DB06719 7531 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
NoneNone
Drug Central None None None None None
3860 7531 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
436 7531 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
50225 7531 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
CHEMBL2110824 7531 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
DB06719 7531 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
1177 10639 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
25074470 10639 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
2968 10639 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
CHEMBL1201334 10639 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
DB06825 10639 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
1162 8612 0 None 16 3 Human 10.0 pEC50 = 10 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
16132914 8612 0 None 16 3 Human 10.0 pEC50 = 10 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
3860 7531 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
436 7531 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
50225 7531 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
CHEMBL2110824 7531 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
DB06719 7531 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
1162 8612 0 None -16 3 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
16132914 8612 0 None -16 3 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
3860 7531 0 None -2 2 Mouse 9.7 pEC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
436 7531 0 None -2 2 Mouse 9.7 pEC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
50225 7531 0 None -2 2 Mouse 9.7 pEC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
CHEMBL2110824 7531 0 None -2 2 Mouse 9.7 pEC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
DB06719 7531 0 None -2 2 Mouse 9.7 pEC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
11980076 215232 29 None 1 2 Rat 8.1 pIC50 = 8.1 Functional
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
Drug Central None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
CHEMBL1007 215232 29 None 1 2 Rat 8.1 pIC50 = 8.1 Functional
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
Drug Central None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
11250647 8327 46 None - 1 Human 8.1 pIC50 = 8.1 Functional
determined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptordetermined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
5293 8327 46 None - 1 Human 8.1 pIC50 = 8.1 Functional
determined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptordetermined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
8362 8327 46 None - 1 Human 8.1 pIC50 = 8.1 Functional
determined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptordetermined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
CHEMBL1208155 8327 46 None - 1 Human 8.1 pIC50 = 8.1 Functional
determined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptordetermined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
DB11979 8327 46 None - 1 Human 8.1 pIC50 = 8.1 Functional
determined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptordetermined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
10348973 10086 58 None 1 2 Rat 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
5432 10086 58 None 1 2 Rat 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
5586 10086 58 None 1 2 Rat 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
CHEMBL1800159 10086 58 None 1 2 Rat 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
DB11853 10086 58 None 1 2 Rat 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
1175 9078 44 None 1 2 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
1559 9078 44 None 1 2 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
657181 9078 44 None 1 2 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
CHEMBL1201199 9078 44 None 1 2 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
DB00007 9078 44 None 1 2 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
10348973 10086 58 None -1 2 Human 8.0 pIC50 = 8 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
5432 10086 58 None -1 2 Human 8.0 pIC50 = 8 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
5586 10086 58 None -1 2 Human 8.0 pIC50 = 8 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
CHEMBL1800159 10086 58 None -1 2 Human 8.0 pIC50 = 8 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
DB11853 10086 58 None -1 2 Human 8.0 pIC50 = 8 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
12784 7365 12 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assayAntagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assay
Guide to Pharmacology 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 32960053
85469632 7365 12 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assayAntagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assay
Guide to Pharmacology 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 32960053
CHEMBL4537788 7365 12 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assayAntagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assay
Guide to Pharmacology 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 32960053
12283 9103 17 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated Ca2+ flux in HEK293 cells stably expressing hGnRHR.Inhibition of GnRH-stimulated Ca2+ flux in HEK293 cells stably expressing hGnRHR.
Guide to Pharmacology 508 7 2 8 3.5 COc1c(c(c(cc1)F)F)COc1c(cc(c(c1)n1c(=O)c2c(scc2[nH]c1=O)C(=O)O)F)OC 35690889
16656889 9103 17 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated Ca2+ flux in HEK293 cells stably expressing hGnRHR.Inhibition of GnRH-stimulated Ca2+ flux in HEK293 cells stably expressing hGnRHR.
Guide to Pharmacology 508 7 2 8 3.5 COc1c(c(c(cc1)F)F)COc1c(cc(c(c1)n1c(=O)c2c(scc2[nH]c1=O)C(=O)O)F)OC 35690889
CHEMBL3668014 9103 17 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated Ca2+ flux in HEK293 cells stably expressing hGnRHR.Inhibition of GnRH-stimulated Ca2+ flux in HEK293 cells stably expressing hGnRHR.
Guide to Pharmacology 508 7 2 8 3.5 COc1c(c(c(cc1)F)F)COc1c(cc(c(c1)n1c(=O)c2c(scc2[nH]c1=O)C(=O)O)F)OC 35690889
11496610 10847 13 None -8 2 Rat 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 19271735
5582 10847 13 None -8 2 Rat 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 19271735
CHEMBL474991 10847 13 None -8 2 Rat 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 19271735
1164 8613 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1164 8613 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17942747
1164 8613 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19638591
5581 8228 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19638591
11496610 10847 13 None 8 2 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 19271735
5582 10847 13 None 8 2 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 19271735
CHEMBL474991 10847 13 None 8 2 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 19271735
1162 8612 0 None 16 3 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
16132914 8612 0 None 16 3 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1190 7669 47 None 6025 3 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
25074887 7669 47 None 6025 3 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
583 7669 47 None 6025 3 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
CHEMBL1200490 7669 47 None 6025 3 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
DB00050 7669 47 None 6025 3 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
10231401 8801 1 None -1 2 Rat 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 11551758
5584 8801 1 None -1 2 Rat 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 11551758
CHEMBL314260 8801 1 None -1 2 Rat 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 11551758
101827019 8887 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
16130938 8887 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
3854 8887 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
73952264 8887 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
CHEMBL3989438 8887 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
1175 9078 44 None -1 2 Rat 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
1559 9078 44 None -1 2 Rat 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
657181 9078 44 None -1 2 Rat 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
CHEMBL1201199 9078 44 None -1 2 Rat 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
DB00007 9078 44 None -1 2 Rat 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
5583 7036 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19638591
10231401 8801 1 None 1 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 11551758
10231401 8801 1 None 1 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 12107234
5584 8801 1 None 1 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 11551758
5584 8801 1 None 1 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 12107234
CHEMBL314260 8801 1 None 1 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 11551758
CHEMBL314260 8801 1 None 1 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 12107234
10348973 10086 58 None -1 2 Human 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
10348973 10086 58 None 1 2 Rat 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
5432 10086 58 None -1 2 Human 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
5432 10086 58 None 1 2 Rat 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
5586 10086 58 None -1 2 Human 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
5586 10086 58 None 1 2 Rat 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
CHEMBL1800159 10086 58 None -1 2 Human 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
CHEMBL1800159 10086 58 None 1 2 Rat 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
DB11853 10086 58 None -1 2 Human 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
DB11853 10086 58 None 1 2 Rat 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
12394 9268 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 752 12 2 9 6.0 C1CN(CCC21c1c(CO2)n(c(=O)n(c1=O)C[C@@H](c1ccccc1)NCCCC(=O)O)Cc1c(cccc1F)C(F)(F)F)Cc1ccc(o1)C(F)(F)F 26321528
71727383 9268 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 752 12 2 9 6.0 C1CN(CCC21c1c(CO2)n(c(=O)n(c1=O)C[C@@H](c1ccccc1)NCCCC(=O)O)Cc1c(cccc1F)C(F)(F)F)Cc1ccc(o1)C(F)(F)F 26321528
1192 6935 47 None -9 4 Human 4.3 pIC50 None 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N 18344315
1794 6935 47 None -9 4 Human 4.3 pIC50 None 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N 18344315
CHEMBL501701 6935 47 None -9 4 Human 4.3 pIC50 None 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N 18344315
10279142 8407 0 None - 1 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 1 8 6.0 COc1nc(OC)c(c(n1)OC)NC(=O)c1ccc(o1)Oc1cc2c(cc1C)C(C)(C)C(CC2(C)C)C 18344315
1182 8407 0 None - 1 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 1 8 6.0 COc1nc(OC)c(c(n1)OC)NC(=O)c1ccc(o1)Oc1cc2c(cc1C)C(C)(C)C(CC2(C)C)C 18344315
1171 10361 0 None - 1 Human 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
118856782 10361 0 None - 1 Human 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1173 10670 0 None - 1 Human 6.7 pIC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1172 10646 0 None - 1 Human 7.0 pIC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
16130930 10646 0 None - 1 Human 7.0 pIC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1169 8589 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
123777 8589 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1162 8612 0 None -39 3 Rat 7.7 pIC50 None 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
16132914 8612 0 None -39 3 Rat 7.7 pIC50 None 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
1179 7748 36 None - 1 Human 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 17176055
9957278 7748 36 None - 1 Human 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 17176055
CHEMBL494803 7748 36 None - 1 Human 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 17176055
1162 8612 0 None -16 3 Mouse 8.3 pIC50 None 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1328228
16132914 8612 0 None -16 3 Mouse 8.3 pIC50 None 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1328228
1184 10505 36 None 2 2 Human 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 9784092
9874838 10505 36 None 2 2 Human 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 9784092
CHEMBL71917 10505 36 None 2 2 Human 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 9784092
1174 8168 0 None - 1 Mouse 9.9 pIC50 None 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1328228


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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44348326 103941 0 None - 0 Rat 10.3 pIC50 = 10.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC(=O)CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL268095 103941 0 None - 0 Rat 10.3 pIC50 = 10.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC(=O)CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
11563584 146326 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 630 10 2 7 6.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)NC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL379629 146326 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 630 10 2 7 6.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)NC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
10100930 70292 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800155 70292 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53388960 70342 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 682 11 2 9 6.0 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800663 70342 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 682 11 2 9 6.0 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
11692959 84889 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 612 10 2 7 6.5 CCOC(=O)c1cn(Cc2ccccc2F)c2sc(-c3ccc(NC(=O)NC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL210294 84889 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 612 10 2 7 6.5 CCOC(=O)c1cn(Cc2ccccc2F)c2sc(-c3ccc(NC(=O)NC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
10348973 10086 58 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 10086 58 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 10086 58 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 10086 58 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 10086 58 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
53387071 70294 5 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800157 70294 5 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL2370519 216646 0 None - 0 Rat 10.1 pIC50 = 10.1 Binding
Evaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptorsEvaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptors
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm010112g
53388958 70340 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 668 10 2 9 5.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800661 70340 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 668 10 2 9 5.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53389117 70345 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 688 11 2 9 4.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN2CCCC2=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800666 70345 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 688 11 2 9 4.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN2CCCC2=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL414239 168581 0 None - 0 Rat 10.1 pIC50 = 10.1 Binding
Evaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptorsEvaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptors
ChEMBL 1530 40 18 21 -1.6 CC(C)C[C@H](NC(=O)[C@H](CCCCNC(=O)CC/N=C1\C(=O)c2ccccc2C(O)=C1Cl)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NOC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm010112g
10258719 160020 0 None - 0 Human 10.0 pIC50 = 10 Binding
125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.
ChEMBL 650 12 2 10 4.8 CCOCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F nan
CHEMBL3977463 160020 0 None - 0 Human 10.0 pIC50 = 10 Binding
125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.
ChEMBL 650 12 2 10 4.8 CCOCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F nan
1185 10473 38 None - 1 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
3038517 10473 38 None - 1 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
CHEMBL22055 10473 38 None - 1 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
DB06494 10473 38 None - 1 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
9939837 84625 0 None - 0 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 651 9 2 7 6.6 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL2092994 84625 0 None - 0 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 651 9 2 7 6.6 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
9961721 175258 0 None - 1 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL435167 175258 0 None - 1 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
1185 10473 38 None - 1 Human 10.0 pIC50 = 10 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm701249f
3038517 10473 38 None - 1 Human 10.0 pIC50 = 10 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm701249f
CHEMBL22055 10473 38 None - 1 Human 10.0 pIC50 = 10 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm701249f
DB06494 10473 38 None - 1 Human 10.0 pIC50 = 10 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm701249f
44395650 176100 0 None - 0 Human 10.0 pIC50 = 10 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 537 7 3 8 4.9 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL441676 176100 0 None - 0 Human 10.0 pIC50 = 10 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 537 7 3 8 4.9 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
1185 10473 38 None - 1 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
3038517 10473 38 None - 1 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL22055 10473 38 None - 1 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
DB06494 10473 38 None - 1 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
53386915 70290 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800153 70290 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53389115 70343 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 698 11 3 10 5.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2cccc(CO)n2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800664 70343 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 698 11 3 10 5.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2cccc(CO)n2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
18324807 70347 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800668 70347 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
44293053 108269 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 602 13 3 4 6.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL297918 108269 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 602 13 3 4 6.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292838 108294 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 574 13 3 4 5.6 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL298074 108294 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 574 13 3 4 5.6 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292827 194967 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49891 194967 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
11700433 84385 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 675 11 1 6 8.5 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)c2ccccc2)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL208812 84385 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 675 11 1 6 8.5 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)c2ccccc2)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
11707186 85047 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 629 11 1 7 7.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL210709 85047 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 629 11 1 7 7.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
20691661 86388 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211485 86388 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
11512905 145196 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL377396 145196 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
155524081 177660 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1542 39 20 23 -4.2 CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)O[C@@H]1[C@@H](CO)O[C@@H](n2ccc(N)nc2=O)C1(F)F)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
CHEMBL4454362 177660 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1542 39 20 23 -4.2 CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)O[C@@H]1[C@@H](CO)O[C@@H](n2ccc(N)nc2=O)C1(F)F)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
10371708 70295 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800158 70295 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
44293177 181482 0 None - 0 Rat 9.9 pIC50 = 9.9 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 644 13 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45597 181482 0 None - 0 Rat 9.9 pIC50 = 9.9 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 644 13 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
67143119 182633 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 742 14 2 11 4.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCCCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4585638 182633 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 742 14 2 11 4.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCCCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143780 179031 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 637 9 1 8 4.7 CC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4474379 179031 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 637 9 1 8 4.7 CC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
67143102 179711 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 9 4.0 Cc1c(N2CCN(Cc3ccc(C#N)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4516712 179711 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 9 4.0 Cc1c(N2CCN(Cc3ccc(C#N)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143023 181776 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 656 9 2 10 4.2 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4566719 181776 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 656 9 2 10 4.2 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
9895596 70289 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F nan
CHEMBL1800152 70289 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F nan
1184 10505 36 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(02)00370-0
9874838 10505 36 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(02)00370-0
CHEMBL71917 10505 36 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(02)00370-0
1184 10505 36 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
9874838 10505 36 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
CHEMBL71917 10505 36 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
9875078 82704 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 680 11 1 8 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(OC)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL20511 82704 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 680 11 1 8 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(OC)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
9853275 86616 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 681 11 2 8 6.9 CCONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21217 86616 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 681 11 2 8 6.9 CCONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
9831689 105793 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 679 10 2 7 7.4 CC(C)NC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL280126 105793 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 679 10 2 7 7.4 CC(C)NC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
1184 10505 36 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm701249f
9874838 10505 36 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm701249f
CHEMBL71917 10505 36 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm701249f
23656390 168462 0 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1021/jm701249f
CHEMBL413245 168462 0 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1021/jm701249f
44321964 103194 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL261979 103194 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
9895596 70289 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800152 70289 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386916 70291 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 654 11 2 10 4.5 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(F)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800154 70291 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 654 11 2 10 4.5 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(F)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386917 70293 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800156 70293 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53388959 70341 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 668 10 2 9 5.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2cccnc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800662 70341 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 668 10 2 9 5.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2cccnc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53389118 70346 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 712 12 2 10 4.2 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN(C)S(C)(=O)=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800667 70346 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 712 12 2 10 4.2 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN(C)S(C)(=O)=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53386756 70348 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 617 13 2 10 3.6 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CCOC)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800669 70348 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 617 13 2 10 3.6 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CCOC)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386757 70349 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 631 14 2 10 4.0 CCOCCn1c(=O)c2c(CN(C)CCOC)c(-c3ccc(NC(=O)NOC)cc3)sc2n(Cc2c(F)cccc2F)c1=O 10.1021/jm200216q
CHEMBL1800670 70349 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 631 14 2 10 4.0 CCOCCn1c(=O)c2c(CN(C)CCOC)c(-c3ccc(NC(=O)NOC)cc3)sc2n(Cc2c(F)cccc2F)c1=O 10.1021/jm200216q
44293348 107268 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL290991 107268 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293075 97439 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 614 12 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL239108 97439 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 614 12 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
18914263 103676 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 630 15 3 4 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL265774 103676 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 630 15 3 4 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44214108 107893 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 656 13 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL295152 107893 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 656 13 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
21254068 108565 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 602 12 3 5 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL300045 108565 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 602 12 3 5 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293070 172874 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 616 15 3 4 7.0 CCN(CC)C(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL42592 172874 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 616 15 3 4 7.0 CCN(CC)C(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
18914272 176460 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 588 14 3 4 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL443768 176460 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 588 14 3 4 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
21254089 188436 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47761 188436 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292988 189220 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 586 12 3 4 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47862 189220 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 586 12 3 4 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
18914248 194510 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 602 15 3 4 6.4 CCN(CC)C(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL49542 194510 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 602 15 3 4 6.4 CCN(CC)C(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
1184 10505 36 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
9874838 10505 36 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
CHEMBL71917 10505 36 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
10794239 19836 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 643 11 1 7 7.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL1190107 19836 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 643 11 1 7 7.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL540109 19836 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 643 11 1 7 7.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
9809590 86412 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 641 11 1 6 8.1 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211503 86412 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 641 11 1 6 8.1 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
11643195 86604 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 2 7 7.2 CC(C)C(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)(C)O)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL212121 86604 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 2 7 7.2 CC(C)C(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)(C)O)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11628915 145003 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 629 11 2 7 6.5 CC(C)C(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)CO)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL377015 145003 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 629 11 2 7 6.5 CC(C)C(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)CO)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11512905 145196 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL377396 145196 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
1184 10505 36 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(01)00779-x
9874838 10505 36 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(01)00779-x
CHEMBL71917 10505 36 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(01)00779-x
1184 10505 36 None 426 2 Human 9.7 pIC50 = 9.7 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
9874838 10505 36 None 426 2 Human 9.7 pIC50 = 9.7 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
CHEMBL71917 10505 36 None 426 2 Human 9.7 pIC50 = 9.7 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
118074127 182496 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 714 12 2 11 3.9 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4582367 182496 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 714 12 2 11 3.9 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44348308 88763 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL216519 88763 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
53387071 70294 5 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800157 70294 5 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
44346805 175633 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Evaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptorsEvaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptors
ChEMBL 1565 40 20 23 -2.2 CC(C)C[C@H](NC(=O)[C@H](CCCCNCc1cc(O)c2c(c1)C(=O)c1cc(C(=O)O)cc(O)c1C2=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NOC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm010112g
91931800 175633 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Evaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptorsEvaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptors
ChEMBL 1565 40 20 23 -2.2 CC(C)C[C@H](NC(=O)[C@H](CCCCNCc1cc(O)c2c(c1)C(=O)c1cc(C(=O)O)cc(O)c1C2=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NOC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm010112g
CHEMBL438099 175633 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Evaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptorsEvaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptors
ChEMBL 1565 40 20 23 -2.2 CC(C)C[C@H](NC(=O)[C@H](CCCCNCc1cc(O)c2c(c1)C(=O)c1cc(C(=O)O)cc(O)c1C2=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NOC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm010112g
1175 9078 44 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL None None None None 10.1039/C5MD00259A
1559 9078 44 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL None None None None 10.1039/C5MD00259A
657181 9078 44 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL None None None None 10.1039/C5MD00259A
CHEMBL1201199 9078 44 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL None None None None 10.1039/C5MD00259A
DB00007 9078 44 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL None None None None 10.1039/C5MD00259A
145958346 168760 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 543 8 1 7 4.3 COc1ccc(F)cc1C(N)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4159155 168760 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 543 8 1 7 4.3 COc1ccc(F)cc1C(N)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
10100930 70292 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800155 70292 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
10985312 85521 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21126 85521 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
9896373 105825 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 694 11 1 8 7.4 COc1cccc(-n2c(=O)c3c(CN(C)Cc4ccccc4)c(-c4ccc(NC(=O)C(C)C)cc4)sc3n(Cc3c(F)cccc3F)c2=O)c1 10.1021/jm020180i
CHEMBL280365 105825 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 694 11 1 8 7.4 COc1cccc(-n2c(=O)c3c(CN(C)Cc4ccccc4)c(-c4ccc(NC(=O)C(C)C)cc4)sc3n(Cc3c(F)cccc3F)c2=O)c1 10.1021/jm020180i
44395623 131435 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 551 7 3 8 5.3 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL364167 131435 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 551 7 3 8 5.3 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
10053165 190778 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL48192 190778 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44321052 213050 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 578 9 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(O)nc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86912 213050 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 578 9 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(O)nc2)c1 10.1016/s0960-894x(01)00512-1
44340906 16343 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 578 9 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL112400 16343 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 578 9 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2)c1 10.1016/s0960-894x(02)00751-5
9985901 117230 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL324654 117230 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
1185 10473 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
53386758 70287 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 603 12 3 10 3.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CCO)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800150 70287 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 603 12 3 10 3.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CCO)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386914 70288 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 631 12 3 10 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CC(C)(C)O)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800151 70288 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 631 12 3 10 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CC(C)(C)O)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53389116 70344 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 672 11 2 11 4.6 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCn2ccnn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800665 70344 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 672 11 2 11 4.6 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCn2ccnn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
9895596 70289 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800152 70289 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386915 70290 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800153 70290 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
10009345 107696 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 642 11 2 8 5.8 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OC(C)C)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
CHEMBL293921 107696 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 642 11 2 8 5.8 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OC(C)C)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
44380643 65492 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 659 10 3 5 7.7 COC(=O)c1nc2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4ccc(C(C)(C)C(=O)N5CC6CCC5CC6)cc34)ccc2[nH]1 10.1016/s0960-894x(02)00026-4
CHEMBL168498 65492 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 659 10 3 5 7.7 COC(=O)c1nc2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4ccc(C(C)(C)C(=O)N5CC6CCC5CC6)cc34)ccc2[nH]1 10.1016/s0960-894x(02)00026-4
44380625 65500 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168538 65500 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
10008768 65508 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168563 65508 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
44380488 65790 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ocnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169238 65790 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ocnc3c2)c1 10.1016/s0960-894x(02)00026-4
9894997 127092 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352806 127092 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
44214098 108071 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL296483 108071 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293443 190830 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48224 190830 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293148 194265 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 524 12 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49412 194265 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 524 12 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
9936150 195515 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50500 195515 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293054 108272 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 603 14 3 5 6.8 CCOC(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL297927 108272 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 603 14 3 5 6.8 CCOC(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292977 181016 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 616 14 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45489 181016 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 616 14 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
1175 9078 44 None - 1 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm0512894
1559 9078 44 None - 1 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm0512894
657181 9078 44 None - 1 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm0512894
CHEMBL1201199 9078 44 None - 1 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm0512894
DB00007 9078 44 None - 1 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm0512894
44348321 103303 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1520 39 15 17 2.3 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](NC(=O)c2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL262825 103303 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1520 39 15 17 2.3 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](NC(=O)c2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348306 163772 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC(=O)CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL407316 163772 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC(=O)CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348399 168104 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](NC(C)=O)N(C)C(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL412472 168104 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](NC(C)=O)N(C)C(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348528 168706 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL415351 168706 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
10053165 190778 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/s0960-894x(00)00318-8
CHEMBL48192 190778 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/s0960-894x(00)00318-8
10053165 190778 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2003.12.101
CHEMBL48192 190778 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2003.12.101
9961721 175258 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL435167 175258 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
1175 9078 44 None - 1 Human 9.5 pIC50 = 9.5 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None None 10.1021/jm9803673
1559 9078 44 None - 1 Human 9.5 pIC50 = 9.5 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None None 10.1021/jm9803673
657181 9078 44 None - 1 Human 9.5 pIC50 = 9.5 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None None 10.1021/jm9803673
CHEMBL1201199 9078 44 None - 1 Human 9.5 pIC50 = 9.5 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None None 10.1021/jm9803673
DB00007 9078 44 None - 1 Human 9.5 pIC50 = 9.5 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None None 10.1021/jm9803673
67144164 180665 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 643 9 1 10 3.9 COC(=O)c1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)o1 10.1021/acs.jmedchem.6b01071
CHEMBL4539811 180665 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 643 9 1 10 3.9 COC(=O)c1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)o1 10.1021/acs.jmedchem.6b01071
9961721 175258 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 175258 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44395435 130590 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 523 7 3 8 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL362371 130590 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 523 7 3 8 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
67143710 177115 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccccc3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4447139 177115 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccccc3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
10348973 10086 58 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 10086 58 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 10086 58 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 10086 58 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 10086 58 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
10348973 10086 58 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 10086 58 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 10086 58 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 10086 58 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 10086 58 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
87285473 180869 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 663 8 1 7 5.6 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4544693 180869 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 663 8 1 7 5.6 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
145955571 169438 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 721 13 2 9 5.2 Cc1cc(F)cc([C@H](Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)NCCCC(=O)O)c1 10.1016/j.ejmech.2017.12.095
CHEMBL4169891 169438 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 721 13 2 9 5.2 Cc1cc(F)cc([C@H](Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)NCCCC(=O)O)c1 10.1016/j.ejmech.2017.12.095
10348973 10086 58 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 10086 58 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 10086 58 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 10086 58 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 10086 58 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
67144353 179002 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 673 9 1 9 4.0 Cc1c(N2CCN(Cc3cccc(S(C)(=O)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4474058 179002 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 673 9 1 9 4.0 Cc1c(N2CCN(Cc3cccc(S(C)(=O)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
145954246 169187 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 529 7 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3Cl)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4165983 169187 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 529 7 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3Cl)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44348533 168519 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL413752 168519 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)cc1 10.1021/jm970024p
67143773 177284 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 619 8 1 8 4.8 Cc1c(N2CCN(Cc3ccc(Cl)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449450 177284 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 619 8 1 8 4.8 Cc1c(N2CCN(Cc3ccc(Cl)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143621 178082 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 653 9 1 9 4.3 COC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4460880 178082 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 653 9 1 9 4.3 COC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
87285554 180109 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 631 8 1 7 4.8 Cc1c(N2CCN(Cc3cccc(F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4526641 180109 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 631 8 1 7 4.8 Cc1c(N2CCN(Cc3cccc(F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
9917618 105418 1 None - 0 Human 9.4 pIC50 = 9.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 653 9 3 8 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NO)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm020180i
CHEMBL277214 105418 1 None - 0 Human 9.4 pIC50 = 9.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 653 9 3 8 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NO)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm020180i
10919567 105806 0 None - 1 Human 9.4 pIC50 = 9.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 664 10 1 7 7.4 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL280213 105806 0 None - 1 Human 9.4 pIC50 = 9.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 664 10 1 7 7.4 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44321963 112718 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 622 11 2 5 6.8 COCn1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccc1=O 10.1016/s0960-894x(01)00512-1
CHEMBL312864 112718 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 622 11 2 5 6.8 COCn1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccc1=O 10.1016/s0960-894x(01)00512-1
44321411 113786 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@@H]5CC[C@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL315326 113786 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@@H]5CC[C@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321345 213021 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 596 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCC2CCC(=O)N(C)C2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86758 213021 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 596 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCC2CCC(=O)N(C)C2)c1 10.1016/s0960-894x(01)00512-1
44293163 195479 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Compound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptorCompound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50433 195479 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Compound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptorCompound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44341082 16549 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 590 9 2 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)nc(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL113574 16549 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 590 9 2 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)nc(C)c2)c1 10.1016/s0960-894x(02)00751-5
44341046 16848 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 634 11 2 5 7.5 CC(=O)OCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL115365 16848 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 634 11 2 5 7.5 CC(=O)OCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
44340888 117302 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 592 10 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(CO)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL325091 117302 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 592 10 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(CO)c2)c1 10.1016/s0960-894x(02)00751-5
1185 10473 38 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
9895731 210217 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 644 11 2 9 5.4 CONC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OC(C)C)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
CHEMBL65769 210217 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 644 11 2 9 5.4 CONC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OC(C)C)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
9873212 64350 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166649 64350 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
9938925 64365 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 616 11 3 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166763 64365 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 616 11 3 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
44380626 65501 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 587 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168539 65501 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 587 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
44380537 103336 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL263004 103336 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
44380394 126726 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 601 9 3 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL349638 126726 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 601 9 3 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44380514 126990 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 645 10 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(=O)O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352051 126990 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 645 10 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(=O)O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
9809394 127290 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 628 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL354524 127290 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 628 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
44292940 108041 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296244 108041 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293651 169893 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL417726 169893 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293335 179406 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL449351 179406 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293349 190903 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL48273 190903 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
10258643 108160 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 644 16 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL297151 108160 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 644 16 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293178 108199 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 658 17 3 4 7.9 CCCN(CCC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL297430 108199 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 658 17 3 4 7.9 CCCN(CCC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293074 194562 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 612 12 3 4 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49578 194562 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 612 12 3 4 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
11614283 84900 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 627 11 1 6 7.9 CCC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL210321 84900 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 627 11 1 6 7.9 CCC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11592777 146031 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 643 11 2 6 8.0 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL378979 146031 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 643 11 2 6 8.0 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
44413067 146078 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 593 11 1 7 6.9 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL379198 146078 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 593 11 1 7 6.9 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44352512 124077 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 483 7 3 7 4.7 Cc1cc(-c2c(O)nc3ccc(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(01)00779-x
CHEMBL339636 124077 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 483 7 3 7 4.7 Cc1cc(-c2c(O)nc3ccc(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(01)00779-x
67143509 176844 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3cccc(C#N)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4443108 176844 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3cccc(C#N)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44348324 164057 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL407681 164057 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44309572 211118 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 517 7 3 7 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(02)00370-0
CHEMBL71561 211118 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 517 7 3 7 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(02)00370-0
10649568 21338 0 None 10 2 Human 9.4 pIC50 = 9.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL120432 21338 0 None 10 2 Human 9.4 pIC50 = 9.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/j.bmcl.2004.08.056
87285768 177274 3 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 177274 3 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
10649568 21338 0 None 10 2 Human 9.4 pIC50 = 9.4 Binding
In vitro inhibition of binding to GnRH receptor in humanIn vitro inhibition of binding to GnRH receptor in human
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 21338 0 None 10 2 Human 9.4 pIC50 = 9.4 Binding
In vitro inhibition of binding to GnRH receptor in humanIn vitro inhibition of binding to GnRH receptor in human
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
10649568 21338 0 None 10 2 Human 9.4 pIC50 = 9.4 Binding
Inhibition of Human gonadotropin-releasing hormone receptorInhibition of Human gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm049218c
CHEMBL120432 21338 0 None 10 2 Human 9.4 pIC50 = 9.4 Binding
Inhibition of Human gonadotropin-releasing hormone receptorInhibition of Human gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm049218c
67142732 176402 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 640 9 1 9 4.5 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4436854 176402 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 640 9 1 9 4.5 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
145949496 169637 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 685 13 2 9 4.9 Cc1cccc(F)c1Cn1c(C)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4173065 169637 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 685 13 2 9 4.9 Cc1cccc(F)c1Cn1c(C)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL2370593 216655 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](N)C(N)=O)cc1 10.1021/jm970024p
44460342 174701 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 9 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL431402 174701 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 9 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
1185 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
18324807 70347 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800668 70347 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
1185 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 10473 38 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
10649568 21338 0 None 10 2 Human 9.3 pIC50 = 9.3 Binding
In vitro inhibition of gonadotropin-releasing hormone receptor in rhesus monkeyIn vitro inhibition of gonadotropin-releasing hormone receptor in rhesus monkey
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 21338 0 None 10 2 Human 9.3 pIC50 = 9.3 Binding
In vitro inhibition of gonadotropin-releasing hormone receptor in rhesus monkeyIn vitro inhibition of gonadotropin-releasing hormone receptor in rhesus monkey
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
9809382 107451 0 None - 1 Human 9.3 pIC50 = 9.3 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 628 11 2 8 5.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
CHEMBL292291 107451 0 None - 1 Human 9.3 pIC50 = 9.3 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 628 11 2 8 5.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
44380538 65859 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 619 9 2 5 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3nsnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169620 65859 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 619 9 2 5 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3nsnc3c2)c1 10.1016/s0960-894x(02)00026-4
44293591 108373 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298700 108373 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293129 188515 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL47772 188515 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293213 194580 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 494 10 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49590 194580 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 494 10 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293071 108378 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 589 14 3 5 6.6 CCOC(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL298748 108378 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 589 14 3 5 6.6 CCOC(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293366 168990 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 511 12 3 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL416285 168990 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 511 12 3 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
1175 9078 44 None - 1 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
1559 9078 44 None - 1 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
657181 9078 44 None - 1 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
CHEMBL1201199 9078 44 None - 1 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
DB00007 9078 44 None - 1 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
CHEMBL2370590 216653 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)CCNC(C)C)cc1 10.1021/jm970024p
44293205 190740 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 643 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)ccc1I 10.1016/s0960-894x(00)00318-8
CHEMBL48165 190740 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 643 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)ccc1I 10.1016/s0960-894x(00)00318-8
44295699 107998 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C)N2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL295948 107998 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C)N2)c1 10.1016/j.bmcl.2003.12.101
9828888 108602 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@@H](C)N2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL300295 108602 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@@H](C)N2)c1 10.1016/j.bmcl.2003.12.101
1175 9078 44 None - 1 Rat 9.3 pIC50 = 9.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None None 10.1021/jm9803673
1559 9078 44 None - 1 Rat 9.3 pIC50 = 9.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None None 10.1021/jm9803673
657181 9078 44 None - 1 Rat 9.3 pIC50 = 9.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None None 10.1021/jm9803673
CHEMBL1201199 9078 44 None - 1 Rat 9.3 pIC50 = 9.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None None 10.1021/jm9803673
DB00007 9078 44 None - 1 Rat 9.3 pIC50 = 9.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None None 10.1021/jm9803673
44348325 103384 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@@H](NC(=O)c2ccc(NC(C)=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL263358 103384 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@@H](NC(=O)c2ccc(NC(C)=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL2370592 216654 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)CC(C)C)cc1 10.1021/jm970024p
44395462 175002 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 551 7 3 8 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL433594 175002 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 551 7 3 8 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
10371708 70295 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800158 70295 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
155531714 182970 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL4593521 182970 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
58239302 168769 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 577 12 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(C)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4159247 168769 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 577 12 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(C)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
11167850 9518 28 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
1178 9518 28 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
1187 9518 28 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL179691 9518 28 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
11167850 9518 28 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
1178 9518 28 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
1187 9518 28 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL179691 9518 28 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
44348454 163999 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 42 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](NC=O)C(N)=O)cc1 10.1021/jm970024p
CHEMBL407615 163999 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 42 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](NC=O)C(N)=O)cc1 10.1021/jm970024p
1184 10505 36 None -426 2 Rat 9.2 pIC50 = 9.2 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(02)00370-0
9874838 10505 36 None -426 2 Rat 9.2 pIC50 = 9.2 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(02)00370-0
CHEMBL71917 10505 36 None -426 2 Rat 9.2 pIC50 = 9.2 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(02)00370-0
9896737 90142 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 695 11 2 8 7.3 CC(C)ONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21936 90142 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 695 11 2 8 7.3 CC(C)ONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
9893269 73070 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 532 7 2 7 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL184819 73070 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 532 7 2 7 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
10187208 73522 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 540 7 2 9 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2OCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185785 73522 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 540 7 2 9 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2OCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44395533 73572 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 577 7 2 8 6.5 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CC3CCN2CC3)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185986 73572 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 577 7 2 8 6.5 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CC3CCN2CC3)cc(C)c1C 10.1016/j.bmcl.2004.08.056
10231401 8801 1 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1016/s0960-894x(01)00512-1
5584 8801 1 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1016/s0960-894x(01)00512-1
CHEMBL314260 8801 1 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1016/s0960-894x(01)00512-1
44321148 103583 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 622 11 2 5 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CC4)OCCO5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL265042 103583 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 622 11 2 5 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CC4)OCCO5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44320895 171041 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccnc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL421160 171041 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccnc2)c1 10.1016/s0960-894x(01)00512-1
44321393 213049 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 606 9 2 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)c(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86911 213049 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 606 9 2 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)c(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
44340928 16516 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 10 3 4 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL113432 16516 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 10 3 4 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
44340929 120279 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 604 10 2 4 7.7 CC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL332049 120279 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 604 10 2 4 7.7 CC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
1185 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
67143618 177074 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 637 8 1 10 4.1 Cc1c(N2CCN(Cc3cccc4nonc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4446435 177074 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 637 8 1 10 4.1 Cc1c(N2CCN(Cc3cccc4nonc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
9960399 57316 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 603 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3nnnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL157412 57316 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 603 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3nnnc-3c2)c1 10.1016/s0960-894x(02)00026-4
44380512 64207 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 617 9 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL165456 64207 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 617 9 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44380236 65495 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 641 11 2 4 8.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168506 65495 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 641 11 2 4 8.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
44380796 65977 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 598 9 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL170159 65977 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 598 9 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
44380798 66100 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 3 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL170606 66100 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 3 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
44380536 127169 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 602 9 2 4 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL353395 127169 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 602 9 2 4 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
44293273 168871 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL416102 168871 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44293592 169669 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL417363 169669 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44292918 178194 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL44627 178194 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293134 194180 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49366 194180 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293411 195547 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 494 10 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50552 195547 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 494 10 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44412890 85085 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 607 11 1 7 7.2 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL210888 85085 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 607 11 1 7 7.2 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44295753 193525 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 559 7 3 7 6.5 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C)N2)cc(C)c1C 10.1016/j.bmcl.2003.12.101
CHEMBL48879 193525 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 559 7 3 7 6.5 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C)N2)cc(C)c1C 10.1016/j.bmcl.2003.12.101
1185 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
3038517 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
CHEMBL22055 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
DB06494 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
44348453 103894 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 42 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](NC=O)C(N)=O)cc1 10.1021/jm970024p
CHEMBL267642 103894 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 42 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](NC=O)C(N)=O)cc1 10.1021/jm970024p
44348316 103305 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)c2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL262842 103305 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)c2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348148 163529 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1545 41 14 16 3.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL407058 163529 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1545 41 14 16 3.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348527 168612 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL414558 168612 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL2370594 216656 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C(N)=O)N(C)C=O)cc1 10.1021/jm970024p
87285708 180684 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 749 13 2 8 6.1 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4540232 180684 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 749 13 2 8 6.1 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
155517188 176942 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1542 39 20 23 -4.2 CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)OC[C@H]1O[C@@H](n2ccc(N)nc2=O)C(F)(F)[C@@H]1O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
CHEMBL4444427 176942 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1542 39 20 23 -4.2 CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)OC[C@H]1O[C@@H](n2ccc(N)nc2=O)C(F)(F)[C@@H]1O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
44395502 172677 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 553 7 3 9 5.0 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2COCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL424991 172677 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 553 7 3 9 5.0 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2COCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
9808288 118258 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL327704 118258 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321498 213084 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL87099 213084 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44341197 115812 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 587 9 2 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C#N)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL321258 115812 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 587 9 2 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C#N)c2)c1 10.1016/s0960-894x(02)00751-5
44341198 119835 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 620 10 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL331144 119835 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 620 10 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
44460343 212124 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 11 2 4 7.6 COCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL79639 212124 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 11 2 4 7.6 COCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
11167850 9518 28 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 10473 38 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44305285 107394 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 630 11 2 9 5.0 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NOC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL291896 107394 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 630 11 2 9 5.0 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NOC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
44380478 65529 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168637 65529 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
44380483 65849 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 635 9 4 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2F)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169569 65849 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 635 9 4 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2F)c1 10.1016/s0960-894x(02)00026-4
9808288 118258 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL327704 118258 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(02)00026-4
44380513 126969 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 631 10 4 4 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(CO)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL351836 126969 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 631 10 4 4 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(CO)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44292919 107922 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295376 107922 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293650 169108 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL416470 169108 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293045 192603 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 543 7 3 7 5.7 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3ccc4c(c3)CCC4)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL48674 192603 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 543 7 3 7 5.7 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3ccc4c(c3)CCC4)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44293206 193968 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1ccc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
CHEMBL49230 193968 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1ccc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
145955844 169471 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 527 7 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cc(C)cc(F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4170478 169471 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 527 7 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cc(C)cc(F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44348534 168605 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1533 37 16 17 -0.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)NC(NC(=O)CN=C(N)N)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
91935482 168605 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1533 37 16 17 -0.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)NC(NC(=O)CN=C(N)N)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL414469 168605 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1533 37 16 17 -0.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)NC(NC(=O)CN=C(N)N)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348307 168604 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](NC(=O)c2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL414468 168604 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](NC(=O)c2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44395491 130628 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 531 7 3 7 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL362544 130628 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 531 7 3 7 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44321412 213031 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 590 11 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86805 213031 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 590 11 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321290 213185 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 548 9 2 3 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL87785 213185 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 548 9 2 3 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44341164 16336 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2C)c1 10.1016/s0960-894x(02)00751-5
CHEMBL112378 16336 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2C)c1 10.1016/s0960-894x(02)00751-5
44341056 121312 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2C)c1 10.1016/s0960-894x(02)00751-5
CHEMBL333614 121312 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2C)c1 10.1016/s0960-894x(02)00751-5
1185 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
1185 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL None None None None 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
53386917 70293 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800156 70293 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
71449058 91181 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2111955 91181 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2219718 91181 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44380222 64369 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 614 10 2 5 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166778 64369 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 614 10 2 5 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
44293605 107950 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295591 107950 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44292874 190619 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 616 13 3 4 7.2 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)(C)C 10.1016/s0960-894x(01)00274-8
CHEMBL48069 190619 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 616 13 3 4 7.2 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)(C)C 10.1016/s0960-894x(01)00274-8
1175 9078 44 None - 1 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
1559 9078 44 None - 1 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
657181 9078 44 None - 1 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
CHEMBL1201199 9078 44 None - 1 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
DB00007 9078 44 None - 1 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
1175 9078 44 None - 1 Rat 9.1 pIC50 = 9.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None None 10.1021/jm9803673
1559 9078 44 None - 1 Rat 9.1 pIC50 = 9.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None None 10.1021/jm9803673
657181 9078 44 None - 1 Rat 9.1 pIC50 = 9.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None None 10.1021/jm9803673
CHEMBL1201199 9078 44 None - 1 Rat 9.1 pIC50 = 9.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None None 10.1021/jm9803673
DB00007 9078 44 None - 1 Rat 9.1 pIC50 = 9.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None None 10.1021/jm9803673
44348056 166797 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1545 41 14 16 3.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL410798 166797 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1545 41 14 16 3.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348400 175472 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)NC(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL436683 175472 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)NC(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44395583 131124 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 524 7 2 8 5.8 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL363663 131124 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 524 7 2 8 5.8 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44341113 16693 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL114438 16693 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C)c2)c1 10.1016/s0960-894x(02)00751-5
44341199 119836 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 620 10 2 5 7.2 COC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL331145 119836 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 620 10 2 5 7.2 COC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
9961721 175258 0 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 175258 0 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
11167850 9518 28 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44295755 199900 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2111956 199900 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL52278 199900 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44380681 65548 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 669 9 3 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(F)(F)F)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168726 65548 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 669 9 3 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(F)(F)F)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44380147 127056 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352566 127056 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
20691661 86388 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211485 86388 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
44348057 103232 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1559 41 13 16 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL262309 103232 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1559 41 13 16 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL2370589 216652 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL None None None CN[C@@H](NC(=O)[C@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm970024p
44293222 182739 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL138464 182739 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL45883 182739 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44295755 199900 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL2111956 199900 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL52278 199900 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
67143518 181653 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4563562 181653 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
87285476 178246 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 653 8 1 8 5.2 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4463476 178246 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 653 8 1 8 5.2 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11017929 105797 0 None - 0 Human 9.0 pIC50 = 9 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 624 9 1 8 6.4 COc1cccc(-n2c(=O)c3c(CN(C)Cc4ccccc4)c(-c4ccc(N)cc4)sc3n(Cc3c(F)cccc3F)c2=O)c1 10.1021/jm020180i
CHEMBL280170 105797 0 None - 0 Human 9.0 pIC50 = 9 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 624 9 1 8 6.4 COc1cccc(-n2c(=O)c3c(CN(C)Cc4ccccc4)c(-c4ccc(N)cc4)sc3n(Cc3c(F)cccc3F)c2=O)c1 10.1021/jm020180i
10930638 105805 0 None - 0 Human 9.0 pIC50 = 9 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm020180i
CHEMBL280212 105805 0 None - 0 Human 9.0 pIC50 = 9 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm020180i
44321101 103623 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL265288 103623 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321394 113716 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 10 2 4 7.5 COc1ccc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)cn1 10.1016/s0960-894x(01)00512-1
CHEMBL314860 113716 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 10 2 4 7.5 COc1ccc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)cn1 10.1016/s0960-894x(01)00512-1
44321410 113785 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL315325 113785 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
11167850 9518 28 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
87285565 177048 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 679 9 1 8 5.4 Cc1c(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4446131 177048 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 679 9 1 8 5.4 Cc1c(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143755 182205 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccccc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4576169 182205 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccccc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
9961721 175258 0 None - 1 Human 9.0 pIC50 = 9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 175258 0 None - 1 Human 9.0 pIC50 = 9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44293377 108680 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 576 12 2 3 7.8 CCC(C)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL300865 108680 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 576 12 2 3 7.8 CCC(C)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293347 169890 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 11 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL417720 169890 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 11 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44412945 103481 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 641 11 1 7 7.8 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)c4ccccc4)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL264121 103481 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 641 11 1 7 7.8 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)c4ccccc4)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44293386 182311 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 571 7 3 7 6.5 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3ccc(Cl)c(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL45784 182311 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 571 7 3 7 6.5 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3ccc(Cl)c(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
67143613 177805 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cccnc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4456703 177805 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cccnc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
22129998 108052 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Compound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptorCompound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptor
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL296321 108052 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Compound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptorCompound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptor
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
11167850 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL None None None None 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 10473 38 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
87285570 177521 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 631 8 1 7 4.8 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4452347 177521 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 631 8 1 7 4.8 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
67143804 179975 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 724 13 3 9 4.1 Cc1c(N2CCN(Cc3cccc(C(=O)NCCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4522657 179975 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 724 13 3 9 4.1 Cc1c(N2CCN(Cc3cccc(C(=O)NCCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
87285767 181656 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 775 13 2 10 5.1 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCS(=O)(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4563686 181656 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 775 13 2 10 5.1 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCS(=O)(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
9961721 175258 0 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 175258 0 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44380146 127055 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 627 10 2 4 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352565 127055 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 627 10 2 4 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
44380318 127157 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL353308 127157 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
44380487 174358 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]ncc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL430069 174358 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]ncc3c2)c1 10.1016/s0960-894x(02)00026-4
44292950 169224 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cnccn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL416651 169224 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cnccn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44292868 183686 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 571 7 3 7 6.5 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3cc(Cl)cc(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL46177 183686 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 571 7 3 7 6.5 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3cc(Cl)cc(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
67143547 178295 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccc(C#N)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4464132 178295 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccc(C#N)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44320921 113946 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 548 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL316362 113946 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 548 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
11167850 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
67143761 178140 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 710 12 3 9 3.8 Cc1c(N2CCN(Cc3cccc(C(=O)NCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4461692 178140 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 710 12 3 9 3.8 Cc1c(N2CCN(Cc3cccc(C(=O)NCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
87285550 181107 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 775 13 3 9 5.4 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCP(=O)(O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4550720 181107 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 775 13 3 9 5.4 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCP(=O)(O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
1185 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44293555 107987 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 574 11 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C4(C(=O)N5C6CCC5CC6)CCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295897 107987 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 574 11 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C4(C(=O)N5C6CCC5CC6)CCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44348297 174245 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2ccc(Cl)cc2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL429902 174245 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2ccc(Cl)cc2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
145953172 169251 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 563 7 1 6 5.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cc(Cl)cc(Cl)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4167067 169251 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 563 7 1 6 5.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cc(Cl)cc(Cl)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL415547 219968 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
67143505 179009 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 601 8 1 8 4.6 Cc1c(N2CCN(Cc3cccs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4474116 179009 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 601 8 1 8 4.6 Cc1c(N2CCN(Cc3cccs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44321146 113182 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC(C)(C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL313946 113182 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC(C)(C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL3085508 217768 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 10473 38 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
3038517 10473 38 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL22055 10473 38 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
DB06494 10473 38 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL415547 219968 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
44395677 73512 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 565 7 2 8 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185738 73512 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 565 7 2 8 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44293249 192222 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL48616 192222 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321509 212968 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CCCC[C@H]5C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86431 212968 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CCCC[C@H]5C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
11167850 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44359285 18399 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180695 18399 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138747 18399 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293249 192222 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48616 192222 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44215053 192399 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48641 192399 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44348149 175497 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)c2ccncc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL436897 175497 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)c2ccncc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
67143570 178536 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 726 14 2 10 5.0 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4467407 178536 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 726 14 2 10 5.0 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
23656390 168462 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1021/jm701249f
CHEMBL413245 168462 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1021/jm701249f
11167850 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL None None None None 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
67142962 181355 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 629 9 1 8 4.6 Cc1c(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4556717 181355 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 629 9 1 8 4.6 Cc1c(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44380797 66066 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL170499 66066 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
44215055 108067 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 576 11 1 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(C)CCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL296442 108067 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 576 11 1 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(C)CCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44593425 183544 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1021/jm701249f
CHEMBL460480 183544 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1021/jm701249f
11167850 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 10473 38 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
3038517 10473 38 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL22055 10473 38 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
DB06494 10473 38 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
70689073 84401 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1835 43 23 28 -2.7 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
91900370 84401 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1835 43 23 28 -2.7 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL2088253 84401 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1835 43 23 28 -2.7 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
155531714 182970 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL4593521 182970 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
10231401 8801 1 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity at rat GnRH receptor by whole cell binding assayBinding affinity at rat GnRH receptor by whole cell binding assay
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1021/jm701249f
5584 8801 1 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity at rat GnRH receptor by whole cell binding assayBinding affinity at rat GnRH receptor by whole cell binding assay
