Ligand source activities (1 row/activity)



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 p-value
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Type		 Activity
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 DOI
1185 3701 38 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 667 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 3701 38 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 667 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 3701 38 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 667 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 3701 38 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 667 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 3701 38 None - 1 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 3701 38 None - 1 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 3701 38 None - 1 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 3701 38 None - 1 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 63519 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 63519 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 63568 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 63568 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 138418 0 None - 1 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 138418 0 None - 1 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 168479 0 None - 1 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 168479 0 None - 1 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 63566 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 63566 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 63573 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 63573 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 79613 0 None - 1 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 79613 0 None - 1 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 63518 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 63518 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 63516 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 63516 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 63571 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 63571 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 63569 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 63569 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 63520 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 63520 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 63521 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 63521 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 63572 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 63572 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 63574 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 63574 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
16221494 161952 0 None - 1 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 161952 0 None - 1 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 3313 58 None -3 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 3313 58 None -3 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 3313 58 None -3 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 3313 58 None -3 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 3313 58 None -3 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 63575 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 63575 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 63518 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 63518 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 63519 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 63519 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 178741 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 178741 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 91010 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 91010 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 168475 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 168475 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 168475 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 168475 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 210546 9 None - 1 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 1359 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 1359 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 1359 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 1359 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 1359 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 1359 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 1359 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 1359 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 1359 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 1359 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 1359 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 1359 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
CHEMBL407661 212675 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 188738 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 188738 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 142002 0 None - 1 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 142002 0 None - 1 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
1184 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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 212675 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 210546 9 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 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 210546 9 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 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 213654 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 124657 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 124657 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 213654 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 85558 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 3.9 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 85558 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 3.9 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 170495 3 None - 1 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 170495 3 None - 1 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
16156699 166566 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 166566 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 166359 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 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 166359 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 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 123812 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 123812 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 85523 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 85523 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 166566 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 166566 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 3313 58 None -3 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 3313 58 None -3 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 3313 58 None -3 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 3313 58 None -3 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 3313 58 None -3 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 63515 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 63515 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 168349 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 168349 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 213536 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 176191 0 None - 1 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 176191 0 None - 1 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 213536 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 142747 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 142747 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 168876 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 168876 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 168876 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 168876 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 14566 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 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 14566 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 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 209404 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 209404 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 63520 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 63520 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 63521 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 63521 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 14566 0 None - 1 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 14566 0 None - 1 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 63517 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 63517 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 14566 0 None - 1 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 14566 0 None - 1 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 206271 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 206271 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 158437 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 158437 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 158437 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 158437 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 212743 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 212743 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 142163 0 None - 1 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 142163 0 None - 1 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 169262 0 None - 1 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 169262 0 None - 1 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
53386915 63516 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 63516 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 169321 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 169321 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 212741 8 None - 1 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 212741 8 None - 1 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 96448 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 96448 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 160215 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 160215 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 96448 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 96448 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 212741 8 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 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 212741 8 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 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 63573 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 63573 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
44321964 96419 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 96419 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 96652 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 96652 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 96913 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 96913 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 96652 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 96652 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 212253 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 212253 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 155713 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 155713 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 1545 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 1545 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 1545 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 1545 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 1545 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 95233 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 95233 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
44380487 167579 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 167579 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 161683 0 None - 1 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 161683 0 None - 1 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 209417 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 209417 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 167010 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 167010 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 162130 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 162130 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 161809 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 161809 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 161990 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 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 161990 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 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 168223 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 168223 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 138136 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 138136 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 161697 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 161697 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 138136 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 138136 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 1359 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 1359 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 1359 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 1359 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 1359 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 1359 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 161731 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 161731 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 161731 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 161731 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 160665 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 160665 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 160665 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 160665 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
44398150 96701 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 96701 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 97146 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 97146 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 161966 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 161966 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
44398151 161950 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 161950 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 161326 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 161326 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 3701 38 None - 1 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 3701 38 None - 1 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 3701 38 None - 1 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 3701 38 None - 1 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 107169 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 107169 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 96804 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 96804 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 168955 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 168955 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
44460342 167922 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 167922 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 128663 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 128663 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 63382 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 63382 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 63382 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 3701 38 None - 1 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 3701 38 None - 1 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 3701 38 None - 1 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 3701 38 None - 1 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 168489 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 168489 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 12206 0 None - 1 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 12206 0 None - 1 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 12206 0 None - 1 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 96633 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 96633 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 96633 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 159480 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 159480 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 159480 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 141776 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 141776 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 209597 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 57595 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 57595 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