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1021/jm701249f
CHEMBL314260 8801 1 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity at rat GnRH receptor by whole cell binding assayBinding affinity at rat GnRH receptor by whole cell binding assay
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1021/jm701249f
44593425 183544 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2009.02.043
CHEMBL460480 183544 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2009.02.043
44593425 183544 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
CHEMBL460480 183544 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
11167850 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
67144370 181394 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3cccc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4557575 181394 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3cccc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44293488 108331 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL298366 108331 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293376 108452 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 590 13 2 3 8.2 CCC(CC)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL299301 108452 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 590 13 2 3 8.2 CCC(CC)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44348172 162531 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1547 39 14 17 1.8 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(C)=O)cc1 10.1021/jm970024p
CHEMBL405736 162531 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1547 39 14 17 1.8 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(C)=O)cc1 10.1021/jm970024p
44402640 168609 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1617 41 17 17 2.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C2CCNC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1016/j.bmcl.2005.03.085
CHEMBL414514 168609 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1617 41 17 17 2.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C2CCNC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1016/j.bmcl.2005.03.085
11167850 9518 28 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 10473 38 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
87285770 182823 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 803 15 2 10 6.4 CCOP(=O)(O)CCCN[C@@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1021/acs.jmedchem.6b01071
CHEMBL4590493 182823 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 803 15 2 10 6.4 CCOP(=O)(O)CCCN[C@@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1021/acs.jmedchem.6b01071
11620431 186148 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL473807 186148 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44359264 18400 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180700 18400 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138866 18400 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293802 108809 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 11 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL301802 108809 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 11 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293081 189483 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL47895 189483 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44402639 162008 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1603 41 16 17 2.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CCC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL402671 162008 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1603 41 16 17 2.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CCC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
164628446 193091 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-DTrp6-LHRH from human GnRH-R by radioligand binding assayDisplacement of [125I]-DTrp6-LHRH from human GnRH-R by radioligand binding assay
ChEMBL 1627 43 20 26 -5.2 CC(C)CC(NC(=O)C(CCCCNC(=O)/C=N/OCC(=O)OCC1OC(n2ccc(N)nc2=O)C(F)(F)C1O)NC(=O)C(Cc1ccc(O)cc1)NC(=O)C(CO)NC(=O)C(Cc1cc2ccccc2[nH]1)NC(=O)C(Cc1c[nH]cn1)NC(=O)C1CCC(=O)N1)C(=O)NC(CCCNC(=N)N)C(=O)N1CCCC1C(=O)NCC(N)=O 10.1016/j.ejmech.2020.113018
CHEMBL4874610 193091 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-DTrp6-LHRH from human GnRH-R by radioligand binding assayDisplacement of [125I]-DTrp6-LHRH from human GnRH-R by radioligand binding assay
ChEMBL 1627 43 20 26 -5.2 CC(C)CC(NC(=O)C(CCCCNC(=O)/C=N/OCC(=O)OCC1OC(n2ccc(N)nc2=O)C(F)(F)C1O)NC(=O)C(Cc1ccc(O)cc1)NC(=O)C(CO)NC(=O)C(Cc1cc2ccccc2[nH]1)NC(=O)C(Cc1c[nH]cn1)NC(=O)C1CCC(=O)N1)C(=O)NC(CCCNC(=N)N)C(=O)N1CCCC1C(=O)NCC(N)=O 10.1016/j.ejmech.2020.113018
CHEMBL436874 220468 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL None None None None 10.1021/jm0506928
1185 10473 38 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 10473 38 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 10473 38 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 10473 38 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 10473 38 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 10473 38 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
10438167 107959 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 578 12 2 3 8.6 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL295641 107959 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 578 12 2 3 8.6 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCCCC1 10.1016/s0960-894x(01)00275-x
44380319 65524 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168615 65524 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
44348174 166823 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)c2ccc(NC(C)=O)cc2)cc1 10.1021/jm970024p
CHEMBL410818 166823 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)c2ccc(NC(C)=O)cc2)cc1 10.1021/jm970024p
67143612 177829 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 638 9 2 8 3.6 Cc1c(N2CCN(Cc3cccc(C(N)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4456937 177829 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 638 9 2 8 3.6 Cc1c(N2CCN(Cc3cccc(C(N)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44402639 162008 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1603 41 16 17 2.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CCC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL402671 162008 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1603 41 16 17 2.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CCC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
44402518 165305 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL409138 165305 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
44402640 168609 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1617 41 17 17 2.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C2CCNC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1016/j.bmcl.2005.03.085
CHEMBL414514 168609 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1617 41 17 17 2.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C2CCNC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1016/j.bmcl.2005.03.085
91810333 186357 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 7 1 4 5.4 C=CCC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCN(C(C)=O)CC2 10.1021/acs.jmedchem.0c01076
CHEMBL4741994 186357 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 7 1 4 5.4 C=CCC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCN(C(C)=O)CC2 10.1021/acs.jmedchem.0c01076
118179218 186794 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 565 5 1 4 5.1 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccc(F)c3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4747248 186794 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 565 5 1 4 5.1 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccc(F)c3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
10004181 107863 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL294910 107863 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(99)00447-3
44573110 193973 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL492327 193973 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
44573113 200017 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
CHEMBL523711 200017 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
1185 10473 38 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44406776 141120 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44577104 185525 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL468565 185525 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
67143054 177068 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 581 8 1 7 3.9 Cc1c(N2CCN(Cc3cccc(F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4446360 177068 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 581 8 1 7 3.9 Cc1c(N2CCN(Cc3cccc(F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
53239181 179283 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 570 8 1 8 3.5 Cc1c(N2CCN(Cc3ccc(C#N)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4483419 179283 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 570 8 1 8 3.5 Cc1c(N2CCN(Cc3ccc(C#N)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
1185 10473 38 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 10473 38 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 10473 38 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 10473 38 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44305605 210110 0 None - 0 Human 8.0 pIC50 = 8 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 613 11 1 8 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL64920 210110 0 None - 0 Human 8.0 pIC50 = 8 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 613 11 1 8 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
11214294 128973 0 None 912 2 Human 8.0 pIC50 = 8 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL359754 128973 0 None 912 2 Human 8.0 pIC50 = 8 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL438652 220564 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm0512894
44293111 107995 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295917 107995 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
10004181 107863 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL294910 107863 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
15895698 213658 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL90725 213658 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
11980076 215232 29 None - 1 Human 8.0 pIC50 = 8 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm9803673
CHEMBL1007 215232 29 None - 1 Human 8.0 pIC50 = 8 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm9803673
CHEMBL436874 220468 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL None None None None 10.1021/jm0506928
CHEMBL448249 220734 14 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
CHEMBL436874 220468 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL None None None None 10.1021/jm0506928
44406776 141120 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 141120 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44359456 18976 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 572 8 3 6 7.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccc(N(C)C)cc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184286 18976 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 572 8 3 6 7.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccc(N(C)C)cc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL342908 18976 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 572 8 3 6 7.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccc(N(C)C)cc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44322384 112916 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 441 6 2 6 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL313501 112916 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 441 6 2 6 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCN2)c1 10.1016/s0960-894x(99)00447-3
44365638 48698 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 518 12 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(OCc4ccccc4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL149441 48698 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 518 12 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(OCc4ccccc4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
44214104 128534 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 540 10 4 5 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCNCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL358901 128534 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 540 10 4 5 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCNCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
44444617 100920 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 656 8 2 5 7.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N(C)C)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249372 100920 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 656 8 2 5 7.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N(C)C)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
10930638 105805 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 105805 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44322165 212996 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 458 5 1 4 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(C(F)(F)F)ccc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL86609 212996 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 458 5 1 4 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(C(F)(F)F)ccc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
11599857 83653 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 597 11 0 9 6.5 CCOC(=O)c1cn(Cc2ccccc2[N+](=O)[O-])c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL206964 83653 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 597 11 0 9 6.5 CCOC(=O)c1cn(Cc2ccccc2[N+](=O)[O-])c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11520078 86500 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 577 10 0 8 6.5 CCOC(=O)c1cn(Cc2ccccc2C#N)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL211588 86500 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 577 10 0 8 6.5 CCOC(=O)c1cn(Cc2ccccc2C#N)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44365131 45297 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 472 13 3 4 6.5 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL146451 45297 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 472 13 3 4 6.5 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44364998 47227 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 443 11 3 4 5.6 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(N)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL148246 47227 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 443 11 3 4 5.6 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(N)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
10808668 213399 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 362 4 1 4 5.2 Oc1nc2cc(Cl)ccc2c(OCc2ccccn2)c1-c1ccccc1 10.1016/s0960-894x(99)00446-1
CHEMBL89086 213399 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 362 4 1 4 5.2 Oc1nc2cc(Cl)ccc2c(OCc2ccccn2)c1-c1ccccc1 10.1016/s0960-894x(99)00446-1
10837806 84801 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 463 7 0 7 5.3 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(C)c2c1=O 10.1021/jm0512894
CHEMBL209836 84801 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 463 7 0 7 5.3 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(C)c2c1=O 10.1021/jm0512894
162653870 187322 0 None - 0 Human 5.0 pIC50 = 5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 489 4 1 4 3.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(C)(=O)=O)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4753775 187322 0 None - 0 Human 5.0 pIC50 = 5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 489 4 1 4 3.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(C)(=O)=O)C2C 10.1021/acs.jmedchem.0c01076
44406776 141120 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44444642 101145 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 629 8 1 6 5.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250770 101145 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 629 8 1 6 5.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67142732 176402 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 640 9 1 9 4.5 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4436854 176402 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 640 9 1 9 4.5 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44417615 148701 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 148701 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
67143815 178319 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 651 8 1 8 5.8 Cc1c(N2CCN(Cc3cccc4ccsc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4464440 178319 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 651 8 1 8 5.8 Cc1c(N2CCN(Cc3cccc4ccsc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143102 179711 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 9 4.0 Cc1c(N2CCN(Cc3ccc(C#N)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4516712 179711 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 9 4.0 Cc1c(N2CCN(Cc3ccc(C#N)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
71623059 187604 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4756920 187604 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44444645 161779 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 672 9 2 6 4.8 CC(=O)NC1CCN(C(=O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL401351 161779 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 672 9 2 6 4.8 CC(=O)NC1CCN(C(=O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
162673323 189895 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccccc4Cl)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4794864 189895 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccccc4Cl)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
86274853 122965 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 662 6 1 7 4.5 N#Cc1cccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ncc(C(F)(F)F)cc4F)cc3C3(CCS(=O)(=O)CC3)C2C2CC2)c1 10.1021/ml5004469
CHEMBL3358414 122965 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 662 6 1 7 4.5 N#Cc1cccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ncc(C(F)(F)F)cc4F)cc3C3(CCS(=O)(=O)CC3)C2C2CC2)c1 10.1021/ml5004469
1185 10473 38 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
67143030 179895 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 8 1 8 4.6 Cc1c(N2CCN(Cc3cccc(F)c3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4520639 179895 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 8 1 8 4.6 Cc1c(N2CCN(Cc3cccc(F)c3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
1185 10473 38 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44406776 141120 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44444668 161058 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 7 1 6 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL398648 161058 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 7 1 6 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67143633 180089 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 612 8 2 8 3.2 Cc1c(N2CCN(Cc3ccc(=O)[nH]c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4526188 180089 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 612 8 2 8 3.2 Cc1c(N2CCN(Cc3ccc(=O)[nH]c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL2370265 216604 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](Cc1ccccn1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm990433g
44573275 194194 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 6 1 5 5.6 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1CC 10.1016/j.bmcl.2009.02.043
CHEMBL493730 194194 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 6 1 5 5.6 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1CC 10.1016/j.bmcl.2009.02.043
44406776 141120 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 141120 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44293151 107951 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 510 12 2 3 6.9 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C(C)C 10.1016/s0960-894x(01)00275-x
CHEMBL295595 107951 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 510 12 2 3 6.9 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C(C)C 10.1016/s0960-894x(01)00275-x
44293250 108510 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 11 2 4 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL299615 108510 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 11 2 4 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44406776 141120 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44406776 141120 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
145973124 169801 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 595 8 1 6 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3ccc(C(F)(F)F)cc3F)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4175801 169801 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 595 8 1 6 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3ccc(C(F)(F)F)cc3F)c2=O)c1F 10.1016/j.ejmech.2017.12.095
11167850 9518 28 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44406776 141120 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL409218 219532 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N1CCC[C@@H]1C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
11496945 183254 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459659 183254 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
21899433 161481 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 631 8 1 6 5.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399772 161481 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 631 8 1 6 5.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44346397 121276 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 121276 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
1185 10473 38 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 10473 38 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 10473 38 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 10473 38 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44359193 18410 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 587 8 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)NCc4ccc5c(c4)OCO5)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180764 18410 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 587 8 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)NCc4ccc5c(c4)OCO5)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL141750 18410 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 587 8 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)NCc4ccc5c(c4)OCO5)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44402335 78391 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 470 8 1 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)CC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL196337 78391 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 470 8 1 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)CC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402468 139598 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL370144 139598 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
70697569 84749 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.6 CC(C)(C)CNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL2096778 84749 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.6 CC(C)(C)CNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
11720984 70253 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 555 9 3 5 4.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL179885 70253 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 555 9 3 5 4.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
162645007 186240 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 186240 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44346398 21310 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 21310 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417614 148396 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 148396 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346667 120520 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 120520 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
15462666 103277 4 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL262557 103277 4 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44391541 72365 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 482 9 1 7 4.6 CCSc1nc2cc(S(=O)(=O)NCc3ccc([N+](=O)[O-])cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183237 72365 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 482 9 1 7 4.6 CCSc1nc2cc(S(=O)(=O)NCc3ccc([N+](=O)[O-])cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44391525 173145 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3ccc(OC)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL427500 173145 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3ccc(OC)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44365375 128294 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 402 9 3 2 5.8 Oc1ccc(CCCCNCCc2c(-c3ccc(F)cc3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL358416 128294 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 402 9 3 2 5.8 Oc1ccc(CCCCNCCc2c(-c3ccc(F)cc3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
11619758 179993 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 470 6 3 5 5.0 S=c1[nH]c2cccc(OCCN3CCN(c4cccc5[nH]c(-c6ccccc6)nc45)CC3)c2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL452293 179993 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 470 6 3 5 5.0 S=c1[nH]c2cccc(OCCN3CCN(c4cccc5[nH]c(-c6ccccc6)nc45)CC3)c2[nH]1 10.1016/j.bmc.2008.05.024
162645007 186240 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 186240 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
67144335 176617 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 658 9 1 9 4.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4439926 176617 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 658 9 1 9 4.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
1185 10473 38 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
118179127 189993 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 599 7 2 5 4.2 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2CCO 10.1021/acs.jmedchem.0c01076
CHEMBL4795998 189993 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 599 7 2 5 4.2 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2CCO 10.1021/acs.jmedchem.0c01076
44444676 161717 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 646 9 1 6 5.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(OCC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401080 161717 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 646 9 1 6 5.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(OCC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44444641 161748 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 601 7 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401212 161748 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 601 7 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67143413 176396 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 8 4.3 Cc1cncc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4436711 176396 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 8 4.3 Cc1cncc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
44365877 126258 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 646 13 3 6 6.2 CCCS(=O)(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL345297 126258 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 646 13 3 6 6.2 CCCS(=O)(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
44573789 194119 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493167 194119 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
11496610 10847 13 None - 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
5582 10847 13 None - 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
CHEMBL474991 10847 13 None - 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
11532637 14486 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL1088866 14486 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
53238728 177453 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 545 8 1 7 3.7 Cc1c(N2CCN(Cc3ccccc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4451627 177453 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 545 8 1 7 3.7 Cc1c(N2CCN(Cc3ccccc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
11496610 10847 13 None - 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
5582 10847 13 None - 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
CHEMBL474991 10847 13 None - 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
1185 10473 38 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 10473 38 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 10473 38 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 10473 38 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44391752 168441 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL413062 168441 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
1185 10473 38 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL None None None None 10.1021/jm0506928
87285476 178246 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 653 8 1 8 5.2 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4463476 178246 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 653 8 1 8 5.2 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL436874 220468 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL None None None None 10.1021/jm0506928
44573278 194226 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL493932 194226 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
44573628 199996 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 473 5 1 5 6.2 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)s1 10.1016/j.bmcl.2009.02.043
CHEMBL523527 199996 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 473 5 1 5 6.2 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)s1 10.1016/j.bmcl.2009.02.043
25194091 195789 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 498 7 3 5 5.5 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL508898 195789 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 498 7 3 5 5.5 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
25193797 196444 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 548 7 2 5 6.4 CC(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL515200 196444 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 548 7 2 5 6.4 CC(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
1185 10473 38 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 10473 38 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 10473 38 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 10473 38 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44267232 16389 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 454 10 3 3 6.0 CC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cn1 10.1016/s0960-894x(01)00133-0
CHEMBL11263 16389 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 454 10 3 3 6.0 CC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cn1 10.1016/s0960-894x(01)00133-0
44402647 76604 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 604 11 3 8 6.5 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL193740 76604 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 604 11 3 8 6.5 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
11525693 76605 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 471 8 2 7 5.6 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL193749 76605 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 471 8 2 7 5.6 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
11237922 72294 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
11237922 72294 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183066 72294 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183066 72294 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
25194092 196655 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 498 6 3 5 5.6 Cc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)c(C)c1 10.1016/j.bmc.2008.05.024
CHEMBL516934 196655 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 498 6 3 5 5.6 Cc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)c(C)c1 10.1016/j.bmc.2008.05.024
44417614 148396 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 148396 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44391541 72365 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 482 9 1 7 4.6 CCSc1nc2cc(S(=O)(=O)NCc3ccc([N+](=O)[O-])cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183237 72365 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 482 9 1 7 4.6 CCSc1nc2cc(S(=O)(=O)NCc3ccc([N+](=O)[O-])cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
87285767 181656 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 775 13 2 10 5.1 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCS(=O)(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4563686 181656 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 775 13 2 10 5.1 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCS(=O)(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11167850 9518 28 None 6309 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44267270 17150 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 450 9 2 1 7.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc3c(c2)CCCC3)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11623 17150 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 450 9 2 1 7.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc3c(c2)CCCC3)c1 10.1016/s0960-894x(01)00133-0
162652474 187230 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 519 5 1 3 5.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(Cc1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4752711 187230 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 519 5 1 3 5.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(Cc1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
67144367 176641 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 454 6 1 6 3.3 Cc1c(N2CCCCC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4440296 176641 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 454 6 1 6 3.3 Cc1c(N2CCCCC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
87285768 177274 3 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 177274 3 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
162650892 187008 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4749974 187008 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
10930638 105805 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 105805 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44406776 141120 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
67144085 177949 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3ccccc3[N+](=O)[O-])CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4458877 177949 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3ccccc3[N+](=O)[O-])CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44406776 141120 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
67144307 179806 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 546 8 1 8 3.1 Cc1c(N2CCN(Cc3cccnc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4518726 179806 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 546 8 1 8 3.1 Cc1c(N2CCN(Cc3cccnc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44365486 45893 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 434 9 3 2 6.8 Oc1ccc(CCCCNCCc2c(-c3cccc4ccccc34)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL146921 45893 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 434 9 3 2 6.8 Oc1ccc(CCCCNCCc2c(-c3cccc4ccccc34)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL329807 218099 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
CHEMBL408737 219507 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](C)C(=O)N[C@H](CCCCNC(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44402467 177435 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL445143 177435 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
44402647 76604 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 604 11 3 8 6.5 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL193740 76604 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 604 11 3 8 6.5 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
44365119 126428 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 384 9 3 2 5.7 Oc1ccc(CCCCNCCc2c(-c3ccccc3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL346852 126428 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 384 9 3 2 5.7 Oc1ccc(CCCCNCCc2c(-c3ccccc3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
25194090 195707 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 484 6 3 5 5.3 Cc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL507973 195707 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 484 6 3 5 5.3 Cc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44346398 21310 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 21310 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44322240 213190 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 396 3 1 4 5.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OC2CCN(C)CC2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL87804 213190 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 396 3 1 4 5.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OC2CCN(C)CC2)c1 10.1016/s0960-894x(99)00446-1
44322436 213443 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 424 4 1 4 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL89387 213443 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 424 4 1 4 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
123549935 186213 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 551 5 1 4 4.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccccc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4740379 186213 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 551 5 1 4 4.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccccc1)C2C 10.1021/acs.jmedchem.0c01076
162647697 186638 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 523 5 1 5 5.2 O=C(Nc1ccc2c(c1)C1(CCSCC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4745391 186638 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 523 5 1 5 5.2 O=C(Nc1ccc2c(c1)C1(CCSCC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
44444665 100976 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 8 1 5 6.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249772 100976 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 8 1 5 6.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL2430899 217239 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma countingDisplacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)CCCNC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.bmcl.2013.08.075
118179265 187292 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 619 5 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(C(F)(F)F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4753358 187292 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 619 5 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(C(F)(F)F)cc1)C2C 10.1021/acs.jmedchem.0c01076
118178983 190210 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 552 5 1 5 4.1 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1cccnc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4798682 190210 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 552 5 1 5 4.1 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1cccnc1)C2C 10.1021/acs.jmedchem.0c01076
44406776 141120 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44328452 103224 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL 1072 26 9 12 1.9 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](C)C(=O)N[C@H](CCCCNNC(=O)c1cccnc1)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
CHEMBL262190 103224 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL 1072 26 9 12 1.9 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](C)C(=O)N[C@H](CCCCNNC(=O)c1cccnc1)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
53238731 177755 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 579 8 1 7 4.3 Cc1c(N2CCN(Cc3ccc(Cl)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4456075 177755 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 579 8 1 7 4.3 Cc1c(N2CCN(Cc3ccc(Cl)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44214070 185952 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 561 13 3 5 6.2 CCOC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL47227 185952 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 561 13 3 5 6.2 CCOC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44391808 72369 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 587 9 3 5 5.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183274 72369 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 587 9 3 5 5.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
67144408 182688 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 586 8 1 9 3.5 Cc1c(N2CCN(Cc3ccon3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4587044 182688 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 586 8 1 9 3.5 Cc1c(N2CCN(Cc3ccon3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67144409 177884 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 8 4.3 Cc1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)cn1 10.1021/acs.jmedchem.6b01071
CHEMBL4457786 177884 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 8 4.3 Cc1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)cn1 10.1021/acs.jmedchem.6b01071
44406776 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67144509 180908 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 575 9 1 8 3.7 COc1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4546034 180908 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 575 9 1 8 3.7 COc1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
162672599 189786 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 481 4 1 5 4.1 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(NC(=O)c3cccnc3)cc2C12CCOCC2 10.1021/acs.jmedchem.0c01076
CHEMBL4793643 189786 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 481 4 1 5 4.1 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(NC(=O)c3cccnc3)cc2C12CCOCC2 10.1021/acs.jmedchem.0c01076
44328414 103230 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL 1028 23 9 10 2.2 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)Nc1ccccc1C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
CHEMBL262292 103230 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL 1028 23 9 10 2.2 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)Nc1ccccc1C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44402404 140342 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 568 9 2 8 5.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N3CCCC3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL371073 140342 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 568 9 2 8 5.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N3CCCC3)c21 10.1016/j.bmcl.2005.03.030
11237922 72294 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
11237922 72294 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183066 72294 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183066 72294 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
15462666 103277 4 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL262557 103277 4 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417614 148396 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 148396 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417615 148701 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 148701 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44322077 213322 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 421 5 1 6 4.9 Cc1cc(C)cc(-c2c(O)nc3cc([N+](=O)[O-])ccc3c2OCC2CCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL88620 213322 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 421 5 1 6 4.9 Cc1cc(C)cc(-c2c(O)nc3cc([N+](=O)[O-])ccc3c2OCC2CCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
44322441 213587 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 412 4 1 5 4.6 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CN(C)CCO2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL90383 213587 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 412 4 1 5 4.6 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CN(C)CCO2)c1 10.1016/s0960-894x(99)00446-1
44391574 72864 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 445 8 1 6 4.2 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccsc1 10.1016/j.bmcl.2004.10.089
CHEMBL183847 72864 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 445 8 1 6 4.2 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccsc1 10.1016/j.bmcl.2004.10.089
162667361 189304 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 468 5 1 3 5.1 CC1N(S(=O)(=O)c2ccccc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C1(C)C 10.1021/acs.jmedchem.0c01076
CHEMBL4787218 189304 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 468 5 1 3 5.1 CC1N(S(=O)(=O)c2ccccc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C1(C)C 10.1021/acs.jmedchem.0c01076
162645007 186240 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 186240 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44322399 213058 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 7 2 6 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCCC2CCCCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL86955 213058 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 7 2 6 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCCC2CCCCN2)c1 10.1016/s0960-894x(99)00447-3
71666542 187126 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 6 4.4 O=C(NCc1ncc(F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4751345 187126 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 6 4.4 O=C(NCc1ncc(F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
67143761 178140 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 710 12 3 9 3.8 Cc1c(N2CCN(Cc3cccc(C(=O)NCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4461692 178140 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 710 12 3 9 3.8 Cc1c(N2CCN(Cc3cccc(C(=O)NCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
1185 10473 38 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
118179051 186997 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4749790 186997 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
44322440 118336 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 441 6 2 6 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL328063 118336 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 441 6 2 6 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCN2)c1 10.1016/s0960-894x(99)00447-3
44365626 213722 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 596 11 3 5 6.4 CCC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL91146 213722 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 596 11 3 5 6.4 CCC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL436874 220468 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL None None None None 10.1021/jm0506928
9918188 161500 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 708 8 2 5 8.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399856 161500 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 708 8 2 5 8.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
10930638 105805 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 105805 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44359252 18403 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 7 6.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C5CC5)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180715 18403 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 7 6.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C5CC5)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL139291 18403 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 7 6.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C5CC5)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
71461676 86274 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 469 6 2 6 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCC[C@H](C)N2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL2113717 86274 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 469 6 2 6 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCC[C@H](C)N2)c1 10.1016/j.bmcl.2003.12.101
44406776 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44406776 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44406776 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44380192 64221 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL165534 64221 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
44406776 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
70691931 80963 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1924 45 22 28 -1.5 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCNC(C)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL2023088 80963 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1924 45 22 28 -1.5 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCNC(C)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
44406776 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
15895698 213658 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL90725 213658 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCCN2)c1 10.1016/s0960-894x(99)00447-3
44322166 213044 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 468 5 1 4 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Br)ccc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL86897 213044 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 468 5 1 4 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Br)ccc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
20691661 86388 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211485 86388 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
9909560 16646 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 411 10 2 2 6.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11420 16646 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 411 10 2 2 6.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
44402492 132962 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1cccnc1 10.1016/j.bmcl.2005.03.030
CHEMBL364933 132962 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1cccnc1 10.1016/j.bmcl.2005.03.030
44391718 72379 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 523 10 3 5 4.0 CC(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183325 72379 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 523 10 3 5 4.0 CC(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44365093 126039 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 520 9 3 2 7.7 Oc1ccc(CCCCNCCc2c(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL343658 126039 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 520 9 3 2 7.7 Oc1ccc(CCCCNCCc2c(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
162645007 186240 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 186240 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL264526 217404 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44560995 185932 0 None - 3 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL472117 185932 0 None - 3 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
10919052 120296 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 120296 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10930638 105805 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 105805 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402232 78186 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 454 8 1 7 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C3CCC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL195920 78186 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 454 8 1 7 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C3CCC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402072 78514 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 442 8 1 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL196616 78514 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 442 8 1 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44561265 179887 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 512 6 3 5 5.0 FC(F)(F)C(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL452044 179887 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 512 6 3 5 5.0 FC(F)(F)C(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44560995 185932 0 None - 3 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL472117 185932 0 None - 3 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
67143374 178520 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cncc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4467261 178520 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cncc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
162645007 186240 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 186240 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
162675445 190187 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 470 6 1 4 4.4 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3CC2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4798298 190187 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 470 6 1 4 4.4 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3CC2C)cc1 10.1021/acs.jmedchem.0c01076
44444647 161780 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 688 10 2 7 4.6 CC(=O)N1CCN(CC(O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL401352 161780 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 688 10 2 7 4.6 CC(=O)N1CCN(CC(O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
71668147 186769 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 637 6 1 6 4.6 O=C(NCc1ccc(C(F)(F)F)cn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4746969 186769 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 637 6 1 6 4.6 O=C(NCc1ccc(C(F)(F)F)cn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
86275342 122964 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL3358413 122964 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44365793 128156 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 499 11 4 4 6.4 CCNC(=O)Oc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
CHEMBL358126 128156 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 499 11 4 4 6.4 CCNC(=O)Oc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
CHEMBL97540 222705 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44444635 161483 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 637 7 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399779 161483 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 637 7 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
145957339 169088 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 561 8 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3c(F)cccc3Cl)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4164508 169088 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 561 8 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3c(F)cccc3Cl)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44572286 187580 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475650 187580 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
10046374 15928 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL11009 15928 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
10046374 15928 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11009 15928 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
44406776 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67143780 179031 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 637 9 1 8 4.7 CC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4474379 179031 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 637 9 1 8 4.7 CC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL436874 220468 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL None None None None 10.1021/jm0506928
44380624 65912 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 587 8 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169873 65912 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 587 8 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
56655880 80962 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1841 41 22 28 -2.8 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL2023087 80962 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1841 41 22 28 -2.8 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
70689073 84401 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1835 43 23 28 -2.7 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
91900370 84401 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1835 43 23 28 -2.7 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL2088253 84401 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1835 43 23 28 -2.7 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL436874 220468 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL None None None None 10.1021/jm0506928
44406776 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44346667 120520 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 120520 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44267237 105149 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 369 7 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL275287 105149 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 369 7 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
44402560 78211 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 429 7 1 5 5.9 COc1ccc(Cl)cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL196088 78211 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 429 7 1 5 5.9 COc1ccc(Cl)cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402468 139598 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL370144 139598 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
44402256 143057 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 519 8 2 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2005.03.030
CHEMBL373340 143057 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 519 8 2 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2005.03.030
11330164 71977 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 540 10 1 7 4.1 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL182513 71977 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 540 10 1 7 4.1 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44346398 21310 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 21310 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346667 120520 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 120520 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
10919052 120296 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 120296 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
15462666 103277 4 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL262557 103277 4 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402426 139535 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 455 8 2 7 5.1 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL370028 139535 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 455 8 2 7 5.1 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391849 129732 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 435 7 1 4 4.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(C1CC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL360743 129732 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 435 7 1 4 4.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(C1CC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
162673323 189895 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccccc4Cl)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4794864 189895 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccccc4Cl)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
21899433 161481 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 631 8 1 6 5.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399772 161481 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 631 8 1 6 5.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44406776 141120 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67143135 181301 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3nccs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4555444 181301 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3nccs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44444670 101254 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 7 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCCC(O)C3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL251388 101254 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 7 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCCC(O)C3)CC2)c1 10.1016/j.bmcl.2007.09.099
67144409 177884 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 8 4.3 Cc1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)cn1 10.1021/acs.jmedchem.6b01071
CHEMBL4457786 177884 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 8 4.3 Cc1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)cn1 10.1021/acs.jmedchem.6b01071
CHEMBL268720 217542 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44572235 196286 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
CHEMBL513998 196286 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
145955182 169191 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 515 8 1 7 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cccs3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4166009 169191 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 515 8 1 7 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cccs3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44593425 183544 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
CHEMBL460480 183544 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
44406776 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67143135 181301 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3nccs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4555444 181301 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3nccs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44406776 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44365087 45623 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 452 9 3 2 7.0 Oc1ccc(CCCCNCCc2c(-c3cc(Cl)cc(Cl)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL146693 45623 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 452 9 3 2 7.0 Oc1ccc(CCCCNCCc2c(-c3cc(Cl)cc(Cl)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
67143397 178925 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 652 9 2 8 3.9 CNC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4473168 178925 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 652 9 2 8 3.9 CNC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
10074296 16160 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00779-x
CHEMBL11149 16160 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00779-x
44444642 101145 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 629 8 1 6 5.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250770 101145 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 629 8 1 6 5.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
10074296 16160 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human Gonadotropin-releasing hormone receptor bindingInhibition of human Gonadotropin-releasing hormone receptor binding
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL11149 16160 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human Gonadotropin-releasing hormone receptor bindingInhibition of human Gonadotropin-releasing hormone receptor binding
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00134-2
10074296 16160 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity evaluated against human Gonadotropin-releasing hormone receptorInhibitory activity evaluated against human Gonadotropin-releasing hormone receptor
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11149 16160 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity evaluated against human Gonadotropin-releasing hormone receptorInhibitory activity evaluated against human Gonadotropin-releasing hormone receptor
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00133-0
44402469 78453 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 599 13 3 9 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)C)c21 10.1016/j.bmcl.2005.03.030
CHEMBL196439 78453 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 599 13 3 9 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)C)c21 10.1016/j.bmcl.2005.03.030
44402463 134302 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 457 7 2 7 5.2 CCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL366236 134302 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 457 7 2 7 5.2 CCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
11720984 70253 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 555 9 3 5 4.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL179885 70253 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 555 9 3 5 4.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
11330164 71977 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 540 10 1 7 4.1 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL182513 71977 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 540 10 1 7 4.1 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44365280 127914 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cccc(C)c1-c1[nH]c2ccccc2c1CCNCCCCc1ccc(O)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL357622 127914 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cccc(C)c1-c1[nH]c2ccccc2c1CCNCCCCc1ccc(O)cc1 10.1016/s0960-894x(00)00707-1
44346667 120520 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 120520 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44348265 174079 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1529 40 15 19 0.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)c2cnccn2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL429381 174079 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1529 40 15 19 0.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)c2cnccn2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
118167818 186211 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 527 5 2 4 4.6 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCNCC2 10.1021/acs.jmedchem.0c01076
CHEMBL4740373 186211 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 527 5 2 4 4.6 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCNCC2 10.1021/acs.jmedchem.0c01076
44444639 161746 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 589 8 1 5 5.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N(C)C)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401193 161746 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 589 8 1 5 5.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N(C)C)CC2)c1 10.1016/j.bmcl.2007.09.099
44444672 176181 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 8 1 5 6.4 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL442283 176181 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 8 1 5 6.4 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
118178986 188978 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 4 4.5 CC(=O)N1CCC2(CC1)CN(S(=O)(=O)c1ccc(F)cc1)c1ccc(C(=O)NCc3ccccc3Cl)cc12 10.1021/acs.jmedchem.0c01076
CHEMBL4782882 188978 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 4 4.5 CC(=O)N1CCC2(CC1)CN(S(=O)(=O)c1ccc(F)cc1)c1ccc(C(=O)NCc3ccccc3Cl)cc12 10.1021/acs.jmedchem.0c01076
44444639 161746 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 589 8 1 5 5.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N(C)C)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401193 161746 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 589 8 1 5 5.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N(C)C)CC2)c1 10.1016/j.bmcl.2007.09.099
67143773 177284 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 619 8 1 8 4.8 Cc1c(N2CCN(Cc3ccc(Cl)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449450 177284 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 619 8 1 8 4.8 Cc1c(N2CCN(Cc3ccc(Cl)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44444652 101277 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 588 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL251578 101277 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 588 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
162651368 187115 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 533 4 1 3 5.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(C(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4751238 187115 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 533 4 1 3 5.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(C(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
162660654 188079 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 539 5 1 5 4.2 O=C(Nc1ccc2c(c1)C1(CC[S+]([O-])CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4762368 188079 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 539 5 1 5 4.2 O=C(Nc1ccc2c(c1)C1(CC[S+]([O-])CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
118179218 186794 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 565 5 1 4 5.1 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccc(F)c3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4747248 186794 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 565 5 1 4 5.1 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccc(F)c3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44593425 183544 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity at rat GnRH receptor by competition binding assayBinding affinity at rat GnRH receptor by competition binding assay
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1021/jm701249f
CHEMBL460480 183544 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity at rat GnRH receptor by competition binding assayBinding affinity at rat GnRH receptor by competition binding assay
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1021/jm701249f
11634198 194145 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
CHEMBL493344 194145 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
44573111 194376 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL494738 194376 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
44593425 183544 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2009.02.043
CHEMBL460480 183544 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2009.02.043
11634198 194145 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmc.2012.09.013
CHEMBL493344 194145 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmc.2012.09.013
44293591 108373 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298700 108373 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
71449141 86273 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 483 7 2 6 6.5 CC[C@H]1CCC[C@@H](CCOc2c(-c3cc(C)cc(C)c3)c(O)nc3cc(Cl)c([N+](=O)[O-])cc23)N1 10.1016/j.bmcl.2003.12.101
CHEMBL2113716 86273 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 483 7 2 6 6.5 CC[C@H]1CCC[C@@H](CCOc2c(-c3cc(C)cc(C)c3)c(O)nc3cc(Cl)c([N+](=O)[O-])cc23)N1 10.1016/j.bmcl.2003.12.101
11525693 76605 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 471 8 2 7 5.6 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL193749 76605 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 471 8 2 7 5.6 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL436874 220468 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL None None None None 10.1021/jm0506928
67143815 178319 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 651 8 1 8 5.8 Cc1c(N2CCN(Cc3cccc4ccsc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4464440 178319 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 651 8 1 8 5.8 Cc1c(N2CCN(Cc3cccc4ccsc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
70691931 80963 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1924 45 22 28 -1.5 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCNC(C)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL2023088 80963 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1924 45 22 28 -1.5 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCNC(C)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL3085508 217768 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44402335 78391 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 470 8 1 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)CC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL196337 78391 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 470 8 1 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)CC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402273 147051 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 456 7 1 7 5.8 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL380576 147051 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 456 7 1 7 5.8 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391771 172801 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.7 CC(C)(C)NC(=O)NCCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL425524 172801 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.7 CC(C)(C)NC(=O)NCCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL405438 162504 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to bind to Gonadotropin-releasing hormone receptor was evaluated in vitro by displacement assay using [125I][D-Lys6]-GnRH as radioligandAbility to bind to Gonadotropin-releasing hormone receptor was evaluated in vitro by displacement assay using [125I][D-Lys6]-GnRH as radioligand
ChEMBL 1820 46 20 18 5.7 C=CC1=C(C)c2cc1cc1[nH]c(cc3nc(cc4[nH]c(c2)c(C=C)c4C)C(C)=C3CCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccc2)NC(=O)C2CCC(=O)N2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)C2CC[C@@H](C(=O)NCC(N)=O)N2)c(CCC(=O)O)c1C 10.1021/jm020535y
44417615 148701 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 148701 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
162653870 187322 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 489 4 1 4 3.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(C)(=O)=O)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4753775 187322 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 489 4 1 4 3.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(C)(=O)=O)C2C 10.1021/acs.jmedchem.0c01076
11167850 9518 28 None 6309 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
162652474 187230 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 519 5 1 3 5.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(Cc1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4752711 187230 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 519 5 1 3 5.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(Cc1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
87285770 182823 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 803 15 2 10 6.4 CCOP(=O)(O)CCCN[C@@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1021/acs.jmedchem.6b01071
CHEMBL4590493 182823 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 803 15 2 10 6.4 CCOP(=O)(O)CCCN[C@@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1021/acs.jmedchem.6b01071
44444673 101058 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 644 8 1 5 6.8 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL250389 101058 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 644 8 1 5 6.8 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL436874 220468 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL None None None None 10.1021/jm0506928
44573790 200041 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 5 1 5 5.9 Cc1c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)ncn1C(C)C 10.1016/j.bmcl.2009.02.043
CHEMBL523849 200041 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 5 1 5 5.9 Cc1c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)ncn1C(C)C 10.1016/j.bmcl.2009.02.043
44402469 78453 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 599 13 3 9 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)C)c21 10.1016/j.bmcl.2005.03.030
CHEMBL196439 78453 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 599 13 3 9 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)C)c21 10.1016/j.bmcl.2005.03.030
67142711 178802 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 579 8 1 7 4.3 Cc1c(N2CCN(Cc3ccccc3Cl)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4471620 178802 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 579 8 1 7 4.3 Cc1c(N2CCN(Cc3ccccc3Cl)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
145957680 168876 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 563 7 1 6 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3C(F)(F)F)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4161096 168876 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 563 7 1 6 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3C(F)(F)F)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44406776 141120 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
1185 10473 38 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 10473 38 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 10473 38 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 10473 38 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44417614 148396 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 148396 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44359200 18977 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 509 8 2 5 6.3 CCN(CC)C(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
CHEMBL1184288 18977 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 509 8 2 5 6.3 CCN(CC)C(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
CHEMBL343040 18977 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 509 8 2 5 6.3 CCN(CC)C(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
44388018 67249 0 None 389 2 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cellsInhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cells
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL175443 67249 0 None 389 2 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cellsInhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cells
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44402649 104962 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 675 15 3 9 6.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)Cc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL274002 104962 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 675 15 3 9 6.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)Cc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
145948913 174265 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1276 29 16 15 -1.9 NC(=O)CNC(=O)[C@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1(NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H]2CCC(=O)N2)CCC1 10.1039/C5MD00259A
CHEMBL4299455 174265 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1276 29 16 15 -1.9 NC(=O)CNC(=O)[C@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1(NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H]2CCC(=O)N2)CCC1 10.1039/C5MD00259A
44365485 128305 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 435 9 3 3 6.2 Oc1ccc(CCCCNCCc2c(-c3cccc4cnccc34)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL358524 128305 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 435 9 3 3 6.2 Oc1ccc(CCCCNCCc2c(-c3cccc4cnccc34)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
15462666 103277 4 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL262557 103277 4 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346398 21310 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 21310 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346398 21310 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 21310 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402426 139535 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 455 8 2 7 5.1 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL370028 139535 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 455 8 2 7 5.1 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391849 129732 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 435 7 1 4 4.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(C1CC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL360743 129732 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 435 7 1 4 4.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(C1CC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44391670 71466 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 473 8 1 5 4.8 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1cccc(Cl)c1 10.1016/j.bmcl.2004.10.089
CHEMBL181864 71466 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 473 8 1 5 4.8 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1cccc(Cl)c1 10.1016/j.bmcl.2004.10.089
1185 10473 38 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL None None None None 10.1021/jm0506928
67143613 177805 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cccnc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4456703 177805 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cccnc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
1185 10473 38 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44185958 161777 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 615 8 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401349 161777 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 615 8 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
10077523 129492 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 613 7 3 7 7.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL360429 129492 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 613 7 3 7 7.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44395463 133553 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 627 7 2 7 7.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL365366 133553 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 627 7 2 7 7.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44380512 64207 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Compound was evaluated for the inhibition of Gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis using functional assayCompound was evaluated for the inhibition of Gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis using functional assay
ChEMBL 617 9 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL165456 64207 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Compound was evaluated for the inhibition of Gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis using functional assayCompound was evaluated for the inhibition of Gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis using functional assay
ChEMBL 617 9 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
11980076 215232 29 None - 1 Rat 8.7 pIC50 = 8.7 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm990433g
CHEMBL1007 215232 29 None - 1 Rat 8.7 pIC50 = 8.7 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm990433g
CHEMBL3085508 217768 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 10473 38 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44444632 101095 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 622 7 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250569 101095 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 622 7 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
67143374 178520 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cncc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4467261 178520 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cncc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67144466 182559 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 596 8 1 8 3.9 Cc1c(N2CCN(Cc3cccnc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4583933 182559 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 596 8 1 8 3.9 Cc1c(N2CCN(Cc3cccnc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
10032223 18975 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184284 18975 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL342822 18975 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
18914263 103676 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 630 15 3 4 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL265774 103676 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 630 15 3 4 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293264 107991 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 560 12 3 4 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL295908 107991 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 560 12 3 4 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44214069 108095 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 575 14 3 5 6.1 CCOC(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL296644 108095 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 575 14 3 5 6.1 CCOC(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292838 108294 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 574 13 3 4 5.6 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL298074 108294 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 574 13 3 4 5.6 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
21254068 108565 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 12 3 5 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL300045 108565 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 12 3 5 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293076 108598 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 600 12 3 4 6.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL300268 108598 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 600 12 3 4 6.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293070 172874 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 15 3 4 7.0 CCN(CC)C(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL42592 172874 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 15 3 4 7.0 CCN(CC)C(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
18914272 176460 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 588 14 3 4 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL443768 176460 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 588 14 3 4 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
21254089 188436 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47761 188436 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44413066 85179 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 579 10 1 7 6.5 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(C)=O)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL211098 85179 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 579 10 1 7 6.5 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(C)=O)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44412947 103536 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 608 10 1 7 6.4 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(N(C)C(=O)NC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL264574 103536 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 608 10 1 7 6.4 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(N(C)C(=O)NC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
1184 10505 36 None 426 2 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
9874838 10505 36 None 426 2 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
CHEMBL71917 10505 36 None 426 2 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
44348572 104076 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](NC(=O)CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL269097 104076 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](NC(=O)CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348571 166799 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](NC(=O)CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL410799 166799 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](NC(=O)CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44292869 183801 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL46312 183801 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44296258 108402 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 613 7 3 7 7.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCC(C(F)(F)F)N2)cc(C)c1C 10.1016/j.bmcl.2003.12.101
CHEMBL298937 108402 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 613 7 3 7 7.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCC(C(F)(F)F)N2)cc(C)c1C 10.1016/j.bmcl.2003.12.101
1184 10505 36 None 426 2 Human 8.7 pIC50 = 8.7 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to monkey Leutinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cellsTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to monkey Leutinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
9874838 10505 36 None 426 2 Human 8.7 pIC50 = 8.7 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to monkey Leutinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cellsTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to monkey Leutinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
CHEMBL71917 10505 36 None 426 2 Human 8.7 pIC50 = 8.7 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to monkey Leutinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cellsTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to monkey Leutinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
44321100 113870 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC(CC5)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL315909 113870 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC(CC5)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL3085508 217768 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
9961721 175258 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 175258 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44380552 65533 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168655 65533 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
44380317 175268 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL435262 175268 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL3085508 217768 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL None None None None 10.1021/jm0506928
44293485 108292 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 590 12 1 3 8.2 CCN(CCCCc1ccncc1)CCc1c(-c2cc(C)cc(C)c2)[nH]c2ccc(C(C)(C)C(=O)N3C4CCC3CC4)cc12 10.1016/s0960-894x(01)00275-x
CHEMBL298051 108292 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 590 12 1 3 8.2 CCN(CCCCc1ccncc1)CCc1c(-c2cc(C)cc(C)c2)[nH]c2ccc(C(C)(C)C(=O)N3C4CCC3CC4)cc12 10.1016/s0960-894x(01)00275-x
44402518 165305 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL409138 165305 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
1185 10473 38 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
15602805 14879 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
CHEMBL1091579 14879 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
145962692 169035 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 485 7 1 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccco3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4163619 169035 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 485 7 1 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccco3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44359287 18407 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180743 18407 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL139993 18407 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293348 107268 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL290991 107268 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293486 194196 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 592 13 2 3 8.5 CCN(C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL49374 194196 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 592 13 2 3 8.5 CCN(C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44292939 108179 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL297269 108179 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44402395 175871 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL439879 175871 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
155569451 182987 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1711 48 21 25 -3.8 CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)CCCCCNC(=O)CCC(=O)OC[C@H]1O[C@@H](n2ccc(N)nc2=O)C(F)(F)[C@@H]1O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
CHEMBL4593899 182987 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1711 48 21 25 -3.8 CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)CCCCCNC(=O)CCC(=O)OC[C@H]1O[C@@H](n2ccc(N)nc2=O)C(F)(F)[C@@H]1O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
CHEMBL436874 220468 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44380212 64392 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166843 64392 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
44348535 167204 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 39 14 17 2.0 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)CCNC(C)C)cc1 10.1021/jm970024p
CHEMBL411144 167204 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 39 14 17 2.0 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)CCNC(C)C)cc1 10.1021/jm970024p
CHEMBL407619 219450 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NCC(=O)n2cc(C)c(=O)[nH]c2=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1016/j.bmcl.2005.03.085
1185 10473 38 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL None None None None 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44402395 175871 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL439879 175871 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL407619 219450 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NCC(=O)n2cc(C)c(=O)[nH]c2=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1016/j.bmcl.2005.03.085
87285521 181798 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3cccnc3Cl)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4567165 181798 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3cccnc3Cl)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11167850 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44321147 170259 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 618 11 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CCCC5)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL420051 170259 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 618 11 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CCCC5)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL3085508 217768 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
53239615 182644 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 585 8 1 8 4.1 Cc1c(N2CCN(Cc3ccco3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4585969 182644 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 585 8 1 8 4.1 Cc1c(N2CCN(Cc3ccco3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11167850 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL None None None None 10.1021/jm0506928
44359458 18919 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184171 18919 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL336884 18919 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
10345138 129335 0 None 2041 2 Human 8.6 pIC50 = 8.6 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL360143 129335 0 None 2041 2 Human 8.6 pIC50 = 8.6 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL75347 129335 0 None 2041 2 Human 8.6 pIC50 = 8.6 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
44293335 179406 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL449351 179406 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293487 108411 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL299006 108411 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293803 195661 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50721 195661 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44402398 103754 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1536 41 17 18 1.6 CC(C)C[C@H](NC(=O)[C@@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)C(N)CN)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL266420 103754 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1536 41 17 18 1.6 CC(C)C[C@H](NC(=O)[C@@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)C(N)CN)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
87285768 177274 3 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells assessed as reduction in ERK1/2 phosphorylation pre-incubated for 5 mins before LHRH stimulation for 5 mins by chemiluminescence based assayAntagonist activity against human GnRH receptor expressed in HEK293 cells assessed as reduction in ERK1/2 phosphorylation pre-incubated for 5 mins before LHRH stimulation for 5 mins by chemiluminescence based assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 177274 3 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells assessed as reduction in ERK1/2 phosphorylation pre-incubated for 5 mins before LHRH stimulation for 5 mins by chemiluminescence based assayAntagonist activity against human GnRH receptor expressed in HEK293 cells assessed as reduction in ERK1/2 phosphorylation pre-incubated for 5 mins before LHRH stimulation for 5 mins by chemiluminescence based assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL3085508 217768 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL None None None None 10.1021/jm0506928
67143420 169687 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4173938 169687 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44359471 18970 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184266 18970 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL341717 18970 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
162649425 186799 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 6 3.9 O=C(Nc1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4747322 186799 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 6 3.9 O=C(Nc1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
86275345 188849 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4781434 188849 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
10897903 86550 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 694 11 0 8 7.2 CCC(=O)N(C)c1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(OC)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21185 86550 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 694 11 0 8 7.2 CCC(=O)N(C)c1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(OC)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44274227 105669 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 654 10 0 9 6.8 COc1cccc(-n2c(=O)c3c(CN(C)Cc4ccccc4)c(-c4ccc([N+](=O)[O-])cc4)sc3n(Cc3c(F)cccc3F)c2=O)c1 10.1021/jm020180i
CHEMBL279223 105669 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 654 10 0 9 6.8 COc1cccc(-n2c(=O)c3c(CN(C)Cc4ccccc4)c(-c4ccc([N+](=O)[O-])cc4)sc3n(Cc3c(F)cccc3F)c2=O)c1 10.1021/jm020180i
44274247 106170 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 639 10 0 8 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(OC)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL282679 106170 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 639 10 0 8 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(OC)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
15895695 113731 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2C)c1 10.1016/s0960-894x(99)00447-3
CHEMBL314963 113731 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2C)c1 10.1016/s0960-894x(99)00447-3
44365771 126362 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 541 10 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL346195 126362 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 541 10 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL96693 222698 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](C)C(=O)N[C@H](CCCCN)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44573628 199996 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 473 5 1 5 6.2 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)s1 10.1016/j.bmcl.2009.02.043
CHEMBL523527 199996 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 473 5 1 5 6.2 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)s1 10.1016/j.bmcl.2009.02.043
44417614 148396 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 148396 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
67142907 177139 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 597 8 1 9 3.3 Cc1c(N2CCN(Cc3cnccn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4447551 177139 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 597 8 1 9 3.3 Cc1c(N2CCN(Cc3cnccn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
10930638 105805 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 105805 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44305306 107393 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 661 11 1 8 6.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)c4ccccc4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL291893 107393 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 661 11 1 8 6.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)c4ccccc4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
9984259 117278 0 None 281 2 Human 7.7 pIC50 = 7.7 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
CHEMBL324912 117278 0 None 281 2 Human 7.7 pIC50 = 7.7 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
44391752 168441 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL413062 168441 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
145958486 168962 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 541 8 1 7 4.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccc(SC)cc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4162543 168962 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 541 8 1 7 4.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccc(SC)cc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44406776 141120 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44365459 105583 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 384 7 3 2 5.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL278496 105583 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 384 7 3 2 5.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44365399 126451 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 9 3 2 6.0 Cc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL347121 126451 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 9 3 2 6.0 Cc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44365457 175446 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 426 10 3 2 6.7 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL436414 175446 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 426 10 3 2 6.7 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44274228 105450 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 643 9 0 7 7.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccc(Cl)cc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL277436 105450 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 643 9 0 7 7.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccc(Cl)cc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44274229 105482 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 643 9 0 7 7.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(Cl)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL277653 105482 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 643 9 0 7 7.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(Cl)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44274475 105928 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 639 10 0 8 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2OC)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL281167 105928 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 639 10 0 8 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2OC)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44346397 121276 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 121276 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44322442 119532 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 424 5 1 4 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL330524 119532 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 424 5 1 4 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
44322433 213450 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 5 1 4 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCCC2CCCN2C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL89443 213450 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 5 1 4 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCCC2CCCN2C)c1 10.1016/s0960-894x(99)00446-1
11692806 86591 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL212051 86591 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11606766 86625 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccccc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL212207 86625 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccccc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11512905 145196 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL377396 145196 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
44267059 15273 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 503 12 3 3 6.4 CCS(=O)(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
CHEMBL10941 15273 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 503 12 3 3 6.4 CCS(=O)(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
44267091 16573 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 453 10 3 2 6.6 CC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
CHEMBL11370 16573 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 453 10 3 2 6.6 CC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
44267250 15942 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 383 8 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11021 15942 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 383 8 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
44267233 16677 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 369 7 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11436 16677 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 369 7 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
44402589 131950 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 542 9 2 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N(C)C)c21 10.1016/j.bmcl.2005.03.030
CHEMBL364510 131950 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 542 9 2 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N(C)C)c21 10.1016/j.bmcl.2005.03.030
44391826 71656 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 549 10 3 6 4.2 COc1ccc(CNS(=O)(=O)c2ccc3c(c2)nc(CCNC(=O)NC(C)(C)C)n3Cc2ccccc2)cc1 10.1016/j.bmcl.2004.10.090
CHEMBL182178 71656 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 549 10 3 6 4.2 COc1ccc(CNS(=O)(=O)c2ccc3c(c2)nc(CCNC(=O)NC(C)(C)C)n3Cc2ccccc2)cc1 10.1016/j.bmcl.2004.10.090
44391566 72385 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 455 8 1 5 4.8 CCSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183376 72385 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 455 8 1 5 4.8 CCSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
9961721 175258 0 None - 1 Rat 6.7 pIC50 = 6.7 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL435167 175258 0 None - 1 Rat 6.7 pIC50 = 6.7 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44365169 47221 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 458 12 3 4 6.1 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL148244 47221 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 458 12 3 4 6.1 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44365616 48147 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 444 11 3 4 5.7 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL149004 48147 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 444 11 3 4 5.7 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44365617 49352 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 460 11 4 5 4.7 COc1ccc(-c2[nH]c3ccccc3c2CCNC[C@H](O)CCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL150041 49352 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 460 11 4 5 4.7 COc1ccc(-c2[nH]c3ccccc3c2CCNC[C@H](O)CCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
3823 56995 42 None -1 11 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity at LH-RH receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at LH-RH receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
76973198 56995 42 None -1 11 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity at LH-RH receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at LH-RH receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
CHEMBL157101 56995 42 None -1 11 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity at LH-RH receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at LH-RH receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
90663999 113607 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 709 12 3 10 3.4 O=C(NC[C@H]1CO[C@](Cn2ccnc2)(c2ccc(Cl)cc2Cl)O1)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1C(=O)OCc1ccccc1 10.1021/jm00129a003
CHEMBL3144570 113607 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 709 12 3 10 3.4 O=C(NC[C@H]1CO[C@](Cn2ccnc2)(c2ccc(Cl)cc2Cl)O1)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1C(=O)OCc1ccccc1 10.1021/jm00129a003
44346667 120520 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 120520 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44346397 121276 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 121276 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10624976 28385 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 492 9 1 8 4.7 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CNC)c2c1=O 10.1021/jm0512894
CHEMBL131751 28385 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 492 9 1 8 4.7 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CNC)c2c1=O 10.1021/jm0512894
11592473 84809 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 568 11 1 8 6.3 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CNCc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL209880 84809 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 568 11 1 8 6.3 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CNCc3ccccc3)c2c1=O 10.1021/jm0512894
44348358 148257 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1529 40 15 19 0.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)c2cnccn2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL384385 148257 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1529 40 15 19 0.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)c2cnccn2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44391574 72864 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 445 8 1 6 4.2 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccsc1 10.1016/j.bmcl.2004.10.089
CHEMBL183847 72864 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 445 8 1 6 4.2 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccsc1 10.1016/j.bmcl.2004.10.089
10624976 28385 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 492 9 1 8 4.7 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CNC)c2c1=O 10.1021/jm9803673
CHEMBL131751 28385 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 492 9 1 8 4.7 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CNC)c2c1=O 10.1021/jm9803673
44365172 49472 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 402 8 3 4 4.9 COc1ccc(-c2[nH]c3ccccc3c2CCNCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL150150 49472 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 402 8 3 4 4.9 COc1ccc(-c2[nH]c3ccccc3c2CCNCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44406776 141120 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67142907 177139 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 597 8 1 9 3.3 Cc1c(N2CCN(Cc3cnccn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4447551 177139 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 597 8 1 9 3.3 Cc1c(N2CCN(Cc3cnccn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
118179174 189255 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 561 6 1 4 4.6 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4786609 189255 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 561 6 1 4 4.6 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
12784 7365 12 None - 1 Human 7.7 pIC50 = 7.7 Binding
Affinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHRAffinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHR
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.6019/CHEMBL5210121
85469632 7365 12 None - 1 Human 7.7 pIC50 = 7.7 Binding
Affinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHRAffinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHR
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.6019/CHEMBL5210121
CHEMBL4537788 7365 12 None - 1 Human 7.7 pIC50 = 7.7 Binding
Affinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHRAffinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHR
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.6019/CHEMBL5210121
118179135 188797 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 5 1 4 4.9 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4780737 188797 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 5 1 4 4.9 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
12784 7365 12 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
85469632 7365 12 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL4537788 7365 12 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
44321458 112742 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 658 11 2 3 9.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCCC5C5CCCCC54)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL313004 112742 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 658 11 2 3 9.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCCC5C5CCCCC54)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
11618517 194335 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 414 4 2 4 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]cn5)CC4)cccc3[nH]2)cc1 10.1016/j.bmcl.2009.02.043
CHEMBL494554 194335 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 414 4 2 4 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]cn5)CC4)cccc3[nH]2)cc1 10.1016/j.bmcl.2009.02.043
44573670 194462 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 459 4 1 5 5.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)s1 10.1016/j.bmcl.2009.02.043
CHEMBL495174 194462 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 459 4 1 5 5.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)s1 10.1016/j.bmcl.2009.02.043
11712618 187005 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6ncccc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL474992 187005 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6ncccc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44402403 78304 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 515 9 3 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)O)c21 10.1016/j.bmcl.2005.03.030
CHEMBL196288 78304 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 515 9 3 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)O)c21 10.1016/j.bmcl.2005.03.030
44402649 104962 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 675 15 3 9 6.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)Cc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL274002 104962 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 675 15 3 9 6.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)Cc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
44406776 141120 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
10919052 120296 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 120296 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346667 120520 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 120520 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44267255 104924 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 383 8 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL273725 104924 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 383 8 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
44402670 78733 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 557 11 4 9 4.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCN)c21 10.1016/j.bmcl.2005.03.030
CHEMBL197317 78733 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 557 11 4 9 4.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCN)c21 10.1016/j.bmcl.2005.03.030
44402673 140046 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 499 10 2 7 6.4 CCCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL370414 140046 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 499 10 2 7 6.4 CCCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
44391516 71147 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 441 7 1 5 4.4 CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL181301 71147 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 441 7 1 5 4.4 CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44417615 148701 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 148701 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402405 148095 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 395 7 1 5 5.3 COc1ccccc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL383393 148095 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 395 7 1 5 5.3 COc1ccccc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391613 175054 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 462 9 1 7 2.4 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1CCN1CCOCC1 10.1016/j.bmcl.2004.10.089
CHEMBL433954 175054 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 462 9 1 7 2.4 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1CCN1CCOCC1 10.1016/j.bmcl.2004.10.089
44593415 196158 0 None - 1 Rat 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL512893 196158 0 None - 1 Rat 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
67143509 176844 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3cccc(C#N)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4443108 176844 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3cccc(C#N)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143490 178388 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cscn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4465381 178388 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cscn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67144353 179002 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 673 9 1 9 4.0 Cc1c(N2CCN(Cc3cccc(S(C)(=O)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4474058 179002 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 673 9 1 9 4.0 Cc1c(N2CCN(Cc3cccc(S(C)(=O)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
87285495 178931 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 664 8 1 8 5.0 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)n3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4473194 178931 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 664 8 1 8 5.0 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)n3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44267258 104149 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 369 7 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2ccccn2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL269636 104149 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 369 7 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2ccccn2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL413854 168529 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Ability to bind to Gonadotropin-releasing hormone receptor was evaluated in vitro by displacement assay using [125I][D-Lys6]-GnRH as radioligandAbility to bind to Gonadotropin-releasing hormone receptor was evaluated in vitro by displacement assay using [125I][D-Lys6]-GnRH as radioligand
ChEMBL 1810 46 21 19 4.4 C=CC1=C(C)c2cc1cc1[nH]c(cc3nc(cc4[nH]c(c2)c(C=C)c4C)C(C)=C3CCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2CCC(=O)N2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)C2CC[C@@H](C(=O)NCC(N)=O)N2)c(CCC(=O)O)c1C 10.1021/jm020535y
91810333 186357 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 7 1 4 5.4 C=CCC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCN(C(C)=O)CC2 10.1021/acs.jmedchem.0c01076
CHEMBL4741994 186357 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 7 1 4 5.4 C=CCC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCN(C(C)=O)CC2 10.1021/acs.jmedchem.0c01076
11619461 194464 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
CHEMBL495183 194464 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
10930638 105805 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 105805 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44391808 72369 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 587 9 3 5 5.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183274 72369 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 587 9 3 5 5.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44406776 141120 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL2430897 217237 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma countingDisplacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)CCCCCCCCCCNC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.bmcl.2013.08.075
56655880 80962 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1841 41 22 28 -2.8 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL2023087 80962 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1841 41 22 28 -2.8 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
25193700 180061 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 534 7 2 5 5.9 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL452547 180061 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 534 7 2 5 5.9 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
10930638 105805 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 105805 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44348055 175788 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](NC(=O)c2ccncc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL439258 175788 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](NC(=O)c2ccncc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44267042 16176 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 517 12 3 3 6.8 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(=O)(=O)C(C)C)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL11156 16176 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 517 12 3 3 6.8 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(=O)(=O)C(C)C)cc2)c1 10.1016/s0960-894x(01)00134-2
44391516 71147 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 441 7 1 5 4.4 CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL181301 71147 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 441 7 1 5 4.4 CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL409979 219571 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None C[C@H](NC(=O)[C@H]1CCCN1C(=O)[C@@H](CCCN=C(N)N)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)OCC1c2ccccc2-c2ccccc21)C(N)=O 10.1021/jm990433g
71623059 187604 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4756920 187604 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44406776 141120 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
155538326 179157 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 664 8 1 8 5.0 Cc1c(N2CCN(Cc3ccnc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4476330 179157 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 664 8 1 8 5.0 Cc1c(N2CCN(Cc3ccnc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
162656174 187653 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 589 5 2 5 5.6 O=C(Nc1ccc2c(c1)C1(CCC(O)(C(F)(F)F)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4757424 187653 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 589 5 2 5 5.6 O=C(Nc1ccc2c(c1)C1(CCC(O)(C(F)(F)F)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
44406776 141120 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL2370263 216603 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm990433g
44573713 199668 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
CHEMBL522202 199668 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
9961721 175258 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 175258 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44359419 18983 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)no4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184330 18983 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)no4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL344688 18983 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)no4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293592 169669 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL417363 169669 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44402471 141999 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 485 9 2 7 6.0 CCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL372316 141999 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 485 9 2 7 6.0 CCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
44402645 175903 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 528 9 3 8 4.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC)c21 10.1016/j.bmcl.2005.03.030
CHEMBL440212 175903 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 528 9 3 8 4.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC)c21 10.1016/j.bmcl.2005.03.030
44406776 141120 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67143621 178082 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 653 9 1 9 4.3 COC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4460880 178082 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 653 9 1 9 4.3 COC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
44406776 141120 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
1185 10473 38 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL265010 217413 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44346667 120520 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 120520 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44391728 72449 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183430 72449 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44391784 129104 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.9 CC(C)(C)NC(=O)CCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL359860 129104 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.9 CC(C)(C)NC(=O)CCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44346667 120520 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 120520 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
86274853 122965 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 662 6 1 7 4.5 N#Cc1cccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ncc(C(F)(F)F)cc4F)cc3C3(CCS(=O)(=O)CC3)C2C2CC2)c1 10.1021/ml5004469
CHEMBL3358414 122965 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 662 6 1 7 4.5 N#Cc1cccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ncc(C(F)(F)F)cc4F)cc3C3(CCS(=O)(=O)CC3)C2C2CC2)c1 10.1021/ml5004469
44215908 101004 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 616 7 1 5 6.1 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249982 101004 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 616 7 1 5 6.1 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
118178976 187960 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 6 1 4 5.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4761024 187960 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 6 1 4 5.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
12784 7365 12 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
85469632 7365 12 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL4537788 7365 12 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
24825725 199406 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL521674 199406 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
24825725 199406 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL521674 199406 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
44572287 187582 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6cccnc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475660 187582 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6cccnc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
1185 10473 38 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 10473 38 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 10473 38 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 10473 38 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
1185 10473 38 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 10473 38 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 10473 38 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 10473 38 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44293343 168991 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 545 12 4 3 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)NCc4ccccc4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL416286 168991 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 545 12 4 3 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)NCc4ccccc4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44406776 141120 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
67144582 182485 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 653 9 1 9 4.3 COC(=O)c1ccccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
CHEMBL4582222 182485 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 653 9 1 9 4.3 COC(=O)c1ccccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
1185 10473 38 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44406776 141120 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44417615 148701 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 148701 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
1185 10473 38 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44346397 121276 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 121276 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346667 120520 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 120520 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44402499 76598 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2005.03.030
CHEMBL193689 76598 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2005.03.030
44391714 128913 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccncc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL359668 128913 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccncc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL4564312 220791 4 None - 0 Human 5.6 pIC50 = 5.6 Binding
Affinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000335a GNRHRAffinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000335a GNRHR
ChEMBL None None None O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)[C@@H](C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.6019/CHEMBL5210121
44346667 120520 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 120520 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
1185 10473 38 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
10208964 73456 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 536 7 2 7 7.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCC2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185438 73456 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 536 7 2 7 7.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCC2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
86275345 188849 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4781434 188849 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44444617 100920 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 656 8 2 5 7.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N(C)C)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249372 100920 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 656 8 2 5 7.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N(C)C)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
71666685 189493 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 6 1 6 3.6 O=C(NCc1ccccn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4789613 189493 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 6 1 6 3.6 O=C(NCc1ccccn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
86275343 190270 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 655 6 1 6 4.7 O=C(NCc1ncc(C(F)(F)F)cc1F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4799511 190270 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 655 6 1 6 4.7 O=C(NCc1ncc(C(F)(F)F)cc1F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44322432 213461 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 427 6 2 6 4.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL89501 213461 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 427 6 2 6 4.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCN2)c1 10.1016/s0960-894x(99)00447-3
44365628 45707 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 554 10 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(C)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL146762 45707 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 554 10 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(C)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL264501 217401 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44365458 48646 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 8 3 2 5.9 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL149387 48646 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 8 3 2 5.9 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
87285565 177048 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 679 9 1 8 5.4 Cc1c(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4446131 177048 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 679 9 1 8 5.4 Cc1c(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11619461 194464 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
CHEMBL495183 194464 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
44402072 78514 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 442 8 1 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL196616 78514 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 442 8 1 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391566 72385 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 455 8 1 5 4.8 CCSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183376 72385 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 455 8 1 5 4.8 CCSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44365251 45348 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 440 9 3 3 6.9 Oc1ccc(CCCCNCCc2c(-c3cc4ccccc4s3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL146484 45348 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 440 9 3 3 6.9 Oc1ccc(CCCCNCCc2c(-c3cc4ccccc4s3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
44214066 175114 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 434 9 3 2 6.8 Oc1ccc(CCCCNCCc2c(-c3ccc4ccccc4c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL434318 175114 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 434 9 3 2 6.8 Oc1ccc(CCCCNCCc2c(-c3ccc4ccccc4c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
44348357 103370 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 17 19 0.2 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)c2c[nH]nc2N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
77068809 103370 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 17 19 0.2 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)c2c[nH]nc2N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL263200 103370 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 17 19 0.2 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)c2c[nH]nc2N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
162670223 189350 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 521 5 2 5 4.6 O=C(Nc1ccc2c(c1)C1(CCC(O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4787856 189350 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 521 5 2 5 4.6 O=C(Nc1ccc2c(c1)C1(CCC(O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
162650892 187008 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4749974 187008 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44573112 194377 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 484 7 1 5 5.9 CCCCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL494739 194377 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 484 7 1 5 5.9 CCCCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
11583756 196433 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL515123 196433 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
9961721 175258 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 175258 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
10930638 105805 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 105805 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL436874 220468 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL None None None None 10.1021/jm0506928
CHEMBL2430898 217238 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma countingDisplacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)CCCCCCCNC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.bmcl.2013.08.075
67143119 182633 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 742 14 2 11 4.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCCCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4585638 182633 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 742 14 2 11 4.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCCCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44402470 147909 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 437 8 1 6 5.5 COc1ccc(C(C)=O)cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL382747 147909 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 437 8 1 6 5.5 COc1ccc(C(C)=O)cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391835 173083 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.8 CC(C)(C)CC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL427146 173083 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.8 CC(C)(C)CC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
11167850 9518 28 None 6309 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44346397 121276 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 121276 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
87285554 180109 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 631 8 1 7 4.8 Cc1c(N2CCN(Cc3cccc(F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4526641 180109 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 631 8 1 7 4.8 Cc1c(N2CCN(Cc3cccc(F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL436874 220468 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL None None None None 10.1021/jm0506928
118178983 190210 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 552 5 1 5 4.1 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1cccnc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4798682 190210 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 552 5 1 5 4.1 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1cccnc1)C2C 10.1021/acs.jmedchem.0c01076
12784 7365 12 None - 1 Human 7.6 pIC50 = 7.6 Binding
Affinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHRAffinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHR
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.6019/CHEMBL5210307
85469632 7365 12 None - 1 Human 7.6 pIC50 = 7.6 Binding
Affinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHRAffinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHR
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.6019/CHEMBL5210307
CHEMBL4537788 7365 12 None - 1 Human 7.6 pIC50 = 7.6 Binding
Affinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHRAffinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHR
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.6019/CHEMBL5210307
118167818 186211 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 527 5 2 4 4.6 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCNCC2 10.1021/acs.jmedchem.0c01076
CHEMBL4740373 186211 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 527 5 2 4 4.6 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCNCC2 10.1021/acs.jmedchem.0c01076
44365919 127836 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 597 12 4 6 4.9 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(CC(N)=O)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL356890 127836 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 597 12 4 6 4.9 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(CC(N)=O)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
44573626 194311 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494416 194311 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)o1 10.1016/j.bmcl.2009.02.043
44573627 199641 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 459 4 1 5 5.9 Cc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)s1 10.1016/j.bmcl.2009.02.043
CHEMBL522188 199641 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 459 4 1 5 5.9 Cc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)s1 10.1016/j.bmcl.2009.02.043
44406776 141120 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44444628 101094 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 722 8 2 5 8.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250568 101094 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 722 8 2 5 8.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
12784 7365 12 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
85469632 7365 12 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL4537788 7365 12 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
9979079 15136 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL10931 15136 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00134-2
9979079 15136 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL10931 15136 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00133-0
44402472 139599 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL370145 139599 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
44406776 141120 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 141120 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44380192 64221 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL165534 64221 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
118074127 182496 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 714 12 2 11 3.9 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4582367 182496 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 714 12 2 11 3.9 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
87285473 180869 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 663 8 1 7 5.6 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4544693 180869 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 663 8 1 7 5.6 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44267251 105254 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 398 9 2 3 5.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cncnc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL275920 105254 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 398 9 2 3 5.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cncnc2)c1 10.1016/s0960-894x(01)00133-0
44402589 131950 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 542 9 2 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N(C)C)c21 10.1016/j.bmcl.2005.03.030
CHEMBL364510 131950 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 542 9 2 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N(C)C)c21 10.1016/j.bmcl.2005.03.030
44391612 70272 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 471 9 2 6 3.8 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCO)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL179977 70272 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 471 9 2 6 3.8 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCO)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44444663 100975 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 645 8 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CNC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249771 100975 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 645 8 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CNC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44406776 141120 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 141120 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
87285768 177274 3 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Antagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 177274 3 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Antagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
118179051 186997 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4749790 186997 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL385022 219120 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@H](C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
CHEMBL405176 219326 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
11604354 194303 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 428 4 2 4 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c[nH]1 10.1016/j.bmcl.2009.02.043
CHEMBL494400 194303 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 428 4 2 4 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c[nH]1 10.1016/j.bmcl.2009.02.043
9961721 175258 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 175258 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44359331 18913 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 551 7 3 8 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nnc(C)s4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184148 18913 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 551 7 3 8 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nnc(C)s4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL334904 18913 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 551 7 3 8 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nnc(C)s4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44267036 16452 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 482 11 4 2 6.7 CCNC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
CHEMBL11299 16452 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 482 11 4 2 6.7 CCNC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
44402256 143057 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 519 8 2 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2005.03.030
CHEMBL373340 143057 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 519 8 2 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2005.03.030
67143633 180089 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 612 8 2 8 3.2 Cc1c(N2CCN(Cc3ccc(=O)[nH]c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4526188 180089 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 612 8 2 8 3.2 Cc1c(N2CCN(Cc3ccc(=O)[nH]c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44406776 141120 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL93608 222685 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None C[C@H](NC(=O)[C@H]1CCCN1C(=O)[C@@H](CCCN=C(N)N)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc2ccccc2c1)C(N)=O 10.1021/jm990433g
44348298 88325 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2ccc(Cl)cc2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL216112 88325 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2ccc(Cl)cc2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44402431 78188 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 440 8 1 7 5.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL195924 78188 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 440 8 1 7 5.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402378 76451 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 457 8 2 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL193529 76451 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 457 8 2 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402553 78208 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 529 9 2 9 5.4 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)OC)c21 10.1016/j.bmcl.2005.03.030
CHEMBL196079 78208 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 529 9 2 9 5.4 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)OC)c21 10.1016/j.bmcl.2005.03.030
44402057 78713 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 487 9 2 8 4.8 COCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL197254 78713 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 487 9 2 8 4.8 COCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
44391548 72807 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 471 8 1 5 5.3 CCSc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183698 72807 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 471 8 1 5 5.3 CCSc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44391728 72449 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183430 72449 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44365250 128636 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 437 9 3 3 6.2 Cn1ccc2cc(-c3[nH]c4ccccc4c3CCNCCCCc3ccc(O)cc3)ccc21 10.1016/s0960-894x(00)00707-1
CHEMBL359001 128636 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 437 9 3 3 6.2 Cn1ccc2cc(-c3[nH]c4ccccc4c3CCNCCCCc3ccc(O)cc3)ccc21 10.1016/s0960-894x(00)00707-1
145948856 174261 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1290 29 16 15 -1.5 NC(=O)CNC(=O)[C@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1(NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H]2CCC(=O)N2)CCCC1 10.1039/C5MD00259A
CHEMBL4299432 174261 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1290 29 16 15 -1.5 NC(=O)CNC(=O)[C@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1(NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H]2CCC(=O)N2)CCCC1 10.1039/C5MD00259A
118179051 186997 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4749790 186997 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
44573277 194225 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493931 194225 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
44346667 120520 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 120520 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
15602808 14881 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091580 14881 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44406776 141120 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67144466 182559 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 596 8 1 8 3.9 Cc1c(N2CCN(Cc3cccnc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4583933 182559 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 596 8 1 8 3.9 Cc1c(N2CCN(Cc3cccnc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11618517 194335 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 414 4 2 4 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]cn5)CC4)cccc3[nH]2)cc1 10.1016/j.bmcl.2009.02.043
CHEMBL494554 194335 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 414 4 2 4 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]cn5)CC4)cccc3[nH]2)cc1 10.1016/j.bmcl.2009.02.043
11583388 15062 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 457 5 2 5 4.8 CCc1nc(CN2CCN(c3cncc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL1092626 15062 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 457 5 2 5 4.8 CCc1nc(CN2CCN(c3cncc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
44359312 18973 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184274 18973 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL342396 18973 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
11167850 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 10473 38 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44305286 107525 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 611 11 1 8 5.4 C=CC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
CHEMBL292773 107525 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 611 11 1 8 5.4 C=CC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
44305362 109461 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 651 11 1 9 6.1 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)c4ccoc4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL304633 109461 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 651 11 1 9 6.1 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)c4ccoc4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
11167850 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1178 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1187 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL179691 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
44380551 65532 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168649 65532 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
44293075 97439 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 614 12 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL239108 97439 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 614 12 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44214108 107893 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 656 13 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL295152 107893 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 656 13 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293053 108269 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 13 3 4 6.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL297918 108269 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 13 3 4 6.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293054 108272 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 603 14 3 5 6.8 CCOC(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL297927 108272 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 603 14 3 5 6.8 CCOC(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292977 181016 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 14 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45489 181016 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 14 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292785 183786 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 499 10 3 4 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL46268 183786 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 499 10 3 4 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293194 193214 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 14 3 4 6.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)C 10.1016/s0960-894x(01)00274-8
CHEMBL48763 193214 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 14 3 4 6.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)C 10.1016/s0960-894x(01)00274-8
18914248 194510 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 15 3 4 6.4 CCN(CC)C(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL49542 194510 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 15 3 4 6.4 CCN(CC)C(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293074 194562 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 612 12 3 4 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49578 194562 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 612 12 3 4 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292827 194967 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49891 194967 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44348401 168478 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](NC(C)=O)NC(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL413456 168478 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](NC(C)=O)NC(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL436874 220468 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL None None None None 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL None None None None 10.1021/jm0506928
67142985 179657 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 579 8 1 7 4.3 Cc1c(N2CCN(Cc3cccc(Cl)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4515452 179657 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 579 8 1 7 4.3 Cc1c(N2CCN(Cc3cccc(Cl)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44293484 103491 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 604 12 1 3 8.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)C(C)C)c1 10.1016/s0960-894x(01)00275-x
CHEMBL264193 103491 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 604 12 1 3 8.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)C(C)C)c1 10.1016/s0960-894x(01)00275-x
44402398 103754 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1536 41 17 18 1.6 CC(C)C[C@H](NC(=O)[C@@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)C(N)CN)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL266420 103754 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1536 41 17 18 1.6 CC(C)C[C@H](NC(=O)[C@@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)C(N)CN)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
44402638 168037 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1592 43 17 18 2.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CCN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL411987 168037 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1592 43 17 18 2.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CCN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL3085508 217768 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
10258659 18971 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184268 18971 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL341809 18971 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
22100905 191045 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL48380 191045 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
86275342 122964 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/ml5004469
CHEMBL3358413 122964 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/ml5004469
44341081 174843 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 590 10 2 3 8.0 CCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL432450 174843 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 590 10 2 3 8.0 CCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL3085508 217768 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL None None None None 10.1021/jm0506928
44293511 108063 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296426 108063 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
11167850 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL None None None None 10.1021/jm0506928
44572235 196286 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
CHEMBL513998 196286 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
44402638 168037 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1592 43 17 18 2.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CCN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL411987 168037 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1592 43 17 18 2.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CCN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL436874 220468 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL None None None None 10.1021/jm0506928
44359333 18402 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180707 18402 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138999 18402 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293617 195454 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50380 195454 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44380148 127089 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352782 127089 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
11167850 9518 28 None 6309 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44406776 141120 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44406776 141120 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 141120 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL None None None None 10.1021/jm0506928
87285732 179731 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3ccc(Cl)nc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4517137 179731 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3ccc(Cl)nc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL3085508 217768 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL None None None None 10.1021/jm0506928
67143598 177420 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 563 8 1 7 3.8 Cc1c(N2CCN(Cc3cccc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4451280 177420 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 563 8 1 7 3.8 Cc1c(N2CCN(Cc3cccc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44359191 18978 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184298 18978 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL343396 18978 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL436874 220468 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL None None None None 10.1021/jm0506928
44293284 190864 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 543 7 3 8 5.9 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3ccc(Cl)s3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL48249 190864 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 543 7 3 8 5.9 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3ccc(Cl)s3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
11478448 72850 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 553 9 3 5 4.9 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183779 72850 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 553 9 3 5 4.9 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
15462663 105823 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 639 10 0 8 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccc(OC)cc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL280350 105823 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 639 10 0 8 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccc(OC)cc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44365612 47598 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 610 12 3 5 6.8 CCCC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL148571 47598 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 610 12 3 5 6.8 CCCC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
44365627 48414 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 582 10 3 5 6.0 CC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL149188 48414 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 582 10 3 5 6.0 CC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
44365595 49304 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 485 10 4 4 6.0 CNC(=O)Oc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
CHEMBL149992 49304 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 485 10 4 4 6.0 CNC(=O)Oc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
44292785 183786 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 499 10 3 4 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL46268 183786 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 499 10 3 4 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
44365865 201574 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 513 12 4 4 6.8 CCCNC(=O)Oc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
CHEMBL538660 201574 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 513 12 4 4 6.8 CCCNC(=O)Oc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
44444670 101254 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 7 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCCC(O)C3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL251388 101254 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 7 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCCC(O)C3)CC2)c1 10.1016/j.bmcl.2007.09.099
44444678 161718 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 618 12 1 5 7.3 CCN(CC)CCOC1CCN(CCc2c(-c3cc(C)cc(C)c3)[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc23)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL401081 161718 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 618 12 1 5 7.3 CCN(CC)CCOC1CCN(CCc2c(-c3cc(C)cc(C)c3)[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc23)CC1 10.1016/j.bmcl.2007.09.099
44417614 148396 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 148396 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
9917213 210187 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 627 11 1 8 5.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL65569 210187 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 627 11 1 8 5.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
11642933 84885 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 570 10 0 7 6.7 CCOC(=O)c1cn(Cc2ccccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL210277 84885 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 570 10 0 7 6.7 CCOC(=O)c1cn(Cc2ccccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44412946 84890 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 656 11 2 7 8.2 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)Nc4ccccc4)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL210295 84890 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 656 11 2 7 8.2 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)Nc4ccccc4)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
70697569 84749 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.6 CC(C)(C)CNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL2096778 84749 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.6 CC(C)(C)CNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44365252 44573 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 440 9 3 3 6.9 Oc1ccc(CCCCNCCc2c(-c3csc4ccccc34)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL145840 44573 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 440 9 3 3 6.9 Oc1ccc(CCCCNCCc2c(-c3csc4ccccc34)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
44322402 212980 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 4 1 4 5.6 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL86490 212980 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 4 1 4 5.6 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
44322443 213273 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 3 1 4 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OC2CCCN(C)CC2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL88293 213273 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 3 1 4 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OC2CCCN(C)CC2)c1 10.1016/s0960-894x(99)00446-1
9873394 86694 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 596 12 0 8 7.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(CC)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL212472 86694 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 596 12 0 8 7.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(CC)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11635837 145866 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2ccc(OC)cc2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL378654 145866 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2ccc(OC)cc2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11527301 146007 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 570 10 0 7 6.7 CCOC(=O)c1cn(Cc2cccc(F)c2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL378845 146007 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 570 10 0 7 6.7 CCOC(=O)c1cn(Cc2cccc(F)c2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44267057 15113 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 411 9 3 2 6.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(N)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL10929 15113 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 411 9 3 2 6.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(N)cc2)c1 10.1016/s0960-894x(01)00134-2
44267073 16007 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 414 9 2 1 6.7 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(F)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL11067 16007 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 414 9 2 1 6.7 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(F)cc2)c1 10.1016/s0960-894x(01)00134-2
44267029 16019 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 551 12 3 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(=O)(=O)c3ccccc3)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL11074 16019 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 551 12 3 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(=O)(=O)c3ccccc3)cc2)c1 10.1016/s0960-894x(01)00134-2
44402105 131581 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 533 9 2 7 6.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1CCc1ccccc1 10.1016/j.bmcl.2005.03.030
CHEMBL364246 131581 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 533 9 2 7 6.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1CCc1ccccc1 10.1016/j.bmcl.2005.03.030
44391499 72707 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 439 8 1 5 4.1 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183600 72707 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 439 8 1 5 4.1 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44365598 48417 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 462 11 4 6 4.1 COc1ccc(-c2[nH]c3ccccc3c2CCNC[C@@H](O)COc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL149189 48417 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 462 11 4 6 4.1 COc1ccc(-c2[nH]c3ccccc3c2CCNC[C@@H](O)COc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44365351 128781 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 462 11 4 6 4.1 COc1ccc(-c2[nH]c3ccccc3c2CCNC[C@H](O)COc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL359370 128781 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 462 11 4 6 4.1 COc1ccc(-c2[nH]c3ccccc3c2CCNC[C@H](O)COc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
15462666 103277 4 None - 1 Human 5.5 pIC50 = 5.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL262557 103277 4 None - 1 Human 5.5 pIC50 = 5.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44365028 49243 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 457 10 3 4 5.1 COc1ccc(-c2[nH]c3ccccc3c2CCNC(=O)CCCc2ccc(N)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL149940 49243 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 457 10 3 4 5.1 COc1ccc(-c2[nH]c3ccccc3c2CCNC(=O)CCCc2ccc(N)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44214065 127845 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 534 14 2 4 7.6 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(OCc3ccccc3)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL356970 127845 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 534 14 2 4 7.6 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(OCc3ccccc3)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
162667361 189304 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 468 5 1 3 5.1 CC1N(S(=O)(=O)c2ccccc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C1(C)C 10.1021/acs.jmedchem.0c01076
CHEMBL4787218 189304 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 468 5 1 3 5.1 CC1N(S(=O)(=O)c2ccccc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C1(C)C 10.1021/acs.jmedchem.0c01076
162675445 190187 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 470 6 1 4 4.4 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3CC2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4798298 190187 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 470 6 1 4 4.4 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3CC2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL428186 220204 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N(C)CC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44573586 194280 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 443 4 1 5 5.5 Cc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494232 194280 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 443 4 1 5 5.5 Cc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
44346667 120520 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 120520 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
10930638 105805 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 105805 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402466 78660 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL197089 78660 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
44573713 199668 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
CHEMBL522202 199668 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
44391754 175452 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 519 9 3 5 4.2 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL436472 175452 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 519 9 3 5 4.2 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL436874 220468 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL None None None None 10.1021/jm0506928
162650892 187008 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4749974 187008 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
9982147 213068 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00447-3
CHEMBL87020 213068 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00447-3
44365644 48405 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 612 11 3 6 6.6 CCOC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL149181 48405 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 612 11 3 6 6.6 CCOC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
44365772 49161 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 539 10 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCCCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL149881 49161 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 539 10 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCCCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
44561397 196603 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL516479 196603 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44359301 18408 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nncs4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180754 18408 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nncs4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL141221 18408 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nncs4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44358957 18916 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184158 18916 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL336039 18916 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293130 188671 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 482 11 3 3 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(N)=O)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL47791 188671 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 482 11 3 3 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(N)=O)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293131 195618 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 520 10 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50663 195618 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 520 10 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44214072 184197 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 484 11 3 4 6.5 CCOC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL46385 184197 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 484 11 3 4 6.5 CCOC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
9982147 213068 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL87020 213068 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
44406776 141120 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44573625 194310 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494415 194310 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
44359303 18409 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 520 7 4 7 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nc[nH]n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180760 18409 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 520 7 4 7 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nc[nH]n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL141539 18409 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 520 7 4 7 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nc[nH]n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44391714 128913 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccncc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL359668 128913 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccncc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44402571 131731 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 379 6 1 4 5.6 Cc1ccccc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL364297 131731 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 379 6 1 4 5.6 Cc1ccccc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391498 172899 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 524 10 1 7 3.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(OCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL426060 172899 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 524 10 1 7 3.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(OCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
67144370 181394 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3cccc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4557575 181394 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3cccc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143547 178295 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccc(C#N)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4464132 178295 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccc(C#N)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11626096 194049 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 428 4 1 5 4.6 Cn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1 10.1016/j.bmcl.2009.02.043
CHEMBL492780 194049 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 428 4 1 5 4.6 Cn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1 10.1016/j.bmcl.2009.02.043
44444678 161718 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 618 12 1 5 7.3 CCN(CC)CCOC1CCN(CCc2c(-c3cc(C)cc(C)c3)[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc23)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL401081 161718 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 618 12 1 5 7.3 CCN(CC)CCOC1CCN(CCc2c(-c3cc(C)cc(C)c3)[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc23)CC1 10.1016/j.bmcl.2007.09.099
11620431 186148 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL473807 186148 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
11671279 137662 0 None 331 2 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cellsInhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cells
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL368511 137662 0 None 331 2 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cellsInhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cells
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44402492 132962 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1cccnc1 10.1016/j.bmcl.2005.03.030
CHEMBL364933 132962 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1cccnc1 10.1016/j.bmcl.2005.03.030
44402471 141999 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 485 9 2 7 6.0 CCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL372316 141999 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 485 9 2 7 6.0 CCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
44391548 72807 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 471 8 1 5 5.3 CCSc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183698 72807 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 471 8 1 5 5.3 CCSc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44561105 193530 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 476 6 3 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL488812 193530 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 476 6 3 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44417615 148701 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 148701 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346398 21310 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 21310 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402572 77969 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 429 7 2 7 4.6 CNC(=O)Nc1ccc2c(c1)nc(SCc1cc([N+](=O)[O-])ccc1OC)n2C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL195626 77969 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 429 7 2 7 4.6 CNC(=O)Nc1ccc2c(c1)nc(SCc1cc([N+](=O)[O-])ccc1OC)n2C(C)C 10.1016/j.bmcl.2005.03.030
44444647 161780 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 688 10 2 7 4.6 CC(=O)N1CCN(CC(O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL401352 161780 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 688 10 2 7 4.6 CC(=O)N1CCN(CC(O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
44444676 161717 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 646 9 1 6 5.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(OCC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401080 161717 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 646 9 1 6 5.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(OCC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
118179235 188714 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 548 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4779806 188714 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 548 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
118179051 186997 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4749790 186997 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
44573110 193973 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL492327 193973 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
44577104 185525 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL468565 185525 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
11294792 70062 0 None 380 2 Human 7.5 pIC50 = 7.5 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL179269 70062 0 None 380 2 Human 7.5 pIC50 = 7.5 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
67143679 180940 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 544 8 1 6 4.8 Cc1c(N2CCC(Cc3ccccc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4546864 180940 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 544 8 1 6 4.8 Cc1c(N2CCC(Cc3ccccc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
67143755 182205 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccccc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4576169 182205 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccccc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44391826 71656 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 549 10 3 6 4.2 COc1ccc(CNS(=O)(=O)c2ccc3c(c2)nc(CCNC(=O)NC(C)(C)C)n3Cc2ccccc2)cc1 10.1016/j.bmcl.2004.10.090
CHEMBL182178 71656 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 549 10 3 6 4.2 COc1ccc(CNS(=O)(=O)c2ccc3c(c2)nc(CCNC(=O)NC(C)(C)C)n3Cc2ccccc2)cc1 10.1016/j.bmcl.2004.10.090
44444645 161779 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 672 9 2 6 4.8 CC(=O)NC1CCN(C(=O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL401351 161779 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 672 9 2 6 4.8 CC(=O)NC1CCN(C(=O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
162665107 188915 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 570 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ncccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4782228 188915 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 570 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ncccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
44444626 161662 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 680 7 2 5 7.6 COC(=O)/N=C(/NC[C@@H](C)c1c(-c2cc(C)cc(C)c2)[nH]c2sc(C(C)(C)C(=O)N3C4CCC3CC4)cc12)N1CCC(c2ccncc2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL400739 161662 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 680 7 2 5 7.6 COC(=O)/N=C(/NC[C@@H](C)c1c(-c2cc(C)cc(C)c2)[nH]c2sc(C(C)(C)C(=O)N3C4CCC3CC4)cc12)N1CCC(c2ccncc2)C1 10.1016/j.bmcl.2007.09.099
44402464 175868 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL439860 175868 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL436874 220468 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL None None None None 10.1021/jm0506928
67143749 176925 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 561 8 2 8 3.4 Cc1c(N2CCN(Cc3ccc(O)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4444237 176925 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 561 8 2 8 3.4 Cc1c(N2CCN(Cc3ccc(O)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
67143490 178388 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cscn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4465381 178388 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cscn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11525358 194121 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmcl.2009.02.043
CHEMBL493185 194121 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmcl.2009.02.043
44417615 148701 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 148701 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402360 140221 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 505 7 2 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1-c1ccccc1 10.1016/j.bmcl.2005.03.030
CHEMBL370623 140221 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 505 7 2 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1-c1ccccc1 10.1016/j.bmcl.2005.03.030
67143710 177115 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccccc3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4447139 177115 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccccc3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
9979079 15136 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human Gonadotropin-releasing hormone receptor bindingInhibition of human Gonadotropin-releasing hormone receptor binding
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL10931 15136 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human Gonadotropin-releasing hormone receptor bindingInhibition of human Gonadotropin-releasing hormone receptor binding
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00134-2
9979079 15136 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity evaluated against human Gonadotropin-releasing hormone receptorInhibitory activity evaluated against human Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL10931 15136 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity evaluated against human Gonadotropin-releasing hormone receptorInhibitory activity evaluated against human Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00133-0
162660654 188079 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 539 5 1 5 4.2 O=C(Nc1ccc2c(c1)C1(CC[S+]([O-])CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4762368 188079 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 539 5 1 5 4.2 O=C(Nc1ccc2c(c1)C1(CC[S+]([O-])CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
44322400 213062 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 2 6 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL86976 213062 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 2 6 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCCN2)c1 10.1016/s0960-894x(99)00447-3
44322420 213474 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 441 5 2 6 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC2CCCNC2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL89672 213474 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 441 5 2 6 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC2CCCNC2)c1 10.1016/s0960-894x(99)00447-3
44293274 108033 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 510 12 1 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCN(C)CCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296199 108033 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 510 12 1 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCN(C)CCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293594 108344 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298497 108344 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293134 194180 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49366 194180 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44348278 163658 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2cccnc2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL407193 163658 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2cccnc2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44267048 169999 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 475 10 3 3 5.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(S(N)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL418339 169999 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 475 10 3 3 5.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(S(N)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00134-2
44267256 15936 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 447 9 2 2 7.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cnc3ccccc3c2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11014 15936 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 447 9 2 2 7.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cnc3ccccc3c2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL2430900 217240 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma countingDisplacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)CCCCCNC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.bmcl.2013.08.075
67143674 181848 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3ccc([N+](=O)[O-])cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4568223 181848 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3ccc([N+](=O)[O-])cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44402105 131581 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 533 9 2 7 6.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1CCc1ccccc1 10.1016/j.bmcl.2005.03.030
CHEMBL364246 131581 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 533 9 2 7 6.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1CCc1ccccc1 10.1016/j.bmcl.2005.03.030
44346397 121276 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 121276 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
162645007 186240 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 186240 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44573625 194310 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494415 194310 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
15602806 15068 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL1092638 15068 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
44402553 78208 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 529 9 2 9 5.4 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)OC)c21 10.1016/j.bmcl.2005.03.030
CHEMBL196079 78208 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 529 9 2 9 5.4 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)OC)c21 10.1016/j.bmcl.2005.03.030
CHEMBL436874 220468 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL None None None None 10.1021/jm0506928
CHEMBL330173 218109 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
10919052 120296 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 120296 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44444668 161058 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 7 1 6 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL398648 161058 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 7 1 6 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67143804 179975 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 724 13 3 9 4.1 Cc1c(N2CCN(Cc3cccc(C(=O)NCCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4522657 179975 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 724 13 3 9 4.1 Cc1c(N2CCN(Cc3cccc(C(=O)NCCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
118179169 186705 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 613 6 1 4 5.4 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccc(F)cc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4746174 186705 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 613 6 1 4 5.4 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccc(F)cc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44328354 103930 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL 980 24 9 10 0.4 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)NCCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
CHEMBL267986 103930 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL 980 24 9 10 0.4 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)NCCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
11518185 194467 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 4 1 5 5.2 Cc1nn(C)c(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL495190 194467 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 4 1 5 5.2 Cc1nn(C)c(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
10930638 105805 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 105805 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44391734 129396 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 509 10 3 5 3.6 CCNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL360297 129396 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 509 10 3 5 3.6 CCNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44406776 141120 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
10919052 120296 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 120296 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417614 148396 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 148396 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10919052 120296 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 120296 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44391692 71074 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 437 7 1 4 4.8 CC(C)c1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL181057 71074 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 437 7 1 4 4.8 CC(C)c1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
25194091 195789 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 498 7 3 5 5.5 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL508898 195789 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 498 7 3 5 5.5 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44322502 213754 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 390 4 1 4 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(C)ccc3c2OCC2CCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL91311 213754 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 390 4 1 4 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(C)ccc3c2OCC2CCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
44309572 211118 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 517 7 3 7 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(02)00370-0
CHEMBL71561 211118 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 517 7 3 7 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(02)00370-0
44352512 124077 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 483 7 3 7 4.7 Cc1cc(-c2c(O)nc3ccc(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(01)00779-x
CHEMBL339636 124077 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 483 7 3 7 4.7 Cc1cc(-c2c(O)nc3ccc(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(01)00779-x
10484172 105817 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 632 12 3 6 5.8 CCS(=O)(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL280296 105817 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 632 12 3 6 5.8 CCS(=O)(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL436874 220468 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL None None None None 10.1021/jm0506928
10649568 21338 0 None -10 2 Rat 8.4 pIC50 = 8.4 Binding
In vitro inhibition of binding to GnRH receptor in ratIn vitro inhibition of binding to GnRH receptor in rat
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 21338 0 None -10 2 Rat 8.4 pIC50 = 8.4 Binding
In vitro inhibition of binding to GnRH receptor in ratIn vitro inhibition of binding to GnRH receptor in rat
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
10649568 21338 0 None -10 2 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of Rat gonadotropin-releasing hormone receptorInhibition of Rat gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm049218c
CHEMBL120432 21338 0 None -10 2 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of Rat gonadotropin-releasing hormone receptorInhibition of Rat gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm049218c
9936667 107294 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 525 10 3 4 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL291201 107294 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 525 10 3 4 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293071 108378 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 589 14 3 5 6.6 CCOC(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL298748 108378 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 589 14 3 5 6.6 CCOC(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293208 177922 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 16 3 4 7.2 CCCCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL445848 177922 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 16 3 4 7.2 CCCCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292988 189220 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 586 12 3 4 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47862 189220 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 586 12 3 4 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
1184 10505 36 None 426 2 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
9874838 10505 36 None 426 2 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
CHEMBL71917 10505 36 None 426 2 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
10603202 175381 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor (LHRH) receptor.The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor (LHRH) receptor.
ChEMBL 573 9 1 7 6.4 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
CHEMBL435974 175381 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor (LHRH) receptor.The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor (LHRH) receptor.