1179 961 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 961 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 961 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 88526 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 88526 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
145993478 167320 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 167320 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 178526 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 178526 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 128657 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 128657 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 58774 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 58774 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 113058 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 113058 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 162283 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 162283 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
11467552 172711 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 172711 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 189824 0 None - 1 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 189824 0 None - 1 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 109035 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 109035 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 106939 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 106939 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 66738 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 66738 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 59085 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 59085 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 120379 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 120379 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 101174 0 None - 1 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 101174 0 None - 1 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
44451397 95903 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 95903 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 94201 0 None - 1 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 94201 0 None - 1 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 86784 0 None - 1 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 86784 0 None - 1 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 66682 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 66682 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 154938 0 None - 1 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 154938 0 None - 1 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 94319 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 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 94319 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 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 113502 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 113502 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 101596 0 None - 1 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 101596 0 None - 1 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
11237922 65520 0 None - 1 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 65520 0 None - 1 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
44292919 101145 0 None - 1 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 101145 0 None - 1 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 170198 0 None - 1 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 170198 0 None - 1 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
44293164 167831 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 167831 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 105963 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 105963 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 166587 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 166587 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
44361524 168594 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 168594 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 94320 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 94320 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 63515 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 63515 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 166016 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 166016 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 187416 0 None - 1 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 187416 0 None - 1 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 107093 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 107093 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 119948 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 119948 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 161965 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 161965 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 12144 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 12144 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 12144 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
44380212 57618 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 57618 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 150973 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 150973 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 11632 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 11632 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 11632 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 161777 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 161777 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 171899 0 None - 1 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 171899 0 None - 1 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 176475 0 None - 1 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 176475 0 None - 1 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 192627 0 None - 1 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 192627 0 None - 1 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 107139 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 107139 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 98982 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 98982 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 185620 0 None - 1 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 185620 0 None - 1 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 11627 0 None - 1 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 11627 0 None - 1 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 11627 0 None - 1 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 180803 0 None - 1 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 180803 0 None - 1 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
145952400 162735 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 162735 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 162805 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 162805 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
24825725 192627 0 None - 1 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 192627 0 None - 1 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 2323 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 2323 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 2323 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 128666 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 128666 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 101182 0 None - 1 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 101182 0 None - 1 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 188882 0 None - 1 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 188882 0 None - 1 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 79613 0 None - 1 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 79613 0 None - 1 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 162417 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 162417 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
44434435 88562 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 88562 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 180801 0 None - 1 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 180801 0 None - 1 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 175960 0 None - 1 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 175960 0 None - 1 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 175960 0 None - 1 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 90227 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 90227 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 100492 0 None - 1 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 100492 0 None - 1 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 86704 0 None - 1 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 86704 0 None - 1 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 120277 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 120277 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
145973813 163023 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 163023 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
44432656 159158 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 159158 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 154969 0 None - 1 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 154969 0 None - 1 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 162908 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 162908 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
145955260 162534 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 162534 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 128664 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 128664 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 58758 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 58758 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
44293555 101210 0 None - 1 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 101210 0 None - 1 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 155005 0 None - 1 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 155005 0 None - 1 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 161294 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 161294 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
10348973 3313 58 None -3 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 3313 58 None -3 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 3313 58 None -3 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 3313 58 None -3 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 3313 58 None -3 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 178746 0 None - 1 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 178746 0 None - 1 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 185443 0 None - 1 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 185443 0 None - 1 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 122714 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 122714 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 126775 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 126775 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 101290 0 None - 1 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 101290 0 None - 1 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 185443 0 None - 1 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 185443 0 None - 1 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 154702 0 None - 1 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 154702 0 None - 1 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 168064 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 168064 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 128662 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 128662 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 11630 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 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 11630 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 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 11630 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 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
44293592 162890 0 None - 1 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 162890 0 None - 1 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 148073 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 148073 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 168998 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 168998 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 94502 0 None - 1 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 94502 0 None - 1 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
44444642 94370 0 None - 1 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 94370 0 None - 1 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 128655 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 128655 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 166700 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 166700 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 166416 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 166416 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 167153 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 167153 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 128658 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 128658 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 59326 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 59326 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 96561 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 96561 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 210129 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 213783 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 213783 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 210130 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 96783 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 96783 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 96783 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 96783 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 161807 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 161807 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 161807 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 123850 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 123850 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 183999 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 183999 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 155231 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 155231 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