ChEMBL 573 9 1 7 6.4 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
1184 10505 36 None -426 2 Rat 8.4 pIC50 = 8.4 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
9874838 10505 36 None -426 2 Rat 8.4 pIC50 = 8.4 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
CHEMBL71917 10505 36 None -426 2 Rat 8.4 pIC50 = 8.4 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
CHEMBL3085508 217768 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL None None None None 10.1021/jm0506928
67142818 180826 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 563 8 1 7 3.8 Cc1c(N2CCN(Cc3ccccc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4543788 180826 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 563 8 1 7 3.8 Cc1c(N2CCN(Cc3ccccc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
11478448 72850 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 553 9 3 5 4.9 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183779 72850 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 553 9 3 5 4.9 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
1185 10473 38 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
15602804 14853 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091209 14853 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44321496 112740 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 657 13 2 5 6.3 CCS(=O)(=O)N1CCN(C(=O)C(C)(C)c2ccc3[nH]c(-c4cc(C)cc(C)c4)c([C@H](C)CNCCCCc4ccncc4)c3c2)CC1 10.1016/s0960-894x(01)00512-1
CHEMBL312995 112740 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 657 13 2 5 6.3 CCS(=O)(=O)N1CCN(C(=O)C(C)(C)c2ccc3[nH]c(-c4cc(C)cc(C)c4)c([C@H](C)CNCCCCc4ccncc4)c3c2)CC1 10.1016/s0960-894x(01)00512-1
CHEMBL436874 220468 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44341080 117355 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 604 11 2 3 8.4 CCCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL325417 117355 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 604 11 2 3 8.4 CCCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL436874 220468 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL None None None None 10.1021/jm0506928
44321291 213056 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 632 11 2 3 9.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5(C)CC4CC(C)(C)C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86950 213056 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 632 11 2 3 9.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5(C)CC4CC(C)(C)C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321292 213065 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCCC4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL87000 213065 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCCC4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL436874 220468 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL None None None None 10.1021/jm0506928
44406776 141120 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44293804 108576 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL300095 108576 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44593424 182912 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459215 182912 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL436874 220468 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL None None None None 10.1021/jm0506928
44593424 182912 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL459215 182912 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
71623059 187604 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4756920 187604 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44365898 126434 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 442 10 3 3 6.3 COc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
CHEMBL346903 126434 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 442 10 3 3 6.3 COc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
44593424 182912 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459215 182912 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44593424 182912 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL459215 182912 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44346397 121276 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 121276 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
9961721 175258 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 175258 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
9961721 175258 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 175258 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44358962 18915 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 559 7 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)nc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184155 18915 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 559 7 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)nc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL335764 18915 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 559 7 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)nc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44267238 103294 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL262715 103294 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44413009 86540 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 537 9 1 7 6.2 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL211808 86540 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 537 9 1 7 6.2 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44266961 15931 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 518 13 4 3 5.9 CCNS(=O)(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
CHEMBL11011 15931 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 518 13 4 3 5.9 CCNS(=O)(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
44267238 103294 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL262715 103294 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
44365269 46642 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1ccc(C)c(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL147740 46642 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1ccc(C)c(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44274327 88958 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 589 10 0 7 6.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(CC(C)C)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21704 88958 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 589 10 0 7 6.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(CC(C)C)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
15462660 89601 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 623 10 0 7 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(Cc2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21804 89601 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 623 10 0 7 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(Cc2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
10930638 105805 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 105805 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10930638 105805 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 105805 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346397 121276 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 121276 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
11527384 84265 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2cccc(OC)c2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL208714 84265 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2cccc(OC)c2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11226884 84443 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 570 10 0 7 6.7 CCOC(=O)c1cn(Cc2ccc(F)cc2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL208904 84443 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 570 10 0 7 6.7 CCOC(=O)c1cn(Cc2ccc(F)cc2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
71459964 86272 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 573 10 2 5 7.7 Cc1cc(C)cc(-c2c(OCC[C@@H]3CCC[C@H](CCCc4ccccc4)N3)c3cc([N+](=O)[O-])c(Cl)cc3[nH]c2=O)c1 10.1016/j.bmcl.2003.12.101
CHEMBL2113713 86272 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 573 10 2 5 7.7 Cc1cc(C)cc(-c2c(OCC[C@@H]3CCC[C@H](CCCc4ccccc4)N3)c3cc([N+](=O)[O-])c(Cl)cc3[nH]c2=O)c1 10.1016/j.bmcl.2003.12.101
44391784 129104 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.9 CC(C)(C)NC(=O)CCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL359860 129104 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.9 CC(C)(C)NC(=O)CCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44365171 45604 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 416 9 3 4 4.9 COc1ccc(-c2[nH]c3ccccc3c2CCNCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL146678 45604 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 416 9 3 4 4.9 COc1ccc(-c2[nH]c3ccccc3c2CCNCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44417614 148396 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 148396 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10919052 120296 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 120296 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44322380 213306 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 382 4 1 4 5.0 CN1CCCC(COc2c(-c3ccccc3)c(O)nc3cc(Cl)ccc23)C1 10.1016/s0960-894x(99)00446-1
CHEMBL88516 213306 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 382 4 1 4 5.0 CN1CCCC(COc2c(-c3ccccc3)c(O)nc3cc(Cl)ccc23)C1 10.1016/s0960-894x(99)00446-1
44322302 213435 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 4 1 4 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL89332 213435 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 4 1 4 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
44391510 129717 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3cccc(OC)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL360693 129717 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3cccc(OC)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
67143420 169687 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4173938 169687 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
145948911 174263 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1304 29 16 15 -1.1 NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1(NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCC(=O)N2)CCCCC1 10.1039/C5MD00259A
CHEMBL4299453 174263 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1304 29 16 15 -1.1 NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1(NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCC(=O)N2)CCCCC1 10.1039/C5MD00259A
86275342 122964 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/ml5004469
CHEMBL3358413 122964 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/ml5004469
118179051 186997 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4749790 186997 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
11634198 194145 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
CHEMBL493344 194145 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
44267278 16082 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 3 5.6 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(N)nc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11101 16082 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 3 5.6 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(N)nc2)c1 10.1016/s0960-894x(01)00133-0
44402645 175903 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 528 9 3 8 4.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC)c21 10.1016/j.bmcl.2005.03.030
CHEMBL440212 175903 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 528 9 3 8 4.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC)c21 10.1016/j.bmcl.2005.03.030
CHEMBL436874 220468 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL None None None None 10.1021/jm0506928
44406776 141120 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44402646 140212 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 570 9 3 8 6.1 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC(C)(C)C)c21 10.1016/j.bmcl.2005.03.030
CHEMBL370587 140212 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 570 9 3 8 6.1 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC(C)(C)C)c21 10.1016/j.bmcl.2005.03.030
87285550 181107 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 775 13 3 9 5.4 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCP(=O)(O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4550720 181107 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 775 13 3 9 5.4 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCP(=O)(O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
71668147 186769 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 637 6 1 6 4.6 O=C(NCc1ccc(C(F)(F)F)cn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4746969 186769 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 637 6 1 6 4.6 O=C(NCc1ccc(C(F)(F)F)cn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
67143723 182178 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 656 9 2 8 3.8 Cc1c(N2CCN(Cc3cccc(C(N)=O)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4575491 182178 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 656 9 2 8 3.8 Cc1c(N2CCN(Cc3cccc(C(N)=O)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL406243 219379 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)NC1(C(=O)N[C@H](CCCN=C(N)N)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)CCC1 10.1021/jm990433g
44402463 134302 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 457 7 2 7 5.2 CCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL366236 134302 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 457 7 2 7 5.2 CCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL436874 220468 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL None None None None 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
118178986 188978 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 4 4.5 CC(=O)N1CCC2(CC1)CN(S(=O)(=O)c1ccc(F)cc1)c1ccc(C(=O)NCc3ccccc3Cl)cc12 10.1021/acs.jmedchem.0c01076
CHEMBL4782882 188978 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 4 4.5 CC(=O)N1CCC2(CC1)CN(S(=O)(=O)c1ccc(F)cc1)c1ccc(C(=O)NCc3ccccc3Cl)cc12 10.1021/acs.jmedchem.0c01076
11167850 9518 28 None 6309 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
86272223 122966 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 737 7 1 7 6.0 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1cccc(OC(F)(F)F)c1 10.1021/ml5004469
CHEMBL3358415 122966 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 737 7 1 7 6.0 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1cccc(OC(F)(F)F)c1 10.1021/ml5004469
11525358 194121 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmcl.2009.02.043
CHEMBL493185 194121 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmcl.2009.02.043
44444675 161501 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)C(C)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399857 161501 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)C(C)C2)c1 10.1016/j.bmcl.2007.09.099
44402293 78203 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2005.03.030
CHEMBL196040 78203 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2005.03.030
86275345 188849 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4781434 188849 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
15602808 14881 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091580 14881 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44417615 148701 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 148701 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346667 120520 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 120520 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
162649425 186799 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 6 3.9 O=C(Nc1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4747322 186799 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 6 3.9 O=C(Nc1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL327359 218070 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)NCC(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44359224 18401 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 565 10 2 5 7.8 CCC(C)N(C(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl)C(C)CC 10.1016/s0960-894x(00)00024-x
CHEMBL1180706 18401 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 565 10 2 5 7.8 CCC(C)N(C(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl)C(C)CC 10.1016/s0960-894x(00)00024-x
CHEMBL138977 18401 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 565 10 2 5 7.8 CCC(C)N(C(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl)C(C)CC 10.1016/s0960-894x(00)00024-x
44293165 108470 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 556 16 2 5 5.7 COCCN(CCOC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL299392 108470 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 556 16 2 5 5.7 COCCN(CCOC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44267275 104915 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 490 11 3 4 5.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)nc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL273625 104915 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 490 11 3 4 5.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)nc2)c1 10.1016/s0960-894x(01)00133-0
44295820 108762 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 469 6 2 6 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2NCCCC2C)c1 10.1016/j.bmcl.2003.12.101
CHEMBL301501 108762 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 469 6 2 6 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2NCCCC2C)c1 10.1016/j.bmcl.2003.12.101
44402467 177435 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL445143 177435 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL410269 219589 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
11518185 194467 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 4 1 5 5.2 Cc1nn(C)c(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL495190 194467 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 4 1 5 5.2 Cc1nn(C)c(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
44346397 121276 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 121276 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44267254 16051 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccccn2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11087 16051 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccccn2)c1 10.1016/s0960-894x(01)00133-0
44267271 16579 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 386 9 3 2 5.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2c[nH]cn2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11375 16579 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 386 9 3 2 5.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2c[nH]cn2)c1 10.1016/s0960-894x(01)00133-0
11318649 71128 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3F)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL181257 71128 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3F)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44561142 193482 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4ccc5[nH]c(=S)[nH]c5c4)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL488478 193482 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4ccc5[nH]c(=S)[nH]c5c4)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44346397 121276 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 121276 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44267242 16824 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 355 6 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11523 16824 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 355 6 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
44573791 194167 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 484 7 1 5 6.2 CCCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493565 194167 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 484 7 1 5 6.2 CCCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
145950097 169581 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 527 8 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cccc(F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4172391 169581 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 527 8 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cccc(F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44406776 141120 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 141120 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
118178976 187960 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 6 1 4 5.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4761024 187960 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 6 1 4 5.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44573789 194119 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493167 194119 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
15602807 14992 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1092245 14992 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44572236 178678 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL446978 178678 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44267035 103986 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 504 12 4 3 5.5 CNS(=O)(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
CHEMBL268479 103986 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 504 12 4 3 5.5 CNS(=O)(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
44402499 76598 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2005.03.030
CHEMBL193689 76598 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2005.03.030
44406776 141120 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
1185 10473 38 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44391499 72707 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 439 8 1 5 4.1 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183600 72707 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 439 8 1 5 4.1 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
162647697 186638 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 523 5 1 5 5.2 O=C(Nc1ccc2c(c1)C1(CCSCC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4745391 186638 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 523 5 1 5 5.2 O=C(Nc1ccc2c(c1)C1(CCSCC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
53239184 176380 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 652 8 1 9 5.2 Cc1c(N2CCN(Cc3nc4ccccc4s3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4436375 176380 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 652 8 1 9 5.2 Cc1c(N2CCN(Cc3nc4ccccc4s3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44267054 16567 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 468 10 4 2 6.4 CNC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
CHEMBL11368 16567 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 468 10 4 2 6.4 CNC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
67144478 177130 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 563 8 1 7 3.8 Cc1c(N2CCN(Cc3ccc(F)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4447332 177130 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 563 8 1 7 3.8 Cc1c(N2CCN(Cc3ccc(F)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44406776 141120 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL None None None None 10.1021/jm0506928
90663998 113606 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 787 14 4 10 4.9 O=C(NC[C@H]1CO[C@](Cn2ccnc2)(c2ccc(Cl)cc2Cl)O1)[C@H](CC1=CNCN1)NC(=O)[C@@H]1CCCN1C(=O)OCC(c1ccccc1)c1ccccc1 10.1021/jm00129a003
CHEMBL3144569 113606 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 787 14 4 10 4.9 O=C(NC[C@H]1CO[C@](Cn2ccnc2)(c2ccc(Cl)cc2Cl)O1)[C@H](CC1=CNCN1)NC(=O)[C@@H]1CCCN1C(=O)OCC(c1ccccc1)c1ccccc1 10.1021/jm00129a003
44417615 148701 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 148701 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44387961 172800 0 None 144 2 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cellsInhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cells
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL425523 172800 0 None 144 2 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cellsInhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cells
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44391510 129717 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3cccc(OC)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL360693 129717 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3cccc(OC)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
162667361 189304 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 468 5 1 3 5.1 CC1N(S(=O)(=O)c2ccccc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C1(C)C 10.1021/acs.jmedchem.0c01076
CHEMBL4787218 189304 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 468 5 1 3 5.1 CC1N(S(=O)(=O)c2ccccc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C1(C)C 10.1021/acs.jmedchem.0c01076
162645007 186240 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 186240 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44573791 194167 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 484 7 1 5 6.2 CCCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493565 194167 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 484 7 1 5 6.2 CCCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
44573276 194195 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 484 6 1 5 5.9 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)n1CC 10.1016/j.bmcl.2009.02.043
CHEMBL493731 194195 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 484 6 1 5 5.9 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)n1CC 10.1016/j.bmcl.2009.02.043
11226753 70118 0 None 389 2 Human 7.3 pIC50 = 7.3 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL179429 70118 0 None 389 2 Human 7.3 pIC50 = 7.3 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
44406776 141120 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
87285708 180684 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 749 13 2 8 6.1 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4540232 180684 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 749 13 2 8 6.1 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
145957335 169084 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 519 7 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)C3CCSCC3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4164417 169084 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 519 7 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)C3CCSCC3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44402646 140212 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 570 9 3 8 6.1 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC(C)(C)C)c21 10.1016/j.bmcl.2005.03.030
CHEMBL370587 140212 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 570 9 3 8 6.1 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC(C)(C)C)c21 10.1016/j.bmcl.2005.03.030
44391628 72646 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 513 10 1 7 4.4 CCOC(=O)CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183572 72646 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 513 10 1 7 4.4 CCOC(=O)CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44391754 175452 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 519 9 3 5 4.2 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL436472 175452 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 519 9 3 5 4.2 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
53239184 176380 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 652 8 1 9 5.2 Cc1c(N2CCN(Cc3nc4ccccc4s3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4436375 176380 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 652 8 1 9 5.2 Cc1c(N2CCN(Cc3nc4ccccc4s3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44444641 161748 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 601 7 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401212 161748 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 601 7 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67143715 180267 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 570 8 1 8 3.5 Cc1c(N2CCN(Cc3cccc(C#N)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4530350 180267 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 570 8 1 8 3.5 Cc1c(N2CCN(Cc3cccc(C#N)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44305604 210194 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 625 11 1 8 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)C4CC4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL65614 210194 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 625 11 1 8 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)C4CC4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
11282957 129111 1 None 1096 2 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
CHEMBL359894 129111 1 None 1096 2 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
44292919 107922 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295376 107922 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293305 108238 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL297703 108238 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44292990 107975 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 16 3 4 7.2 CCCN(CCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL295731 107975 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 16 3 4 7.2 CCCN(CCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293178 108199 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 658 17 3 4 7.9 CCCN(CCC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL297430 108199 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 658 17 3 4 7.9 CCCN(CCC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292979 194968 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 483 10 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49893 194968 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 483 10 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44348173 177260 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1533 39 15 17 1.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL444903 177260 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1533 39 15 17 1.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
67143432 178906 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 8 4.3 Cc1ncccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
CHEMBL4472942 178906 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 8 4.3 Cc1ncccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
11526254 194392 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 504 5 1 7 4.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccnc(S(C)(=O)=O)n5)CC4)cccc3[nH]2)cc1 10.1021/jm701249f
CHEMBL494797 194392 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 504 5 1 7 4.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccnc(S(C)(=O)=O)n5)CC4)cccc3[nH]2)cc1 10.1021/jm701249f
CHEMBL3085508 217768 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 10473 38 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44321695 112758 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccn(C)c2=O)c1 10.1016/s0960-894x(01)00512-1
CHEMBL313086 112758 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccn(C)c2=O)c1 10.1016/s0960-894x(01)00512-1
CHEMBL3085508 217768 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44348310 164600 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)c2ccc(NC(C)=O)cc2)cc1 10.1021/jm970024p
CHEMBL408335 164600 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)c2ccc(NC(C)=O)cc2)cc1 10.1021/jm970024p
155531714 182970 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL4593521 182970 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
44406776 141120 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL None None None None 10.1021/jm0506928
145952094 169684 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 523 7 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccc(C)cc3C)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4173914 169684 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 523 7 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccc(C)cc3C)c2=O)c1F 10.1016/j.ejmech.2017.12.095
86275573 122967 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 687 6 1 6 5.8 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(Cl)cc1 10.1021/ml5004469
CHEMBL3358416 122967 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 687 6 1 6 5.8 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(Cl)cc1 10.1021/ml5004469
44561397 196603 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL516479 196603 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
11167850 9518 28 None 6309 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44348418 103420 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1559 41 13 16 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL263629 103420 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1559 41 13 16 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44321510 113916 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 608 15 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL316159 113916 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 608 15 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL436874 220468 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL None None None None 10.1021/jm0506928
44572236 178678 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL446978 178678 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44561369 197247 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL517881 197247 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL436874 220468 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL None None None None 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
15602805 14879 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
CHEMBL1091579 14879 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
44292888 181557 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 567 14 3 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45614 181557 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 567 14 3 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44295630 197607 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 559 8 3 7 6.6 CCC1CCC[C@@H](CCOc2c(-c3cc(C)cc(C)c3)c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc23)N1 10.1016/j.bmcl.2003.12.101
CHEMBL51841 197607 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 559 8 3 7 6.6 CCC1CCC[C@@H](CCOc2c(-c3cc(C)cc(C)c3)c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc23)N1 10.1016/j.bmcl.2003.12.101
CHEMBL436874 220468 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL None None None None 10.1021/jm0506928
24825725 199406 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL521674 199406 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL436874 220468 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL None None None None 10.1021/jm0506928
9979079 15136 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL10931 15136 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
15462657 86998 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 609 9 0 7 6.8 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21373 86998 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 609 9 0 7 6.8 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
9979079 15136 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL10931 15136 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
25193798 176977 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 562 6 2 5 6.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL444509 176977 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 562 6 2 5 6.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
9961721 175258 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 175258 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
9979079 15136 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL10931 15136 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44267231 16368 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 411 10 2 2 6.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11253 16368 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 411 10 2 2 6.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
44391735 129115 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 591 10 3 5 5.7 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1Cl 10.1016/j.bmcl.2004.10.090
CHEMBL359914 129115 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 591 10 3 5 5.7 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1Cl 10.1016/j.bmcl.2004.10.090
CHEMBL436874 220468 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44365420 47994 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 9 3 2 6.0 Cc1ccccc1-c1[nH]c2ccccc2c1CCNCCCCc1ccc(O)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL148884 47994 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 9 3 2 6.0 Cc1ccccc1-c1[nH]c2ccccc2c1CCNCCCCc1ccc(O)cc1 10.1016/s0960-894x(00)00707-1
90663997 113605 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 849 14 6 11 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC1=CNCN1)C(=O)NC[C@H]1CO[C@](Cn2ccnc2)(c2ccc(Cl)cc2Cl)O1 10.1021/jm00129a003
CHEMBL3144568 113605 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 849 14 6 11 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC1=CNCN1)C(=O)NC[C@H]1CO[C@](Cn2ccnc2)(c2ccc(Cl)cc2Cl)O1 10.1021/jm00129a003
44417614 148396 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 148396 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10919052 120296 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 120296 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44322401 113327 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 396 4 2 4 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCNC2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL314147 113327 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 396 4 2 4 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCNC2)c1 10.1016/s0960-894x(99)00446-1
44322444 213411 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 396 4 1 4 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL89186 213411 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 396 4 1 4 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
11570616 85081 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 506 9 0 8 5.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(C)C)c2c1=O 10.1021/jm0512894
CHEMBL210845 85081 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 506 9 0 8 5.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(C)C)c2c1=O 10.1021/jm0512894
44412978 86533 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3cccc(OC)c3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL211752 86533 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3cccc(OC)c3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44267086 104853 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 441 10 2 3 6.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc([N+](=O)[O-])cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL273296 104853 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 441 10 2 3 6.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc([N+](=O)[O-])cc2)c1 10.1016/s0960-894x(01)00134-2
10603202 175381 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 573 9 1 7 6.4 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
CHEMBL435974 175381 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 573 9 1 7 6.4 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
44365118 48323 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 473 12 2 5 5.9 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc([N+](=O)[O-])cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL149124 48323 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 473 12 2 5 5.9 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc([N+](=O)[O-])cc2)cc1OC 10.1016/s0960-894x(00)00707-1
11167850 9518 28 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44346398 21310 0 None - 1 Human 5.3 pIC50 = 5.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 21310 0 None - 1 Human 5.3 pIC50 = 5.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417615 148701 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 148701 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
11511860 146112 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 476 8 0 7 5.1 CCOC(=O)c1cn(C)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL379274 146112 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 476 8 0 7 5.1 CCOC(=O)c1cn(C)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11167850 9518 28 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44573113 200017 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
CHEMBL523711 200017 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
44444665 100976 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 8 1 5 6.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249772 100976 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 8 1 5 6.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44444652 101277 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 588 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL251578 101277 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 588 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44402466 78660 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL197089 78660 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
44391693 70541 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 605 9 3 5 5.4 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(C(F)(F)F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL180167 70541 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 605 9 3 5 5.4 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(C(F)(F)F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
67144162 181832 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 657 9 1 8 4.3 Cc1c(N2CCN(Cc3cccc([S+](C)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4567854 181832 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 657 9 1 8 4.3 Cc1c(N2CCN(Cc3cccc([S+](C)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44402403 78304 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 515 9 3 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)O)c21 10.1016/j.bmcl.2005.03.030
CHEMBL196288 78304 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 515 9 3 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)O)c21 10.1016/j.bmcl.2005.03.030
44561141 200581 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 432 3 3 4 4.4 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL527422 200581 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 432 3 3 4 4.4 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44346397 121276 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 121276 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346667 120520 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 120520 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL436874 220468 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL None None None None 10.1021/jm0506928
87285768 177274 3 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 177274 3 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
25193700 180061 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 534 7 2 5 5.9 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL452547 180061 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 534 7 2 5 5.9 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
11167850 9518 28 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44417615 148701 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 148701 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
87285521 181798 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3cccnc3Cl)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4567165 181798 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3cccnc3Cl)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44444644 161778 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 601 6 1 4 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(C(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401350 161778 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 601 6 1 4 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(C(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67143487 177542 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 662 9 1 9 5.2 Cc1c(N2CCN(Cc3cccc(-c4ncco4)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4452636 177542 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 662 9 1 9 5.2 Cc1c(N2CCN(Cc3cccc(-c4ncco4)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
123549935 186213 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 551 5 1 4 4.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccccc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4740379 186213 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 551 5 1 4 4.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccccc1)C2C 10.1021/acs.jmedchem.0c01076
162672599 189786 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 481 4 1 5 4.1 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(NC(=O)c3cccnc3)cc2C12CCOCC2 10.1021/acs.jmedchem.0c01076
CHEMBL4793643 189786 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 481 4 1 5 4.1 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(NC(=O)c3cccnc3)cc2C12CCOCC2 10.1021/acs.jmedchem.0c01076
44391703 175282 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 575 10 3 5 5.2 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1F 10.1016/j.bmcl.2004.10.090
CHEMBL435334 175282 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 575 10 3 5 5.2 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1F 10.1016/j.bmcl.2004.10.090
162665107 188915 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 570 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ncccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4782228 188915 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 570 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ncccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
10919052 120296 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 120296 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44391526 129384 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 560 12 2 6 5.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCNCc1ccccc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL360244 129384 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 560 12 2 6 5.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCNCc1ccccc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
86275342 122964 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL3358413 122964 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44402465 142013 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL372455 142013 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
44391821 72355 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 538 9 2 6 4.8 CC(C)(C)OC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183197 72355 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 538 9 2 6 4.8 CC(C)(C)OC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
67143432 178906 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 8 4.3 Cc1ncccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
CHEMBL4472942 178906 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 8 4.3 Cc1ncccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
127037454 144243 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1250 31 17 15 -2.5 CC(C)C[C@H](NC(=O)C1(NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCC(=O)N2)CCCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1039/C5MD00259A
CHEMBL3753755 144243 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1250 31 17 15 -2.5 CC(C)C[C@H](NC(=O)C1(NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCC(=O)N2)CCCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1039/C5MD00259A
9918188 161500 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 708 8 2 5 8.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399856 161500 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 708 8 2 5 8.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
44444649 161784 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 646 10 3 7 4.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(O)CN3CCNCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401418 161784 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 646 10 3 7 4.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(O)CN3CCNCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44293164 174610 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 482 11 3 3 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)NC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL430763 174610 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 482 11 3 3 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)NC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44402670 78733 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 557 11 4 9 4.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCN)c21 10.1016/j.bmcl.2005.03.030
CHEMBL197317 78733 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 557 11 4 9 4.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCN)c21 10.1016/j.bmcl.2005.03.030
CHEMBL318127 217990 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@H](CCCCN)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44573626 194311 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494416 194311 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)o1 10.1016/j.bmcl.2009.02.043
118179174 189255 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 561 6 1 4 4.6 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4786609 189255 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 561 6 1 4 4.6 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
87285732 179731 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3ccc(Cl)nc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4517137 179731 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3ccc(Cl)nc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
118178989 187933 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccc(Cl)cc4)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4760799 187933 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccc(Cl)cc4)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44444635 161483 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 637 7 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399779 161483 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 637 7 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
44402472 139599 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL370145 139599 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
44406776 141120 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
162645007 186240 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 186240 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44573278 194226 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL493932 194226 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
44573277 194225 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493931 194225 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
44267239 103885 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 413 9 3 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)nc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL267558 103885 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 413 9 3 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)nc2)c1 10.1016/s0960-894x(01)00133-0
44293285 169554 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cncnc4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL417189 169554 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cncnc4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44402057 78713 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 487 9 2 8 4.8 COCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL197254 78713 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 487 9 2 8 4.8 COCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
44391693 70541 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 605 9 3 5 5.4 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(C(F)(F)F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL180167 70541 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 605 9 3 5 5.4 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(C(F)(F)F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44406776 141120 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
162645007 186240 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 186240 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44402672 78410 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 420 7 1 6 5.1 COc1ccc(C#N)cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL196351 78410 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 420 7 1 6 5.1 COc1ccc(C#N)cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44573112 194377 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 484 7 1 5 5.9 CCCCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL494739 194377 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 484 7 1 5 5.9 CCCCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
11583388 15062 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 457 5 2 5 4.8 CCc1nc(CN2CCN(c3cncc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL1092626 15062 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 457 5 2 5 4.8 CCc1nc(CN2CCN(c3cncc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
44346397 121276 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 121276 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
162650892 187008 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4749974 187008 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44561141 200581 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 432 3 3 4 4.4 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL527422 200581 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 432 3 3 4 4.4 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44391498 172899 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 524 10 1 7 3.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(OCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL426060 172899 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 524 10 1 7 3.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(OCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
118179127 189993 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 599 7 2 5 4.2 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2CCO 10.1021/acs.jmedchem.0c01076
CHEMBL4795998 189993 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 599 7 2 5 4.2 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2CCO 10.1021/acs.jmedchem.0c01076
127036617 144320 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1236 31 17 15 -2.9 CC(C)C[C@H](NC(=O)C1(NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCC(=O)N2)CCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1039/C5MD00259A
CHEMBL3754384 144320 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1236 31 17 15 -2.9 CC(C)C[C@H](NC(=O)C1(NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCC(=O)N2)CCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1039/C5MD00259A
155531714 182970 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Antagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL4593521 182970 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Antagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
44365609 46478 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 618 11 3 6 5.4 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(S(C)(=O)=O)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL147537 46478 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 618 11 3 6 5.4 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(S(C)(=O)=O)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
10930638 105805 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 105805 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44406776 141120 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
1185 10473 38 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 10473 38 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 10473 38 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 10473 38 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44293366 168990 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 511 12 3 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL416285 168990 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 511 12 3 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293236 181658 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 560 13 4 4 5.7 CCNC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL45639 181658 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 560 13 4 4 5.7 CCNC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
10674894 32312 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 588 10 0 7 6.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL135103 32312 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 588 10 0 7 6.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL438652 220564 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm0512894
10674894 32312 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 588 10 0 7 6.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
CHEMBL135103 32312 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 588 10 0 7 6.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
11980076 215232 29 None - 1 Rat 8.2 pIC50 = 8.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm9803673
CHEMBL1007 215232 29 None - 1 Rat 8.2 pIC50 = 8.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm9803673
44321497 104869 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 665 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCN(C(=O)OC(C)(C)C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL273390 104869 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 665 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCN(C(=O)OC(C)(C)C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL436874 220468 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL None None None None 10.1021/jm0506928
11496945 183254 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459659 183254 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
145957893 168849 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 545 8 1 6 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cc(F)cc(F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4160683 168849 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 545 8 1 6 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cc(F)cc(F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
11455317 69662 0 None 851 2 Human 8.2 pIC50 = 8.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL178457 69662 0 None 851 2 Human 8.2 pIC50 = 8.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
1185 10473 38 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44402396 168458 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1663 44 18 19 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CCC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL413216 168458 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1663 44 18 19 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CCC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
44402397 168646 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1578 42 17 18 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL414899 168646 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1578 42 17 18 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
87285768 177274 3 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 177274 3 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44402397 168646 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1578 42 17 18 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL414899 168646 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1578 42 17 18 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL3085508 217768 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL None None None None 10.1021/jm0506928
11180219 117998 0 None 112 2 Human 8.2 pIC50 = 8.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL326504 117998 0 None 112 2 Human 8.2 pIC50 = 8.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
67142995 177106 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 585 8 1 8 4.1 Cc1c(N2CCN(Cc3ccoc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4446997 177106 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 585 8 1 8 4.1 Cc1c(N2CCN(Cc3ccoc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44577104 185525 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1021/jm701249f
CHEMBL468565 185525 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1021/jm701249f
11167850 9518 28 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL None None None None 10.1021/jm0506928
11532637 14486 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL1088866 14486 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
44406776 141120 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67144450 179088 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 570 8 1 8 3.5 Cc1c(N2CCN(Cc3ccccc3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4475210 179088 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 570 8 1 8 3.5 Cc1c(N2CCN(Cc3ccccc3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44402396 168458 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1663 44 18 19 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CCC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL413216 168458 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1663 44 18 19 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CCC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
67143570 178536 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 726 14 2 10 5.0 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4467407 178536 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 726 14 2 10 5.0 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
71623059 187604 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4756920 187604 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
1184 10505 36 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(01)00779-x
9874838 10505 36 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(01)00779-x
CHEMBL71917 10505 36 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(01)00779-x
1184 10505 36 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm701249f
9874838 10505 36 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm701249f
CHEMBL71917 10505 36 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm701249f
9961721 175258 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 175258 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
9961721 175258 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 175258 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
10649568 21338 0 None 10 2 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of binding to gonadotropin-releasing hormone receptor in dogIn vitro inhibition of binding to gonadotropin-releasing hormone receptor in dog
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 21338 0 None 10 2 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of binding to gonadotropin-releasing hormone receptor in dogIn vitro inhibition of binding to gonadotropin-releasing hormone receptor in dog
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
1184 10505 36 None 426 2 Human 7.2 pIC50 = 7.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptorInhibition of Human gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm049218c
9874838 10505 36 None 426 2 Human 7.2 pIC50 = 7.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptorInhibition of Human gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm049218c
CHEMBL71917 10505 36 None 426 2 Human 7.2 pIC50 = 7.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptorInhibition of Human gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm049218c
1184 10505 36 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of Rat gonadotropin-releasing hormone receptor(moderate affinity)Inhibition of Rat gonadotropin-releasing hormone receptor(moderate affinity)
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm049218c
9874838 10505 36 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of Rat gonadotropin-releasing hormone receptor(moderate affinity)Inhibition of Rat gonadotropin-releasing hormone receptor(moderate affinity)
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm049218c
CHEMBL71917 10505 36 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of Rat gonadotropin-releasing hormone receptor(moderate affinity)Inhibition of Rat gonadotropin-releasing hormone receptor(moderate affinity)
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm049218c
1184 10505 36 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
9874838 10505 36 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
CHEMBL71917 10505 36 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
1184 10505 36 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
9874838 10505 36 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
CHEMBL71917 10505 36 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
1184 10505 36 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
9874838 10505 36 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
CHEMBL71917 10505 36 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
44406776 141120 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL436874 220468 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL None None None None 10.1021/jm0506928
44365078 48228 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 414 10 3 3 5.7 COc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL149062 48228 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 414 10 3 3 5.7 COc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44365456 49568 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 440 11 3 2 7.1 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL150223 49568 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 440 11 3 2 7.1 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
15462666 103277 4 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL262557 103277 4 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417614 148396 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 148396 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44292915 189670 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 590 12 3 4 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)O)cc3c2CCN(CCCCc2ccc(O)cc2)C(=O)OCc2ccccc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47921 189670 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 590 12 3 4 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)O)cc3c2CCN(CCCCc2ccc(O)cc2)C(=O)OCc2ccccc2)c1 10.1016/s0960-894x(01)00274-8
44402378 76451 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 457 8 2 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL193529 76451 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 457 8 2 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391612 70272 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 471 9 2 6 3.8 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCO)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL179977 70272 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 471 9 2 6 3.8 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCO)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44365170 47226 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 430 10 3 4 5.3 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL148245 47226 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 430 10 3 4 5.3 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44417614 148396 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 148396 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
67144531 179932 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 8 1 8 4.6 Cc1c(N2CCN(Cc3cccc(C#N)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4521484 179932 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 8 1 8 4.6 Cc1c(N2CCN(Cc3cccc(C#N)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
162670223 189350 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 521 5 2 5 4.6 O=C(Nc1ccc2c(c1)C1(CCC(O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4787856 189350 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 521 5 2 5 4.6 O=C(Nc1ccc2c(c1)C1(CCC(O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
44573790 200041 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 5 1 5 5.9 Cc1c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)ncn1C(C)C 10.1016/j.bmcl.2009.02.043
CHEMBL523849 200041 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 5 1 5 5.9 Cc1c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)ncn1C(C)C 10.1016/j.bmcl.2009.02.043
44402464 175868 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL439860 175868 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
44402404 140342 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 568 9 2 8 5.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N3CCCC3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL371073 140342 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 568 9 2 8 5.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N3CCCC3)c21 10.1016/j.bmcl.2005.03.030
87285668 180498 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 669 8 1 8 5.6 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)s3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4536130 180498 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 669 8 1 8 5.6 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)s3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44444672 176181 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 8 1 5 6.4 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL442283 176181 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 8 1 5 6.4 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
44402538 175214 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 471 7 2 7 5.7 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL434955 175214 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 471 7 2 7 5.7 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402538 175214 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 471 7 2 7 5.7 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL434955 175214 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 471 7 2 7 5.7 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
145954593 169312 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 561 8 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3ccc(F)cc3Cl)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4167945 169312 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 561 8 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3ccc(F)cc3Cl)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44406776 141120 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44296134 195177 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 469 6 2 6 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCC(C)CN2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL50182 195177 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 469 6 2 6 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCC(C)CN2)c1 10.1016/j.bmcl.2003.12.101
44406776 141120 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44402232 78186 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 454 8 1 7 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C3CCC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL195920 78186 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 454 8 1 7 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C3CCC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44561265 179887 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 512 6 3 5 5.0 FC(F)(F)C(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL452044 179887 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 512 6 3 5 5.0 FC(F)(F)C(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44322336 112917 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 398 6 1 4 5.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC(C)CN(C)C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL313517 112917 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 398 6 1 4 5.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC(C)CN(C)C)c1 10.1016/s0960-894x(99)00446-1
44402462 76680 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 399 6 1 4 5.9 CC(C)n1c(SCc2ccccc2Cl)nc2cc(NC(=O)C3CC3)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL193897 76680 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 399 6 1 4 5.9 CC(C)n1c(SCc2ccccc2Cl)nc2cc(NC(=O)C3CC3)ccc21 10.1016/j.bmcl.2005.03.030
67144164 180665 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 643 9 1 10 3.9 COC(=O)c1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)o1 10.1021/acs.jmedchem.6b01071
CHEMBL4539811 180665 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 643 9 1 10 3.9 COC(=O)c1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)o1 10.1021/acs.jmedchem.6b01071
44215908 101004 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 616 7 1 5 6.1 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249982 101004 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 616 7 1 5 6.1 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44444630 161602 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 596 7 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4CCCC4)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL400390 161602 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 596 7 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4CCCC4)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
44561108 193209 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 468 3 2 4 4.8 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL487627 193209 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 468 3 2 4 4.8 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
71666542 187126 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 6 4.4 O=C(NCc1ncc(F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4751345 187126 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 6 4.4 O=C(NCc1ncc(F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL436874 220468 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL None None None None 10.1021/jm0506928
67143743 178084 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 559 8 1 7 4.0 Cc1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)cc1 10.1021/acs.jmedchem.6b01071
CHEMBL4460966 178084 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 559 8 1 7 4.0 Cc1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)cc1 10.1021/acs.jmedchem.6b01071
67144486 178018 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccccc3C(F)(F)F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4459812 178018 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccccc3C(F)(F)F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
67143407 177547 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4452793 177547 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44402377 140217 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 379 6 1 4 5.6 Cc1cccc(CSc2nc3cc(NC(=O)C4CC4)ccc3n2C(C)C)c1 10.1016/j.bmcl.2005.03.030
CHEMBL370603 140217 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 379 6 1 4 5.6 Cc1cccc(CSc2nc3cc(NC(=O)C4CC4)ccc3n2C(C)C)c1 10.1016/j.bmcl.2005.03.030
44391703 175282 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 575 10 3 5 5.2 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1F 10.1016/j.bmcl.2004.10.090
CHEMBL435334 175282 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 575 10 3 5 5.2 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1F 10.1016/j.bmcl.2004.10.090
CHEMBL436874 220468 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL None None None None 10.1021/jm0506928
162645007 186240 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 186240 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44402293 78203 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2005.03.030
CHEMBL196040 78203 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2005.03.030
44391526 129384 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 560 12 2 6 5.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCNCc1ccccc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL360244 129384 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 560 12 2 6 5.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCNCc1ccccc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
86272223 122966 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 737 7 1 7 6.0 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1cccc(OC(F)(F)F)c1 10.1021/ml5004469
CHEMBL3358415 122966 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 737 7 1 7 6.0 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1cccc(OC(F)(F)F)c1 10.1021/ml5004469
118179235 188714 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 548 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4779806 188714 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 548 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44573714 194465 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 2 4 5.2 Cc1n[nH]c(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL495189 194465 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 2 4 5.2 Cc1n[nH]c(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
44561368 183593 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL460892 183593 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44573275 194194 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 6 1 5 5.6 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1CC 10.1016/j.bmcl.2009.02.043
CHEMBL493730 194194 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 6 1 5 5.6 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1CC 10.1016/j.bmcl.2009.02.043
44402465 142013 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL372455 142013 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
145949379 169493 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 496 7 1 7 3.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cccnc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4170863 169493 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 496 7 1 7 3.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cccnc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL3085508 217768 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44391734 129396 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 509 10 3 5 3.6 CCNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL360297 129396 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 509 10 3 5 3.6 CCNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44391692 71074 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 437 7 1 4 4.8 CC(C)c1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL181057 71074 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 437 7 1 4 4.8 CC(C)c1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44444644 161778 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 601 6 1 4 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(C(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401350 161778 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 601 6 1 4 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(C(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44365844 48704 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 646 12 3 6 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(S(=O)(=O)C(C)C)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL149447 48704 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 646 12 3 6 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(S(=O)(=O)C(C)C)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL97265 222702 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)NCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
24825725 199406 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL521674 199406 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
44305274 109546 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 667 11 1 9 6.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)c4ccsc4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL305155 109546 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 667 11 1 9 6.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)c4ccsc4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
44293222 182739 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138464 182739 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL45883 182739 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
11525358 194121 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmc.2012.09.013
CHEMBL493185 194121 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmc.2012.09.013
10074296 16160 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL11149 16160 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL438652 220564 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm0512894
10074296 16160 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL11149 16160 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00134-2
10074296 16160 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11149 16160 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00133-0
10074296 16160 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00779-x
CHEMBL11149 16160 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00779-x
11980076 215232 29 None - 1 Rat 8.2 pIC50 = 8.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm9803673
CHEMBL1007 215232 29 None - 1 Rat 8.2 pIC50 = 8.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm9803673
67144646 179916 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 586 8 1 9 3.5 Cc1c(N2CCN(Cc3cocn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4521118 179916 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 586 8 1 9 3.5 Cc1c(N2CCN(Cc3cocn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
155559612 181662 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1612 43 20 24 -4.1 CC(C)C[C@H](NC(=O)[C@H](CCCCNC(=O)CCCC(=O)OC[C@H]1O[C@@H](n2ccc(N)nc2=O)C(F)(F)[C@@H]1O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
CHEMBL4563936 181662 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1612 43 20 24 -4.1 CC(C)C[C@H](NC(=O)[C@H](CCCCNC(=O)CCCC(=O)OC[C@H]1O[C@@H](n2ccc(N)nc2=O)C(F)(F)[C@@H]1O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
44292918 178194 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL44627 178194 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
67143413 176396 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 8 4.3 Cc1cncc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4436711 176396 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 8 4.3 Cc1cncc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL3085508 217768 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
70691201 84428 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1952 47 22 28 -0.7 CCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CO/N=C(\C)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1c(OC)cccc1C3=O)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2012.08.014
CHEMBL2088506 84428 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1952 47 22 28 -0.7 CCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CO/N=C(\C)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1c(OC)cccc1C3=O)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2012.08.014
11604354 194303 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 428 4 2 4 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c[nH]1 10.1016/j.bmcl.2009.02.043
CHEMBL494400 194303 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 428 4 2 4 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c[nH]1 10.1016/j.bmcl.2009.02.043
11167850 9518 28 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
145952802 169376 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 579 8 1 7 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cccc(OC(F)(F)F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4169027 169376 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 579 8 1 7 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cccc(OC(F)(F)F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL3085508 217768 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44406776 141120 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL94842 222691 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44417614 148396 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 148396 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417614 148396 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 148396 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10722009 123331 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL336319 123331 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44295982 195079 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 503 6 2 6 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2Cc3ccccc3CN2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL50035 195079 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 503 6 2 6 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2Cc3ccccc3CN2)c1 10.1016/j.bmcl.2003.12.101
10722009 123331 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
CHEMBL336319 123331 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
44365281 49572 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 444 11 3 4 5.7 COc1cc(OC)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL150228 49572 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 444 11 3 4 5.7 COc1cc(OC)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
15462665 175438 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 615 9 0 7 7.4 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(C2CCCCC2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL436346 175438 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 615 9 0 7 7.4 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(C2CCCCC2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44412876 84685 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccccc3OC)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL209419 84685 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccccc3OC)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
10985312 85521 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21126 85521 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44322390 213389 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 382 3 1 4 5.1 CN1CCCCC(Oc2c(-c3ccccc3)c(O)nc3cc(Cl)ccc23)C1 10.1016/s0960-894x(99)00446-1
CHEMBL89041 213389 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 382 3 1 4 5.1 CN1CCCCC(Oc2c(-c3ccccc3)c(O)nc3cc(Cl)ccc23)C1 10.1016/s0960-894x(99)00446-1
11512807 146914 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 610 11 0 8 6.5 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(Cc3ccccc3)C(C)=O)c2c1=O 10.1021/jm0512894
CHEMBL380200 146914 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 610 11 0 8 6.5 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(Cc3ccccc3)C(C)=O)c2c1=O 10.1021/jm0512894
44573507 194333 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 428 4 1 4 5.8 Cc1ccc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494548 194333 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 428 4 1 4 5.8 Cc1ccc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
11496610 10847 13 None - 2 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
5582 10847 13 None - 2 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
CHEMBL474991 10847 13 None - 2 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
25193798 176977 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 562 6 2 5 6.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL444509 176977 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 562 6 2 5 6.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
10919052 120296 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 120296 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402038 76982 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 472 7 1 8 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)OC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL194074 76982 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 472 7 1 8 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)OC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44346398 21310 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 21310 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
162675445 190187 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 470 6 1 4 4.4 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3CC2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4798298 190187 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 470 6 1 4 4.4 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3CC2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL2370256 216599 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm990433g
44561369 197247 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL517881 197247 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
11496610 10847 13 None - 2 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
5582 10847 13 None - 2 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
CHEMBL474991 10847 13 None - 2 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
44391613 175054 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 462 9 1 7 2.4 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1CCN1CCOCC1 10.1016/j.bmcl.2004.10.089
CHEMBL433954 175054 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 462 9 1 7 2.4 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1CCN1CCOCC1 10.1016/j.bmcl.2004.10.089
127036774 144287 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1146 25 12 13 -1.5 CC(C)C[C@H](NC(=O)CN1CN(c2ccccc2)C2(CCN(C(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@@H]3CCC(=O)N3)CC2)C1=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1039/C5MD00259A
CHEMBL3754120 144287 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1146 25 12 13 -1.5 CC(C)C[C@H](NC(=O)CN1CN(c2ccccc2)C2(CCN(C(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@@H]3CCC(=O)N3)CC2)C1=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1039/C5MD00259A
162645007 186240 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 186240 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
145949556 169712 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 485 7 1 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)c3ccco3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4174298 169712 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 485 7 1 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)c3ccco3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
67142794 180902 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 559 8 1 7 4.0 Cc1ccccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
CHEMBL4545859 180902 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 559 8 1 7 4.0 Cc1ccccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
162645007 186240 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 186240 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL428619 220240 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44444649 161784 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 646 10 3 7 4.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(O)CN3CCNCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401418 161784 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 646 10 3 7 4.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(O)CN3CCNCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44185958 161777 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 615 8 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401349 161777 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 615 8 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44573586 194280 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 443 4 1 5 5.5 Cc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494232 194280 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 443 4 1 5 5.5 Cc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
44391821 72355 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 538 9 2 6 4.8 CC(C)(C)OC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183197 72355 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 538 9 2 6 4.8 CC(C)(C)OC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
67143567 178048 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 468 6 1 6 3.6 Cc1c(N2CCC(C)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4460413 178048 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 468 6 1 6 3.6 Cc1c(N2CCC(C)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44295833 174689 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 503 6 2 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2NCCc3ccccc32)c1 10.1016/j.bmcl.2003.12.101
CHEMBL431344 174689 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 503 6 2 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2NCCc3ccccc32)c1 10.1016/j.bmcl.2003.12.101
11318649 71128 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3F)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL181257 71128 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3F)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44322434 118193 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 424 6 1 4 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCCCN2CCCCC2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL327323 118193 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 424 6 1 4 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCCCN2CCCCC2)c1 10.1016/s0960-894x(99)00446-1
44444673 101058 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 644 8 1 5 6.8 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL250389 101058 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 644 8 1 5 6.8 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
118179169 186705 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 613 6 1 4 5.4 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccc(F)cc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4746174 186705 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 613 6 1 4 5.4 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccc(F)cc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
162656174 187653 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 589 5 2 5 5.6 O=C(Nc1ccc2c(c1)C1(CCC(O)(C(F)(F)F)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4757424 187653 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 589 5 2 5 5.6 O=C(Nc1ccc2c(c1)C1(CCC(O)(C(F)(F)F)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
44573111 194376 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL494738 194376 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
44444628 101094 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 722 8 2 5 8.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250568 101094 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 722 8 2 5 8.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
44402616 77911 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 469 7 2 7 5.5 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C1CC1 10.1016/j.bmcl.2005.03.030
CHEMBL195516 77911 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 469 7 2 7 5.5 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C1CC1 10.1016/j.bmcl.2005.03.030
44391718 72379 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 523 10 3 5 4.0 CC(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183325 72379 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 523 10 3 5 4.0 CC(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44593415 196158 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL512893 196158 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44573276 194195 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 484 6 1 5 5.9 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)n1CC 10.1016/j.bmcl.2009.02.043
CHEMBL493731 194195 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 484 6 1 5 5.9 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)n1CC 10.1016/j.bmcl.2009.02.043
11167850 9518 28 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44444626 161662 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 680 7 2 5 7.6 COC(=O)/N=C(/NC[C@@H](C)c1c(-c2cc(C)cc(C)c2)[nH]c2sc(C(C)(C)C(=O)N3C4CCC3CC4)cc12)N1CCC(c2ccncc2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL400739 161662 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 680 7 2 5 7.6 COC(=O)/N=C(/NC[C@@H](C)c1c(-c2cc(C)cc(C)c2)[nH]c2sc(C(C)(C)C(=O)N3C4CCC3CC4)cc12)N1CCC(c2ccncc2)C1 10.1016/j.bmcl.2007.09.099
11592658 86526 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 642 11 2 6 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)NC(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211731 86526 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 642 11 2 6 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)NC(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL436874 220468 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL None None None None 10.1021/jm0506928
44341186 16816 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 10 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(=O)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL115192 16816 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 10 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(=O)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL436874 220468 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL None None None None 10.1021/jm0506928
44293378 108670 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 618 13 1 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)CC(C)C)c1 10.1016/s0960-894x(01)00275-x
CHEMBL300792 108670 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 618 13 1 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)CC(C)C)c1 10.1016/s0960-894x(01)00275-x
1185 10473 38 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44561368 183593 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL460892 183593 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44406776 141120 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
11167850 9518 28 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44406776 141120 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67144496 176613 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cncs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4439817 176613 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cncs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44274248 105449 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 643 9 0 7 7.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2Cl)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL277435 105449 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 643 9 0 7 7.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2Cl)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
11167850 9518 28 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
67143514 180180 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 468 6 1 6 3.6 Cc1c(N2CCCC(C)C2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4528231 180180 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 468 6 1 6 3.6 Cc1c(N2CCCC(C)C2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44593415 196158 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1021/jm701249f
CHEMBL512893 196158 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1021/jm701249f
10930638 105805 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 105805 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417615 148701 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 148701 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10674894 32312 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 588 10 0 7 6.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
CHEMBL135103 32312 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 588 10 0 7 6.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
CHEMBL261927 217300 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
15602807 14992 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1092245 14992 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44391628 72646 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 513 10 1 7 4.4 CCOC(=O)CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183572 72646 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 513 10 1 7 4.4 CCOC(=O)CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44406776 141120 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44391542 72001 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL182639 72001 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44573753 194250 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmcl.2009.02.043
CHEMBL494021 194250 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmcl.2009.02.043
44391735 129115 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 591 10 3 5 5.7 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1Cl 10.1016/j.bmcl.2004.10.090
CHEMBL359914 129115 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 591 10 3 5 5.7 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1Cl 10.1016/j.bmcl.2004.10.090
44391771 172801 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.7 CC(C)(C)NC(=O)NCCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL425524 172801 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.7 CC(C)(C)NC(=O)NCCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
86275343 190270 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 655 6 1 6 4.7 O=C(NCc1ncc(C(F)(F)F)cc1F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4799511 190270 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 655 6 1 6 4.7 O=C(NCc1ncc(C(F)(F)F)cc1F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44391835 173083 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.8 CC(C)(C)CC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL427146 173083 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.8 CC(C)(C)CC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
15895696 119241 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCCN2C)c1 10.1016/s0960-894x(99)00447-3
CHEMBL329834 119241 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCCN2C)c1 10.1016/s0960-894x(99)00447-3
44573585 194019 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 429 4 1 5 5.1 Cc1ncoc1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL492587 194019 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 429 4 1 5 5.1 Cc1ncoc1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
67143612 177829 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 9 2 8 3.6 Cc1c(N2CCN(Cc3cccc(C(N)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4456937 177829 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 9 2 8 3.6 Cc1c(N2CCN(Cc3cccc(C(N)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44359289 18923 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 547 8 3 7 6.3 CCn1nccc1NC(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
CHEMBL1184180 18923 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 547 8 3 7 6.3 CCn1nccc1NC(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
CHEMBL337323 18923 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 547 8 3 7 6.3 CCn1nccc1NC(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
44402616 77911 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 469 7 2 7 5.5 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C1CC1 10.1016/j.bmcl.2005.03.030
CHEMBL195516 77911 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 469 7 2 7 5.5 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C1CC1 10.1016/j.bmcl.2005.03.030
11167850 9518 28 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
1178 9518 28 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
1187 9518 28 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL179691 9518 28 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
118179135 188797 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 5 1 4 4.9 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4780737 188797 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 5 1 4 4.9 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
44572286 187580 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475650 187580 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44406776 141120 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL2370262 216602 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](C)NC(=O)[C@@H](Cc1ccccn1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44444675 161501 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)C(C)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399857 161501 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)C(C)C2)c1 10.1016/j.bmcl.2007.09.099
44402038 76982 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 472 7 1 8 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)OC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL194074 76982 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 472 7 1 8 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)OC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402673 140046 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 499 10 2 7 6.4 CCCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL370414 140046 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 499 10 2 7 6.4 CCCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
44391670 71466 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 473 8 1 5 4.8 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1cccc(Cl)c1 10.1016/j.bmcl.2004.10.089
CHEMBL181864 71466 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 473 8 1 5 4.8 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1cccc(Cl)c1 10.1016/j.bmcl.2004.10.089
67143618 177074 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 637 8 1 10 4.1 Cc1c(N2CCN(Cc3cccc4nonc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4446435 177074 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 637 8 1 10 4.1 Cc1c(N2CCN(Cc3cccc4nonc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143023 181776 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 656 9 2 10 4.2 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4566719 181776 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 656 9 2 10 4.2 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
155531714 182970 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL4593521 182970 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
145949399 169513 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 577 8 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cccc(C(F)(F)F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4171288 169513 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 577 8 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cccc(C(F)(F)F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
9961721 175258 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 175258 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44359254 18404 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 561 8 3 8 5.8 COc1nccc(NC(=O)c2cc3c(OCCC4CCCCN4)c(-c4cc(C)cc(C)c4)c(O)nc3cc2Cl)n1 10.1016/s0960-894x(00)00024-x
CHEMBL1180716 18404 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 561 8 3 8 5.8 COc1nccc(NC(=O)c2cc3c(OCCC4CCCCN4)c(-c4cc(C)cc(C)c4)c(O)nc3cc2Cl)n1 10.1016/s0960-894x(00)00024-x
CHEMBL139292 18404 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 561 8 3 8 5.8 COc1nccc(NC(=O)c2cc3c(OCCC4CCCCN4)c(-c4cc(C)cc(C)c4)c(O)nc3cc2Cl)n1 10.1016/s0960-894x(00)00024-x
11549071 145724 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 628 11 2 7 6.4 CC(C)C(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)CN)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL378481 145724 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 628 11 2 7 6.4 CC(C)C(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)CN)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
10985312 85521 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21126 85521 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
70691201 84428 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1952 47 22 28 -0.7 CCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CO/N=C(\C)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1c(OC)cccc1C3=O)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2012.08.014
CHEMBL2088506 84428 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1952 47 22 28 -0.7 CCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CO/N=C(\C)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1c(OC)cccc1C3=O)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2012.08.014
11167850 9518 28 None 6309 2 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44348333 103668 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)N(C)C(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL265727 103668 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)N(C)C(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL3085508 217768 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44406776 141120 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 141120 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 10473 38 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 217768 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
15602806 15068 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL1092638 15068 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
71623059 187604 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4756920 187604 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
118179135 188797 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 5 1 4 4.9 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4780737 188797 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 5 1 4 4.9 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
44573585 194019 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 429 4 1 5 5.1 Cc1ncoc1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL492587 194019 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 429 4 1 5 5.1 Cc1ncoc1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
44267240 16468 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 427 10 2 3 6.0 COc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cn1 10.1016/s0960-894x(01)00133-0
CHEMBL11310 16468 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 427 10 2 3 6.0 COc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cn1 10.1016/s0960-894x(01)00133-0
44365088 128273 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 10 3 2 6.3 CCc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL358260 128273 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 10 3 2 6.3 CCc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44365500 172062 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1C 10.1016/s0960-894x(00)00707-1
CHEMBL423215 172062 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1C 10.1016/s0960-894x(00)00707-1
44417614 148396 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 148396 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346397 121276 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 121276 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44365374 48429 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 9 3 2 6.0 Cc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL149196 48429 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 9 3 2 6.0 Cc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)cc1 10.1016/s0960-894x(00)00707-1
44365249 127854 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 370 6 3 2 5.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL357025 127854 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 370 6 3 2 5.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44322272 212957 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 382 4 1 4 5.1 CN1CCCCC1COc1c(-c2ccccc2)c(O)nc2cc(Cl)ccc12 10.1016/s0960-894x(99)00446-1
CHEMBL86365 212957 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 382 4 1 4 5.1 CN1CCCCC1COc1c(-c2ccccc2)c(O)nc2cc(Cl)ccc12 10.1016/s0960-894x(99)00446-1
44322052 213475 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 356 6 1 4 4.6 CN(C)CCCOc1c(-c2ccccc2)c(O)nc2cc(Cl)ccc12 10.1016/s0960-894x(99)00446-1
CHEMBL89675 213475 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 356 6 1 4 4.6 CN(C)CCCOc1c(-c2ccccc2)c(O)nc2cc(Cl)ccc12 10.1016/s0960-894x(99)00446-1
44267257 16135 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 355 6 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11134 16135 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 355 6 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
118178989 187933 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccc(Cl)cc4)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4760799 187933 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccc(Cl)cc4)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
71666685 189493 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 6 1 6 3.6 O=C(NCc1ccccn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4789613 189493 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 6 1 6 3.6 O=C(NCc1ccccn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
67144496 176613 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cncs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4439817 176613 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cncs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
86275573 122967 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 687 6 1 6 5.8 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(Cl)cc1 10.1021/ml5004469
CHEMBL3358416 122967 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 687 6 1 6 5.8 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(Cl)cc1 10.1021/ml5004469
44444663 100975 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 645 8 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CNC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249771 100975 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 645 8 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CNC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
1185 10473 38 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 10473 38 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 10473 38 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 10473 38 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44391525 173145 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3ccc(OC)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL427500 173145 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3ccc(OC)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
15602804 14853 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091209 14853 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
10919052 120296 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 120296 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44561108 193209 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 468 3 2 4 4.8 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL487627 193209 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 468 3 2 4 4.8 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL436874 220468 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL None None None None 10.1021/jm0506928
44444630 161602 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 596 7 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4CCCC4)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL400390 161602 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 596 7 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4CCCC4)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
44391542 72001 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL182639 72001 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
11626096 194049 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 428 4 1 5 4.6 Cn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1 10.1016/j.bmcl.2009.02.043
CHEMBL492780 194049 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 428 4 1 5 4.6 Cn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1 10.1016/j.bmcl.2009.02.043
11167850 9518 28 None 6309 2 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 9518 28 None 6309 2 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 9518 28 None 6309 2 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 9518 28 None 6309 2 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44402648 78072 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 453 8 1 7 5.1 COC(=O)c1ccc(OC)c(CSc2nc3cc(NC(=O)C4CC4)ccc3n2C(C)C)c1 10.1016/j.bmcl.2005.03.030
CHEMBL195726 78072 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 453 8 1 7 5.1 COC(=O)c1ccc(OC)c(CSc2nc3cc(NC(=O)C4CC4)ccc3n2C(C)C)c1 10.1016/j.bmcl.2005.03.030
118167818 186211 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 527 5 2 4 4.6 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCNCC2 10.1021/acs.jmedchem.0c01076
CHEMBL4740373 186211 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 527 5 2 4 4.6 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCNCC2 10.1021/acs.jmedchem.0c01076
118179051 186997 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4749790 186997 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
25193797 196444 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 548 7 2 5 6.4 CC(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL515200 196444 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 548 7 2 5 6.4 CC(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL414113 219889 0 None - 1 Rat 10.1 pKd = 10.1 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
101609491 148594 0 None - 1 Rat 10.0 pKd = 10.0 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL 1555 45 18 19 -1.1 CCCC/N=C(/NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O)NC(N)=O 10.1021/jm00112a013
44317046 148594 0 None - 1 Rat 10.0 pKd = 10.0 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL 1555 45 18 19 -1.1 CCCC/N=C(/NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O)NC(N)=O 10.1021/jm00112a013
77058850 148594 0 None - 1 Rat 10.0 pKd = 10.0 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL 1555 45 18 19 -1.1 CCCC/N=C(/NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O)NC(N)=O 10.1021/jm00112a013
CHEMBL386314 148594 0 None - 1 Rat 10.0 pKd = 10.0 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL 1555 45 18 19 -1.1 CCCC/N=C(/NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O)NC(N)=O 10.1021/jm00112a013
1190 7669 47 None - 1 Human 9.9 pKd = 9.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01076
25074887 7669 47 None - 1 Human 9.9 pKd = 9.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01076
583 7669 47 None - 1 Human 9.9 pKd = 9.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01076
CHEMBL1200490 7669 47 None - 1 Human 9.9 pKd = 9.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01076
DB00050 7669 47 None - 1 Human 9.9 pKd = 9.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01076
CHEMBL2369860 216491 0 None - 1 Rat 9.7 pKd = 9.7 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCNc1n[nH]c(N)n1)NC(=O)[C@H](CCCNc1n[nH]c(N)n1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL2370807 216702 0 None - 1 Human 9.7 pKd = 9.7 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNc1n[nH]c(N)n1)C(=O)N[C@@H](CCCNc1n[nH]c(N)n1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00101a003
3823 56995 42 None -1 11 Rat 9.7 pKd = 9.7 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
76973198 56995 42 None -1 11 Rat 9.7 pKd = 9.7 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
CHEMBL157101 56995 42 None -1 11 Rat 9.7 pKd = 9.7 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
CHEMBL414391 219909 0 None - 1 Rat 9.6 pKd = 9.6 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None C/N=C(\NC#N)NCCCC[C@@H](NC(=O)[C@H](CCCCN/C(=N\C)NC#N)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL407225 219428 0 None - 1 Rat 9.6 pKd = 9.6 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(N)=O)c1cccnc1)c1cccnc1 10.1021/jm00398a030
CHEMBL266716 217473 0 None - 1 Human 9.6 pKd = 9.6 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00101a003
CHEMBL218396 216174 0 None - 1 Rat 9.6 pKd = 9.6 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](CCCCNc1n[nH]c(N)n1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL269583 217577 0 None - 1 Rat 9.6 pKd = 9.6 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCC/N=C(\NC#N)NCc1ccccn1)NC(=O)[C@H](CCCC/N=C(\NC#N)NCc1ccccn1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL376017 219019 0 None - 1 Rat 9.6 pKd = 9.6 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N1CC=C[C@H]1C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(=O)O 10.1021/jm00398a030
CHEMBL438762 220574 0 None - 1 Rat 9.5 pKd = 9.5 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCC/N=C(/NC#N)NC(C)C)NC(=O)[C@H](CCCC/N=C(/NC#N)NC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL2370809 216704 0 None - 1 Human 9.5 pKd = 9.5 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCNC(=O)c1cccnc1)C(=O)N[C@@H](CCCCNC(=O)c1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00101a003
10348973 10086 58 None - 1 Human 9.4 pKd = 9.4 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
5432 10086 58 None - 1 Human 9.4 pKd = 9.4 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
5586 10086 58 None - 1 Human 9.4 pKd = 9.4 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
CHEMBL1800159 10086 58 None - 1 Human 9.4 pKd = 9.4 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
DB11853 10086 58 None - 1 Human 9.4 pKd = 9.4 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
3823 56995 42 None -1 11 Rat 9.4 pKd = 9.4 Binding
Dissociation constant was determined in vitro using rat pituitary membranes, at concentration 1.0*10e-5 MDissociation constant was determined in vitro using rat pituitary membranes, at concentration 1.0*10e-5 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
76973198 56995 42 None -1 11 Rat 9.4 pKd = 9.4 Binding
Dissociation constant was determined in vitro using rat pituitary membranes, at concentration 1.0*10e-5 MDissociation constant was determined in vitro using rat pituitary membranes, at concentration 1.0*10e-5 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
CHEMBL157101 56995 42 None -1 11 Rat 9.4 pKd = 9.4 Binding
Dissociation constant was determined in vitro using rat pituitary membranes, at concentration 1.0*10e-5 MDissociation constant was determined in vitro using rat pituitary membranes, at concentration 1.0*10e-5 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
CHEMBL261999 217304 0 None - 1 Rat 9.4 pKd = 9.4 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCC/N=C(\NC#N)NCc1ccccn1)NC(=O)[C@H](CCC/N=C(\NC#N)NCc1ccccn1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
44316759 175647 0 None - 1 Rat 9.4 pKd = 9.4 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL 1537 45 17 19 -0.7 CCCC/N=C(\NC#N)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL438191 175647 0 None - 1 Rat 9.4 pKd = 9.4 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL 1537 45 17 19 -0.7 CCCC/N=C(\NC#N)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL2369851 216490 0 None - 1 Rat 9.3 pKd = 9.3 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCNc1n[nH]c(N)n1)NC(=O)[C@H](CCCCNc1n[nH]c(N)n1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL2370818 216706 0 None - 1 Human 9.3 pKd = 9.3 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCNc1n[nH]c(N)n1)C(=O)N[C@@H](CCCCNc1n[nH]c(N)n1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00101a003
CHEMBL441741 220672 1 None - 1 Rat 9.2 pKd = 9.2 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm00398a030
CHEMBL2370808 216703 0 None - 1 Human 9.2 pKd = 9.2 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00101a003
CHEMBL439892 220631 0 None - 1 Rat 9.1 pKd = 9.1 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](c2cccnc2)NC(=O)[C@H](CCCN=C(N)N)NC1=O)c1cccnc1 10.1021/jm00398a030
10348973 10086 58 None - 1 Human 9.1 pKd = 9.1 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
5432 10086 58 None - 1 Human 9.1 pKd = 9.1 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
5586 10086 58 None - 1 Human 9.1 pKd = 9.1 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
CHEMBL1800159 10086 58 None - 1 Human 9.1 pKd = 9.1 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
DB11853 10086 58 None - 1 Human 9.1 pKd = 9.1 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
CHEMBL2370803 216701 0 None - 1 Human 9.1 pKd = 9.1 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCNc1n[nH]c(N)n1)C(=O)N[C@@H](CCCCNc1n[nH]c(N)n1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm00101a003
CHEMBL2370814 216705 0 None - 1 Human 9.1 pKd = 9.1 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CCNC(=O)CNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCNc1n[nH]c(N)n1)NC(=O)[C@H](CCCCNc1n[nH]c(N)n1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O 10.1021/jm00101a003
CHEMBL407482 219443 0 None - 1 Rat 9.0 pKd = 9 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CCCC/N=C(\NC#N)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL411806 219738 0 None - 1 Rat 9.0 pKd = 9 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)NC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(C)=O)c1cccnc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(N)=O)c1cccnc1 10.1021/jm00398a030
CHEMBL436334 220458 0 None - 1 Rat 9.0 pKd = 9 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@H]1CCC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](c2cccnc2)NC(=O)[C@H](CCCN=C(N)N)NC1=O)c1cccnc1 10.1021/jm00398a030
CHEMBL2371272 216807 0 None - 1 Rat 9.0 pKd = 9.0 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CCC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm00398a030
CHEMBL414149 219893 0 None - 1 Rat 9.0 pKd = 9.0 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](c2cccnc2)NC(=O)[C@H](CCCN=C(N)N)NC1=O)c1cccnc1 10.1021/jm00398a030
11250647 8327 46 None 117 2 Human 8.9 pKd = 8.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
5293 8327 46 None 117 2 Human 8.9 pKd = 8.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
8362 8327 46 None 117 2 Human 8.9 pKd = 8.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
CHEMBL1208155 8327 46 None 117 2 Human 8.9 pKd = 8.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
DB11979 8327 46 None 117 2 Human 8.9 pKd = 8.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
CHEMBL407023 219411 0 None - 1 Rat 8.9 pKd = 8.9 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CCCC/N=C(\NC#N)NCCCC[C@@H](NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL439359 220618 0 None - 1 Rat 8.9 pKd = 8.9 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCC/N=C(\NC#N)NC1CCCCC1)NC(=O)[C@H](CCCC/N=C(\NC#N)NC1CCCCC1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL411586 219725 0 None - 1 Rat 8.9 pKd = 8.9 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CCCC/N=C(\NC#N)NCCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](CCCCN/C(=N/CCCC)NC#N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL412802 219805 0 None - 1 Rat 8.8 pKd = 8.8 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CCCC/N=C(\NC#N)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL2371274 216809 0 None - 1 Rat 8.7 pKd = 8.7 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm00398a030
CHEMBL2371275 216810 0 None - 1 Rat 8.0 pKd = 8 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CNC(=O)C[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm00398a030
CHEMBL442303 220688 0 None - 1 Rat 8.0 pKd = 8 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@H]1CNC(=O)C[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](c2cccnc2)NC(=O)[C@H](CCCN=C(N)N)NC1=O)c1cccnc1 10.1021/jm00398a030
CHEMBL265825 217444 0 None - 1 Rat 8.0 pKd = 8.0 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@H]1CC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](c2cccnc2)NC(=O)[C@H](CCCN=C(N)N)NC1=O)c1cccnc1 10.1021/jm00398a030
CHEMBL428837 220258 0 None - 1 Rat 8.7 pKd = 8.7 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CCCC/N=C(\NC#N)NCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](CCCN/C(=N/CCCC)NC#N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
11250647 8327 46 None 117 2 Human 8.5 pKd = 8.5 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
5293 8327 46 None 117 2 Human 8.5 pKd = 8.5 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
8362 8327 46 None 117 2 Human 8.5 pKd = 8.5 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
CHEMBL1208155 8327 46 None 117 2 Human 8.5 pKd = 8.5 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
DB11979 8327 46 None 117 2 Human 8.5 pKd = 8.5 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
CHEMBL265522 217431 0 None - 1 Rat 8.5 pKd = 8.5 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CCCCCC/N=C(\NC#N)NCCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](CCCCN/C(=N/CCCCCC)NC#N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL442303 220688 0 None - 1 Rat 8.4 pKd = 8.4 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@H]1CNC(=O)C[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](c2cccnc2)NC(=O)[C@H](CCCN=C(N)N)NC1=O)c1cccnc1 10.1021/jm00398a030
CHEMBL2371273 216808 0 None - 1 Rat 7.4 pKd = 7.4 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm00398a030
12784 7365 12 None - 1 Human 8.3 pKd = 8.3 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
85469632 7365 12 None - 1 Human 8.3 pKd = 8.3 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL4537788 7365 12 None - 1 Human 8.3 pKd = 8.3 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL2371277 216812 0 None - 1 Rat 8.2 pKd = 8.2 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm00398a030
3823 56995 42 None -1 11 Rat 6.1 pKd = 6.1 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]leuprolide as radioligand, at concentration 3.16*10e-5 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]leuprolide as radioligand, at concentration 3.16*10e-5 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
76973198 56995 42 None -1 11 Rat 6.1 pKd = 6.1 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]leuprolide as radioligand, at concentration 3.16*10e-5 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]leuprolide as radioligand, at concentration 3.16*10e-5 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
CHEMBL157101 56995 42 None -1 11 Rat 6.1 pKd = 6.1 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]leuprolide as radioligand, at concentration 3.16*10e-5 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]leuprolide as radioligand, at concentration 3.16*10e-5 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
12784 7365 12 None - 1 Human 8.0 pKd = 8.0 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
85469632 7365 12 None - 1 Human 8.0 pKd = 8.0 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL4537788 7365 12 None - 1 Human 8.0 pKd = 8.0 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL409219 219533 0 None - 1 Rat 10.9 pKi = 10.9 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N(C)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL268397 217530 0 None - 1 Rat 10.6 pKi = 10.6 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CO)C(=O)N(C)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
44383749 103443 0 None - 1 Rat 10.5 pKi = 10.5 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL 1534 41 13 18 3.1 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N(C)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCC(N)C(=O)c1ccncc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC(N)C(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL263839 103443 0 None - 1 Rat 10.5 pKi = 10.5 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL 1534 41 13 18 3.1 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N(C)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCC(N)C(=O)c1ccncc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC(N)C(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL263840 217370 0 None - 1 Rat 10.5 pKi = 10.5 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL268319 217524 0 None - 1 Rat 10.3 pKi = 10.3 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL None None None COc1ccc(C(=O)CC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)cc1 10.1021/jm00059a020
44383968 166102 0 None - 1 Rat 10.2 pKi = 10.2 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL 1590 45 14 20 2.5 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC(N)C(=O)c1cccnc1)C(=O)N[C@@H](CCCC(N)C(=O)c1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC(N)C(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL409990 166102 0 None - 1 Rat 10.2 pKi = 10.2 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL 1590 45 14 20 2.5 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC(N)C(=O)c1cccnc1)C(=O)N[C@@H](CCCC(N)C(=O)c1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC(N)C(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL2371478 216830 0 None - 1 Rat 10.0 pKi = 10 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](Cc3c[nH]cn3)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44267907 23103 0 None 3 3 Rat 10.0 pKi = 10.0 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12282 23103 0 None 3 3 Rat 10.0 pKi = 10.0 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL438829 220580 0 None - 1 Rat 9.9 pKi = 9.9 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL2371592 216881 0 None - 1 Rat 9.9 pKi = 9.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCNC(=O)CNC(=O)CC[C@H](NC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990116+
CHEMBL386166 219156 0 None - 1 Rat 9.9 pKi = 9.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL405548 219344 0 None - 1 Human 9.9 pKi = 9.9 Binding
Binding affinity towards Gonadotropin-releasing hormone receptorBinding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCNC(=O)CNC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990118u
CHEMBL2371557 216862 0 None - 1 Rat 9.9 pKi = 9.9 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)NCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44379996 103615 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1441 14 16 15 -2.1 CC(=O)N[C@@H]1CC(=O)NCCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
91931282 103615 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1441 14 16 15 -2.1 CC(=O)N[C@@H]1CC(=O)NCCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL265240 103615 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1441 14 16 15 -2.1 CC(=O)N[C@@H]1CC(=O)NCCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44378966 103219 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1336 26 15 17 -3.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCC(=O)NC(=O)CC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
CHEMBL262160 103219 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1336 26 15 17 -3.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCC(=O)NC(=O)CC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
CHEMBL2371516 216846 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)CNC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
CHEMBL2371582 216874 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)NCCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371533 216853 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)NCCCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
11364940 185304 0 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 555 8 1 8 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL466731 185304 0 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 555 8 1 8 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
1185 10473 38 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1016/s0960-894x(03)00746-7
3038517 10473 38 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1016/s0960-894x(03)00746-7
CHEMBL22055 10473 38 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1016/s0960-894x(03)00746-7
DB06494 10473 38 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1016/s0960-894x(03)00746-7
1184 10505 36 None 426 2 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(03)00746-7
9874838 10505 36 None 426 2 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(03)00746-7
CHEMBL71917 10505 36 None 426 2 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(03)00746-7
CHEMBL2371483 216832 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](Cc3ccccc3)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
CHEMBL2371485 216834 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](CCCN=C(N)N)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
CHEMBL2371515 216845 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)CN(C)C(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
23656390 168462 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL413245 168462 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
1184 10505 36 None 426 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]leuprorelin from human GnRHR expressed in CHO cell membranes after 60 mins by gamma-ray counting methodDisplacement of [125I]leuprorelin from human GnRHR expressed in CHO cell membranes after 60 mins by gamma-ray counting method
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
9874838 10505 36 None 426 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]leuprorelin from human GnRHR expressed in CHO cell membranes after 60 mins by gamma-ray counting methodDisplacement of [125I]leuprorelin from human GnRHR expressed in CHO cell membranes after 60 mins by gamma-ray counting method
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
CHEMBL71917 10505 36 None 426 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]leuprorelin from human GnRHR expressed in CHO cell membranes after 60 mins by gamma-ray counting methodDisplacement of [125I]leuprorelin from human GnRHR expressed in CHO cell membranes after 60 mins by gamma-ray counting method
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
CHEMBL407361 219436 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)N[C@H](C)C(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL439083 220598 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL2371514 216844 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](Cc3ccccc3)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
CHEMBL2371522 216850 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](Cc3ccc(Cl)cc3)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44267812 104879 0 None 7 3 Rat 9.6 pKi = 9.6 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 941 10 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273440 104879 0 None 7 3 Rat 9.6 pKi = 9.6 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 941 10 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL438897 220583 0 None -1 2 Rat 9.6 pKi = 9.6 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL438897 220583 0 None 1 2 Human 9.6 pKi = 9.6 Binding
Binding affinity towards Gonadotropin-releasing hormone receptorBinding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990118u
CHEMBL436657 220463 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL406809 219399 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Affinity for rat Gonadotropin-releasing hormone receptor membrane evaluated using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat Gonadotropin-releasing hormone receptor membrane evaluated using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCCCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL2371591 216880 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N1CC=C[C@H]1C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm990116+
CHEMBL269726 217583 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding affinity towards Gonadotropin-releasing hormone receptorBinding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N1CC=C[C@@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm990118u
CHEMBL2371507 216841 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCNC(=O)[C@H](Cc3ccccc3)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44379287 168195 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1299 26 14 15 -1.6 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
CHEMBL412681 168195 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1299 26 14 15 -1.6 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44449120 102008 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL256109 102008 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
44432648 157006 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 643 9 2 4 7.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4nccnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL395225 157006 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 643 9 2 4 7.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4nccnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL411964 219744 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL2371537 216854 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CCCCC1C[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)CC[C@H](NC(C)=O)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N1 10.1021/jm9901172
CHEMBL2371587 216878 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCCNC(=O)CC[C@H](NC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990116+
CHEMBL441208 220665 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity towards Gonadotropin-releasing hormone receptorBinding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCCNC(=O)CC[C@H](NC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990118u
CHEMBL2371566 216867 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CCCCC1C[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)CCNC(=O)C[C@H](NC(C)=O)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N1 10.1021/jm9901172
44378889 175936 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1251 27 13 16 -2.8 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H]1CC(=O)N(CC(N)=O)C(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm990115h
CHEMBL440436 175936 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1251 27 13 16 -2.8 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H]1CC(=O)N(CC(N)=O)C(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm990115h
CHEMBL2371519 216849 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCCNC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44267907 23103 0 None -3 3 Human 9.5 pKi = 9.5 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL12282 23103 0 None -3 3 Human 9.5 pKi = 9.5 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44267907 23103 0 None -3 3 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12282 23103 0 None -3 3 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL2371568 216868 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)NCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371578 216871 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)NCCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371517 216847 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)CNC(=O)C[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44448991 162120 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL403234 162120 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL556355 162120 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL2371470 216829 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/jm990115h
CHEMBL2371486 216835 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)CCNC(=O)C[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
CHEMBL410779 219618 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
9872676 84970 0 None 1 17 Human 9.4 pKi = 9.4 Binding
Binding affinity to human recombinant GnRH receptorBinding affinity to human recombinant GnRH receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
CHEMBL210514 84970 0 None 1 17 Human 9.4 pKi = 9.4 Binding
Binding affinity to human recombinant GnRH receptorBinding affinity to human recombinant GnRH receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
9872676 84970 0 None -1 17 Rat 9.4 pKi = 9.4 Binding
Binding affinity to rat pituitary GnRH receptorBinding affinity to rat pituitary GnRH receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
CHEMBL210514 84970 0 None -1 17 Rat 9.4 pKi = 9.4 Binding
Binding affinity to rat pituitary GnRH receptorBinding affinity to rat pituitary GnRH receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
10649568 21338 0 None 10 2 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/s0960-894x(03)00746-7
CHEMBL120432 21338 0 None 10 2 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/s0960-894x(03)00746-7
9961721 175258 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL435167 175258 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
44432647 93515 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 622 9 2 4 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(=O)n(C)c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231954 93515 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 622 9 2 4 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(=O)n(C)c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL216634 216114 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC(=O)NC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
11376252 76145 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 547 7 1 6 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1021/jm701249f
CHEMBL192955 76145 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 547 7 1 6 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1021/jm701249f
11376252 76145 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 547 7 1 6 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1016/j.bmcl.2005.03.057
CHEMBL192955 76145 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 547 7 1 6 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1016/j.bmcl.2005.03.057
CHEMBL2371577 216870 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL429007 220271 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
11421412 185520 15 None 2398 2 Human 9.3 pKi = 9.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL468551 185520 15 None 2398 2 Human 9.3 pKi = 9.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
44388510 173019 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 538 9 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)Cc3ccccn3)c2=O)c1F 10.1021/jm049218c
CHEMBL426780 173019 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 538 9 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)Cc3ccccn3)c2=O)c1F 10.1021/jm049218c
11421412 185520 15 None 2398 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL468551 185520 15 None 2398 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
44432651 93478 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 632 9 3 4 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231760 93478 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 632 9 3 4 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44432643 153545 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 592 9 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL392446 153545 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 592 9 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
11167850 9518 28 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
1178 9518 28 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
1187 9518 28 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
CHEMBL179691 9518 28 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
11167850 9518 28 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1178 9518 28 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1187 9518 28 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL179691 9518 28 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
11167850 9518 28 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2008.04.029
1178 9518 28 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2008.04.029
1187 9518 28 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2008.04.029
CHEMBL179691 9518 28 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2008.04.029
11167850 9518 28 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2005.03.057
1178 9518 28 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2005.03.057
1187 9518 28 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2005.03.057
CHEMBL179691 9518 28 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2005.03.057
11167850 9518 28 None 6309 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
1178 9518 28 None 6309 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
1187 9518 28 None 6309 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
CHEMBL179691 9518 28 None 6309 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
CHEMBL2371579 216872 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CCCCC1C[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)[C@@H](C)NC(=O)C[C@H](NC(C)=O)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N1 10.1021/jm9901172
CHEMBL2371508 216842 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](CCCN=C(N)N)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
11443711 16904 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 515 8 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C3CCCC3)N(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL115703 16904 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 515 8 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C3CCCC3)N(C)C)c2=O)c1F 10.1021/jm049791w
44346397 121276 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL333518 121276 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44432652 103916 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 633 9 3 5 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cnc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL267838 103916 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 633 9 3 5 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cnc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44432654 166574 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 660 10 3 6 6.1 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)nc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL410547 166574 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 660 10 3 6 6.1 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)nc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44400235 175210 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.07.059
CHEMBL434936 175210 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.07.059
10345138 129335 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL360143 129335 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL75347 129335 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
44449681 102820 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 551 8 1 6 5.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL259906 102820 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 551 8 1 6 5.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
9854500 109049 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/s0960-894x(02)00370-0
CHEMBL303274 109049 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/s0960-894x(02)00370-0
9854500 109049 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm701249f
CHEMBL303274 109049 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm701249f
44400235 175210 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL434936 175210 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
44400235 175210 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL434936 175210 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
44400235 175210 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL434936 175210 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
44400235 175210 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL434936 175210 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
9854500 109049 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL303274 109049 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
44267887 105257 0 None -5 3 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 967 10 1 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275935 105257 0 None -5 3 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 967 10 1 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
10345138 129335 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm701249f
CHEMBL360143 129335 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm701249f
CHEMBL75347 129335 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm701249f
44448991 162120 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL403234 162120 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL556355 162120 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
10345138 129335 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL360143 129335 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL75347 129335 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL2371541 216857 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CCCCC1C[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)CNC(=O)C[C@H](NC(C)=O)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N1 10.1021/jm9901172
44432653 93479 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 650 9 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cc4nn[nH]c4cc2F)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231761 93479 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 650 9 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cc4nn[nH]c4cc2F)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44451355 164945 0 None - 1 Human 9.2 pKi = 9.2 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 577 11 2 4 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(C)CNCCCCc2ccnnc2)c1 10.1016/j.bmc.2007.09.026
CHEMBL408746 164945 0 None - 1 Human 9.2 pKi = 9.2 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 577 11 2 4 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(C)CNCCCCc2ccnnc2)c1 10.1016/j.bmc.2007.09.026
CHEMBL2371502 216840 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@](C)(Cc2ccc(O)cc2)NC1=O 10.1021/jm990115h
CHEMBL2371484 216833 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCNC(=O)[C@H](Cc3ccccc3)NC(=O)C[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44380258 168036 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1441 14 16 15 -2.1 CC(=O)N[C@@H]1CCC(=O)NCCC(=O)NC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
91931283 168036 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1441 14 16 15 -2.1 CC(=O)N[C@@H]1CCC(=O)NCCC(=O)NC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL411963 168036 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1441 14 16 15 -2.1 CC(=O)N[C@@H]1CCC(=O)NCCC(=O)NC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
10985312 85521 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL21126 85521 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
10985312 85521 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/j.bmc.2007.09.026
CHEMBL21126 85521 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/j.bmc.2007.09.026
CHEMBL2371575 216869 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL405420 219338 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44288080 166967 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 1009 15 2 14 7.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(CC3CC3)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL410940 166967 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 1009 15 2 14 7.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(CC3CC3)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL407800 219463 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44400245 132859 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 541 8 1 8 3.1 COc1cccc(-c2cn(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL364914 132859 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 541 8 1 8 3.1 COc1cccc(-c2cn(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
44400245 132859 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 541 8 1 8 3.1 COc1cccc(-c2cn(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL364914 132859 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 541 8 1 8 3.1 COc1cccc(-c2cn(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
11250647 8327 46 None 117 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
5293 8327 46 None 117 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
8362 8327 46 None 117 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
CHEMBL1208155 8327 46 None 117 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
DB11979 8327 46 None 117 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
44400271 76103 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 497 7 1 6 4.4 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1016/j.bmcl.2005.03.057
CHEMBL192912 76103 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 497 7 1 6 4.4 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1016/j.bmcl.2005.03.057
CHEMBL2371549 216859 0 None - 1 Rat 9.0 pKi = 9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CN)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm990115h
44432649 93474 0 None - 1 Rat 9.0 pKi = 9 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 645 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]c(C)nc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231739 93474 0 None - 1 Rat 9.0 pKi = 9 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 645 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]c(C)nc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
11365653 180969 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 631 12 2 7 5.7 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL454774 180969 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 631 12 2 7 5.7 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
10311600 167687 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 523 10 3 9 4.4 CNCCNc1nc(OC)c(NC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)OC4(C)C)o2)c(OC)n1 10.1016/j.bmc.2007.09.026
CHEMBL411526 167687 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 523 10 3 9 4.4 CNCCNc1nc(OC)c(NC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)OC4(C)C)o2)c(OC)n1 10.1016/j.bmc.2007.09.026
CHEMBL385982 219151 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC(=O)NCCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL410357 219594 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)NCCCC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@@H]3CCCN3C2=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
11477988 97785 0 None 954 2 Human 9.0 pKi = 9.0 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm701249f
CHEMBL23969 97785 0 None 954 2 Human 9.0 pKi = 9.0 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm701249f
11477988 97785 0 None 954 2 Human 9.0 pKi = 9.0 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
CHEMBL23969 97785 0 None 954 2 Human 9.0 pKi = 9.0 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
21018389 74236 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 517 6 1 5 5.2 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL189164 74236 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 517 6 1 5 5.2 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44353277 27042 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 712 16 2 7 7.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NCCCc4ccccc4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL130558 27042 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 712 16 2 7 7.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NCCCc4ccccc4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
25156943 195216 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 597 12 2 7 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL502341 195216 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 597 12 2 7 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
21036877 180429 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 627 13 2 7 5.9 Cc1c(-c2cccc(OCCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL453441 180429 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 627 13 2 7 5.9 Cc1c(-c2cccc(OCCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44340749 115895 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/j.bmcl.2004.11.026
CHEMBL321376 115895 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/j.bmcl.2004.11.026
44267868 104851 0 None 10 2 Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 933 10 1 14 7.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273275 104851 0 None 10 2 Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 933 10 1 14 7.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
9809065 108408 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 611 11 0 9 5.2 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)CCc1ccccn1 10.1021/jm0205402
CHEMBL298982 108408 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 611 11 0 9 5.2 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)CCc1ccccn1 10.1021/jm0205402
11202636 17003 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 489 9 1 6 4.1 CN[C@H](CC(C)C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
CHEMBL116071 17003 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 489 9 1 6 4.1 CN[C@H](CC(C)C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
44353248 26524 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 623 13 1 8 5.9 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL130126 26524 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 623 13 1 8 5.9 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
11202636 17003 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 489 9 1 6 4.1 CN[C@H](CC(C)C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
CHEMBL116071 17003 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 489 9 1 6 4.1 CN[C@H](CC(C)C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
21018389 74236 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 517 6 1 5 5.2 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL189164 74236 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 517 6 1 5 5.2 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
44379167 174540 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL 1376 16 15 15 -1.0 CC(=O)NC1CC(=O)NC(C(=O)N[C@H]2CC(=O)NC(C(=O)O)CNC(=O)[C@@H]3CCCN3C(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)C(Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccc(O)cc3)NC2=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL430344 174540 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL 1376 16 15 15 -1.0 CC(=O)NC1CC(=O)NC(C(=O)N[C@H]2CC(=O)NC(C(=O)O)CNC(=O)[C@@H]3CCCN3C(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)C(Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccc(O)cc3)NC2=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371487 216836 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCCNC(=O)CC[C@H](NC1=O)C(=O)N[C@H](Cc1ccc3ccccc3c1)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
11331001 195801 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL509075 195801 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
21036878 179825 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 645 13 2 7 5.9 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL451916 179825 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 645 13 2 7 5.9 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
11365653 180969 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 631 12 2 7 5.7 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL454774 180969 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 631 12 2 7 5.7 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
11331001 195801 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.07.059
CHEMBL509075 195801 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.07.059
11262242 195517 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 645 13 2 7 6.1 Cc1c(-c2cccc(OCCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL505033 195517 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 645 13 2 7 6.1 Cc1c(-c2cccc(OCCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44288081 165103 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 993 13 1 14 8.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(CC3CC3)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL408925 165103 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 993 13 1 14 8.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(CC3CC3)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44400261 140792 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 527 7 1 7 3.6 CS(=O)(=O)c1cccc(F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2008.04.036
CHEMBL371613 140792 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 527 7 1 7 3.6 CS(=O)(=O)c1cccc(F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2008.04.036
44400261 140792 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 527 7 1 7 3.6 CS(=O)(=O)c1cccc(F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2005.03.057
CHEMBL371613 140792 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 527 7 1 7 3.6 CS(=O)(=O)c1cccc(F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2005.03.057
44378649 103929 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1287 27 14 15 -1.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCC(=O)N(CC(N)=O)C(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm990115h
CHEMBL267984 103929 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1287 27 14 15 -1.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCC(=O)N(CC(N)=O)C(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm990115h
44379259 148382 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1277 24 12 15 -0.4 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2cccnc2)NC1=O 10.1021/jm990115h
CHEMBL385090 148382 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1277 24 12 15 -0.4 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2cccnc2)NC1=O 10.1021/jm990115h
44378908 168611 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1273 27 14 15 -2.3 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)N(CC(=O)O)C(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm990115h
CHEMBL414556 168611 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1273 27 14 15 -2.3 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)N(CC(=O)O)C(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm990115h
CHEMBL2371518 216848 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCCNC(=O)CC[C@H](NC1=O)C(=O)N[C@H](Cc1ccc3ccccc3c1)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44432635 93558 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 512 8 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2C(C)(C)C2(C)C)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232150 93558 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 512 8 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2C(C)(C)C2(C)C)CC3)c1 10.1016/j.bmcl.2007.05.009
11262242 195517 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 645 13 2 7 6.1 Cc1c(-c2cccc(OCCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL505033 195517 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 645 13 2 7 6.1 Cc1c(-c2cccc(OCCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44434386 96583 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 638 11 2 8 5.1 C#CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL237734 96583 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 638 11 2 8 5.1 C#CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
86276160 116631 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cellsDisplacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 485 9 1 8 5.0 COc1nc(OCCF)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1016/j.bmcl.2014.02.002
CHEMBL3233521 116631 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cellsDisplacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 485 9 1 8 5.0 COc1nc(OCCF)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1016/j.bmcl.2014.02.002
44400229 75458 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 497 7 1 6 4.4 COc1cccc(-c2cn(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL192171 75458 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 497 7 1 6 4.4 COc1cccc(-c2cn(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL2371559 216864 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)NCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44432636 94160 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 550 8 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C24CC5CC(CC(C5)C2)C4)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL233341 94160 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 550 8 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C24CC5CC(CC(C5)C2)C4)CC3)c1 10.1016/j.bmcl.2007.05.009
44432642 160373 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 574 9 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL398060 160373 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 574 9 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44287759 103472 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 999 12 2 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL264043 103472 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 999 12 2 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL407589 219449 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)N[C@@H](C)C(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL410382 219596 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3cccnc3)NC2=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL2371538 216855 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44347047 23371 0 None 5 2 Rat 8.8 pKi = 8.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL124056 23371 0 None 5 2 Rat 8.8 pKi = 8.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL264332 217392 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL2371531 216851 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC1=O 10.1021/jm9901172
CHEMBL412009 219749 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCCCC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@@H]3CCCN3C2=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
11168776 70384 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.4 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL180076 70384 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.4 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
44400352 74576 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 545 8 1 6 5.1 CCOc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL190929 74576 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 545 8 1 6 5.1 CCOc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL2371539 216856 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CCCCC1C[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)[C@H](C)NC(=O)C[C@H](NC(C)=O)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N1 10.1021/jm9901172
44378966 103219 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1336 26 15 17 -3.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCC(=O)NC(=O)CC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
CHEMBL262160 103219 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1336 26 15 17 -3.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCC(=O)NC(=O)CC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44432650 93546 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 703 10 3 5 6.5 CCn1c(=O)[nH]c2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4c3CN(C(=O)Cc3c(F)cccc3C(F)(F)F)CC4)ccc2c1=O 10.1016/j.bmcl.2007.05.009
CHEMBL232097 93546 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 703 10 3 5 6.5 CCn1c(=O)[nH]c2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4c3CN(C(=O)Cc3c(F)cccc3C(F)(F)F)CC4)ccc2c1=O 10.1016/j.bmcl.2007.05.009
44432640 161752 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 524 9 2 3 5.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL401226 161752 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 524 9 2 3 5.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2F)CC3)c1 10.1016/j.bmcl.2007.05.009
9854500 109049 0 None -2 3 Human 8.7 pKi = 8.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL303274 109049 0 None -2 3 Human 8.7 pKi = 8.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
9854500 109049 0 None -2 3 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL303274 109049 0 None -2 3 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
9854500 109049 0 None -2 3 Human 8.7 pKi = 8.7 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/s0960-894x(02)00370-0
CHEMBL303274 109049 0 None -2 3 Human 8.7 pKi = 8.7 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/s0960-894x(02)00370-0
11331001 195801 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL509075 195801 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
44576645 194975 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 571 9 2 8 3.6 N[C@@H](Cn1c(=O)c(-c2ccc(COC(=O)CO)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL499026 194975 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 571 9 2 8 3.6 N[C@@H](Cn1c(=O)c(-c2ccc(COC(=O)CO)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44353201 27819 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 650 15 2 7 6.3 CCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL131182 27819 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 650 15 2 7 6.3 CCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
44394589 73694 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 453 6 1 6 4.1 Cc1c(-c2cccs2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL186563 73694 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 453 6 1 6 4.1 Cc1c(-c2cccs2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
11752130 20910 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 487 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL119808 20910 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 487 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL405806 219362 0 None - 1 Rat 8.0 pKi = 8 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/jm990115h
44435979 95316 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 591 11 0 8 4.2 CSc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
CHEMBL235269 95316 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 591 11 0 8 4.2 CSc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
44436017 95507 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 605 9 0 7 4.7 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCN1CCc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL236152 95507 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 605 9 0 7 4.7 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCN1CCc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
44435993 168460 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 665 10 0 8 5.9 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3C(F)(F)F)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
CHEMBL413238 168460 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 665 10 0 8 5.9 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3C(F)(F)F)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
44347085 22024 0 None -3 2 Human 8.0 pKi = 8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121145 22024 0 None -3 2 Human 8.0 pKi = 8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44587396 180035 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 603 10 2 7 4.9 Cc1c(-c2cccc(OCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL452474 180035 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 603 10 2 7 4.9 Cc1c(-c2cccc(OCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44343914 121587 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 635 13 0 9 6.1 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL334063 121587 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 635 13 0 9 6.1 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11330603 135456 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 459 7 1 6 3.9 COc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
CHEMBL366865 135456 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 459 7 1 6 3.9 COc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
CHEMBL430613 135456 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 459 7 1 6 3.9 COc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
11156980 69367 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 505 7 1 7 4.0 CN[C@@H](Cn1c(=O)c(-c2ccc3c(c2)OCO3)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL178281 69367 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 505 7 1 7 4.0 CN[C@@H](Cn1c(=O)c(-c2ccc3c(c2)OCO3)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
44353229 26962 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 580 11 1 7 6.5 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL130487 26962 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 580 11 1 7 6.5 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
44343914 121587 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 635 13 0 9 6.1 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL334063 121587 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 635 13 0 9 6.1 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
44309615 109446 0 None - 1 Human 7.0 pKi = 7 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 655 10 0 7 7.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cc(Cl)cc(Cl)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL304548 109446 0 None - 1 Human 7.0 pKi = 7 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 655 10 0 7 7.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cc(Cl)cc(Cl)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44435978 95272 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 575 11 0 8 3.5 COc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
CHEMBL235051 95272 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 575 11 0 8 3.5 COc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
11284357 67791 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 7 1 5 4.1 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CCc1ccccc1 10.1016/j.bmcl.2004.02.004
CHEMBL176270 67791 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 7 1 5 4.1 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CCc1ccccc1 10.1016/j.bmcl.2004.02.004
CHEMBL72913 67791 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 7 1 5 4.1 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CCc1ccccc1 10.1016/j.bmcl.2004.02.004
44451476 102619 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1535 30 8 18 8.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccccc2C#CCNC(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL258970 102619 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1535 30 8 18 8.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccccc2C#CCNC(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44267883 23085 0 None -3 2 Human 5.0 pKi = 5 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 780 9 2 11 5.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12265 23085 0 None -3 2 Human 5.0 pKi = 5 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 780 9 2 11 5.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11249548 105866 0 None -97 2 Rat 5.0 pKi = 5 Binding
In vivo inhibition of rat Gonadotropin releasing hormone receptorIn vivo inhibition of rat Gonadotropin releasing hormone receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
CHEMBL280664 105866 0 None -97 2 Rat 5.0 pKi = 5 Binding
In vivo inhibition of rat Gonadotropin releasing hormone receptorIn vivo inhibition of rat Gonadotropin releasing hormone receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
44340637 16351 0 None 1479 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards monkey gonadotropin releasing hormone receptorBinding affinity towards monkey gonadotropin releasing hormone receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL112466 16351 0 None 1479 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards monkey gonadotropin releasing hormone receptorBinding affinity towards monkey gonadotropin releasing hormone receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
21048269 117873 0 None 2 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 415 5 1 2 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccccc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL326313 117873 0 None 2 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 415 5 1 2 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccccc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21047785 22231 0 None 20 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ccnc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121576 22231 0 None 20 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ccnc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11227010 92440 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 580 12 0 9 3.9 COc1cc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc(OC)c1OC 10.1021/jm030472z
CHEMBL22852 92440 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 580 12 0 9 3.9 COc1cc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc(OC)c1OC 10.1021/jm030472z
CHEMBL438103 220529 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CC(=O)NCCCC[C@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]3CCCN3C2=O)NC1=O 10.1021/jm990116+
9807700 194081 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 553 8 0 7 6.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)Cc4ccccn4)n3c2=O)c1 10.1021/jm0205402
CHEMBL49297 194081 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 553 8 0 7 6.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)Cc4ccccn4)n3c2=O)c1 10.1021/jm0205402
44346376 120583 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 622 10 1 7 7.3 CCNc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL332463 120583 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 622 10 1 7 7.3 CCNc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
44309440 109411 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 631 10 0 9 6.1 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL304308 109411 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 631 10 0 9 6.1 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44387924 67253 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3ccccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL175465 67253 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3ccccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21047534 23213 0 None 1 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 609 13 3 7 7.3 COCCCNc1ccnc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL123284 23213 0 None 1 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 609 13 3 7 7.3 COCCCNc1ccnc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
21047534 23213 0 None -1 2 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 609 13 3 7 7.3 COCCCNc1ccnc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL123284 23213 0 None -1 2 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 609 13 3 7 7.3 COCCCNc1ccnc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL263542 217353 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC1=O 10.1021/jm990116+
12986401 194420 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 464 7 1 7 3.0 COc1cccc(-n2c(=O)c(Cc3c(F)cccc3F)nn(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm701249f
CHEMBL494968 194420 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 464 7 1 7 3.0 COc1cccc(-n2c(=O)c(Cc3c(F)cccc3F)nn(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm701249f
10226423 196187 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 459 5 1 6 4.2 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)[C@@H](c1ccccc1)CS2)c1ccccc1 10.1021/jm701249f
CHEMBL513126 196187 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 459 5 1 6 4.2 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)[C@@H](c1ccccc1)CS2)c1ccccc1 10.1021/jm701249f
11330034 91175 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 532 10 0 6 5.0 Cc1c(-c2ccc(C(C)C)cc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL22196 91175 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 532 10 0 6 5.0 Cc1c(-c2ccc(C(C)C)cc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
44593613 195438 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 598 11 2 8 4.2 CCOC(=O)CNCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.04.036
CHEMBL503624 195438 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 598 11 2 8 4.2 CCOC(=O)CNCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.04.036
44389658 70020 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 459 5 1 6 4.2 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1)CS2)c1ccccc1 10.1016/j.bmcl.2005.01.009
CHEMBL179101 70020 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 459 5 1 6 4.2 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1)CS2)c1ccccc1 10.1016/j.bmcl.2005.01.009
44309541 210653 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 647 12 0 9 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc(OC)c(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL68753 210653 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 647 12 0 9 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc(OC)c(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44309439 210685 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 630 10 0 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccc2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL68988 210685 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 630 10 0 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccc2)cc1 10.1016/s0960-894x(02)00371-2
44593613 195438 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 598 11 2 8 4.2 CCOC(=O)CNCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.07.059
CHEMBL503624 195438 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 598 11 2 8 4.2 CCOC(=O)CNCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.07.059
21045834 23217 0 None 3 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4ncccn4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL123301 23217 0 None 3 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4ncccn4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44451367 66440 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 556 6 1 6 4.4 Cc1ccc(CN2CCc3c(c(=O)n(CC4NCCc5ccccc54)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.09.026
CHEMBL172192 66440 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 556 6 1 6 4.4 Cc1ccc(CN2CCc3c(c(=O)n(CC4NCCc5ccccc54)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.09.026
9892420 209920 0 None - 1 Human 6.0 pKi = 6.0 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 10 1 7 3.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL64148 209920 0 None - 1 Human 6.0 pKi = 6.0 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 10 1 7 3.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11294757 70612 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 489 8 0 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C(C)C)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL180280 70612 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 489 8 0 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C(C)C)N(C)C)c2=O)c1F 10.1021/jm049218c
44576643 194832 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 512 7 2 6 4.0 NCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.04.036
CHEMBL497747 194832 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 512 7 2 6 4.0 NCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.04.036
11329628 69798 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 393 6 1 5 3.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CC1 10.1016/j.bmcl.2004.02.004
CHEMBL178805 69798 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 393 6 1 5 3.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CC1 10.1016/j.bmcl.2004.02.004
CHEMBL73575 69798 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 393 6 1 5 3.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CC1 10.1016/j.bmcl.2004.02.004
10983979 209954 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 505 10 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3ccccc3)c2=O)c1 10.1021/jm034041s
CHEMBL64252 209954 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 505 10 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3ccccc3)c2=O)c1 10.1021/jm034041s
44451485 164954 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1607 32 8 20 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2cccc(C#CCNC(=O)CNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL408759 164954 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1607 32 8 20 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2cccc(C#CCNC(=O)CNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
11226753 70118 0 None -389 2 Rat 5.0 pKi = 5.0 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL179429 70118 0 None -389 2 Rat 5.0 pKi = 5.0 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
9984259 117278 0 None -281 2 Rat 5.0 pKi = 5.0 Binding
Tested for binding affinity towards rat gonadotropin releasing hormone receptorTested for binding affinity towards rat gonadotropin releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
CHEMBL324912 117278 0 None -281 2 Rat 5.0 pKi = 5.0 Binding
Tested for binding affinity towards rat gonadotropin releasing hormone receptorTested for binding affinity towards rat gonadotropin releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
44267881 24845 0 None 14 2 Rat 7.0 pKi = 7.0 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 877 10 1 12 6.9 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12666 24845 0 None 14 2 Rat 7.0 pKi = 7.0 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 877 10 1 12 6.9 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44267876 104882 0 None -53 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 14 6.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273466 104882 0 None -53 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 14 6.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44309511 211035 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 624 13 1 9 5.3 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL71141 211035 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 624 13 1 9 5.3 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00370-0
44340788 16314 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL112287 16314 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44343804 17344 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 517 10 1 6 4.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](CC(C)C)NC(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL116976 17344 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 517 10 1 6 4.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](CC(C)C)NC(C)C)c2=O)c1F 10.1021/jm049791w
44343779 17794 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 529 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NC(C)C)C3CCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL117504 17794 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 529 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NC(C)C)C3CCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL2371488 216837 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](Cc3ccccc3)NC(=O)C[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
25156946 195148 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 617 11 2 7 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL501329 195148 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 617 11 2 7 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
11168634 91863 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 536 10 0 7 4.6 CSc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
CHEMBL22459 91863 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 536 10 0 7 4.6 CSc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
11226753 70118 0 None 389 2 Human 6.9 pKi = 6.9 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL179429 70118 0 None 389 2 Human 6.9 pKi = 6.9 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
11180219 117998 0 None 112 2 Human 6.9 pKi = 6.9 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL326504 117998 0 None 112 2 Human 6.9 pKi = 6.9 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
44394723 131122 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 468 6 1 7 3.8 Cc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
CHEMBL363659 131122 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 468 6 1 7 3.8 Cc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
44400146 74347 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 570 9 1 8 3.0 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)N(C)C)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL189984 74347 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 570 9 1 8 3.0 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)N(C)C)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL2371493 216838 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@@H](Cc3ccccc3)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
CHEMBL265232 217420 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44432627 154907 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 430 7 2 3 4.5 CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
CHEMBL393540 154907 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 430 7 2 3 4.5 CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
44387880 67312 0 None - 1 Human 6.9 pKi = 6.9 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 498 7 1 8 2.3 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL175821 67312 0 None - 1 Human 6.9 pKi = 6.9 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 498 7 1 8 2.3 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
44387979 67376 0 None - 1 Human 6.9 pKi = 6.9 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 492 8 1 9 2.1 COc1ccccc1Cn1c(=O)n(C[C@H](N)c2ccccc2)c(=O)n(-c2cccc(OC)c2F)c1=O 10.1016/j.bmcl.2005.05.038
CHEMBL176020 67376 0 None - 1 Human 6.9 pKi = 6.9 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 492 8 1 9 2.1 COc1ccccc1Cn1c(=O)n(C[C@H](N)c2ccccc2)c(=O)n(-c2cccc(OC)c2F)c1=O 10.1016/j.bmcl.2005.05.038
23450008 139185 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2004.11.026
CHEMBL369723 139185 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2004.11.026
44267904 105192 0 None 6 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275521 105192 0 None 6 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44352734 25287 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2cc(F)ccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL127384 25287 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2cc(F)ccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11443571 171591 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 508 9 0 6 4.0 Cc1c(-c2cccc(F)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL421858 171591 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 508 9 0 6 4.0 Cc1c(-c2cccc(F)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
11168176 129800 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 397 7 1 6 2.5 COCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
CHEMBL360910 129800 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 397 7 1 6 2.5 COCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
CHEMBL73526 129800 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 397 7 1 6 2.5 COCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
21047799 117180 0 None -6 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 559 9 2 5 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4c(C)noc4C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL324394 117180 0 None -6 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 559 9 2 5 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4c(C)noc4C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44340631 16280 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 471 9 1 6 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112131 16280 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 471 9 1 6 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00619-x
11421412 185520 15 None -2398 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL468551 185520 15 None -2398 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
11763365 107980 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 551 7 0 7 5.4 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc4c(n3c2=O)CN(CCc2ccccn2)CC4(C)C)c1 10.1021/jm0205402
CHEMBL295807 107980 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 551 7 0 7 5.4 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc4c(n3c2=O)CN(CCc2ccccn2)CC4(C)C)c1 10.1021/jm0205402
9984259 117278 0 None -281 2 Rat 4.9 pKi = 4.9 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
CHEMBL324912 117278 0 None -281 2 Rat 4.9 pKi = 4.9 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
44309440 109411 0 None - 1 Human 4.9 pKi = 4.9 Binding
Compound was evaluated in cloned rat Gonadotropin-releasing hormone receptor assay for its ability to displace the binding of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistCompound was evaluated in cloned rat Gonadotropin-releasing hormone receptor assay for its ability to displace the binding of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 631 10 0 9 6.1 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL304308 109411 0 None - 1 Human 4.9 pKi = 4.9 Binding
Compound was evaluated in cloned rat Gonadotropin-releasing hormone receptor assay for its ability to displace the binding of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistCompound was evaluated in cloned rat Gonadotropin-releasing hormone receptor assay for its ability to displace the binding of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 631 10 0 9 6.1 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44267903 169012 0 None 3 2 Rat 5.9 pKi = 5.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 906 10 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCN(C)C2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL416337 169012 0 None 3 2 Rat 5.9 pKi = 5.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 906 10 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCN(C)C2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44389652 172803 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 473 6 1 7 3.5 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2)CO3)c1F 10.1016/j.bmcl.2005.01.009
CHEMBL425529 172803 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 473 6 1 7 3.5 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2)CO3)c1F 10.1016/j.bmcl.2005.01.009
10347081 96285 0 None -223 2 Rat 4.9 pKi = 4.9 Binding
Binding affinity towards rat gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards rat gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23730 96285 0 None -223 2 Rat 4.9 pKi = 4.9 Binding
Binding affinity towards rat gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards rat gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
44435817 95879 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 489 6 0 6 3.9 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccccc2)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL236544 95879 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 489 6 0 6 3.9 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccccc2)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL410452 219602 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CC(=O)NCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm990116+
CHEMBL438901 220584 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm990116+
44577101 185306 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 532 7 1 7 4.1 COc1cccc(-c2nn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL466736 185306 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 532 7 1 7 4.1 COc1cccc(-c2nn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
11249548 105866 0 None 97 2 Human 7.9 pKi = 7.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
CHEMBL280664 105866 0 None 97 2 Human 7.9 pKi = 7.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
11179420 70123 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 493 7 1 6 4.7 CSc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1021/jm049218c
CHEMBL179460 70123 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 493 7 1 6 4.7 CSc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1021/jm049218c
11341364 172865 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 519 7 1 7 4.0 CN[C@@H](Cn1c(=O)c(-c2ccc3c(c2)OCCO3)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL425864 172865 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 519 7 1 7 4.0 CN[C@@H](Cn1c(=O)c(-c2ccc3c(c2)OCCO3)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
44388018 67249 0 None 389 2 Human 7.9 pKi = 7.9 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL175443 67249 0 None 389 2 Human 7.9 pKi = 7.9 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
10050123 17954 0 None 20 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 464 6 2 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(N)=O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117863 17954 0 None 20 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 464 6 2 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(N)=O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44288074 107004 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 951 13 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL288534 107004 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 951 13 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
11179660 96487 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL23767 96487 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
10930118 108736 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 610 11 0 8 5.8 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)CCc1ccccc1 10.1021/jm0205402
CHEMBL301322 108736 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 610 11 0 8 5.8 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)CCc1ccccc1 10.1021/jm0205402
11179660 96487 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccc3)c2=O)c1 10.1021/jm030472z
CHEMBL23767 96487 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccc3)c2=O)c1 10.1021/jm030472z
44353254 28580 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 574 12 1 7 6.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)C)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL131942 28580 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 574 12 1 7 6.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)C)cc1 10.1016/s0960-894x(01)00780-6
44394651 129703 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 573 8 2 8 5.8 Cc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)c(C)c1 10.1016/j.bmcl.2004.07.022
CHEMBL360625 129703 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 573 8 2 8 5.8 Cc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)c(C)c1 10.1016/j.bmcl.2004.07.022
44394685 134283 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 575 9 2 9 5.2 COc1ccccc1Nc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
CHEMBL366127 134283 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 575 9 2 9 5.2 COc1ccccc1Nc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
10951713 109025 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 546 9 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN3CCC[C@H]3Cc3ccccn3)c2=O)c1 10.1021/jm034041s
CHEMBL303140 109025 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 546 9 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN3CCC[C@H]3Cc3ccccn3)c2=O)c1 10.1021/jm034041s
44309573 210444 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 625 12 0 9 5.8 CCN(CC)CCN(C)Cc1c(-c2ccc(OC)cc2)nc2n(Cc3ccccc3F)c(C)c(-c3ccc4c(c3)OCO4)c(=O)n12 10.1016/s0960-894x(02)00371-2
CHEMBL67370 210444 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 625 12 0 9 5.8 CCN(CC)CCN(C)Cc1c(-c2ccc(OC)cc2)nc2n(Cc3ccccc3F)c(C)c(-c3ccc4c(c3)OCO4)c(=O)n12 10.1016/s0960-894x(02)00371-2
CHEMBL405961 219367 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
21045818 119873 0 None 3 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncccn4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331337 119873 0 None 3 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncccn4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44388018 67249 0 None -389 2 Rat 4.9 pKi = 4.9 Binding
Inhibition constant against rat GnRH receptorInhibition constant against rat GnRH receptor
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL175443 67249 0 None -389 2 Rat 4.9 pKi = 4.9 Binding
Inhibition constant against rat GnRH receptorInhibition constant against rat GnRH receptor
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44436014 95361 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 568 7 0 6 5.0 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCN1C1CCCC1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL235519 95361 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 568 7 0 6 5.0 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCN1C1CCCC1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
44436016 154351 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 688 10 0 8 5.3 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@@H]1CCCN(C[C@@H]3CCCN3Cc3ccccn3)C1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL393093 154351 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 688 10 0 8 5.3 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@@H]1CCCN(C[C@@H]3CCCN3Cc3ccccn3)C1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
44309535 109767 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 665 15 1 8 7.1 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccc2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL306684 109767 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 665 15 1 8 7.1 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccc2)cc1 10.1016/s0960-894x(02)00370-0
44379747 103560 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1350 15 13 13 1.4 CC(C)C[C@H]1C(=O)N[C@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)NCCC(=O)N2CC=C[C@H]2C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1C 10.1021/jm990116+
CHEMBL264806 103560 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1350 15 13 13 1.4 CC(C)C[C@H]1C(=O)N[C@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)NCCC(=O)N2CC=C[C@H]2C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1C 10.1021/jm990116+
CHEMBL410451 219601 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CC(=O)NCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm990116+
44577097 185270 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 6 1 5 4.4 C=C1C(Cl)=CC=C1c1c(C)n(Cc2c(F)cccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm701249f
CHEMBL466531 185270 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 6 1 5 4.4 C=C1C(Cl)=CC=C1c1c(C)n(Cc2c(F)cccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm701249f
11261693 70182 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 463 6 1 5 4.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Cl 10.1021/jm049218c
CHEMBL179612 70182 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 463 6 1 5 4.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Cl 10.1021/jm049218c
CHEMBL74721 70182 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 463 6 1 5 4.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Cl 10.1021/jm049218c
44353270 121993 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 623 12 1 8 5.8 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL334537 121993 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 623 12 1 8 5.8 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
44353230 123564 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 610 13 0 8 6.4 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL337748 123564 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 610 13 0 8 6.4 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
44379747 103560 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Gonadotropin-releasing hormone receptorBinding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL 1350 15 13 13 1.4 CC(C)C[C@H]1C(=O)N[C@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)NCCC(=O)N2CC=C[C@H]2C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1C 10.1021/jm990118u
CHEMBL264806 103560 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Gonadotropin-releasing hormone receptorBinding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL 1350 15 13 13 1.4 CC(C)C[C@H]1C(=O)N[C@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)NCCC(=O)N2CC=C[C@H]2C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1C 10.1021/jm990118u
44394567 72956 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccc(Cl)cc2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL184345 72956 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccc(Cl)cc2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
21047618 121308 0 None -1 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 635 11 3 7 7.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncc(C)c(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333574 121308 0 None -1 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 635 11 3 7 7.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncc(C)c(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44267874 103989 0 None 15 2 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 878 11 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL268489 103989 0 None 15 2 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 878 11 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11283517 102229 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL25714 102229 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11283517 102229 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1 10.1021/jm030472z
CHEMBL25714 102229 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1 10.1021/jm030472z
11330280 129830 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 435 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CCCCC1 10.1021/jm049218c
CHEMBL360934 129830 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 435 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CCCCC1 10.1021/jm049218c
CHEMBL72606 129830 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 435 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CCCCC1 10.1021/jm049218c
21047937 118074 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 472 7 1 3 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN(C)C)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL326606 118074 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 472 7 1 3 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN(C)C)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44312724 19172 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1C(C)c1ccccc1 10.1016/j.bmcl.2004.02.004
CHEMBL1185733 19172 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1C(C)c1ccccc1 10.1016/j.bmcl.2004.02.004
CHEMBL430618 19172 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1C(C)c1ccccc1 10.1016/j.bmcl.2004.02.004
44309616 210522 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 655 10 0 7 7.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(C(F)(F)F)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL67820 210522 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 655 10 0 7 7.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(C(F)(F)F)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
25113693 168693 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 896 15 3 10 6.2 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3ccccc3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL415279 168693 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 896 15 3 10 6.2 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3ccccc3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21047859 20935 0 None 1 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL119856 20935 0 None 1 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
11376064 173918 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 11 0 7 4.0 COCc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
CHEMBL429062 173918 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 11 0 7 4.0 COCc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
44400147 74432 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 612 9 1 9 2.7 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)N3CCOCC3)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL190676 74432 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 612 9 1 9 2.7 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)N3CCOCC3)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
44309403 210684 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 631 10 0 9 6.1 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccncc2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL68985 210684 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 631 10 0 9 6.1 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccncc2)cc1 10.1016/s0960-894x(02)00371-2
44435994 153821 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 482 8 0 6 3.0 CCc1ccc(CN2CCc3c(c(=O)n(CCN(C)C)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
CHEMBL392688 153821 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 482 8 0 6 3.0 CCc1ccc(CN2CCc3c(c(=O)n(CCN(C)C)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
44267811 103990 0 None 14 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 864 12 1 12 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL268491 103990 0 None 14 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 864 12 1 12 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
21047807 119763 0 None -23 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 568 8 3 7 6.4 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncc(C#N)c(N)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331087 119763 0 None -23 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 568 8 3 7 6.4 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncc(C#N)c(N)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11249167 97075 0 None - 1 Human 7.8 pKi = 7.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL23854 97075 0 None - 1 Human 7.8 pKi = 7.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL216526 216109 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H]1CCC(=O)NCCCC[C@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@@H]3CCCN3C2=O)NC(=O)[C@@H](Cc2cccnc2)NC1=O 10.1021/jm990116+
44435979 95316 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 591 11 0 8 4.2 CSc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1021/jm701249f
CHEMBL235269 95316 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 591 11 0 8 4.2 CSc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1021/jm701249f
11249167 97075 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1 10.1021/jm701249f
CHEMBL23854 97075 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1 10.1021/jm701249f
11214860 91546 0 None 323 2 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
CHEMBL22314 91546 0 None 323 2 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
11249167 97075 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23854 97075 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1 10.1021/jm030472z
11192229 129897 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL361128 129897 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
11168776 70384 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.4 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL180076 70384 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.4 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
44394661 72884 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 564 7 1 7 5.8 Cc1c(-c2csc(-c3ccc(Cl)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL183938 72884 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 564 7 1 7 5.8 Cc1c(-c2csc(-c3ccc(Cl)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44435982 64871 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 605 12 0 8 4.6 CCSc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
CHEMBL16745 64871 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 605 12 0 8 4.6 CCSc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
44435986 103280 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 615 10 0 8 5.0 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
CHEMBL262579 103280 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 615 10 0 8 5.0 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
44587398 195814 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 659 13 1 7 6.3 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@@H](c2ccccc2)N(C)C)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL509267 195814 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 659 13 1 7 6.3 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@@H](c2ccccc2)N(C)C)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
11214860 91546 0 None 323 2 Human 7.8 pKi = 7.8 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
CHEMBL22314 91546 0 None 323 2 Human 7.8 pKi = 7.8 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
44267812 104879 0 None -64 3 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 941 10 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273440 104879 0 None -64 3 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 941 10 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
44394753 130080 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 598 7 1 7 6.2 Cc1c(-c2csc(-c3cccc(C(F)(F)F)c3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL361513 130080 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 598 7 1 7 6.2 Cc1c(-c2csc(-c3cccc(C(F)(F)F)c3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44346261 120646 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 651 10 2 8 5.7 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)CN)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL332570 120646 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 651 10 2 8 5.7 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)CN)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44340720 16480 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 0 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CN(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL113183 16480 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 0 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CN(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44309296 210360 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 584 10 0 9 5.1 COCCN(C)Cc1c(-c2ccc(OC)cc2)nc2n(Cc3ccccc3F)c(C)c(-c3ccc4c(c3)OCO4)c(=O)n12 10.1016/s0960-894x(02)00371-2
CHEMBL66808 210360 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 584 10 0 9 5.1 COCCN(C)Cc1c(-c2ccc(OC)cc2)nc2n(Cc3ccccc3F)c(C)c(-c3ccc4c(c3)OCO4)c(=O)n12 10.1016/s0960-894x(02)00371-2
21045833 120468 0 None 11 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncccn4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL332305 120468 0 None 11 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncccn4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11330072 93712 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 11 0 7 4.0 COCc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23231 93712 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 11 0 7 4.0 COCc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
44394835 129411 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 539 7 1 9 3.3 Cc1c(-c2csc(N3CCOCC3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL360384 129411 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 539 7 1 9 3.3 Cc1c(-c2csc(N3CCOCC3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44387885 139074 0 None - 1 Human 5.8 pKi = 5.8 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 492 9 1 8 2.4 COc1cccc(-n2c(=O)n(CC[C@H](N)CC(C)C)c(=O)n(Cc3c(F)cccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL369706 139074 0 None - 1 Human 5.8 pKi = 5.8 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 492 9 1 8 2.4 COc1cccc(-n2c(=O)n(CC[C@H](N)CC(C)C)c(=O)n(Cc3c(F)cccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44341075 16680 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 427 5 1 6 2.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C3CCNC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL114370 16680 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 427 5 1 6 2.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C3CCNC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44353266 123866 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 635 14 2 6 6.9 CCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL339273 123866 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 635 14 2 6 6.9 CCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
21045817 121328 0 None -22 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNc4ncccn4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333730 121328 0 None -22 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNc4ncccn4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44587401 195012 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 660 14 3 8 4.7 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCNCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL499442 195012 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 660 14 3 8 4.7 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCNCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
21048323 174489 0 None -8 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 421 5 1 2 6.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL430250 174489 0 None -8 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 421 5 1 2 6.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44435819 95970 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 490 6 0 7 3.3 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccncc2)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL236750 95970 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 490 6 0 7 3.3 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccncc2)CC3)c1 10.1016/j.bmc.2007.05.029
11225960 17781 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049218c
CHEMBL117396 17781 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049218c
11225960 17781 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049791w
CHEMBL117396 17781 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049791w
44346375 22135 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 690 9 1 7 7.3 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)C(F)(F)F)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL121441 22135 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 690 9 1 7 7.3 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)C(F)(F)F)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
9891852 16867 1 None 23 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL115482 16867 1 None 23 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
9959327 108733 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 553 9 1 7 5.7 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCCc4ccccn4)n3c2=O)c1 10.1021/jm0205402
CHEMBL301285 108733 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 553 9 1 7 5.7 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCCc4ccccn4)n3c2=O)c1 10.1021/jm0205402
44394714 129406 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 590 9 2 10 5.1 Cc1c(-c2csc(Nc3ccc([N+](=O)[O-])cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL360363 129406 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 590 9 2 10 5.1 Cc1c(-c2csc(Nc3ccc([N+](=O)[O-])cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
10347081 96285 0 None 223 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards monkey gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards monkey gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23730 96285 0 None 223 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards monkey gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards monkey gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
44436009 96136 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 598 8 0 6 5.4 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(Cc5ccccc5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL236966 96136 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 598 8 0 6 5.4 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(Cc5ccccc5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44340845 16642 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 469 9 1 6 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL114183 16642 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 469 9 1 6 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44432656 165937 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 645 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL409825 165937 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 645 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44451397 102678 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 856 16 4 10 5.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL259220 102678 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 856 16 4 10 5.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44434373 96823 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 637 11 3 7 4.6 C#CCNC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL238160 96823 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 637 11 3 7 4.6 C#CCNC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44267881 24845 0 None -14 2 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 877 10 1 12 6.9 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12666 24845 0 None -14 2 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 877 10 1 12 6.9 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL406628 219395 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL415179 219957 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CC(=O)NCCCC[C@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@@H](CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]3CCCN3C2=O)NC1=O 10.1021/jm990116+
44353276 124005 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 697 15 2 6 7.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NCCCc4ccccc4)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL339468 124005 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 697 15 2 6 7.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NCCCc4ccccc4)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(01)00780-6
44346479 120902 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 650 11 1 7 7.9 CC(C)CNc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL332837 120902 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 650 11 1 7 7.9 CC(C)CNc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
44435977 95501 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 579 10 0 7 4.1 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL236127 95501 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 579 10 0 7 4.1 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
9911446 17553 0 None 33 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 446 5 1 3 6.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(C#N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117170 17553 0 None 33 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 446 5 1 3 6.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(C#N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44340785 121581 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL334037 121581 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11467328 93519 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 580 9 0 7 5.8 Cc1c(-c2ccc3oc4ccccc4c3c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL23198 93519 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 580 9 0 7 5.8 Cc1c(-c2ccc3oc4ccccc4c3c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
44346398 21310 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL120260 21310 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44346663 121593 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 592 10 0 9 5.2 COCCN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL334110 121593 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 592 10 0 9 5.2 COCCN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44451396 163452 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 842 16 4 10 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL406958 163452 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 842 16 4 10 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21047815 21720 0 None 30 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120834 21720 0 None 30 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11733484 193624 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 476 6 0 6 5.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)C)n3c2=O)c1 10.1021/jm0205402
CHEMBL48944 193624 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 476 6 0 6 5.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)C)n3c2=O)c1 10.1021/jm0205402
11168176 129800 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 397 7 1 6 2.5 COCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL360910 129800 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 397 7 1 6 2.5 COCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL73526 129800 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 397 7 1 6 2.5 COCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
10874838 107595 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 506 10 0 7 3.6 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm034041s
CHEMBL293247 107595 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 506 10 0 7 3.6 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm034041s
44435998 153073 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 522 6 0 6 4.0 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4C)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL392087 153073 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 522 6 0 6 4.0 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4C)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
21047631 17732 0 None 5 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CN)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117330 17732 0 None 5 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CN)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44346848 119847 0 None 1 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331204 119847 0 None 1 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
21045833 120468 0 None -11 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncccn4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL332305 120468 0 None -11 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncccn4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11318370 16474 0 None - 1 Human 7.8 pKi = 7.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL113151 16474 0 None - 1 Human 7.8 pKi = 7.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44394857 131136 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 544 7 1 7 5.4 Cc1ccc(-c2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
CHEMBL363731 131136 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 544 7 1 7 5.4 Cc1ccc(-c2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
44400204 175337 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 517 6 2 6 4.4 N[C@@H](Cn1c(=O)c(-c2cccc(O)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL435689 175337 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 517 6 2 6 4.4 N[C@@H](Cn1c(=O)c(-c2cccc(O)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
44309390 174900 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc(OC)cc4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL432922 174900 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc(OC)cc4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44432628 94530 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 484 8 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2CCCC2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL233762 94530 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 484 8 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2CCCC2)CC3)c1 10.1016/j.bmcl.2007.05.009
44387961 172800 0 None 144 2 Human 7.8 pKi = 7.8 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL425523 172800 0 None 144 2 Human 7.8 pKi = 7.8 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44267864 174535 0 None 30 2 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CCC1CN(C(=O)O[C@H]2[C@H](C)[C@@H](OC3O[C@H](C)C[C@H](N(C)C(C)C)[C@H]3O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]3N(CCc4ccc(Cl)cc4)C(=O)O[C@]3(C)[C@@H](CC)OC(=O)[C@@H]2C)C(=O)O1 10.1021/jm030418i
CHEMBL430312 174535 0 None 30 2 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CCC1CN(C(=O)O[C@H]2[C@H](C)[C@@H](OC3O[C@H](C)C[C@H](N(C)C(C)C)[C@H]3O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]3N(CCc4ccc(Cl)cc4)C(=O)O[C@]3(C)[C@@H](CC)OC(=O)[C@@H]2C)C(=O)O1 10.1021/jm030418i
44267902 105180 0 None -6 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL275467 105180 0 None -6 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44287893 169984 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 919 11 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL418256 169984 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 919 11 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44267902 105180 0 None -6 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275467 105180 0 None -6 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44352665 125052 0 None 43 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 635 13 0 9 6.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL340934 125052 0 None 43 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 635 13 0 9 6.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11319703 129873 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 529 7 1 6 5.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1SC(F)(F)F 10.1021/jm049218c
CHEMBL361016 129873 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 529 7 1 6 5.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1SC(F)(F)F 10.1021/jm049218c
15462666 103277 4 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL262557 103277 4 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44435996 95560 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 559 9 0 7 4.0 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)Cc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL236342 95560 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 559 9 0 7 4.0 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)Cc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44387926 137393 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 528 8 1 8 3.2 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3Cl)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL368153 137393 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 528 8 1 8 3.2 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3Cl)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
21047799 117180 0 None 6 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 559 9 2 5 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4c(C)noc4C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL324394 117180 0 None 6 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 559 9 2 5 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4c(C)noc4C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21048323 174489 0 None 8 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 421 5 1 2 6.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL430250 174489 0 None 8 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 421 5 1 2 6.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
9851194 123462 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 578 10 0 8 5.6 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL337172 123462 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 578 10 0 8 5.6 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00779-x
44341057 170136 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 10 0 7 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL419212 170136 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 10 0 7 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44435995 95504 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 524 9 0 6 4.1 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)CC(C)C)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL236137 95504 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 524 9 0 6 4.1 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)CC(C)C)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44340649 116412 0 None - 1 Human 4.8 pKi = 4.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 415 6 1 6 2.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL322283 116412 0 None - 1 Human 4.8 pKi = 4.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 415 6 1 6 2.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N)c2=O)c1 10.1016/s0960-894x(03)00620-6
11214294 128973 0 None -912 2 Rat 4.8 pKi = 4.8 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL359754 128973 0 None -912 2 Rat 4.8 pKi = 4.8 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
11467134 130331 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1021/jm701249f
CHEMBL361798 130331 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1021/jm701249f
CHEMBL74686 130331 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1021/jm701249f
44400099 134204 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 509 8 1 7 4.4 COc1cccc(-c2cn(Cc3c(F)cccc3SC)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL366020 134204 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 509 8 1 7 4.4 COc1cccc(-c2cn(Cc3c(F)cccc3SC)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
10962804 108572 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 566 9 0 6 6.6 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)CCc4ccccc4)n3c2=O)c1 10.1021/jm0205402
CHEMBL300080 108572 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 566 9 0 6 6.6 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)CCc4ccccc4)n3c2=O)c1 10.1021/jm0205402
44448991 162120 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL403234 162120 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL556355 162120 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
44353246 26993 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 538 9 1 7 5.3 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL130513 26993 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 538 9 1 7 5.3 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
44340635 16462 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 471 9 1 6 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL113068 16462 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 471 9 1 6 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00619-x
44288078 163860 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 910 11 2 14 5.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL40743 163860 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 910 11 2 14 5.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL317064 217976 15 None - 1 Rat 5.7 pKi = 5.7 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
44451349 102927 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 508 6 1 6 3.5 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCNCC4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.09.026
CHEMBL260540 102927 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 508 6 1 6 3.5 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCNCC4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.09.026
44434438 152973 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1707 45 6 28 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL392008 152973 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1707 45 6 28 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44267875 22342 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity was determined against human Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity was determined against human Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 879 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12204 22342 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity was determined against human Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity was determined against human Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 879 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
10323198 131142 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 487 6 1 6 4.7 Cc1c(-c2ccc(Cl)s2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
CHEMBL363759 131142 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 487 6 1 6 4.7 Cc1c(-c2ccc(Cl)s2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
10323198 131142 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 487 6 1 6 4.7 Cc1c(-c2ccc(Cl)s2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL363759 131142 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 487 6 1 6 4.7 Cc1c(-c2ccc(Cl)s2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44432657 156246 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 635 10 3 3 7.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(C(=O)O)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL394613 156246 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 635 10 3 3 7.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(C(=O)O)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
11671279 137662 0 None 331 2 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL368511 137662 0 None 331 2 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44353262 123593 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 664 15 1 7 7.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccc2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL337919 123593 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 664 15 1 7 7.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccc2)cc1 10.1016/s0960-894x(01)00780-6
25156400 195638 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 581 12 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL506877 195638 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 581 12 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
21036877 180429 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 627 13 2 7 5.9 Cc1c(-c2cccc(OCCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL453441 180429 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 627 13 2 7 5.9 Cc1c(-c2cccc(OCCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44267876 104882 0 None 53 2 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 14 6.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273466 104882 0 None 53 2 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 14 6.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11331001 195801 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL509075 195801 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
1179 7748 36 None 1 3 Mouse 8.7 pKi = 8.7 Binding
Binding affinity to mouse gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to mouse gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
9957278 7748 36 None 1 3 Mouse 8.7 pKi = 8.7 Binding
Binding affinity to mouse gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to mouse gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
CHEMBL494803 7748 36 None 1 3 Mouse 8.7 pKi = 8.7 Binding
Binding affinity to mouse gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to mouse gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
CHEMBL2371556 216861 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCCNC(=O)CCNC(=O)C[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371558 216863 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)NCCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL439470 220620 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm990116+
11282957 129111 1 None 1096 2 Human 8.6 pKi = 8.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm701249f
CHEMBL359894 129111 1 None 1096 2 Human 8.6 pKi = 8.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm701249f
16058727 201598 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 548 7 1 7 4.6 COc1cccc(-c2nn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1021/jm701249f
CHEMBL539167 201598 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 548 7 1 7 4.6 COc1cccc(-c2nn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1021/jm701249f
11282957 129111 1 None 1096 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
CHEMBL359894 129111 1 None 1096 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
11282957 129111 1 None 1096 2 Human 8.6 pKi = 8.6 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2005.01.009
CHEMBL359894 129111 1 None 1096 2 Human 8.6 pKi = 8.6 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2005.01.009
CHEMBL2371498 216839 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)C(C)(C)OC(C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)C(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
71459935 85733 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 466 7 1 4 4.5 COc1cccc(N2CN(Cc3c(F)cccc3F)C(=O)N(C[C@H](N)c3ccccc3)C2=O)c1 10.1016/j.bmcl.2004.11.026
CHEMBL2113012 85733 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 466 7 1 4 4.5 COc1cccc(N2CN(Cc3c(F)cccc3F)C(=O)N(C[C@H](N)c3ccccc3)C2=O)c1 10.1016/j.bmcl.2004.11.026
11466452 121514 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 515 8 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C3CCCC3)N(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL333850 121514 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 515 8 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C3CCCC3)N(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL2371560 216865 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)N[C@H](C)C(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL410819 219625 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)N[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@@H]2C(=O)NCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O)C(=O)O 10.1021/jm990115h
44347085 22024 0 None 3 2 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121145 22024 0 None 3 2 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44400350 133774 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 531 6 1 5 5.5 Cc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c(Cl)c1 10.1016/j.bmcl.2005.03.057
CHEMBL365561 133774 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 531 6 1 5 5.5 Cc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c(Cl)c1 10.1016/j.bmcl.2005.03.057
44432641 174282 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 540 9 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2Cl)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL429976 174282 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 540 9 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2Cl)CC3)c1 10.1016/j.bmcl.2007.05.009
9831160 170249 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 665 15 1 8 7.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL419998 170249 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 665 15 1 8 7.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00370-0
9831160 170249 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 665 15 1 8 7.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL419998 170249 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 665 15 1 8 7.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL385505 219132 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCCN)N(C(C)C)C(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3cccnc3)NC2=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
11168311 173021 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL426783 173021 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
10077844 110561 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 637 13 1 8 6.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(C)=O)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL308910 110561 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 637 13 1 8 6.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(C)=O)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
44267869 104895 0 None - 1 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 10 1 14 7.0 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)O[C@H](C)[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273535 104895 0 None - 1 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 10 1 14 7.0 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)O[C@H](C)[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44267902 105180 0 None 6 2 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275467 105180 0 None 6 2 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL405265 219331 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Affinity for rat Gonadotropin-releasing hormone receptor membrane evaluated using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat Gonadotropin-releasing hormone receptor membrane evaluated using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC(=O)NCC[C@@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
10919567 105806 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 664 10 1 7 7.4 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL280213 105806 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 664 10 1 7 7.4 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
10347081 96285 0 None 223 2 Human 7.7 pKi = 7.7 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1021/jm030472z
CHEMBL23730 96285 0 None 223 2 Human 7.7 pKi = 7.7 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1021/jm030472z
11467134 130331 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1021/jm049218c
CHEMBL361798 130331 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1021/jm049218c
CHEMBL74686 130331 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1021/jm049218c
11272935 138565 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 443 6 1 5 4.2 Cc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
CHEMBL369326 138565 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 443 6 1 5 4.2 Cc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
CHEMBL75954 138565 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 443 6 1 5 4.2 Cc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
44449186 102327 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 565 9 1 6 5.7 CC[C@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
CHEMBL257599 102327 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 565 9 1 6 5.7 CC[C@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
44394615 132663 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 572 7 1 8 5.1 Cc1c(-c2csc(-c3ccc4c(c3)CCO4)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL364840 132663 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 572 7 1 8 5.1 Cc1c(-c2csc(-c3ccc4c(c3)CCO4)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
10007333 16374 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(CNC[C@@H](C)n2c(=O)c(-c3cccc(OC)c3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112559 16374 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(CNC[C@@H](C)n2c(=O)c(-c3cccc(OC)c3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/s0960-894x(03)00619-x
10347081 96285 0 None 223 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23730 96285 0 None 223 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
10098618 118107 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 10 0 7 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL326804 118107 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 10 0 7 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
11467134 130331 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1016/j.bmcl.2004.02.004
CHEMBL361798 130331 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1016/j.bmcl.2004.02.004
CHEMBL74686 130331 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1016/j.bmcl.2004.02.004
44379092 164629 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1337 26 15 14 -0.6 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
CHEMBL408372 164629 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1337 26 15 14 -0.6 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44435975 98954 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 573 11 0 7 4.0 CCc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
CHEMBL242399 98954 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 573 11 0 7 4.0 CCc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
44436015 154349 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 591 8 0 7 4.6 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCN1Cc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL393092 154349 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 591 8 0 7 4.6 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCN1Cc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
44387907 67455 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 516 7 1 8 2.5 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL176056 67455 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 516 7 1 8 2.5 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44387992 69299 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 496 7 1 8 2.7 COc1cccc(-n2c(=O)n(Cc3ccccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL178218 69299 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 496 7 1 8 2.7 COc1cccc(-n2c(=O)n(Cc3ccccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21045797 177381 0 None 12 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNC(=O)C(F)(F)F)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL445074 177381 0 None 12 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNC(=O)C(F)(F)F)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL2371581 216873 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CCCCC1C[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)CNC(=O)CC[C@H](NC(C)=O)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N1 10.1021/jm9901172
9984259 117278 0 None 281 2 Human 6.7 pKi = 6.7 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
CHEMBL324912 117278 0 None 281 2 Human 6.7 pKi = 6.7 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
44343975 17349 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 586 11 0 8 5.3 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3cccc(OC)c3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL116988 17349 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 586 11 0 8 5.3 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3cccc(OC)c3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
11238637 74346 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 585 6 1 5 6.3 N[C@@H](Cn1c(=O)c(-c2ccc(C(F)(F)F)cc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL189964 74346 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 585 6 1 5 6.3 N[C@@H](Cn1c(=O)c(-c2ccc(C(F)(F)F)cc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
11330280 129830 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 435 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CCCCC1 10.1016/j.bmcl.2004.02.004
CHEMBL360934 129830 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 435 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CCCCC1 10.1016/j.bmcl.2004.02.004
CHEMBL72606 129830 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 435 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CCCCC1 10.1016/j.bmcl.2004.02.004
9983568 105758 0 None 263 2 Human 6.7 pKi = 6.7 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL279885 105758 0 None 263 2 Human 6.7 pKi = 6.7 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
9984259 117278 0 None 281 2 Human 6.7 pKi = 6.7 Binding
Tested for binding affinity towards monkey gonadotropin releasing hormone receptorTested for binding affinity towards monkey gonadotropin releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
CHEMBL324912 117278 0 None 281 2 Human 6.7 pKi = 6.7 Binding
Tested for binding affinity towards monkey gonadotropin releasing hormone receptorTested for binding affinity towards monkey gonadotropin releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
44352801 27115 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL130607 27115 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44340670 16413 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 0 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CN(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112730 16413 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 0 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CN(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL317341 217981 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
44287779 148352 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 979 12 2 14 7.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL384920 148352 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 979 12 2 14 7.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
21046762 17348 0 None -9 2 Rat 5.7 pKi = 5.7 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 464 5 3 3 4.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL116986 17348 0 None -9 2 Rat 5.7 pKi = 5.7 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 464 5 3 3 4.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44267885 24593 0 None -9 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 892 10 2 13 5.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCNC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12589 24593 0 None -9 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 892 10 2 13 5.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCNC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44267811 103990 0 None -14 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 864 12 1 12 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL268491 103990 0 None -14 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 864 12 1 12 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44380024 175812 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1459 18 13 14 2.4 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC1=O 10.1021/jm990116+
91931289 175812 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1459 18 13 14 2.4 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC1=O 10.1021/jm990116+
CHEMBL439439 175812 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1459 18 13 14 2.4 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC1=O 10.1021/jm990116+
CHEMBL407855 219468 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm990116+
11490288 175426 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1Cl 10.1021/jm049218c
CHEMBL436276 175426 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1Cl 10.1021/jm049218c
CHEMBL75439 175426 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1Cl 10.1021/jm049218c
44353304 25788 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 664 15 2 7 6.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL128810 25788 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 664 15 2 7 6.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL2371498 216839 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)C(C)(C)OC(C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)C(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
11354193 102989 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 640 9 1 8 3.8 COc1ccc(CN2CC3CC(c4ccc(N(C)C)c5ccccc45)N4C(=O)N(CCN5CCOCC5)C(=O)C34C2)cc1NC(C)=O 10.1016/j.bmc.2007.09.026
CHEMBL260816 102989 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 640 9 1 8 3.8 COc1ccc(CN2CC3CC(c4ccc(N(C)C)c5ccccc45)N4C(=O)N(CCN5CCOCC5)C(=O)C34C2)cc1NC(C)=O 10.1016/j.bmc.2007.09.026
44340783 174678 0 None - 1 Human 6.7 pKi = 6.7 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 532 8 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H]3CCCN3Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL431248 174678 0 None - 1 Human 6.7 pKi = 6.7 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 532 8 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H]3CCCN3Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44394577 130000 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 8 2 8 5.5 Cc1ccccc1Nc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
CHEMBL361313 130000 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 8 2 8 5.5 Cc1ccccc1Nc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
44352513 124878 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 635 11 0 10 4.9 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC4CCOC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
CHEMBL340677 124878 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 635 11 0 10 4.9 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC4CCOC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
44340637 16351 0 None -1479 2 Rat 4.7 pKi = 4.7 Binding
Binding affinity towards rat GnRH gonadotropin releasing hormone receptorBinding affinity towards rat GnRH gonadotropin releasing hormone receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL112466 16351 0 None -1479 2 Rat 4.7 pKi = 4.7 Binding
Binding affinity towards rat GnRH gonadotropin releasing hormone receptorBinding affinity towards rat GnRH gonadotropin releasing hormone receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44267874 103989 0 None -15 2 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 878 11 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL268489 103989 0 None -15 2 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 878 11 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
21047785 22231 0 None -20 2 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ccnc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121576 22231 0 None -20 2 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ccnc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44267885 24593 0 None 9 2 Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 892 10 2 13 5.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCNC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12589 24593 0 None 9 2 Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 892 10 2 13 5.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCNC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11191153 201649 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)c3ccccc3)c2=O)c1F 10.1021/jm049218c
CHEMBL540207 201649 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)c3ccccc3)c2=O)c1F 10.1021/jm049218c
44576679 200217 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 567 12 2 7 4.3 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL526327 200217 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 567 12 2 7 4.3 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
21047516 22118 0 None 1 2 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 595 12 3 7 6.9 COCCNc1nccc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL121412 22118 0 None 1 2 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 595 12 3 7 6.9 COCCNc1nccc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
44267810 104867 0 None -5 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 939 12 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL273387 104867 0 None -5 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 939 12 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44267810 104867 0 None -5 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 939 12 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273387 104867 0 None -5 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 939 12 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44577067 200016 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 477 5 1 6 4.4 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CS2)c1ccccc1 10.1021/jm701249f
CHEMBL523709 200016 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 477 5 1 6 4.4 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CS2)c1ccccc1 10.1021/jm701249f
11352630 95483 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 504 9 0 6 4.2 Cc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
CHEMBL23604 95483 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 504 9 0 6 4.2 Cc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
22716564 130568 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 477 5 1 6 4.4 NC(Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CS2)c1ccccc1 10.1016/j.bmcl.2005.01.009
CHEMBL362283 130568 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 477 5 1 6 4.4 NC(Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CS2)c1ccccc1 10.1016/j.bmcl.2005.01.009
10994908 169787 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 518 10 0 6 4.4 CCc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm034041s
CHEMBL417558 169787 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 518 10 0 6 4.4 CCc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm034041s
44309321 210632 1 None - 1 Human 6.7 pKi = 6.7 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 582 10 0 8 6.3 CCCCN(C)Cc1c(-c2ccc(OC)cc2)nc2n(Cc3ccccc3F)c(C)c(-c3ccc4c(c3)OCO4)c(=O)n12 10.1016/s0960-894x(02)00371-2
CHEMBL68625 210632 1 None - 1 Human 6.7 pKi = 6.7 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 582 10 0 8 6.3 CCCCN(C)Cc1c(-c2ccc(OC)cc2)nc2n(Cc3ccccc3F)c(C)c(-c3ccc4c(c3)OCO4)c(=O)n12 10.1016/s0960-894x(02)00371-2
21046762 17348 0 None 9 2 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 464 5 3 3 4.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL116986 17348 0 None 9 2 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 464 5 3 3 4.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21047538 21330 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 555 8 3 6 6.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncc(F)c(N)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120397 21330 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 555 8 3 6 6.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncc(F)c(N)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44390769 71645 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 486 6 1 7 2.5 N[C@@H](Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2004.11.026
CHEMBL182145 71645 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 486 6 1 7 2.5 N[C@@H](Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2004.11.026
44309323 210827 0 None - 1 Human 5.7 pKi = 5.7 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 601 12 1 8 6.0 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN2CCCC2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL69914 210827 0 None - 1 Human 5.7 pKi = 5.7 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 601 12 1 8 6.0 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN2CCCC2)cc1 10.1016/s0960-894x(02)00370-0
44352735 125225 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 647 14 0 10 6.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL341124 125225 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 647 14 0 10 6.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11071561 109231 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 534 11 0 7 4.1 CCc1c(-c2cccc(OC)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL304002 109231 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 534 11 0 7 4.1 CCc1c(-c2cccc(OC)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44435820 168120 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 542 7 1 6 4.4 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(CCc2c[nH]c4ccccc24)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL412581 168120 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 542 7 1 6 4.4 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(CCc2c[nH]c4ccccc24)CC3)c1 10.1016/j.bmc.2007.05.029
44451460 163227 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1691 34 8 20 10.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2cccc(C#CCNC(=O)[C@@H](NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)C(C)C)c2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL406713 163227 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1691 34 8 20 10.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2cccc(C#CCNC(=O)[C@@H](NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)C(C)C)c2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
11191675 70156 0 None -186 2 Rat 5.7 pKi = 5.7 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL179600 70156 0 None -186 2 Rat 5.7 pKi = 5.7 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL3085404 70156 0 None -186 2 Rat 5.7 pKi = 5.7 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
9958318 97002 0 None -15 2 Rat 5.7 pKi = 5.7 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23830 97002 0 None -15 2 Rat 5.7 pKi = 5.7 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL266536 217466 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm990116+
44577051 194209 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 509 7 1 6 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)(N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL493794 194209 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 509 7 1 6 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)(N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
44344157 118153 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 543 9 1 6 5.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NC(C)C)C3CCCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL327076 118153 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 543 9 1 6 5.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NC(C)C)C3CCCCC3)c2=O)c1F 10.1021/jm049791w
44434404 173347 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1477 33 4 24 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL427981 173347 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1477 33 4 24 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44309582 210981 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 569 11 0 9 4.6 CCOC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00370-0
CHEMBL70851 210981 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 569 11 0 9 4.6 CCOC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00370-0
44389658 70020 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 459 5 1 6 4.2 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1)CS2)c1ccccc1 10.1021/jm701249f
CHEMBL179101 70020 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 459 5 1 6 4.2 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1)CS2)c1ccccc1 10.1021/jm701249f
12991507 194355 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 461 5 1 6 3.6 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CO2)c1ccccc1 10.1021/jm701249f
CHEMBL494621 194355 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 461 5 1 6 3.6 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CO2)c1ccccc1 10.1021/jm701249f
10940289 97423 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
CHEMBL23900 97423 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
44312821 18835 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 409 8 1 5 4.0 CCCCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL1183624 18835 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 409 8 1 5 4.0 CCCCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL308154 18835 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 409 8 1 5 4.0 CCCCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
11330603 135456 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 459 7 1 6 3.9 COc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL366865 135456 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 459 7 1 6 3.9 COc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL430613 135456 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 459 7 1 6 3.9 COc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
22716524 130434 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 461 5 1 6 3.6 NC(Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CO2)c1ccccc1 10.1016/j.bmcl.2005.01.009
CHEMBL362025 130434 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 461 5 1 6 3.6 NC(Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CO2)c1ccccc1 10.1016/j.bmcl.2005.01.009
10940289 97423 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm034041s
CHEMBL23900 97423 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm034041s
44309525 110051 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 611 13 0 9 5.8 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00371-2
CHEMBL308446 110051 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 611 13 0 9 5.8 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00371-2
10557573 118224 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL 870 22 9 8 3.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)N1C(=O)N[C@H](Cc2c[nH]c3ccccc23)C1=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
CHEMBL327528 118224 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL 870 22 9 8 3.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)N1C(=O)N[C@H](Cc2c[nH]c3ccccc23)C1=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
11671279 137662 0 None -331 2 Rat 5.6 pKi = 5.6 Binding
Inhibition constant against rat GnRH receptorInhibition constant against rat GnRH receptor
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL368511 137662 0 None -331 2 Rat 5.6 pKi = 5.6 Binding
Inhibition constant against rat GnRH receptorInhibition constant against rat GnRH receptor
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44346848 119847 0 None -1 2 Rat 6.6 pKi = 6.6 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331204 119847 0 None -1 2 Rat 6.6 pKi = 6.6 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
10929667 92547 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 548 9 0 8 3.7 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL22929 92547 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 548 9 0 8 3.7 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
10929667 92547 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 548 9 0 8 3.7 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL22929 92547 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 548 9 0 8 3.7 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44388002 129165 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CC[C@H](N)c3ccccc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL360047 129165 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CC[C@H](N)c3ccccc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21047784 117414 0 None 36 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 574 9 4 7 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4cc(O)nc(O)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL325747 117414 0 None 36 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 574 9 4 7 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4cc(O)nc(O)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21046570 119864 0 None 34 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 479 6 1 4 6.2 COC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
CHEMBL331277 119864 0 None 34 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 479 6 1 4 6.2 COC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
11671279 137662 0 None 331 2 Human 7.6 pKi = 7.6 Binding
Inhibition constant against monkey GnRH receptorInhibition constant against monkey GnRH receptor
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL368511 137662 0 None 331 2 Human 7.6 pKi = 7.6 Binding
Inhibition constant against monkey GnRH receptorInhibition constant against monkey GnRH receptor
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
10929667 92547 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 548 9 0 8 3.7 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmc.2007.09.026
CHEMBL22929 92547 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 548 9 0 8 3.7 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmc.2007.09.026
44340780 16521 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 543 13 0 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)CCCOCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL113455 16521 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 543 13 0 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)CCCOCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00620-6
10929574 107911 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 538 8 1 6 6.3 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCc4ccccc4)n3c2=O)c1 10.1021/jm0205402
CHEMBL295275 107911 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 538 8 1 6 6.3 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCc4ccccc4)n3c2=O)c1 10.1021/jm0205402
11421243 97435 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 532 10 0 6 5.0 Cc1c(-c2cccc(C(C)C)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL23908 97435 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 532 10 0 6 5.0 Cc1c(-c2cccc(C(C)C)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
21048269 117873 0 None -2 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 415 5 1 2 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccccc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL326313 117873 0 None -2 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 415 5 1 2 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccccc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
11123821 210086 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity was determined towards human Gonadotropin-releasing hormone receptorBinding affinity was determined towards human Gonadotropin-releasing hormone receptor
ChEMBL 491 9 1 6 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCc3ccccc3)c2=O)c1 10.1021/jm034041s
CHEMBL64795 210086 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity was determined towards human Gonadotropin-releasing hormone receptorBinding affinity was determined towards human Gonadotropin-releasing hormone receptor
ChEMBL 491 9 1 6 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCc3ccccc3)c2=O)c1 10.1021/jm034041s
44387961 172800 0 None 144 2 Human 6.6 pKi = 6.6 Binding
Inhibition constant against monkey GnRH receptorInhibition constant against monkey GnRH receptor
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL425523 172800 0 None 144 2 Human 6.6 pKi = 6.6 Binding
Inhibition constant against monkey GnRH receptorInhibition constant against monkey GnRH receptor
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44352548 175353 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2cccc(F)c2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL435793 175353 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2cccc(F)c2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44343932 175351 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 561 10 0 8 5.5 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3cccc(OC)c3)c(CN(C)Cc3ccco3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL435784 175351 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 561 10 0 8 5.5 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3cccc(OC)c3)c(CN(C)Cc3ccco3)n2c1=O 10.1016/s0960-894x(02)00745-x
44436004 95521 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 619 9 0 7 5.0 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@@H]1CCCCN1CCc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL236197 95521 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 619 9 0 7 5.0 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@@H]1CCCCN1CCc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
44436005 95890 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 508 6 1 6 3.5 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCNC4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL236550 95890 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 508 6 1 6 3.5 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCNC4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
10439527 176259 0 None 288 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 677 15 0 9 7.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL443027 176259 0 None 288 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 677 15 0 9 7.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11477970 96274 0 None 281 2 Human 7.6 pKi = 7.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
CHEMBL23729 96274 0 None 281 2 Human 7.6 pKi = 7.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
44436002 153874 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 599 8 0 7 5.0 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4Cc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL392731 153874 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 599 8 0 7 5.0 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4Cc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44340784 16275 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 519 9 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL112093 16275 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 519 9 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
21045797 177381 0 None -12 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNC(=O)C(F)(F)F)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL445074 177381 0 None -12 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNC(=O)C(F)(F)F)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44340804 15921 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccc(F)cc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL110052 15921 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccc(F)cc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
9825757 116935 0 None 12 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 465 6 2 3 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(=O)O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL323687 116935 0 None 12 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 465 6 2 3 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(=O)O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44340636 118018 0 None - 1 Human 5.6 pKi = 5.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 415 6 1 6 2.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL326510 118018 0 None - 1 Human 5.6 pKi = 5.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 415 6 1 6 2.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N)c2=O)c1 10.1016/s0960-894x(03)00620-6
44352514 25649 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 659 13 0 9 6.3 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC(C4CC4)C4CC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
CHEMBL128262 25649 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 659 13 0 9 6.3 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC(C4CC4)C4CC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
44309252 210613 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 589 9 0 7 5.5 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(Br)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL68537 210613 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 589 9 0 7 5.5 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(Br)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44451385 102852 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 580 10 0 7 4.4 CC(C)CN(C)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(OC(F)(F)F)cc1)C2 10.1016/j.bmc.2007.09.026
CHEMBL260058 102852 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 580 10 0 7 4.4 CC(C)CN(C)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(OC(F)(F)F)cc1)C2 10.1016/j.bmc.2007.09.026
11477970 96274 0 None -281 2 Rat 4.6 pKi = 4.6 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
CHEMBL23729 96274 0 None -281 2 Rat 4.6 pKi = 4.6 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
44267883 23085 0 None 3 2 Rat 5.6 pKi = 5.6 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 780 9 2 11 5.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12265 23085 0 None 3 2 Rat 5.6 pKi = 5.6 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 780 9 2 11 5.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44435985 153728 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 613 10 0 7 4.8 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)c(Cl)c1)C2 10.1016/j.bmc.2007.05.029
CHEMBL392604 153728 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 613 10 0 7 4.8 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)c(Cl)c1)C2 10.1016/j.bmc.2007.05.029
44436008 96135 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 576 7 0 6 5.2 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(C5CCCC5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL236965 96135 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 576 7 0 6 5.2 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(C5CCCC5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44435999 153876 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 564 8 0 6 5.0 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4CC(C)C)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL392733 153876 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 564 8 0 6 5.0 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4CC(C)C)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44394818 172898 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 530 7 1 7 5.1 Cc1c(-c2csc(-c3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL426058 172898 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 530 7 1 7 5.1 Cc1c(-c2csc(-c3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
21045828 21336 0 None 2 2 Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(NCC5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120420 21336 0 None 2 2 Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(NCC5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44352515 123849 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 633 11 0 9 6.0 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC4CCCC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
CHEMBL339211 123849 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 633 11 0 9 6.0 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC4CCCC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
11766904 193420 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 561 11 0 7 5.7 CCN(CC)CCN(C)Cc1c(C(C)(C)C)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
CHEMBL48806 193420 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 561 11 0 7 5.7 CCN(CC)CCN(C)Cc1c(C(C)(C)C)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
44312666 18841 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 421 5 1 5 4.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1C1CCCCC1 10.1016/j.bmcl.2004.02.004
CHEMBL1183666 18841 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 421 5 1 5 4.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1C1CCCCC1 10.1016/j.bmcl.2004.02.004
CHEMBL310716 18841 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 421 5 1 5 4.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1C1CCCCC1 10.1016/j.bmcl.2004.02.004
44451319 102950 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 882 15 3 10 6.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL260647 102950 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 882 15 3 10 6.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44352874 29089 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 575 11 0 9 4.9 CCOC(=O)c1cn(Cc2ccccc2)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL132387 29089 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 575 11 0 9 4.9 CCOC(=O)c1cn(Cc2ccccc2)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44343976 17350 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 571 10 0 7 5.9 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3cccc(OC)c3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL116989 17350 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 571 10 0 7 5.9 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3cccc(OC)c3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00745-x
11319401 128921 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 489 8 0 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C(C)C)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL359681 128921 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 489 8 0 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C(C)C)N(C)C)c2=O)c1F 10.1021/jm049218c
11261693 70182 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 463 6 1 5 4.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL179612 70182 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 463 6 1 5 4.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL74721 70182 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 463 6 1 5 4.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Cl 10.1016/j.bmcl.2004.02.004
44587399 195401 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 646 13 3 8 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCNCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL502967 195401 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 646 13 3 8 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCNCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
44387908 69963 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 500 8 1 9 2.6 COc1cccc(-n2c(=O)n(CCC(N)c3cccs3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL179023 69963 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 500 8 1 9 2.6 COc1cccc(-n2c(=O)n(CCC(N)c3cccs3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
44287778 88355 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 993 15 2 14 7.8 CCC(C)N(CC1CC1)[C@H]1C[C@@H](C)OC(O[C@@H]2[C@@H](C)[C@H](OC3C[C@@](C)(OC)[C@@H](O)[C@H](C)O3)[C@@H](C)C(=O)O[C@H](CC)[C@@]3(C)OC(=O)N(CCc4ccc(Cl)cc4)[C@@H]3[C@@H](C)C(=O)[C@H](C)C[C@]2(C)OC)[C@@H]1O 10.1016/j.bmcl.2003.12.059
CHEMBL216252 88355 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 993 15 2 14 7.8 CCC(C)N(CC1CC1)[C@H]1C[C@@H](C)OC(O[C@@H]2[C@@H](C)[C@H](OC3C[C@@](C)(OC)[C@@H](O)[C@H](C)O3)[C@@H](C)C(=O)O[C@H](CC)[C@@]3(C)OC(=O)N(CCc4ccc(Cl)cc4)[C@@H]3[C@@H](C)C(=O)[C@H](C)C[C@]2(C)OC)[C@@H]1O 10.1016/j.bmcl.2003.12.059
44353264 29023 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 608 10 0 9 5.5 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)cc2n(Cc3ccccc3F)cc(C3=NC(C)(C)CO3)c(=O)n12 10.1016/s0960-894x(01)00780-6
CHEMBL132339 29023 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 608 10 0 9 5.5 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)cc2n(Cc3ccccc3F)cc(C3=NC(C)(C)CO3)c(=O)n12 10.1016/s0960-894x(01)00780-6
10050123 17954 0 None -20 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 464 6 2 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(N)=O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117863 17954 0 None -20 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 464 6 2 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(N)=O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44394852 133943 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 497 8 2 8 3.9 CCNc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
CHEMBL365695 133943 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 497 8 2 8 3.9 CCNc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
44346374 121206 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 590 10 0 8 6.3 CCCCN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL333233 121206 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 590 10 0 8 6.3 CCCCN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
21045823 120919 0 None -40 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=O)C(F)(F)F)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL332923 120919 0 None -40 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=O)C(F)(F)F)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21046387 117429 0 None -53 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 493 7 1 4 6.6 CCOC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
CHEMBL325843 117429 0 None -53 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 493 7 1 4 6.6 CCOC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
44267863 105294 0 None 2 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 950 12 1 14 7.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL276217 105294 0 None 2 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 950 12 1 14 7.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44387935 68873 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 494 8 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(CN)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL177523 68873 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 494 8 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(CN)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2005.05.038
44347004 22221 0 None 13 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121535 22221 0 None 13 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44340798 115564 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL320920 115564 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
21047859 20935 0 None -1 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL119856 20935 0 None -1 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44340644 16686 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 517 7 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C3CCN(Cc4ccccc4)C3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL114399 16686 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 517 7 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C3CCN(Cc4ccccc4)C3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44309399 210682 0 None - 1 Human 4.6 pKi = 4.6 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 518 10 1 7 5.4 CCCC(=O)Nc1ccc(-c2cn3c(=O)c(C(=O)OC(CC)CC)cn(Cc4ccccc4F)c3n2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL68964 210682 0 None - 1 Human 4.6 pKi = 4.6 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 518 10 1 7 5.4 CCCC(=O)Nc1ccc(-c2cn3c(=O)c(C(=O)OC(CC)CC)cn(Cc4ccccc4F)c3n2)cc1 10.1016/s0960-894x(02)00370-0
44352566 27430 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2ccc(F)cc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3cccnc3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL130861 27430 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2ccc(F)cc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3cccnc3)n2c1=O 10.1016/s0960-894x(01)00779-x
44309361 109512 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 582 7 0 9 4.9 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN2CCOCC2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL304950 109512 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 582 7 0 9 4.9 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN2CCOCC2)cc1 10.1016/s0960-894x(02)00371-2
44309585 211157 0 None - 1 Human 7.5 pKi = 7.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 641 14 1 9 6.7 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)Cc2ccco2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL71793 211157 0 None - 1 Human 7.5 pKi = 7.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 641 14 1 9 6.7 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)Cc2ccco2)cc1 10.1016/s0960-894x(02)00370-0
44587405 179019 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 673 13 2 7 6.6 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCC(C)(C)CC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL447424 179019 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 673 13 2 7 6.6 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCC(C)(C)CC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
44387918 67434 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 476 7 1 8 2.4 COc1cccc(-n2c(=O)n(Cc3ccccc3C)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL176029 67434 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 476 7 1 8 2.4 COc1cccc(-n2c(=O)n(Cc3ccccc3C)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21047519 21194 0 None 1 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 551 8 3 6 6.8 Cc1cc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)nc(N)n1 10.1016/s0960-894x(02)00756-4
CHEMBL120048 21194 0 None 1 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 551 8 3 6 6.8 Cc1cc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)nc(N)n1 10.1016/s0960-894x(02)00756-4
44434411 153531 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1521 36 4 25 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL392434 153531 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1521 36 4 25 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44309375 110394 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 651 11 1 8 7.0 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2N2CCC3C=CC=CC3C2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL308696 110394 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 651 11 1 8 7.0 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2N2CCC3C=CC=CC3C2)cc1 10.1016/s0960-894x(02)00370-0
10345138 129335 0 None -2041 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL360143 129335 0 None -2041 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL75347 129335 0 None -2041 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
11226470 169848 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 538 10 0 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1F 10.1021/jm030472z
CHEMBL417645 169848 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 538 10 0 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1F 10.1021/jm030472z
10027591 133049 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 467 6 1 6 4.4 Cc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)s1 10.1016/j.bmcl.2004.07.022
CHEMBL365012 133049 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 467 6 1 6 4.4 Cc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)s1 10.1016/j.bmcl.2004.07.022
44387977 67294 0 None - 1 Human 8.5 pKi = 8.5 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 548 7 1 8 3.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL175711 67294 0 None - 1 Human 8.5 pKi = 8.5 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 548 7 1 8 3.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44347048 21282 0 None 18 2 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120164 21282 0 None 18 2 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL438374 220546 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCC[C@@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
11375759 70609 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 479 6 1 5 4.5 Cc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm049218c
CHEMBL180262 70609 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 479 6 1 5 4.5 Cc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm049218c
11444886 129408 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 497 6 1 5 4.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1C(F)(F)F 10.1021/jm049218c
CHEMBL308289 129408 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 497 6 1 5 4.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1C(F)(F)F 10.1021/jm049218c
CHEMBL360367 129408 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 497 6 1 5 4.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1C(F)(F)F 10.1021/jm049218c
11467552 179490 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 603 11 2 6 5.7 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL450471 179490 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 603 11 2 6 5.7 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
11282957 129111 1 None 1096 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2008.04.029
CHEMBL359894 129111 1 None 1096 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2008.04.029
44576644 195754 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 581 9 1 7 5.0 N[C@@H](Cn1c(=O)c(-c2ccc(COC(=O)C3CC3)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL508435 195754 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 581 9 1 7 5.0 N[C@@H](Cn1c(=O)c(-c2ccc(COC(=O)C3CC3)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44353285 124512 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 678 17 2 7 7.1 CCCCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL340156 124512 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 678 17 2 7 7.1 CCCCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL2371585 216877 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)N[C@@H](C)C(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44378834 103603 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1291 24 12 15 -0.1 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2cccnc2)NC1=O 10.1021/jm990115h
CHEMBL265169 103603 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1291 24 12 15 -0.1 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2cccnc2)NC1=O 10.1021/jm990115h
11455317 69662 0 None 851 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL178457 69662 0 None 851 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
11467552 179490 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 603 11 2 6 5.7 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL450471 179490 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 603 11 2 6 5.7 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44576680 180320 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 627 13 2 9 3.6 COc1cccc(-c2cn(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL453167 180320 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 627 13 2 9 3.6 COc1cccc(-c2cn(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
11167850 9518 28 None 6309 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1178 9518 28 None 6309 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1187 9518 28 None 6309 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL179691 9518 28 None 6309 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
11191675 70156 0 None 186 2 Human 8.4 pKi = 8.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL179600 70156 0 None 186 2 Human 8.4 pKi = 8.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL3085404 70156 0 None 186 2 Human 8.4 pKi = 8.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm049218c
11456285 195713 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 613 12 2 8 4.1 CS(=O)(=O)c1cccc(F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.bmcl.2008.04.036
CHEMBL508020 195713 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 613 12 2 8 4.1 CS(=O)(=O)c1cccc(F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.bmcl.2008.04.036
44379006 175733 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1257 22 13 15 -1.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CC(=O)NCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](C)NC1=O 10.1021/jm990115h
CHEMBL438899 175733 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1257 22 13 15 -1.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CC(=O)NCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](C)NC1=O 10.1021/jm990115h
11421518 172075 0 None 1047 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm701249f
CHEMBL423291 172075 0 None 1047 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm701249f
44449095 162288 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 581 9 1 6 6.2 CC[C@@H](Cn1c(=O)c(-c2cccc(OC)c2Cl)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
CHEMBL404180 162288 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 581 9 1 6 6.2 CC[C@@H](Cn1c(=O)c(-c2cccc(OC)c2Cl)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
25156942 195446 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 645 12 1 7 5.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@@H](c3ccccc3)N(C)CCCC(=O)O)c2=O)c1F 10.1021/jm8006454
CHEMBL503705 195446 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 645 12 1 7 5.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@@H](c3ccccc3)N(C)CCCC(=O)O)c2=O)c1F 10.1021/jm8006454
1179 7748 36 None -1 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity at rat GnRH receptor by competition binding assayBinding affinity at rat GnRH receptor by competition binding assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1021/jm701249f
9957278 7748 36 None -1 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity at rat GnRH receptor by competition binding assayBinding affinity at rat GnRH receptor by competition binding assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1021/jm701249f
CHEMBL494803 7748 36 None -1 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity at rat GnRH receptor by competition binding assayBinding affinity at rat GnRH receptor by competition binding assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1021/jm701249f
44353258 122858 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 650 14 1 7 7.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL335647 122858 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 650 14 1 7 7.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(01)00780-6
1179 7748 36 None -1 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity to rat gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to rat gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
9957278 7748 36 None -1 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity to rat gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to rat gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
CHEMBL494803 7748 36 None -1 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity to rat gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to rat gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
44267868 104851 0 None -10 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 933 10 1 14 7.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL273275 104851 0 None -10 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 933 10 1 14 7.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
11421518 172075 0 None 1047 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL423291 172075 0 None 1047 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
44388511 130445 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 515 6 1 5 5.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cc(F)ccc1C(F)(F)F 10.1021/jm049218c
CHEMBL362065 130445 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 515 6 1 5 5.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cc(F)ccc1C(F)(F)F 10.1021/jm049218c
9850211 195057 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 539 8 1 7 5.7 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCc4ccccn4)n3c2=O)c1 10.1021/jm0205402
CHEMBL50009 195057 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 539 8 1 7 5.7 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCc4ccccn4)n3c2=O)c1 10.1021/jm0205402
10886383 207686 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 582 11 0 7 5.7 Cc1c(-c2ccc(Oc3ccccc3)cc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
CHEMBL60153 207686 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 582 11 0 7 5.7 Cc1c(-c2ccc(Oc3ccccc3)cc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
44394901 73136 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 564 7 1 7 5.8 Cc1c(-c2csc(-c3ccccc3Cl)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL185154 73136 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 564 7 1 7 5.8 Cc1c(-c2csc(-c3ccccc3Cl)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44400246 74430 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 569 9 1 8 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)C(C)C)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL190671 74430 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 569 9 1 8 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)C(C)C)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
10886383 207686 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 582 11 0 7 5.7 Cc1c(-c2ccc(Oc3ccccc3)cc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL60153 207686 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 582 11 0 7 5.7 Cc1c(-c2ccc(Oc3ccccc3)cc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44436003 95505 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 619 9 0 7 5.0 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCCN1CCc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL236142 95505 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 619 9 0 7 5.0 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCCN1CCc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
44435980 153725 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 613 10 0 7 4.5 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(C(F)(F)F)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL392602 153725 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 613 10 0 7 4.5 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(C(F)(F)F)cc1)C2 10.1016/j.bmc.2007.05.029
11421518 172075 0 None 1047 2 Human 7.5 pKi = 7.5 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL423291 172075 0 None 1047 2 Human 7.5 pKi = 7.5 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
44309376 210884 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 600 13 1 9 5.4 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CC#N)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL70276 210884 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 600 13 1 9 5.4 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CC#N)cc1 10.1016/s0960-894x(02)00370-0
10929801 108714 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 564 11 0 9 4.2 COCCN(C)Cc1c(C(C)(C)C(=O)OC)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
CHEMBL301103 108714 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 564 11 0 9 4.2 COCCN(C)Cc1c(C(C)(C)C(=O)OC)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
44346349 120747 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 679 12 2 8 6.5 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)CCCN)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL332616 120747 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 679 12 2 8 6.5 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)CCCN)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44435976 95271 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 601 10 0 7 4.8 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(C(C)(C)C)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL235050 95271 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 601 10 0 7 4.8 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(C(C)(C)C)cc1)C2 10.1016/j.bmc.2007.05.029
21047805 121227 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 588 10 2 7 7.0 COc1cc(OC)nc(NCC2CCC(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)CC2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL333349 121227 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 588 10 2 7 7.0 COc1cc(OC)nc(NCC2CCC(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)CC2)n1 10.1016/s0960-894x(02)00756-4
11167850 9518 28 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
1178 9518 28 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
1187 9518 28 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
CHEMBL179691 9518 28 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
11167850 9518 28 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat gonadotropin-releasing hormone receptorBinding affinity for rat gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1178 9518 28 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat gonadotropin-releasing hormone receptorBinding affinity for rat gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1187 9518 28 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat gonadotropin-releasing hormone receptorBinding affinity for rat gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL179691 9518 28 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat gonadotropin-releasing hormone receptorBinding affinity for rat gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
9825757 116935 0 None -12 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 465 6 2 3 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(=O)O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL323687 116935 0 None -12 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 465 6 2 3 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(=O)O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44394893 136448 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 469 6 2 8 3.1 Cc1c(-c2csc(N)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL367369 136448 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 469 6 2 8 3.1 Cc1c(-c2csc(N)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44451418 175496 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1620 32 9 19 8.2 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccccc2C#CCNC(=O)[C@H](C)NC(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL436878 175496 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1620 32 9 19 8.2 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccccc2C#CCNC(=O)[C@H](C)NC(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44309522 103301 0 None - 1 Human 4.5 pKi = 4.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 476 8 1 7 4.3 CCCC(=O)Nc1ccc(-c2cn3c(=O)c(C(=O)OCC)cn(Cc4ccccc4F)c3n2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL262787 103301 0 None - 1 Human 4.5 pKi = 4.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 476 8 1 7 4.3 CCCC(=O)Nc1ccc(-c2cn3c(=O)c(C(=O)OCC)cn(Cc4ccccc4F)c3n2)cc1 10.1016/s0960-894x(02)00370-0
44435991 153733 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 579 10 0 8 4.7 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3ccccc3)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
CHEMBL392607 153733 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 579 10 0 8 4.7 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3ccccc3)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
44352652 124262 0 None 245 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 689 14 0 9 7.6 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC4CCCC4)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL339968 124262 0 None 245 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 689 14 0 9 7.6 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC4CCCC4)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL2371532 216852 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371584 216876 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44340825 174860 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 519 9 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL432585 174860 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 519 9 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44400255 141508 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 577 7 1 7 4.5 CS(=O)(=O)c1cccc(C(F)(F)F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2005.03.057
CHEMBL371855 141508 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 577 7 1 7 4.5 CS(=O)(=O)c1cccc(C(F)(F)F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2005.03.057
44340808 117344 0 None - 1 Human 7.5 pKi = 7.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 532 8 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H]3CCCN3Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL325326 117344 0 None - 1 Human 7.5 pKi = 7.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 532 8 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H]3CCCN3Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44593615 181400 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 631 12 1 8 5.3 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL455769 181400 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 631 12 1 8 5.3 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44353200 27741 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 676 13 2 7 6.8 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NC4CCCCC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL131127 27741 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 676 13 2 7 6.8 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NC4CCCCC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
44593615 181400 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 631 12 1 8 5.3 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL455769 181400 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 631 12 1 8 5.3 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
10995320 194949 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 562 11 0 8 5.4 CCCCN(C)Cc1c(C(C)(C)C(=O)OC)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
CHEMBL49872 194949 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 562 11 0 8 5.4 CCCCN(C)Cc1c(C(C)(C)C(=O)OC)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
11785958 93814 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3OC)c2=O)c1 10.1021/jm030472z
CHEMBL23256 93814 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3OC)c2=O)c1 10.1021/jm030472z
11785958 93814 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23256 93814 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
44327851 118225 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL 872 11 9 8 3.3 CC[C@H](C)[C@@H]1NC(=O)CSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]([C@@H](C)CC)NC1=O 10.1021/jm990432o
CHEMBL327529 118225 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL 872 11 9 8 3.3 CC[C@H](C)[C@@H]1NC(=O)CSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]([C@@H](C)CC)NC1=O 10.1021/jm990432o
11180219 117998 0 None -112 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL326504 117998 0 None -112 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
11226531 106296 0 None -169 2 Rat 5.5 pKi = 5.5 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
CHEMBL283381 106296 0 None -169 2 Rat 5.5 pKi = 5.5 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
44451331 166660 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 556 8 1 6 4.8 NC(CC1CCCCC1)Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.09.026
CHEMBL410680 166660 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 556 8 1 6 4.8 NC(CC1CCCCC1)Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.09.026
21048462 117094 0 None -60 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 522 5 1 4 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=O)OC(C)(C)C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL323863 117094 0 None -60 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 522 5 1 4 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=O)OC(C)(C)C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44352657 28323 0 None 269 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 687 12 0 9 7.3 CN(CCc1ccccn1)Cc1c(-c2ccc(OC3CCCC3)cc2)c(C#N)c2n(Cc3ccccc3F)cc(C(=O)OC3CCCC3)c(=O)n12 10.1016/s0960-894x(01)00779-x
CHEMBL131665 28323 0 None 269 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 687 12 0 9 7.3 CN(CCc1ccccn1)Cc1c(-c2ccc(OC3CCCC3)cc2)c(C#N)c2n(Cc3ccccc3F)cc(C(=O)OC3CCCC3)c(=O)n12 10.1016/s0960-894x(01)00779-x
24857895 162099 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 551 8 1 6 5.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL403081 162099 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 551 8 1 6 5.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
44394768 131161 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 605 10 2 10 5.2 COc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1OC 10.1016/j.bmcl.2004.07.022
CHEMBL363900 131161 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 605 10 2 10 5.2 COc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1OC 10.1016/j.bmcl.2004.07.022
11490288 175426 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL436276 175426 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL75439 175426 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1Cl 10.1016/j.bmcl.2004.02.004
44587392 177321 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 631 13 2 7 5.7 N[C@@H](Cn1c(=O)c(-c2cccc(OCCCCCC(=O)O)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL444989 177321 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 631 13 2 7 5.7 N[C@@H](Cn1c(=O)c(-c2cccc(OCCCCCC(=O)O)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
21045805 20556 0 None -5 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL119546 20556 0 None -5 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
21045829 120175 0 None 1 2 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4nccc(NCC5CCCO5)n4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331855 120175 0 None 1 2 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4nccc(NCC5CCCO5)n4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44340771 16487 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 519 9 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL113216 16487 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 519 9 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44451398 175474 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1676 34 9 19 9.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccccc2C#CCNC(=O)[C@@H](NC(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)C(C)C)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL436697 175474 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1676 34 9 19 9.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccccc2C#CCNC(=O)[C@@H](NC(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)C(C)C)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
9958318 97002 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL23830 97002 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44577096 185519 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 524 10 0 7 3.7 COc1cccc(-c2c(F)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm701249f
CHEMBL468546 185519 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 524 10 0 7 3.7 COc1cccc(-c2c(F)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm701249f
9958318 97002 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23830 97002 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
44394649 136950 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 8 1 8 5.2 Cc1c(-c2csc(N(C)c3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL367812 136950 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 8 1 8 5.2 Cc1c(-c2csc(N(C)c3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
9958318 97002 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm049791w
CHEMBL23830 97002 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm049791w
9958318 97002 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23830 97002 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
9892420 209920 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity was determined towards human Gonadotropin-releasing hormone receptorBinding affinity was determined towards human Gonadotropin-releasing hormone receptor
ChEMBL 506 10 1 7 3.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3ccccn3)c2=O)c1 10.1021/jm034041s
CHEMBL64148 209920 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity was determined towards human Gonadotropin-releasing hormone receptorBinding affinity was determined towards human Gonadotropin-releasing hormone receptor
ChEMBL 506 10 1 7 3.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3ccccn3)c2=O)c1 10.1021/jm034041s
44587391 179345 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 617 12 2 7 5.4 N[C@@H](Cn1c(=O)c(-c2cccc(OCCCCC(=O)O)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL448656 179345 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 617 12 2 7 5.4 N[C@@H](Cn1c(=O)c(-c2cccc(OCCCCC(=O)O)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
9958318 97002 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1016/j.bmcl.2004.11.026
CHEMBL23830 97002 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1016/j.bmcl.2004.11.026
11352834 95966 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 516 10 0 6 4.5 C=Cc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
CHEMBL23673 95966 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 516 10 0 6 4.5 C=Cc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
44394614 73716 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 9 2 8 5.1 Cc1c(-c2csc(NCc3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL186646 73716 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 9 2 8 5.1 Cc1c(-c2csc(NCc3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
11272935 138565 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 6 1 5 4.2 Cc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL369326 138565 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 6 1 5 4.2 Cc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL75954 138565 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 6 1 5 4.2 Cc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
44435829 95362 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 559 10 0 7 3.8 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
CHEMBL235520 95362 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 559 10 0 7 3.8 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
44587402 179484 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 674 14 2 8 5.1 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCN(C)CC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL450414 179484 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 674 14 2 8 5.1 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCN(C)CC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
21047518 22222 0 None 10 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 6 7.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4cc(Cl)nc(N)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121551 22222 0 None 10 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 6 7.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4cc(Cl)nc(N)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11145953 190779 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 539 10 1 7 5.2 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)CNCCc4ccccn4)cn3c2=O)c1 10.1021/jm0205402
CHEMBL48193 190779 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 539 10 1 7 5.2 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)CNCCc4ccccn4)cn3c2=O)c1 10.1021/jm0205402
CHEMBL2371565 216866 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)N[C@@H](C)C(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44309576 109045 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 619 15 1 9 5.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCOC)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL303260 109045 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 619 15 1 9 5.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCOC)cc1 10.1016/s0960-894x(02)00370-0
10919052 120296 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL332138 120296 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44387988 138623 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 530 7 1 8 3.4 COc1cccc(-n2c(=O)n(Cc3c(Cl)cccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL369453 138623 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 530 7 1 8 3.4 COc1cccc(-n2c(=O)n(Cc3c(Cl)cccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44267866 103887 0 None -4 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CC(C)OC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL267568 103887 0 None -4 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CC(C)OC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44346260 121602 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 665 11 2 8 6.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)CCN)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL334148 121602 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 665 11 2 8 6.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)CCN)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
11225384 135283 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm701249f
CHEMBL366701 135283 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm701249f
11225384 135283 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL366701 135283 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2005.05.038
11225384 135283 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2004.11.026
CHEMBL366701 135283 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2004.11.026
11375912 91998 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 524 9 0 6 4.5 Cc1c(-c2cccc(Cl)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL22559 91998 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 524 9 0 6 4.5 Cc1c(-c2cccc(Cl)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
11260648 174816 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3)c2=O)c1 10.1021/jm030472z
CHEMBL432262 174816 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3)c2=O)c1 10.1021/jm030472z
11260648 174816 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL432262 174816 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44309372 210642 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 677 13 0 10 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cc(OC)c(OC)c(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL68698 210642 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 677 13 0 10 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cc(OC)c(OC)c(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44347004 22221 0 None -13 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121535 22221 0 None -13 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44352933 28265 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2ccc(F)cc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL131589 28265 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2ccc(F)cc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44576657 195026 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 587 10 2 7 4.9 N[C@@H](Cn1c(=O)c(-c2ccc(CSCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL499589 195026 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 587 10 2 7 4.9 N[C@@H](Cn1c(=O)c(-c2ccc(CSCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
11005990 96698 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 9 0 8 3.6 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL23797 96698 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 9 0 8 3.6 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
11005990 96698 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 534 9 0 8 3.6 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL23797 96698 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 534 9 0 8 3.6 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44587404 195819 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 661 14 2 8 5.2 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCOCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL509347 195819 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 661 14 2 8 5.2 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCOCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
44267868 104851 0 None -10 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 933 10 1 14 7.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273275 104851 0 None -10 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 933 10 1 14 7.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44435990 103281 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 585 10 0 8 5.2 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3CC3CCCCC3)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
CHEMBL262580 103281 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 585 10 0 8 5.2 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3CC3CCCCC3)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
44451342 103240 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 898 20 4 10 6.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL262334 103240 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 898 20 4 10 6.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21047518 22222 0 None -10 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 6 7.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4cc(Cl)nc(N)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121551 22222 0 None -10 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 6 7.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4cc(Cl)nc(N)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44390795 128956 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 539 7 2 7 2.8 NC(Cc1c[nH]c2ccccc12)Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2c(F)cccc2F)c1=O 10.1016/j.bmcl.2004.11.026
CHEMBL359741 128956 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 539 7 2 7 2.8 NC(Cc1c[nH]c2ccccc12)Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2c(F)cccc2F)c1=O 10.1016/j.bmcl.2004.11.026
11113778 209901 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 495 10 2 7 2.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3c[nH]cn3)c2=O)c1 10.1021/jm034041s
CHEMBL64066 209901 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 495 10 2 7 2.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3c[nH]cn3)c2=O)c1 10.1021/jm034041s
9891852 16867 1 None -23 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL115482 16867 1 None -23 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
11178994 17174 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)CC(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL116259 17174 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)CC(C)C)c2=O)c1F 10.1021/jm049218c
11178994 17174 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)CC(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL116259 17174 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)CC(C)C)c2=O)c1F 10.1021/jm049791w
44593614 195041 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 570 10 3 7 3.8 N[C@@H](Cn1c(=O)c(-c2ccc(CNCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL499849 195041 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 570 10 3 7 3.8 N[C@@H](Cn1c(=O)c(-c2ccc(CNCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44593614 195041 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 570 10 3 7 3.8 N[C@@H](Cn1c(=O)c(-c2ccc(CNCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL499849 195041 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 570 10 3 7 3.8 N[C@@H](Cn1c(=O)c(-c2ccc(CNCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
11226531 106296 0 None 169 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
CHEMBL283381 106296 0 None 169 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
44353228 26861 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 622 12 1 7 6.9 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(C)=O)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL130400 26861 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 622 12 1 7 6.9 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(C)=O)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
44400187 142061 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 551 6 1 5 5.6 N[C@@H](Cn1c(=O)c(-c2ccccc2C(F)(F)F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL372680 142061 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 551 6 1 5 5.6 N[C@@H](Cn1c(=O)c(-c2ccccc2C(F)(F)F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
11444886 129408 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 497 6 1 5 4.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1C(F)(F)F 10.1016/j.bmcl.2004.02.004
CHEMBL308289 129408 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 497 6 1 5 4.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1C(F)(F)F 10.1016/j.bmcl.2004.02.004
CHEMBL360367 129408 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 497 6 1 5 4.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1C(F)(F)F 10.1016/j.bmcl.2004.02.004
10649568 21338 0 None -10 2 Rat 8.4 pKi = 8.4 Binding
Binding affinity towards rat Gonadotropin-releasing hormone receptorBinding affinity towards rat Gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/s0960-894x(03)00746-7
CHEMBL120432 21338 0 None -10 2 Rat 8.4 pKi = 8.4 Binding
Binding affinity towards rat Gonadotropin-releasing hormone receptorBinding affinity towards rat Gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/s0960-894x(03)00746-7
9983568 105758 0 None 263 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL279885 105758 0 None 263 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
11283954 20868 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 529 8 0 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C3CCCCC3)N(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL119774 20868 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 529 8 0 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C3CCCCC3)N(C)C)c2=O)c1F 10.1021/jm049791w
44346667 120520 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL332355 120520 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
44587393 179413 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 613 12 2 7 5.5 Cc1c(-c2cccc(OCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL449468 179413 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 613 12 2 7 5.5 Cc1c(-c2cccc(OCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
10995569 108461 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 597 10 0 9 5.1 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1ccccn1 10.1021/jm0205402
CHEMBL299348 108461 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 597 10 0 9 5.1 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1ccccn1 10.1021/jm0205402
44449156 161823 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 565 9 1 6 5.7 CC[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
CHEMBL401632 161823 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 565 9 1 6 5.7 CC[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
CHEMBL2371583 216875 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)NCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371479 216831 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H]1NC(=O)CC[C@@H]2NC(=O)[C@@H](NC(=O)[C@@H](Cc3cccnc3)NC(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(C)=O)CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CCNC1=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC2=O 10.1021/jm990115h
25156944 195891 1 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 645 12 1 8 5.6 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1021/jm8006454
CHEMBL510285 195891 1 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 645 12 1 8 5.6 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1021/jm8006454
44577098 185303 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 539 8 1 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3[S+](C)[O-])c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL466730 185303 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 539 8 1 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3[S+](C)[O-])c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
44267810 104867 0 None 5 2 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 939 12 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273387 104867 0 None 5 2 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 939 12 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11214614 196208 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 523 6 1 7 4.9 COc1cccc(-c2c3n(c(=O)n(C[C@H](N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1Cl 10.1021/jm701249f
CHEMBL513346 196208 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 523 6 1 7 4.9 COc1cccc(-c2c3n(c(=O)n(C[C@H](N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1Cl 10.1021/jm701249f
10051739 92208 0 None 501 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL22653 92208 0 None 501 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
10051739 92208 0 None 501 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL22653 92208 0 None 501 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
44449682 102821 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 533 8 1 6 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1 10.1016/j.bmcl.2008.04.029
CHEMBL259907 102821 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 533 8 1 6 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1 10.1016/j.bmcl.2008.04.029
10051739 92208 0 None 501 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL22653 92208 0 None 501 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm049791w
22716581 129301 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 523 6 1 7 4.9 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1Cl 10.1016/j.bmcl.2005.01.009
CHEMBL360126 129301 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 523 6 1 7 4.9 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1Cl 10.1016/j.bmcl.2005.01.009
44432638 93559 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 506 9 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232151 93559 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 506 9 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
11490509 70138 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 507 6 1 5 4.6 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Br 10.1021/jm049218c
CHEMBL179531 70138 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 507 6 1 5 4.6 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Br 10.1021/jm049218c
9986320 108211 9 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human Gonadotropin-releasing hormone receptorBinding affinity to human Gonadotropin-releasing hormone receptor
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1021/jm0205402
CHEMBL297491 108211 9 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human Gonadotropin-releasing hormone receptorBinding affinity to human Gonadotropin-releasing hormone receptor
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1021/jm0205402
9986320 108211 9 None - 1 Human 8.3 pKi = 8.3 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL297491 108211 9 None - 1 Human 8.3 pKi = 8.3 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL2371555 216860 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)N[C@@H](C(=O)N[C@@H]2CC(=O)N[C@H](C(=O)O)CNC(=O)[C@@H]3CCCN3C(=O)[C@@H]3CCCCNC(=O)CC[C@H](NC2=O)C(=O)N[C@H](Cc2ccc4ccccc4c2)C(=O)N[C@@H](CC(C)C)C(=O)N3)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
10394119 121225 0 None 1 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards rat pituitary Gonadotropin-releasing hormone receptorBinding affinity towards rat pituitary Gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333345 121225 0 None 1 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards rat pituitary Gonadotropin-releasing hormone receptorBinding affinity towards rat pituitary Gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44432646 154012 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 581 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCC2CCOCC2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL392843 154012 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 581 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCC2CCOCC2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44587395 179407 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 617 11 2 7 5.3 Cc1c(-c2cccc(OCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL449373 179407 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 617 11 2 7 5.3 Cc1c(-c2cccc(OCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
10394119 121225 0 None 1 2 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333345 121225 0 None 1 2 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
9809382 107451 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 628 11 2 8 5.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL292291 107451 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 628 11 2 8 5.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL216633 216113 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NC[C@@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44449683 164092 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 517 9 2 7 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL407719 164092 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 517 9 2 7 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
44577099 185521 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 507 6 1 7 4.4 COc1cccc(-c2c3n(c(=O)n(C[C@H](N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1F 10.1021/jm701249f
CHEMBL468552 185521 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 507 6 1 7 4.4 COc1cccc(-c2c3n(c(=O)n(C[C@H](N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1F 10.1021/jm701249f
9891852 103053 1 None 13 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
CHEMBL261145 103053 1 None 13 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
22716552 130548 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 507 6 1 7 4.4 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1F 10.1016/j.bmcl.2005.01.009
CHEMBL362237 130548 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 507 6 1 7 4.4 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1F 10.1016/j.bmcl.2005.01.009
9891852 17828 1 None 18 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117736 17828 1 None 18 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
9891852 103053 1 None 13 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL261145 103053 1 None 13 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21045829 120175 0 None -1 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4nccc(NCC5CCCO5)n4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331855 120175 0 None -1 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4nccc(NCC5CCCO5)n4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
9891852 103053 1 None 13 2 Human 7.4 pKi = 7.4 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/j.bmc.2007.09.026
CHEMBL261145 103053 1 None 13 2 Human 7.4 pKi = 7.4 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/j.bmc.2007.09.026
44352607 27422 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 607 11 0 9 5.5 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC(C)C)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
CHEMBL130855 27422 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 607 11 0 9 5.5 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC(C)C)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
44352678 122012 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2ccc(F)cc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL334729 122012 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2ccc(F)cc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
10908122 191052 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 597 10 0 9 5.1 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1cccnc1 10.1021/jm0205402
CHEMBL48389 191052 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 597 10 0 9 5.1 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1cccnc1 10.1021/jm0205402
11027376 92004 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 490 9 0 6 3.9 Cc1c(-c2ccccc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL22563 92004 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 490 9 0 6 3.9 Cc1c(-c2ccccc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
11168330 106175 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3C)c2=O)c1 10.1021/jm030472z
CHEMBL282707 106175 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3C)c2=O)c1 10.1021/jm030472z
44353238 25309 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 553 10 0 7 5.8 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL127502 25309 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 553 10 0 7 5.8 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
11168330 106175 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3C)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL282707 106175 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3C)c2=O)c1 10.1016/s0960-894x(03)00619-x
11027376 92004 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 490 9 0 6 3.9 Cc1c(-c2ccccc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL22563 92004 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 490 9 0 6 3.9 Cc1c(-c2ccccc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44451399 175499 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1715 30 6 20 10.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3cccc(C#CCNC(=O)C4CCN(C(=O)CN(Cc5ccccc5)Cc5c(-c6ccc(NC(=O)NCC)cc6)nc6n(Cc7c(F)cccc7F)cc(C(=O)OCC)c(=O)n56)CC4)c3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL436906 175499 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1715 30 6 20 10.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3cccc(C#CCNC(=O)C4CCN(C(=O)CN(Cc5ccccc5)Cc5c(-c6ccc(NC(=O)NCC)cc6)nc6n(Cc7c(F)cccc7F)cc(C(=O)OCC)c(=O)n56)CC4)c3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL2370259 216600 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None None 10.1021/jm990432o
44309357 104864 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 651 13 1 8 6.9 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00370-0
CHEMBL273358 104864 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 651 13 1 8 6.9 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00370-0
44390780 70267 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 508 6 1 10 2.2 N[C@@H](Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2ccc3nsnc3c2)c1=O)c1ccccc1 10.1016/j.bmcl.2004.11.026
CHEMBL179953 70267 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 508 6 1 10 2.2 N[C@@H](Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2ccc3nsnc3c2)c1=O)c1ccccc1 10.1016/j.bmcl.2004.11.026
11455317 69662 0 None 851 2 Human 7.4 pKi = 7.4 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL178457 69662 0 None 851 2 Human 7.4 pKi = 7.4 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
44576681 200362 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 553 11 2 6 4.9 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL526887 200362 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 553 11 2 6 4.9 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44353271 29340 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 580 10 1 7 5.7 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(C)=O)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL132616 29340 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 580 10 1 7 5.7 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(C)=O)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
44394767 132981 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 575 9 2 9 5.2 COc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
CHEMBL365001 132981 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 575 9 2 9 5.2 COc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
44394894 175648 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 548 7 1 7 5.3 Cc1c(-c2csc(-c3ccc(F)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL438201 175648 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 548 7 1 7 5.3 Cc1c(-c2csc(-c3ccc(F)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
9873729 18143 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 613 12 0 7 6.9 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3ccc(OCC(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL117977 18143 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 613 12 0 7 6.9 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3ccc(OCC(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00745-x
86276161 116630 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Displacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cellsDisplacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 441 6 1 7 4.8 COc1nc(F)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1016/j.bmcl.2014.02.002
CHEMBL3233520 116630 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Displacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cellsDisplacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 441 6 1 7 4.8 COc1nc(F)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1016/j.bmcl.2014.02.002
21047858 16860 0 None 17 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CN)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL115425 16860 0 None 17 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CN)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
9828154 70643 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 523 10 0 9 2.1 COc1cccc(-n2c(=O)n(CCN(C)CCc3ccccn3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2004.11.026
CHEMBL180352 70643 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 523 10 0 9 2.1 COc1cccc(-n2c(=O)n(CCN(C)CCc3ccccn3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2004.11.026
44352747 28859 0 None - 1 Human 4.4 pKi = 4.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 560 10 0 8 5.5 CCOC(=O)c1cn(Cc2ccccc2)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL132179 28859 0 None - 1 Human 4.4 pKi = 4.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 560 10 0 8 5.5 CCOC(=O)c1cn(Cc2ccccc2)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00779-x
44267905 105140 0 None 13 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275251 105140 0 None 13 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44346348 121131 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 665 10 2 8 6.1 C[C@H](N)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL333103 121131 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 665 10 2 8 6.1 C[C@H](N)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
11477988 97785 0 None 954 2 Human 7.4 pKi = 7.4 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
CHEMBL23969 97785 0 None 954 2 Human 7.4 pKi = 7.4 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
11092567 108275 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 520 9 0 7 5.0 COCCN(C)Cc1c(C(C)(C)C)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
CHEMBL297938 108275 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 520 9 0 7 5.0 COCCN(C)Cc1c(C(C)(C)C)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
11103551 108455 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 544 8 1 6 6.6 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCC4CCCCC4)n3c2=O)c1 10.1021/jm0205402
CHEMBL299320 108455 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 544 8 1 6 6.6 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCC4CCCCC4)n3c2=O)c1 10.1021/jm0205402
44340632 16293 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNC3CCCC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112188 16293 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNC3CCCC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44312806 18093 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 433 6 1 6 3.8 Cc1ccc(Cn2c(C)c(-c3ccccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)o1 10.1016/j.bmcl.2004.02.004
CHEMBL1179388 18093 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 433 6 1 6 3.8 Cc1ccc(Cn2c(C)c(-c3ccccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)o1 10.1016/j.bmcl.2004.02.004
CHEMBL73454 18093 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 433 6 1 6 3.8 Cc1ccc(Cn2c(C)c(-c3ccccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)o1 10.1016/j.bmcl.2004.02.004
44353247 122839 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 608 11 1 7 6.4 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL335610 122839 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 608 11 1 7 6.4 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
21047516 22118 0 None -1 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 595 12 3 7 6.9 COCCNc1nccc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL121412 22118 0 None -1 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 595 12 3 7 6.9 COCCNc1nccc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
44353247 122839 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 608 11 1 7 6.4 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.09.026
CHEMBL335610 122839 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 608 11 1 7 6.4 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.09.026
44353265 29097 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 644 17 2 7 6.0 CCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)CCN(CC)CC)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL132392 29097 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 644 17 2 7 6.0 CCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)CCN(CC)CC)n2c1=O 10.1016/s0960-894x(01)00780-6
21045834 23217 0 None -3 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4ncccn4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL123301 23217 0 None -3 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4ncccn4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11250647 8327 46 None -117 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
5293 8327 46 None -117 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
8362 8327 46 None -117 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
CHEMBL1208155 8327 46 None -117 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
DB11979 8327 46 None -117 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
44451406 103357 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 530 9 0 6 4.6 CC(CCN1CCc2c(c(=O)n(CCN3CCCCC3)c(=O)n2Cc2c(F)cccc2F)C1)CC(C)(C)C 10.1016/j.bmc.2007.09.026
CHEMBL263118 103357 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 530 9 0 6 4.6 CC(CCN1CCc2c(c(=O)n(CCN3CCCCC3)c(=O)n2Cc2c(F)cccc2F)C1)CC(C)(C)C 10.1016/j.bmc.2007.09.026
11282957 129111 1 None 1096 2 Human 7.4 pKi = 7.4 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
CHEMBL359894 129111 1 None 1096 2 Human 7.4 pKi = 7.4 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
44436018 153843 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 550 8 1 6 4.5 CN[C@@H](Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2)c1ccccc1 10.1016/j.bmc.2007.05.029
CHEMBL392709 153843 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 550 8 1 6 4.5 CN[C@@H](Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2)c1ccccc1 10.1016/j.bmc.2007.05.029
44353305 26596 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 568 10 0 8 5.7 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc([N+](=O)[O-])cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL130195 26596 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 568 10 0 8 5.7 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc([N+](=O)[O-])cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL405918 219365 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
11261195 70480 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL180124 70480 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
11261195 70480 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL180124 70480 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049791w
11386605 96969 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL23823 96969 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11786039 92556 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 540 9 0 6 5.0 Cc1c(-c2ccc3ccccc3c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL22937 92556 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 540 9 0 6 5.0 Cc1c(-c2ccc3ccccc3c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
11386605 96969 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23823 96969 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccn3)c2=O)c1 10.1021/jm030472z
44346649 120343 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 589 7 1 9 4.5 O=c1c2c(CN3CCNCC3)c(-c3ccc([N+](=O)[O-])cc3)sc2n(Cc2c(F)cccc2F)c(=O)n1-c1ccccc1 10.1016/s0960-894x(03)00746-7
CHEMBL332194 120343 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 589 7 1 9 4.5 O=c1c2c(CN3CCNCC3)c(-c3ccc([N+](=O)[O-])cc3)sc2n(Cc2c(F)cccc2F)c(=O)n1-c1ccccc1 10.1016/s0960-894x(03)00746-7
44389571 69923 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 471 6 1 6 4.1 COc1cccc(-c2c3n(c(=O)n(C[C@H](N)c4ccccc4)c2=O)C(c2ccccc2)CC3)c1F 10.1016/j.bmcl.2005.01.009
CHEMBL178961 69923 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 471 6 1 6 4.1 COc1cccc(-c2c3n(c(=O)n(C[C@H](N)c4ccccc4)c2=O)C(c2ccccc2)CC3)c1F 10.1016/j.bmcl.2005.01.009
44267903 169012 0 None -3 2 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 906 10 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCN(C)C2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL416337 169012 0 None -3 2 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 906 10 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCN(C)C2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44394779 73842 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 598 7 1 7 6.2 Cc1c(-c2csc(-c3ccc(C(F)(F)F)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL187243 73842 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 598 7 1 7 6.2 Cc1c(-c2csc(-c3ccc(C(F)(F)F)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44309559 109739 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 616 9 0 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL306431 109739 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 616 9 0 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00371-2
44309559 109739 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 616 9 0 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.09.026
CHEMBL306431 109739 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 616 9 0 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.09.026
44340656 117254 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL324759 117254 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44340652 16227 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1021/jm701249f
CHEMBL111820 16227 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1021/jm701249f
11238459 96315 1 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 570 9 0 8 4.2 Cc1c(-c2ccc3c(c2)OC(F)(F)O3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL23737 96315 1 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 570 9 0 8 4.2 Cc1c(-c2ccc3c(c2)OC(F)(F)O3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
44432645 93977 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 487 5 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CN)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232752 93977 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 487 5 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CN)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44267906 174271 0 None -9 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL429949 174271 0 None -9 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
10983989 208452 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 506 9 1 7 3.6 Cc1c(-c2cccc(O)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL60618 208452 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 506 9 1 7 3.6 Cc1c(-c2cccc(O)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44451276 102816 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1635 32 8 20 9.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccc(C#CCNC(=O)[C@H](C)NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL259878 102816 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1635 32 8 20 9.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccc(C#CCNC(=O)[C@H](C)NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
11284264 91530 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 550 11 0 8 3.9 COc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1OC 10.1021/jm030472z
CHEMBL22300 91530 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 550 11 0 8 3.9 COc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1OC 10.1021/jm030472z
10907714 209940 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 546 9 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN3CCC[C@@H]3Cc3ccccn3)c2=O)c1 10.1021/jm034041s
CHEMBL64212 209940 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 546 9 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN3CCC[C@@H]3Cc3ccccn3)c2=O)c1 10.1021/jm034041s
11124671 209963 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 574 10 0 7 4.8 Cc1c(-c2cccc(OC(F)(F)F)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL64273 209963 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 574 10 0 7 4.8 Cc1c(-c2cccc(OC(F)(F)F)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44394608 73837 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 8 2 8 5.5 Cc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
CHEMBL187217 73837 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 8 2 8 5.5 Cc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
44394841 172741 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 562 7 1 7 5.6 Cc1ccc(-c2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1F 10.1016/j.bmcl.2004.07.022
CHEMBL425178 172741 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 562 7 1 7 5.6 Cc1ccc(-c2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1F 10.1016/j.bmcl.2004.07.022
CHEMBL412504 219778 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CC(=O)NCC(=O)NC[C@@H]2NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm990116+
11124921 198579 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 612 10 1 9 5.5 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1ccccc1O 10.1021/jm0205402
CHEMBL51983 198579 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 612 10 1 9 5.5 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1ccccc1O 10.1021/jm0205402
44436010 96137 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 599 8 0 7 4.8 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(Cc5ccccn5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL236967 96137 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 599 8 0 7 4.8 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(Cc5ccccn5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44352957 123510 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 600 11 0 10 4.8 CCOC(=O)c1cn(Cc2ccccc2C#N)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL337433 123510 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 600 11 0 10 4.8 CCOC(=O)c1cn(Cc2ccccc2C#N)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11214860 91546 0 None -323 2 Rat 5.3 pKi = 5.3 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
CHEMBL22314 91546 0 None -323 2 Rat 5.3 pKi = 5.3 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
11191675 70156 0 None 186 2 Human 8.3 pKi = 8.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL179600 70156 0 None 186 2 Human 8.3 pKi = 8.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL3085404 70156 0 None 186 2 Human 8.3 pKi = 8.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
44340637 16351 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/j.bmcl.2004.07.022
CHEMBL112466 16351 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/j.bmcl.2004.07.022
44340652 16227 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL111820 16227 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
17757566 95317 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 573 10 0 7 4.1 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL235270 95317 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 573 10 0 7 4.1 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
17757565 153732 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 593 10 0 7 4.4 Cc1cc(Cl)ccc1CN1CCc2c(c(=O)n(CCN(C)CCc3ccccn3)c(=O)n2Cc2c(F)cccc2F)C1 10.1016/j.bmc.2007.05.029
CHEMBL392605 153732 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 593 10 0 7 4.4 Cc1cc(Cl)ccc1CN1CCc2c(c(=O)n(CCN(C)CCc3ccccn3)c(=O)n2Cc2c(F)cccc2F)C1 10.1016/j.bmc.2007.05.029
44387972 70650 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 514 7 1 8 2.8 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL180372 70650 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 514 7 1 8 2.8 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
11214294 128973 0 None 912 2 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL359754 128973 0 None 912 2 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
44340749 115895 0 None - 1 Human 8.3 pKi = 8.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL321376 115895 0 None - 1 Human 8.3 pKi = 8.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
9829468 195546 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 567 9 0 7 6.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)CCc4ccccn4)n3c2=O)c1 10.1021/jm0205402
CHEMBL50546 195546 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 567 9 0 7 6.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)CCc4ccccn4)n3c2=O)c1 10.1021/jm0205402
44340749 115895 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1021/jm701249f
CHEMBL321376 115895 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1021/jm701249f
9829468 195546 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 567 9 0 7 6.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)CCc4ccccn4)n3c2=O)c1 10.1021/jm701249f
CHEMBL50546 195546 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 567 9 0 7 6.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)CCc4ccccn4)n3c2=O)c1 10.1021/jm701249f
CHEMBL2371542 216858 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44434414 95301 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 709 14 3 9 4.6 C#CCNC(=O)CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCC)cc2)nc2n(Cc3c(F)cccc3F)cc(C(=O)OCC)c(=O)n12 10.1016/j.bmc.2007.04.065
CHEMBL235179 95301 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 709 14 3 9 4.6 C#CCNC(=O)CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCC)cc2)nc2n(Cc3c(F)cccc3F)cc(C(=O)OCC)c(=O)n12 10.1016/j.bmc.2007.04.065
44267906 174271 0 None 9 2 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL429949 174271 0 None 9 2 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44399944 75410 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL191817 75410 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
44399944 75410 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
44399944 75410 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL191817 75410 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL191817 75410 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
44399944 75410 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL191817 75410 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
44340637 16351 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL112466 16351 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44340637 16351 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1021/jm701249f
CHEMBL112466 16351 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1021/jm701249f
44340637 16351 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/j.bmcl.2005.01.009
CHEMBL112466 16351 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/j.bmcl.2005.01.009
11156980 69367 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 505 7 1 7 4.0 CN[C@@H](Cn1c(=O)c(-c2ccc3c(c2)OCO3)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL178281 69367 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 505 7 1 7 4.0 CN[C@@H](Cn1c(=O)c(-c2ccc3c(c2)OCO3)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
11374717 129073 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL359810 129073 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL419270 129073 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
44399944 75410 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL191817 75410 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
44432639 93738 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 536 10 2 4 5.8 COc1ccccc1CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
CHEMBL232356 93738 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 536 10 2 4 5.8 COc1ccccc1CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
44267887 105257 0 None -41 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 967 10 1 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275935 105257 0 None -41 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 967 10 1 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL414275 219898 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CSSC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44353249 175224 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 659 17 1 8 6.8 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCN(CC)CC)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL434995 175224 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 659 17 1 8 6.8 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCN(CC)CC)cc1 10.1016/s0960-894x(01)00780-6
10051739 92208 0 None 501 2 Human 7.3 pKi = 7.3 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL22653 92208 0 None 501 2 Human 7.3 pKi = 7.3 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
44451350 102931 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 544 8 1 6 4.5 CNC(Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(C)cc1C)C2)c1ccccc1 10.1016/j.bmc.2007.09.026
CHEMBL260552 102931 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 544 8 1 6 4.5 CNC(Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(C)cc1C)C2)c1ccccc1 10.1016/j.bmc.2007.09.026
9939030 162507 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 623 11 1 6 7.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2cc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)cc2c1=O 10.1016/j.bmc.2007.09.026
CHEMBL405449 162507 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 623 11 1 6 7.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2cc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)cc2c1=O 10.1016/j.bmc.2007.09.026
44267882 173363 0 None 12 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 876 11 1 12 7.4 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL428008 173363 0 None 12 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 876 11 1 12 7.4 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
14557580 96145 0 None - 1 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity towards luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity towards luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 972 26 11 11 0.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369785 96145 0 None - 1 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity towards luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity towards luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 972 26 11 11 0.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cccc2ccccc12 10.1021/jm00130a019
9916573 163834 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 593 11 0 9 5.1 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL407399 163834 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 593 11 0 9 5.1 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44394578 136949 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 586 7 1 7 6.4 Cc1c(-c2csc(-c3ccc(C(C)(C)C)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL367806 136949 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 586 7 1 7 6.4 Cc1c(-c2csc(-c3ccc(C(C)(C)C)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
11752557 70473 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 395 6 1 5 3.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC(C)C 10.1016/j.bmcl.2004.02.004
CHEMBL180117 70473 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 395 6 1 5 3.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC(C)C 10.1016/j.bmcl.2004.02.004
CHEMBL74925 70473 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 395 6 1 5 3.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC(C)C 10.1016/j.bmcl.2004.02.004
44451498 162400 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1700 30 7 19 9.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCC(=O)N2CCC(C(=O)NCC#Cc3ccccc3C#CCNC(=O)C3CCN(C(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)CC3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL404611 162400 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1700 30 7 19 9.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCC(=O)N2CCC(C(=O)NCC#Cc3ccccc3C#CCNC(=O)C3CCN(C(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)CC3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL2370249 216594 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
11202795 119610 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL330804 119610 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C(C)C)c2=O)c1F 10.1021/jm049218c
11477970 96274 0 None 281 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm049791w
CHEMBL23729 96274 0 None 281 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm049791w
11202795 119610 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL330804 119610 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C(C)C)c2=O)c1F 10.1021/jm049791w
21046387 117429 0 None 53 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 493 7 1 4 6.6 CCOC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
CHEMBL325843 117429 0 None 53 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 493 7 1 4 6.6 CCOC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
44267875 22342 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity was determined against rat Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity was determined against rat Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 879 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12204 22342 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity was determined against rat Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity was determined against rat Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 879 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44451391 175643 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1715 30 6 20 10.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3ccc(C#CCNC(=O)C4CCN(C(=O)CN(Cc5ccccc5)Cc5c(-c6ccc(NC(=O)NCC)cc6)nc6n(Cc7c(F)cccc7F)cc(C(=O)OCC)c(=O)n56)CC4)cc3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL438168 175643 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1715 30 6 20 10.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3ccc(C#CCNC(=O)C4CCN(C(=O)CN(Cc5ccccc5)Cc5c(-c6ccc(NC(=O)NCC)cc6)nc6n(Cc7c(F)cccc7F)cc(C(=O)OCC)c(=O)n56)CC4)cc3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21046569 18780 0 None - 1 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 594 9 2 7 7.0 COC(=O)c1cc(C)nc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL118330 18780 0 None - 1 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 594 9 2 7 7.0 COC(=O)c1cc(C)nc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
21045818 119873 0 None -3 2 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncccn4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331337 119873 0 None -3 2 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncccn4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11050500 108625 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 636 9 0 8 6.5 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN1CCC(c2ccccc2)CC1 10.1021/jm0205402
CHEMBL300484 108625 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 636 9 0 8 6.5 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN1CCC(c2ccccc2)CC1 10.1021/jm0205402
44435828 95881 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 598 11 1 7 4.0 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(CCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2007.05.029
CHEMBL236546 95881 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 598 11 1 7 4.0 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(CCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2007.05.029
44309631 109386 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 652 14 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)Cc2cccnc2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL304156 109386 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 652 14 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)Cc2cccnc2)cc1 10.1016/s0960-894x(02)00370-0
44587397 179132 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 589 9 2 7 4.5 Cc1c(-c2cccc(OCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL447592 179132 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 589 9 2 7 4.5 Cc1c(-c2cccc(OCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
9891852 103053 1 None -13 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL261145 103053 1 None -13 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44436000 153980 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 576 7 0 6 5.3 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4C4CCCC4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL392815 153980 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 576 7 0 6 5.3 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4C4CCCC4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
21045831 17267 0 None -7 2 Rat 5.3 pKi = 5.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 422 5 2 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCNCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL116611 17267 0 None -7 2 Rat 5.3 pKi = 5.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 422 5 2 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCNCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21047815 21720 0 None -30 2 Rat 5.3 pKi = 5.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120834 21720 0 None -30 2 Rat 5.3 pKi = 5.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44340646 16461 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL113059 16461 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11421385 175200 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 429 6 1 5 3.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1 10.1021/jm049218c
CHEMBL433302 175200 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 429 6 1 5 3.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1 10.1021/jm049218c
CHEMBL434906 175200 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 429 6 1 5 3.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1 10.1021/jm049218c
11049737 109139 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 532 8 0 7 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN3CCCC3c3ccccn3)c2=O)c1 10.1021/jm034041s
CHEMBL303811 109139 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 532 8 0 7 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN3CCCC3c3ccccn3)c2=O)c1 10.1021/jm034041s
44451345 103285 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1607 32 8 20 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccc(C#CCNC(=O)CNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL262599 103285 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1607 32 8 20 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccc(C#CCNC(=O)CNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44451474 175536 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1635 32 8 20 9.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2cccc(C#CCNC(=O)[C@H](C)NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL437260 175536 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1635 32 8 20 9.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2cccc(C#CCNC(=O)[C@H](C)NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21048462 117094 0 None 60 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 522 5 1 4 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=O)OC(C)(C)C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL323863 117094 0 None 60 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 522 5 1 4 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=O)OC(C)(C)C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44433200 156963 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 555 7 0 8 4.1 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccc(-n4ccnc4)cc2)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL395183 156963 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 555 7 0 8 4.1 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccc(-n4ccnc4)cc2)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL415608 219974 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44343931 117178 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 568 11 0 8 5.2 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL324375 117178 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 568 11 0 8 5.2 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
9910626 17160 0 None 1 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 431 5 1 4 5.6 Cc1cnc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cn1 10.1016/s0960-894x(02)00755-2
CHEMBL116246 17160 0 None 1 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 431 5 1 4 5.6 Cc1cnc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cn1 10.1016/s0960-894x(02)00755-2
44343931 117178 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 568 11 0 8 5.2 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL324375 117178 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 568 11 0 8 5.2 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
44400195 76163 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL193089 76163 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
21047519 21194 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 551 8 3 6 6.8 Cc1cc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)nc(N)n1 10.1016/s0960-894x(02)00756-4
CHEMBL120048 21194 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 551 8 3 6 6.8 Cc1cc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)nc(N)n1 10.1016/s0960-894x(02)00756-4
44340697 117446 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 492 9 1 7 3.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL325942 117446 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 492 9 1 7 3.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44340612 16350 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3F)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112461 16350 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3F)c2=O)c1 10.1016/s0960-894x(03)00619-x
11477970 96274 0 None 281 2 Human 6.3 pKi = 6.3 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
CHEMBL23729 96274 0 None 281 2 Human 6.3 pKi = 6.3 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
44309359 109103 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 619 10 1 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(S)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL303621 109103 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 619 10 1 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(S)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
9910626 17160 0 None -1 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 431 5 1 4 5.6 Cc1cnc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cn1 10.1016/s0960-894x(02)00755-2
CHEMBL116246 17160 0 None -1 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 431 5 1 4 5.6 Cc1cnc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cn1 10.1016/s0960-894x(02)00755-2
44347048 21282 0 None -18 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120164 21282 0 None -18 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
9911446 17553 0 None -33 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 446 5 1 3 6.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(C#N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117170 17553 0 None -33 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 446 5 1 3 6.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(C#N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44267864 174535 0 None -30 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CCC1CN(C(=O)O[C@H]2[C@H](C)[C@@H](OC3O[C@H](C)C[C@H](N(C)C(C)C)[C@H]3O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]3N(CCc4ccc(Cl)cc4)C(=O)O[C@]3(C)[C@@H](CC)OC(=O)[C@@H]2C)C(=O)O1 10.1021/jm030418i
CHEMBL430312 174535 0 None -30 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CCC1CN(C(=O)O[C@H]2[C@H](C)[C@@H](OC3O[C@H](C)C[C@H](N(C)C(C)C)[C@H]3O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]3N(CCc4ccc(Cl)cc4)C(=O)O[C@]3(C)[C@@H](CC)OC(=O)[C@@H]2C)C(=O)O1 10.1021/jm030418i
44267905 105140 0 None -13 2 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275251 105140 0 None -13 2 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11421385 175200 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 429 6 1 5 3.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1 10.1016/j.bmcl.2004.02.004
CHEMBL433302 175200 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 429 6 1 5 3.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1 10.1016/j.bmcl.2004.02.004
CHEMBL434906 175200 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 429 6 1 5 3.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1 10.1016/j.bmcl.2004.02.004
44347005 121242 0 None -6 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 613 10 3 7 7.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(Nc4nccc(NCC5CCCO5)n4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333461 121242 0 None -6 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 613 10 3 7 7.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(Nc4nccc(NCC5CCCO5)n4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11752557 70473 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 395 6 1 5 3.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC(C)C 10.1021/jm049218c
CHEMBL180117 70473 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 395 6 1 5 3.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC(C)C 10.1021/jm049218c
CHEMBL74925 70473 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 395 6 1 5 3.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC(C)C 10.1021/jm049218c
44399956 130823 3 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL363094 130823 3 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
44346239 21280 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 707 12 2 8 7.2 CC(C)C[C@H](N)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL120149 21280 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 707 12 2 8 7.2 CC(C)C[C@H](N)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
44434436 157751 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1619 39 6 26 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL395825 157751 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1619 39 6 26 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44577100 185271 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 452 6 1 6 3.1 N[C@@H](Cn1c(=O)c(Cc2c(F)cccc2F)nn(-c2ccccc2F)c1=O)c1ccccc1 10.1021/jm701249f
CHEMBL466541 185271 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 452 6 1 6 3.1 N[C@@H](Cn1c(=O)c(Cc2c(F)cccc2F)nn(-c2ccccc2F)c1=O)c1ccccc1 10.1021/jm701249f
44451356 103138 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 870 18 4 10 5.9 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL261649 103138 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 870 18 4 10 5.9 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44387909 129545 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 495 8 1 9 2.0 COc1cccc(-n2c(=O)n(CCC(N)c3cccnc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL360472 129545 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 495 8 1 9 2.0 COc1cccc(-n2c(=O)n(CCC(N)c3cccnc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
9960268 195766 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 596 10 0 8 5.8 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1ccccc1 10.1021/jm0205402
CHEMBL50856 195766 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 596 10 0 8 5.8 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1ccccc1 10.1021/jm0205402
44340844 117330 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 9 0 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CN(C)CC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL325233 117330 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 9 0 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CN(C)CC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
11751752 20334 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 433 6 1 6 2.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N)c2=O)c1F 10.1021/jm049791w
CHEMBL119391 20334 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 433 6 1 6 2.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N)c2=O)c1F 10.1021/jm049791w
11374717 129073 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
CHEMBL359810 129073 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
CHEMBL419270 129073 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
44400230 75459 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 467 6 1 5 4.4 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL192172 75459 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 467 6 1 5 4.4 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
1179 7748 36 None -4 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
9957278 7748 36 None -4 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
CHEMBL494803 7748 36 None -4 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
44400230 75459 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 467 6 1 5 4.4 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL192172 75459 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 467 6 1 5 4.4 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
11374717 129073 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.02.004
CHEMBL359810 129073 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.02.004
CHEMBL419270 129073 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.02.004
1179 7748 36 None -4 3 Human 8.2 pKi = 8.2 Binding
Displacement of lzsI-GnRH-A from human GnRHR expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting methodDisplacement of lzsI-GnRH-A from human GnRHR expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
9957278 7748 36 None -4 3 Human 8.2 pKi = 8.2 Binding
Displacement of lzsI-GnRH-A from human GnRHR expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting methodDisplacement of lzsI-GnRH-A from human GnRHR expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
CHEMBL494803 7748 36 None -4 3 Human 8.2 pKi = 8.2 Binding
Displacement of lzsI-GnRH-A from human GnRHR expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting methodDisplacement of lzsI-GnRH-A from human GnRHR expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
21045805 20556 0 None 5 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL119546 20556 0 None 5 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44215933 102853 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCc3nccs3)c2=O)c1F 10.1016/j.bmc.2007.09.026
CHEMBL260062 102853 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCc3nccs3)c2=O)c1F 10.1016/j.bmc.2007.09.026
44432655 156265 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 675 11 3 6 6.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCOc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL394634 156265 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 675 11 3 6 6.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCOc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44400354 140282 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 559 8 1 6 5.5 CC(C)Oc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL370711 140282 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 559 8 1 6 5.5 CC(C)Oc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
44267865 168163 0 None 10 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CC[C@H]1COC(=O)N1C(=O)O[C@H]1[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]2(C)[C@@H](CC)OC(=O)[C@@H]1C 10.1021/jm030418i
CHEMBL412634 168163 0 None 10 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CC[C@H]1COC(=O)N1C(=O)O[C@H]1[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]2(C)[C@@H](CC)OC(=O)[C@@H]1C 10.1021/jm030418i
11236870 17818 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)CC(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL117670 17818 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)CC(C)C)c2=O)c1F 10.1021/jm049218c
11294792 70062 0 None 380 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL179269 70062 0 None 380 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
10345138 129335 0 None 2041 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL360143 129335 0 None 2041 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL75347 129335 0 None 2041 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
11236870 17818 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)CC(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL117670 17818 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)CC(C)C)c2=O)c1F 10.1021/jm049791w
11226753 70118 0 None 389 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL179429 70118 0 None 389 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
11180219 117998 0 None 112 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL326504 117998 0 None 112 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
11180219 117998 0 None 112 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL326504 117998 0 None 112 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049791w
9823968 117258 0 None 1 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 429 5 1 2 6.8 Cc1ccc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cc1 10.1016/s0960-894x(02)00755-2
CHEMBL324771 117258 0 None 1 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 429 5 1 2 6.8 Cc1ccc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cc1 10.1016/s0960-894x(02)00755-2
1184 10505 36 None -426 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity towards rat Gonadotropin-releasing hormone receptorBinding affinity towards rat Gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(03)00746-7
9874838 10505 36 None -426 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity towards rat Gonadotropin-releasing hormone receptorBinding affinity towards rat Gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(03)00746-7
CHEMBL71917 10505 36 None -426 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity towards rat Gonadotropin-releasing hormone receptorBinding affinity towards rat Gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(03)00746-7
11751752 20334 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 433 6 1 6 2.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N)c2=O)c1F 10.1021/jm049218c
CHEMBL119391 20334 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 433 6 1 6 2.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N)c2=O)c1F 10.1021/jm049218c
44436011 95270 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 613 9 0 7 4.9 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(CCc5ccccn5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL235046 95270 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 613 9 0 7 4.9 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(CCc5ccccn5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44451447 163453 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1663 36 8 20 10.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccc(C#CCNC(=O)CCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL406960 163453 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1663 36 8 20 10.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccc(C#CCNC(=O)CCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44352949 122859 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2cc(F)ccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL335650 122859 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2cc(F)ccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11444384 70193 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccc(F)c1 10.1021/jm049218c
CHEMBL179663 70193 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccc(F)c1 10.1021/jm049218c
CHEMBL311380 70193 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccc(F)c1 10.1021/jm049218c
44449120 102008 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL256109 102008 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
44346666 119615 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 622 9 0 7 6.9 CN(Cc1ccccc1)Cc1c(-c2ccc(N(C)C)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL330835 119615 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 622 9 0 7 6.9 CN(Cc1ccccc1)Cc1c(-c2ccc(N(C)C)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
9958318 97002 0 None 15 2 Human 6.2 pKi = 6.2 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23830 97002 0 None 15 2 Human 6.2 pKi = 6.2 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
11167850 9518 28 None -6309 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
1178 9518 28 None -6309 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
1187 9518 28 None -6309 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
CHEMBL179691 9518 28 None -6309 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
CHEMBL216930 216125 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44353231 123587 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 595 12 0 7 6.9 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL337865 123587 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 595 12 0 7 6.9 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
44451420 102988 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1719 40 8 20 11.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccc(C#CCNC(=O)CCCCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL260812 102988 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1719 40 8 20 11.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccc(C#CCNC(=O)CCCCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44387883 70048 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 478 8 1 8 2.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)CC(C)C)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL179212 70048 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 478 8 1 8 2.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)CC(C)C)c2=O)c1F 10.1016/j.bmcl.2005.05.038
11341990 69274 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1 10.1021/jm049218c
CHEMBL178127 69274 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1 10.1021/jm049218c
CHEMBL76277 69274 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1 10.1021/jm049218c
21047807 119763 0 None 23 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 568 8 3 7 6.4 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncc(C#N)c(N)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331087 119763 0 None 23 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 568 8 3 7 6.4 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncc(C#N)c(N)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44353284 175167 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 652 15 2 8 5.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NCCOC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL434621 175167 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 652 15 2 8 5.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NCCOC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
44388009 135462 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 7 1 8 2.9 COc1cccc(-n2c(=O)n(C[C@H](N)c3ccccc3)c(=O)n(C(C)c3c(F)cccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL366883 135462 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 7 1 8 2.9 COc1cccc(-n2c(=O)n(C[C@H](N)c3ccccc3)c(=O)n(C(C)c3c(F)cccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44267882 173363 0 None -12 2 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 876 11 1 12 7.4 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL428008 173363 0 None -12 2 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 876 11 1 12 7.4 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11238091 69280 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccn1 10.1021/jm049218c
CHEMBL178142 69280 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccn1 10.1021/jm049218c
CHEMBL311407 69280 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccn1 10.1021/jm049218c
44353263 29020 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 634 10 0 9 6.9 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)cc2n(Cc3ccccc3F)cc(-c3nc(C(C)(C)C)co3)c(=O)n12 10.1016/s0960-894x(01)00780-6
CHEMBL132338 29020 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 634 10 0 9 6.9 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)cc2n(Cc3ccccc3F)cc(-c3nc(C(C)(C)C)co3)c(=O)n12 10.1016/s0960-894x(01)00780-6
44346594 22346 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 548 7 0 8 5.2 CN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL122064 22346 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 548 7 0 8 5.2 CN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44295109 108458 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 530 8 1 6 6.2 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCC4CCCC4)n3c2=O)c1 10.1021/jm0205402
CHEMBL299335 108458 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 530 8 1 6 6.2 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCC4CCCC4)n3c2=O)c1 10.1021/jm0205402
11477988 97785 0 None -954 2 Rat 5.2 pKi = 5.2 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
CHEMBL23969 97785 0 None -954 2 Rat 5.2 pKi = 5.2 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
11294792 70062 0 None 380 2 Human 7.2 pKi = 7.2 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL179269 70062 0 None 380 2 Human 7.2 pKi = 7.2 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
44309652 211084 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccccc4OC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL71400 211084 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccccc4OC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
11192019 20032 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human gonadotropin-releasing hormone receptorBinding affinity for human gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049218c
CHEMBL119149 20032 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human gonadotropin-releasing hormone receptorBinding affinity for human gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049218c
44576678 177827 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 617 11 1 7 5.8 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL445691 177827 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 617 11 1 7 5.8 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
11192019 20032 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049791w
CHEMBL119149 20032 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049791w
44387888 67259 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CCC(N)c3cccc(F)c3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL175491 67259 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CCC(N)c3cccc(F)c3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
44388033 68536 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 497 7 1 9 2.1 COc1cccc(-n2c(=O)n(Cc3cccnc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL177182 68536 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 497 7 1 9 2.1 COc1cccc(-n2c(=O)n(Cc3cccnc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21045823 120919 0 None 40 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=O)C(F)(F)F)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL332923 120919 0 None 40 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=O)C(F)(F)F)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44267865 168163 0 None -10 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CC[C@H]1COC(=O)N1C(=O)O[C@H]1[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]2(C)[C@@H](CC)OC(=O)[C@@H]1C 10.1021/jm030418i
CHEMBL412634 168163 0 None -10 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CC[C@H]1COC(=O)N1C(=O)O[C@H]1[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]2(C)[C@@H](CC)OC(=O)[C@@H]1C 10.1021/jm030418i
44400122 140139 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 467 6 2 6 3.5 N[C@@H](Cn1c(=O)c(-c2cccc(O)c2F)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL370480 140139 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 467 6 2 6 3.5 N[C@@H](Cn1c(=O)c(-c2cccc(O)c2F)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
44432637 161751 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 492 8 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)c2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL401225 161751 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 492 8 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)c2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
44352641 124941 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 605 12 0 10 5.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL340856 124941 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 605 12 0 10 5.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL263690 217365 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H]1CC(=O)NC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC1=O 10.1021/jm990116+
11444384 70193 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccc(F)c1 10.1016/j.bmcl.2004.02.004
CHEMBL179663 70193 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccc(F)c1 10.1016/j.bmcl.2004.02.004
CHEMBL311380 70193 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccc(F)c1 10.1016/j.bmcl.2004.02.004
44309404 109526 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 648 10 0 8 6.9 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccc2F)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL305034 109526 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 648 10 0 8 6.9 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccc2F)cc1 10.1016/s0960-894x(02)00371-2
21045817 121328 0 None 22 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNc4ncccn4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333730 121328 0 None 22 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNc4ncccn4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44448860 101839 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL255242 101839 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
11295556 106026 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 11 0 7 4.3 CCOc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
CHEMBL281776 106026 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 11 0 7 4.3 CCOc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
44576642 194573 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 513 7 2 6 4.1 N[C@@H](Cn1c(=O)c(-c2ccc(CO)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL495882 194573 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 513 7 2 6 4.1 N[C@@H](Cn1c(=O)c(-c2ccc(CO)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44434437 157752 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1663 42 6 27 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL395826 157752 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1663 42 6 27 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44267863 105294 0 None -2 2 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 950 12 1 14 7.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL276217 105294 0 None -2 2 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 950 12 1 14 7.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11353175 106255 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 537 9 1 6 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3C)c2=O)c1F 10.1021/jm030472z
CHEMBL283170 106255 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 537 9 1 6 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3C)c2=O)c1F 10.1021/jm030472z
44394616 73132 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 617 9 2 9 5.7 CCOC(=O)Nc1ccc(-c2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
CHEMBL185143 73132 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 617 9 2 9 5.7 CCOC(=O)Nc1ccc(-c2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
21047618 121308 0 None 1 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 635 11 3 7 7.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncc(C)c(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333574 121308 0 None 1 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 635 11 3 7 7.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncc(C)c(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44288082 169947 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 981 10 1 14 8.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL418067 169947 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 981 10 1 14 8.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44449153 161855 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 581 9 1 6 6.2 CC[C@H](Cn1c(=O)c(-c2cccc(OC)c2Cl)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
CHEMBL401807 161855 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 581 9 1 6 6.2 CC[C@H](Cn1c(=O)c(-c2cccc(OC)c2Cl)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
10439419 108960 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 666 15 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL302769 108960 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 666 15 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00370-0
10439419 108960 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 666 15 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1021/jm701249f
CHEMBL302769 108960 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 666 15 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1021/jm701249f
11477615 128922 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 503 9 0 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](CC(C)C)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL359682 128922 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 503 9 0 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](CC(C)C)N(C)C)c2=O)c1F 10.1021/jm049218c
10439419 108960 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 666 15 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL302769 108960 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 666 15 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44587394 179252 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 599 11 2 7 5.1 Cc1c(-c2cccc(OCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL448253 179252 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 599 11 2 7 5.1 Cc1c(-c2cccc(OCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
21047583 22073 0 None 10 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 607 9 2 7 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(N5CCOCC5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121367 22073 0 None 10 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 607 9 2 7 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(N5CCOCC5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44288073 176206 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 965 12 2 14 7.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL442482 176206 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 965 12 2 14 7.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
25156669 195909 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 645 13 2 7 5.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL510538 195909 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 645 13 2 7 5.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
44400121 134196 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 483 6 1 5 4.6 N[C@@H](Cn1c(=O)c(-c2ccccc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL365985 134196 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 483 6 1 5 4.6 N[C@@H](Cn1c(=O)c(-c2ccccc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44400121 134196 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 483 6 1 5 4.6 N[C@@H](Cn1c(=O)c(-c2ccccc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL365985 134196 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 483 6 1 5 4.6 N[C@@H](Cn1c(=O)c(-c2ccccc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
11050145 200146 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 581 10 0 7 6.4 CCN(CCc1ccccn1)Cc1c(C(C)(C)C)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
CHEMBL52506 200146 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 581 10 0 7 6.4 CCN(CCc1ccccn1)Cc1c(C(C)(C)C)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
11387100 17009 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 537 9 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](Cc3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL116074 17009 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 537 9 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](Cc3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
11387100 17009 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 537 9 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](Cc3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL116074 17009 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 537 9 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](Cc3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049791w
44267866 103887 0 None 4 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CC(C)OC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL267568 103887 0 None 4 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CC(C)OC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11179922 94095 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3C)c2=O)c1 10.1021/jm030472z
CHEMBL23321 94095 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3C)c2=O)c1 10.1021/jm030472z
44394896 73079 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 545 8 2 8 5.2 Cc1c(-c2csc(Nc3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL184855 73079 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 545 8 2 8 5.2 Cc1c(-c2csc(Nc3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
11179922 94095 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3C)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23321 94095 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3C)c2=O)c1 10.1016/s0960-894x(03)00619-x
44436019 174428 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 564 8 0 6 4.9 CN(C)[C@@H](Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2)c1ccccc1 10.1016/j.bmc.2007.05.029
CHEMBL430171 174428 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 564 8 0 6 4.9 CN(C)[C@@H](Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2)c1ccccc1 10.1016/j.bmc.2007.05.029
44387945 129494 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 494 8 1 8 2.6 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL360447 129494 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 494 8 1 8 2.6 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
11157017 129167 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccnc1 10.1016/j.bmcl.2004.02.004
CHEMBL360056 129167 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccnc1 10.1016/j.bmcl.2004.02.004
CHEMBL72199 129167 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccnc1 10.1016/j.bmcl.2004.02.004
20728209 130101 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 443 5 1 6 3.5 NC(Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1)CO2)c1ccccc1 10.1016/j.bmcl.2005.01.009
CHEMBL361619 130101 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 443 5 1 6 3.5 NC(Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1)CO2)c1ccccc1 10.1016/j.bmcl.2005.01.009
44451294 102891 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1647 38 8 18 11.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccccc2C#CCNC(=O)CCCCCNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL260318 102891 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1647 38 8 18 11.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccccc2C#CCNC(=O)CCCCCNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21045831 17267 0 None 7 2 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 422 5 2 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCNCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL116611 17267 0 None 7 2 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 422 5 2 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCNCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL2370251 216595 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
CHEMBL329695 218098 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]([C@@H](C)CC)NC1=O 10.1021/jm990432o
44340860 16387 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 9 0 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CN(C)CC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112625 16387 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 9 0 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CN(C)CC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
11363829 16947 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 489 7 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)CC(C)(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL115965 16947 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 489 7 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)CC(C)(C)C)c2=O)c1F 10.1021/jm049791w
25156399 195827 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 603 10 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL509440 195827 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 603 10 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
9915597 190969 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 552 8 0 6 6.6 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)Cc4ccccc4)n3c2=O)c1 10.1021/jm0205402
CHEMBL48316 190969 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 552 8 0 6 6.6 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)Cc4ccccc4)n3c2=O)c1 10.1021/jm0205402
44340840 120101 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1ccc(CNC[C@@H](C)n2c(=O)c(-c3cccc(OC)c3)c(C)n(Cc3c(F)cccc3F)c2=O)cc1 10.1016/s0960-894x(03)00619-x
CHEMBL331592 120101 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1ccc(CNC[C@@H](C)n2c(=O)c(-c3cccc(OC)c3)c(C)n(Cc3c(F)cccc3F)c2=O)cc1 10.1016/s0960-894x(03)00619-x
CHEMBL405420 219338 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44451486 164956 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1691 34 8 20 10.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccc(C#CCNC(=O)[C@@H](NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)C(C)C)cc2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL408760 164956 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1691 34 8 20 10.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccc(C#CCNC(=O)[C@@H](NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)C(C)C)cc2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44388026 136596 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 521 7 1 9 2.6 COc1cccc(-n2c(=O)n(Cc3c(Cl)cccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL367548 136596 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 521 7 1 9 2.6 COc1cccc(-n2c(=O)n(Cc3c(Cl)cccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21047858 16860 0 None -17 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CN)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL115425 16860 0 None -17 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CN)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
9891852 17828 1 None -18 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117736 17828 1 None -18 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
10439527 176259 0 None -288 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 677 15 0 9 7.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL443027 176259 0 None -288 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 677 15 0 9 7.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11214294 128973 0 None 912 2 Human 7.1 pKi = 7.1 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL359754 128973 0 None 912 2 Human 7.1 pKi = 7.1 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
21045828 21336 0 None -2 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(NCC5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120420 21336 0 None -2 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(NCC5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44451408 102971 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1687 30 6 20 10.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccc(C#CCNC(=O)[C@@H]3CCCN3C(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL260750 102971 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1687 30 6 20 10.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccc(C#CCNC(=O)[C@@H]3CCCN3C(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
11214295 93765 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3)c2=O)c1 10.1021/jm030472z
CHEMBL23237 93765 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3)c2=O)c1 10.1021/jm030472z
11214295 93765 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23237 93765 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
11341990 69274 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1 10.1016/j.bmcl.2004.02.004
CHEMBL178127 69274 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1 10.1016/j.bmcl.2004.02.004
CHEMBL76277 69274 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1 10.1016/j.bmcl.2004.02.004
44387898 67818 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 508 8 1 8 2.9 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3C)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL176284 67818 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 508 8 1 8 2.9 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3C)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
10051739 92208 0 None -501 2 Rat 5.1 pKi = 5.1 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL22653 92208 0 None -501 2 Rat 5.1 pKi = 5.1 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
44346662 121203 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 633 12 0 9 5.9 CCN(CC)CCN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL333213 121203 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 633 12 0 9 5.9 CCN(CC)CCN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44352652 124262 0 None -245 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 689 14 0 9 7.6 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC4CCCC4)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL339968 124262 0 None -245 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 689 14 0 9 7.6 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC4CCCC4)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11282957 129111 1 None -1096 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
CHEMBL359894 129111 1 None -1096 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
9983568 105758 0 None -263 2 Rat 5.1 pKi = 5.1 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL279885 105758 0 None -263 2 Rat 5.1 pKi = 5.1 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
44576655 195000 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 570 9 2 8 3.6 NCC(=O)OCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.04.036
CHEMBL499307 195000 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 570 9 2 8 3.6 NCC(=O)OCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.04.036
11238091 69280 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccn1 10.1016/j.bmcl.2004.02.004
CHEMBL178142 69280 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccn1 10.1016/j.bmcl.2004.02.004
CHEMBL311407 69280 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccn1 10.1016/j.bmcl.2004.02.004
44451379 175759 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 884 17 4 10 6.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccccc2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL439076 175759 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 884 17 4 10 6.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccccc2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44352665 125052 0 None -43 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 635 13 0 9 6.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL340934 125052 0 None -43 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 635 13 0 9 6.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
10875519 196092 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 575 8 0 9 3.9 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN1CCN(C)CC1 10.1021/jm0205402
CHEMBL51232 196092 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 575 8 0 9 3.9 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN1CCN(C)CC1 10.1021/jm0205402
11294792 70062 0 None -380 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL179269 70062 0 None -380 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
11455176 105835 0 None - 1 Human 6.1 pKi = 6.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL280430 105835 0 None - 1 Human 6.1 pKi = 6.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11455176 105835 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL280430 105835 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCCc3ccccn3)c2=O)c1 10.1021/jm030472z
44341074 16715 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 469 9 1 6 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL114619 16715 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 469 9 1 6 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
21045807 23086 0 None - 1 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 590 8 2 5 7.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(C(F)(F)F)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL122653 23086 0 None - 1 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 590 8 2 5 7.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(C(F)(F)F)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11226171 94225 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL23337 94225 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11226171 94225 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23337 94225 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCCc3ccccn3)c2=O)c1 10.1021/jm030472z
44309617 210736 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 605 10 0 7 6.5 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(F)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL69361 210736 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 605 10 0 7 6.5 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(F)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
21047937 118074 0 None 1 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 472 7 1 3 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN(C)C)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL326606 118074 0 None 1 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 472 7 1 3 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN(C)C)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44288079 106989 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 896 11 3 14 5.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](NC)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL288396 106989 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 896 11 3 14 5.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](NC)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44267870 104896 0 None -8 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 10 1 14 7.0 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OCC2(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273536 104896 0 None -8 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 10 1 14 7.0 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OCC2(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11421518 172075 0 None -1047 2 Rat 5.1 pKi = 5.1 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL423291 172075 0 None -1047 2 Rat 5.1 pKi = 5.1 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
44267904 105192 0 None -6 2 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275521 105192 0 None -6 2 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11103767 108571 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 569 10 1 8 5.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)CO)c(CN(C)Cc4ccccn4)n3c2=O)c1 10.1021/jm0205402
CHEMBL300079 108571 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 569 10 1 8 5.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)CO)c(CN(C)Cc4ccccn4)n3c2=O)c1 10.1021/jm0205402
44400188 76155 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 501 6 1 5 4.7 N[C@@H](Cn1c(=O)c(-c2ccccc2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL193031 76155 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 501 6 1 5 4.7 N[C@@H](Cn1c(=O)c(-c2ccccc2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
44347047 23371 0 None -5 2 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL124056 23371 0 None -5 2 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
9984259 117278 0 None 281 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm701249f
CHEMBL324912 117278 0 None 281 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm701249f
9984259 117278 0 None 281 2 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
CHEMBL324912 117278 0 None 281 2 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
9984259 117278 0 None 281 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
CHEMBL324912 117278 0 None 281 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
44400353 75449 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 599 8 1 6 5.7 N[C@@H](Cn1c(=O)c(-c2cccc(OCC(F)(F)F)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL192096 75449 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 599 8 1 6 5.7 N[C@@H](Cn1c(=O)c(-c2cccc(OCC(F)(F)F)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
11307227 129831 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 539 8 1 6 5.8 Cc1c(-c2ccc(Oc3ccccc3)cc2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL360935 129831 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 539 8 1 6 5.8 Cc1c(-c2ccc(Oc3ccccc3)cc2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL2371513 216843 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H](CC(=O)O)C(=O)N[C@H]1CCC(=O)NCCC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44267870 104896 0 None 8 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 10 1 14 7.0 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OCC2(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273536 104896 0 None 8 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 10 1 14 7.0 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OCC2(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44309319 210493 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 609 12 1 8 5.9 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL67638 210493 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 609 12 1 8 5.9 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00370-0
44435992 103282 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 597 10 0 8 4.8 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3ccccc3F)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
CHEMBL262581 103282 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 597 10 0 8 4.8 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3ccccc3F)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
21047583 22073 0 None -10 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 607 9 2 7 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(N5CCOCC5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121367 22073 0 None -10 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 607 9 2 7 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(N5CCOCC5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44352679 122279 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL335196 122279 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44387920 70658 0 None - 1 Human 6.1 pKi = 6.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3F)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL180421 70658 0 None - 1 Human 6.1 pKi = 6.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3F)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL2370261 216601 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
CHEMBL329946 218102 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
44435981 153727 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 623 11 0 9 2.9 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(S(C)(=O)=O)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL392603 153727 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 623 11 0 9 2.9 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(S(C)(=O)=O)cc1)C2 10.1016/j.bmc.2007.05.029
44340641 117354 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 529 13 1 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCCCOCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL325391 117354 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 529 13 1 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCCCOCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00620-6
11260704 105451 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 508 9 0 6 4.0 Cc1c(-c2ccccc2F)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL277439 105451 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 508 9 0 6 4.0 Cc1c(-c2ccccc2F)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
44451446 175495 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1663 36 8 20 10.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2cccc(C#CCNC(=O)CCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL436862 175495 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1663 36 8 20 10.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2cccc(C#CCNC(=O)CCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
11249548 105866 0 None 97 2 Human 6.1 pKi = 6.1 Binding
In vivo inhibition of monkey Gonadotropin releasing hormone receptorIn vivo inhibition of monkey Gonadotropin releasing hormone receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
CHEMBL280664 105866 0 None 97 2 Human 6.1 pKi = 6.1 Binding
In vivo inhibition of monkey Gonadotropin releasing hormone receptorIn vivo inhibition of monkey Gonadotropin releasing hormone receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
44387922 67320 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CCC(N)c3ccc(F)cc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL175869 67320 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CCC(N)c3ccc(F)cc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
9823968 117258 0 None -1 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 429 5 1 2 6.8 Cc1ccc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cc1 10.1016/s0960-894x(02)00755-2
CHEMBL324771 117258 0 None -1 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 429 5 1 2 6.8 Cc1ccc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cc1 10.1016/s0960-894x(02)00755-2
21046570 119864 0 None -34 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 479 6 1 4 6.2 COC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
CHEMBL331277 119864 0 None -34 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 479 6 1 4 6.2 COC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
44340643 118121 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 532 8 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C3CCN(CCc4ccccn4)C3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL326885 118121 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 532 8 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C3CCN(CCc4ccccn4)C3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44451343 103241 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1591 34 8 18 9.9 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccccc2C#CCNC(=O)CCCNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL262335 103241 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1591 34 8 18 9.9 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccccc2C#CCNC(=O)CCCNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44340824 16244 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3cccc(F)c3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL111933 16244 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3cccc(F)c3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44435984 95555 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 559 10 0 7 3.8 Cc1ccccc1CN1CCc2c(c(=O)n(CCN(C)CCc3ccccn3)c(=O)n2Cc2c(F)cccc2F)C1 10.1016/j.bmc.2007.05.029
CHEMBL236332 95555 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 559 10 0 7 3.8 Cc1ccccc1CN1CCc2c(c(=O)n(CCN(C)CCc3ccccn3)c(=O)n2Cc2c(F)cccc2F)C1 10.1016/j.bmc.2007.05.029
44435983 95554 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 579 10 0 7 4.1 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1cccc(Cl)c1)C2 10.1016/j.bmc.2007.05.029
CHEMBL236331 95554 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 579 10 0 7 4.1 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1cccc(Cl)c1)C2 10.1016/j.bmc.2007.05.029
44451258 174205 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1729 32 8 20 8.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccccc2C#CCNC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL429690 174205 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1729 32 8 20 8.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccccc2C#CCNC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44352942 29383 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 609 11 0 9 5.6 CCOC(=O)c1cn(Cc2ccccc2Cl)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL132661 29383 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 609 11 0 9 5.6 CCOC(=O)c1cn(Cc2ccccc2Cl)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44388018 67249 0 None 389 2 Human 7.1 pKi = 7.1 Binding
Inhibition constant against monkey GnRH receptorInhibition constant against monkey GnRH receptor
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL175443 67249 0 None 389 2 Human 7.1 pKi = 7.1 Binding
Inhibition constant against monkey GnRH receptorInhibition constant against monkey GnRH receptor
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21047784 117414 0 None -36 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 574 9 4 7 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4cc(O)nc(O)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL325747 117414 0 None -36 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 574 9 4 7 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4cc(O)nc(O)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
11191675 70156 0 None 186 2 Human 7.1 pKi = 7.1 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL179600 70156 0 None 186 2 Human 7.1 pKi = 7.1 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL3085404 70156 0 None 186 2 Human 7.1 pKi = 7.1 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
11226531 106296 0 None 169 2 Human 7.1 pKi = 7.1 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
CHEMBL283381 106296 0 None 169 2 Human 7.1 pKi = 7.1 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
44389647 71348 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 455 6 1 7 3.4 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2)CO3)c1 10.1016/j.bmcl.2005.01.009
CHEMBL181582 71348 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 455 6 1 7 3.4 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2)CO3)c1 10.1016/j.bmcl.2005.01.009
44346665 119614 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 636 10 1 7 7.7 CC(C)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL330834 119614 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 636 10 1 7 7.7 CC(C)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
11284357 67791 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 443 7 1 5 4.1 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CCc1ccccc1 10.1021/jm049218c
CHEMBL176270 67791 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 443 7 1 5 4.1 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CCc1ccccc1 10.1021/jm049218c
CHEMBL72913 67791 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 443 7 1 5 4.1 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CCc1ccccc1 10.1021/jm049218c
11329628 69798 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 393 6 1 5 3.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CC1 10.1021/jm049218c
CHEMBL178805 69798 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 393 6 1 5 3.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CC1 10.1021/jm049218c
CHEMBL73575 69798 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 393 6 1 5 3.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CC1 10.1021/jm049218c
CHEMBL405837 219363 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44390758 71720 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 468 6 1 7 2.3 N[C@@H](Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2ccccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2004.11.026
CHEMBL182284 71720 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 468 6 1 7 2.3 N[C@@H](Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2ccccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2004.11.026
44340652 16227 0 None - 1 Human 6.1 pKi = 6.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL111820 16227 0 None - 1 Human 6.1 pKi = 6.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
21047631 17732 0 None -5 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CN)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117330 17732 0 None -5 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CN)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44352657 28323 0 None -269 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 687 12 0 9 7.3 CN(CCc1ccccn1)Cc1c(-c2ccc(OC3CCCC3)cc2)c(C#N)c2n(Cc3ccccc3F)cc(C(=O)OC3CCCC3)c(=O)n12 10.1016/s0960-894x(01)00779-x
CHEMBL131665 28323 0 None -269 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 687 12 0 9 7.3 CN(CCc1ccccn1)Cc1c(-c2ccc(OC3CCCC3)cc2)c(C#N)c2n(Cc3ccccc3F)cc(C(=O)OC3CCCC3)c(=O)n12 10.1016/s0960-894x(01)00779-x
44387896 136452 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 498 7 1 8 2.3 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL367388 136452 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 498 7 1 8 2.3 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
44394778 132665 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 544 8 1 7 5.1 Cc1c(-c2csc(Cc3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL364842 132665 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 544 8 1 7 5.1 Cc1c(-c2csc(Cc3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
9852184 17461 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 628 13 0 8 6.4 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL117069 17461 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 628 13 0 8 6.4 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
44346396 120149 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 625 9 0 9 6.1 CN(Cc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL331762 120149 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 625 9 0 9 6.1 CN(Cc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44387896 136452 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 498 7 1 8 2.3 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL367388 136452 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 498 7 1 8 2.3 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44347005 121242 0 None 6 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 613 10 3 7 7.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(Nc4nccc(NCC5CCCO5)n4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333461 121242 0 None 6 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 613 10 3 7 7.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(Nc4nccc(NCC5CCCO5)n4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44400247 128820 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 571 10 2 9 2.5 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)CCO)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL359558 128820 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 571 10 2 9 2.5 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)CCO)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
44353288 175136 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 662 13 2 7 6.4 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NC4CCCC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL434423 175136 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 662 13 2 7 6.4 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NC4CCCC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
44587403 195606 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 647 13 2 8 4.8 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCOCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL506338 195606 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 647 13 2 8 4.8 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCOCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
10394119 121225 0 None -1 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333345 121225 0 None -1 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL438712 220566 0 None - 1 Rat 8.0 pKi = 8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm990116+
44340623 16252 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3F)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL111980 16252 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3F)c2=O)c1 10.1016/s0960-894x(03)00619-x
21047633 171253 0 None 1 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CN)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL421418 171253 0 None 1 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CN)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44343881 17751 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 603 12 0 8 6.5 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3ccc(OCC(C)C)cc3)c(CN(C)Cc3ccco3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL117346 17751 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 603 12 0 8 6.5 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3ccc(OCC(C)C)cc3)c(CN(C)Cc3ccco3)n2c1=O 10.1016/s0960-894x(02)00745-x
11082604 108536 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 608 8 0 8 5.7 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN1CCc2ccccc2C1 10.1021/jm0205402
CHEMBL299850 108536 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 608 8 0 8 5.7 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN1CCc2ccccc2C1 10.1021/jm0205402
22716607 71553 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 493 5 1 6 4.9 NC(Cn1c(=O)c(-c2ccccc2Cl)c2n(c1=O)C(c1ccccc1F)CS2)c1ccccc1 10.1016/j.bmcl.2005.01.009
CHEMBL181945 71553 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 493 5 1 6 4.9 NC(Cn1c(=O)c(-c2ccccc2Cl)c2n(c1=O)C(c1ccccc1F)CS2)c1ccccc1 10.1016/j.bmcl.2005.01.009
44451419 103723 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1687 30 6 20 10.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2cccc(C#CCNC(=O)[C@@H]3CCCN3C(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL266172 103723 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1687 30 6 20 10.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2cccc(C#CCNC(=O)[C@@H]3CCCN3C(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44451430 162693 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1719 40 8 20 11.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2cccc(C#CCNC(=O)CCCCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL406084 162693 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1719 40 8 20 11.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2cccc(C#CCNC(=O)CCCCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21047633 171253 0 None -1 2 Rat 7.0 pKi = 7.0 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CN)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL421418 171253 0 None -1 2 Rat 7.0 pKi = 7.0 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CN)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
11431754 20070 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 487 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C3CCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL119185 20070 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 487 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C3CCCC3)c2=O)c1F 10.1021/jm049791w
44387961 172800 0 None -144 2 Rat 5.0 pKi = 5.0 Binding
Inhibition constant against rat GnRH receptorInhibition constant against rat GnRH receptor
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL425523 172800 0 None -144 2 Rat 5.0 pKi = 5.0 Binding
Inhibition constant against rat GnRH receptorInhibition constant against rat GnRH receptor
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44436001 168461 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 598 8 0 6 5.6 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4Cc4ccccc4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL413239 168461 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 598 8 0 6 5.6 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4Cc4ccccc4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44309671 210636 0 None - 1 Human 6.0 pKi = 6.0 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 554 10 0 8 5.2 CCOC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00370-0
CHEMBL68664 210636 0 None - 1 Human 6.0 pKi = 6.0 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 554 10 0 8 5.2 CCOC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00370-0
44340642 16441 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNC3CCCC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112881 16441 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNC3CCCC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44309388 109323 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 609 7 0 9 5.2 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN2CCCN(C)CC2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL304067 109323 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 609 7 0 9 5.2 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN2CCCN(C)CC2)cc1 10.1016/s0960-894x(02)00371-2
44340688 16381 0 None - 1 Human 7.0 pKi = 7.0 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 0 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL112611 16381 0 None - 1 Human 7.0 pKi = 7.0 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 0 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11489334 17265 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 523 9 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)CCc3ccccc3)c2=O)c1F 10.1021/jm049791w
CHEMBL116576 17265 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 523 9 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)CCc3ccccc3)c2=O)c1F 10.1021/jm049791w
11294949 20813 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL119739 20813 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C(C)C)c2=O)c1F 10.1021/jm049218c
44435818 95880 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 399 4 1 6 2.0 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CNCC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL236545 95880 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 399 4 1 6 2.0 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CNCC3)c1 10.1016/j.bmc.2007.05.029
11294949 20813 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL119739 20813 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C(C)C)c2=O)c1F 10.1021/jm049791w
44587400 179952 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 660 13 2 8 4.7 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCN(C)CC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL452198 179952 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 660 13 2 8 4.7 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCN(C)CC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
11157017 129167 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccnc1 10.1021/jm049218c
CHEMBL360056 129167 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccnc1 10.1021/jm049218c
CHEMBL72199 129167 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccnc1 10.1021/jm049218c
44435822 160970 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 519 7 0 7 3.9 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccccc2OC)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL398583 160970 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 519 7 0 7 3.9 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccccc2OC)CC3)c1 10.1016/j.bmc.2007.05.029
44435825 95279 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 545 10 0 7 3.5 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccccc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL235084 95279 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 545 10 0 7 3.5 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccccc1)C2 10.1016/j.bmc.2007.05.029
11455317 69662 0 None -851 2 Rat 5.0 pKi = 5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL178457 69662 0 None -851 2 Rat 5.0 pKi = 5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
11980076 215232 29 None - 1 Human 8.1 pIC50 = 8.1 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
Drug Central None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
CHEMBL1007 215232 29 None - 1 Human 8.1 pIC50 = 8.1 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
Drug Central None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
1175 9078 44 None - 1 Rat 8.0 pIC50 = 8.0 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
Drug Central None None None None None
1559 9078 44 None - 1 Rat 8.0 pIC50 = 8.0 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
Drug Central None None None None None
657181 9078 44 None - 1 Rat 8.0 pIC50 = 8.0 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
Drug Central None None None None None
CHEMBL1201199 9078 44 None - 1 Rat 8.0 pIC50 = 8.0 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
Drug Central None None None None None
DB00007 9078 44 None - 1 Rat 8.0 pIC50 = 8.0 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
Drug Central None None None None None
3823 56995 42 None -1 11 Rat 8.0 pKd = 8.0 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
76973198 56995 42 None -1 11 Rat 8.0 pKd = 8.0 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
CHEMBL157101 56995 42 None -1 11 Rat 8.0 pKd = 8.0 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
25077405 9492 0 None - 1 Human 8.0 pKd = 8.0 Binding
NoneNone
Drug Central None None None None None
3902 9492 0 None - 1 Human 8.0 pKd = 8.0 Binding
NoneNone
Drug Central None None None None None
CHEMBL1201309 9492 0 None - 1 Human 8.0 pKd = 8.0 Binding
NoneNone
Drug Central None None None None None
DB00666 9492 0 None - 1 Human 8.0 pKd = 8.0 Binding
NoneNone
Drug Central None None None None None
1162 8612 0 None 16 2 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
16132914 8612 0 None 16 2 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
3878 8614 0 None - 1 Human 8.2 pKd = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17254668
188304 8412 0 None - 1 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9341 8412 0 None - 1 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL3272563 8412 0 None - 1 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9342 7114 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9855027 7114 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL3272561 7114 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9344 8715 0 None - 1 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
25077495 8172 0 None - 1 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9343 8172 0 None - 1 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL2365665 8172 0 None - 1 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
DB11510 8172 0 None - 1 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
3860 7531 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
3860 7531 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
436 7531 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
436 7531 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
50225 7531 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
50225 7531 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
CHEMBL2110824 7531 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL2110824 7531 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
DB06719 7531 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
DB06719 7531 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
11167850 9518 28 None 6309 2 Human 9.7 pKd None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 16930559
1178 9518 28 None 6309 2 Human 9.7 pKd None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 16930559
1187 9518 28 None 6309 2 Human 9.7 pKd None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 16930559
CHEMBL179691 9518 28 None 6309 2 Human 9.7 pKd None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 16930559
11250647 8327 46 None -117 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
5293 8327 46 None -117 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
8362 8327 46 None -117 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
CHEMBL1208155 8327 46 None -117 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
DB11979 8327 46 None -117 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
101755083 8141 47 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
16136245 8141 47 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
4379 8141 47 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
5585 8141 47 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
CHEMBL415606 8141 47 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
DB06699 8141 47 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
1190 7669 47 None - 1 Human 8.1 pKi = 8.1 Binding
GRAC: human GnRH1 selective antagonistGRAC: human GnRH1 selective antagonist
Drug Central None None None None None
25074887 7669 47 None - 1 Human 8.1 pKi = 8.1 Binding
GRAC: human GnRH1 selective antagonistGRAC: human GnRH1 selective antagonist
Drug Central None None None None None
583 7669 47 None - 1 Human 8.1 pKi = 8.1 Binding
GRAC: human GnRH1 selective antagonistGRAC: human GnRH1 selective antagonist
Drug Central None None None None None
CHEMBL1200490 7669 47 None - 1 Human 8.1 pKi = 8.1 Binding
GRAC: human GnRH1 selective antagonistGRAC: human GnRH1 selective antagonist
Drug Central None None None None None
DB00050 7669 47 None - 1 Human 8.1 pKi = 8.1 Binding
GRAC: human GnRH1 selective antagonistGRAC: human GnRH1 selective antagonist
Drug Central None None None None None
1177 10639 0 None -10 2 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
25074470 10639 0 None -10 2 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
2968 10639 0 None -10 2 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
CHEMBL1201334 10639 0 None -10 2 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
DB06825 10639 0 None -10 2 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
1188 7007 48 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
16131215 7007 48 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
35 7007 48 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
CHEMBL1252 7007 48 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
DB00106 7007 48 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
11225 7900 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Binding affinity to rat GnRH receptors as determined from competitive binding studies against [<sup>125</sup>I]buserelin.Binding affinity to rat GnRH receptors as determined from competitive binding studies against [<sup>125</sup>I]buserelin.
Guide to Pharmacology 645 10 0 6 6.0 FCCOc1cccc(c1F)c1c(C)n(Cc2c(F)cccc2C(F)(F)F)c(=O)n(c1=O)C[C@H](N1CCCC1=O)c1ccccc1 32677155
154699464 7900 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Binding affinity to rat GnRH receptors as determined from competitive binding studies against [<sup>125</sup>I]buserelin.Binding affinity to rat GnRH receptors as determined from competitive binding studies against [<sup>125</sup>I]buserelin.
Guide to Pharmacology 645 10 0 6 6.0 FCCOc1cccc(c1F)c1c(C)n(Cc2c(F)cccc2C(F)(F)F)c(=O)n(c1=O)C[C@H](N1CCCC1=O)c1ccccc1 32677155
1162 8612 0 None -16 2 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
16132914 8612 0 None -16 2 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
1162 8612 0 None 16 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
1162 8612 0 None 16 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
16132914 8612 0 None 16 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
16132914 8612 0 None 16 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
1162 8612 0 None 16 2 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
16132914 8612 0 None 16 2 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
101755083 8141 47 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
16136245 8141 47 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
4379 8141 47 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
5585 8141 47 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
CHEMBL415606 8141 47 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
DB06699 8141 47 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
1175 9078 44 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
1559 9078 44 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
657181 9078 44 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
CHEMBL1201199 9078 44 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
DB00007 9078 44 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
11250647 8327 46 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 19006286
11250647 8327 46 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 30194661
5293 8327 46 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 19006286
5293 8327 46 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 30194661
8362 8327 46 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 19006286
8362 8327 46 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 30194661
CHEMBL1208155 8327 46 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 19006286
CHEMBL1208155 8327 46 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 30194661
DB11979 8327 46 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 19006286
DB11979 8327 46 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 30194661
188304 8412 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9341 8412 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL3272563 8412 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9342 7114 0 None - 1 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9855027 7114 0 None - 1 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL3272561 7114 0 None - 1 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9344 8715 0 None - 1 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
1188 7007 48 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
16131215 7007 48 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
35 7007 48 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
CHEMBL1252 7007 48 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
DB00106 7007 48 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
1177 10639 0 None 10 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
25074470 10639 0 None 10 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
2968 10639 0 None 10 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
CHEMBL1201334 10639 0 None 10 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
DB06825 10639 0 None 10 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
101827019 8887 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850267
16130938 8887 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850267
3854 8887 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850267
73952264 8887 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850267
CHEMBL3989438 8887 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850267
25077495 8172 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9343 8172 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL2365665 8172 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
DB11510 8172 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
1190 7669 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
1190 7669 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7649152
1190 7669 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
25074887 7669 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
25074887 7669 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7649152
25074887 7669 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
583 7669 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
583 7669 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7649152
583 7669 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
CHEMBL1200490 7669 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
CHEMBL1200490 7669 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7649152
CHEMBL1200490 7669 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
DB00050 7669 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
DB00050 7669 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7649152
DB00050 7669 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
3860 7531 0 None 57 2 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
436 7531 0 None 57 2 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
50225 7531 0 None 57 2 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL2110824 7531 0 None 57 2 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
DB06719 7531 0 None 57 2 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
1180 8085 0 None - 1 Human 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
1185 10473 38 None - 1 Human 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 12502365
3038517 10473 38 None - 1 Human 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 12502365
CHEMBL22055 10473 38 None - 1 Human 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 12502365
DB06494 10473 38 None - 1 Human 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 12502365
1191 8071 0 None - 1 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
1170 8712 0 None - 1 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
1179 7748 36 None -4 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 12606616
9957278 7748 36 None -4 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 12606616
CHEMBL494803 7748 36 None -4 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 12606616
10279142 8407 0 None - 1 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 509 7 1 8 6.0 COc1nc(OC)c(c(n1)OC)NC(=O)c1ccc(o1)Oc1cc2c(cc1C)C(C)(C)C(CC2(C)C)C 18344315
1182 8407 0 None - 1 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 509 7 1 8 6.0 COc1nc(OC)c(c(n1)OC)NC(=O)c1ccc(o1)Oc1cc2c(cc1C)C(C)(C)C(CC2(C)C)C 18344315
1181 8086 0 None - 1 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
1177 10639 0 None -10 2 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
25074470 10639 0 None -10 2 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
2968 10639 0 None -10 2 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
CHEMBL1201334 10639 0 None -10 2 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
DB06825 10639 0 None -10 2 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
11167850 9518 28 None 6309 2 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
1178 9518 28 None 6309 2 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
1187 9518 28 None 6309 2 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
CHEMBL179691 9518 28 None 6309 2 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
11167850 9518 28 None 6309 2 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
1178 9518 28 None 6309 2 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
1187 9518 28 None 6309 2 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
CHEMBL179691 9518 28 None 6309 2 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
1189 7215 0 None - 1 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
16132443 7215 0 None - 1 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077