9873212 57576 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 57576 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 58734 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 58734 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 210755 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 210755 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 174190 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 174190 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 155341 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 155341 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 155341 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 164262 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 164262 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 58727 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 58727 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 166078 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 166078 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 166078 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 166078 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 161829 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 161829 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 168498 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 168498 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 210801 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 173650 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 173650 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 2741 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 2741 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 2741 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 2741 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 96848 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 96848 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 50542 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 50542 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 168811 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 168811 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 210630 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 210765 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 210630 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 210765 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
15602804 8081 0 None - 1 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 8081 0 None - 1 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 9744 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 9744 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 128665 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 128665 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
44293484 96716 0 None - 1 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 96716 0 None - 1 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
16221614 136548 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 136548 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 147234 0 None - 1 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 147234 0 None - 1 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 154967 0 None - 1 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 154967 0 None - 1 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 206305 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 206305 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 12198 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 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 12198 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 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 12198 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 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 169402 0 None - 1 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 169402 0 None - 1 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
44561108 186430 0 None - 1 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 186430 0 None - 1 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 94479 0 None - 1 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 94479 0 None - 1 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 94283 0 None - 1 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 94283 0 None - 1 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 162656 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 162656 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 10076 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 10076 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 11636 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 11636 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 11636 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 101554 0 None - 1 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 101554 0 None - 1 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 172627 0 None - 1 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 172627 0 None - 1 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 149467 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 149467 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 161923 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 161923 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
44444675 154722 0 None - 1 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 154722 0 None - 1 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 98093 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 98093 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
44587394 172473 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 172473 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 187194 0 None - 1 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 187194 0 None - 1 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
25193700 173282 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 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 173282 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 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
44444668 154279 0 None - 1 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 154279 0 None - 1 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 168904 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 168904 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
44561369 190468 0 None - 1 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 190468 0 None - 1 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 9777 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 9777 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
54584354 61255 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 61255 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
16221434 97187 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 97187 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
44341199 113059 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 113059 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 97259 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 97259 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 11631 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 11631 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 11631 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
44448991 155341 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 155341 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 155341 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
44434387 152775 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 152775 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 172634 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 172634 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 9564 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 9564 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 86703 0 None - 1 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 86703 0 None - 1 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
44293594 101567 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 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 101567 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 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 188839 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 188839 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
44432641 167503 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 167503 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
25156400 188859 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 188859 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 84771 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 84771 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 59075 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 59075 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
1185 3701 38 None - 1 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 3701 38 None - 1 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 3701 38 None - 1 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 3701 38 None - 1 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
44432640 154973 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 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 154973 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 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 128660 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 128660 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
11496610 4075 13 None 4 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 4075 13 None 4 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 4075 13 None 4 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 4075 13 None 4 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 4075 13 None 4 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 4075 13 None 4 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
44444647 155001 0 None - 1 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 155001 0 None - 1 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
25194090 188928 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 188928 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
44444635 154704 0 None - 1 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 154704 0 None - 1 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 128661 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 128661 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 128668 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 128668 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
16146022 170119 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 170119 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 154721 0 None - 1 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 154721 0 None - 1 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 154883 0 None - 1 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 154883 0 None - 1 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 166331 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 166331 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 162629 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 162629 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 160727 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 160727 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 209416 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 160727 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 160727 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 209416 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 61253 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 61253 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 188437 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 188437 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
CHEMBL2370890 209945 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 96045 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 96045 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 78195 0 None - 1 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 78195 0 None - 1 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 66296 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 66296 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 166822 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 166822 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 166822 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 166822 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 161946 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 161946 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 219 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 219 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
35 219 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 219 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 219 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 208661 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 208661 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 161808 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 161808 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 105941 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 105941 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 120391 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 120391 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 101893 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 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 101893 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 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 78746 0 None - 1 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 78746 0 None - 1 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 151643 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 151643 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 146195 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 146195 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 105965 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 105965 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 57447 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 57447 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 146751 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 146751 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 162312 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 162312 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
44395502 165898 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 165898 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 86740 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 86740 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
44359264 11628 0 None - 1 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 11628 0 None - 1 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 11628 0 None - 1 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
44380796 59203 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 59203 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
44561141 193802 0 None - 1 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 193802 0 None - 1 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 178716 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 178716 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 87755 0 None - 1 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 87755 0 None - 1 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 14566 0 None - 1 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 14566 0 None - 1 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 181892 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 181892 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 146753 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 146753 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 154939 0 None - 1 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 154939 0 None - 1 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
44359456 12204 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 12204 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 12204 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
44434388 89804 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 89804 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 10044 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 10044 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
11477970 89499 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 89499 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 101903 0 None - 1 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 101903 0 None - 1 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 102032 0 None - 1 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 102032 0 None - 1 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 162194 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 162194 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
44215908 94229 0 None - 1 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 94229 0 None - 1 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 136547 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 136547 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 95233 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 95233 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 166994 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 166994 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 8109 0 None - 1 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 8109 0 None - 1 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 106405 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 106405 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 176765 0 None - 1 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 176765 0 None - 1 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 176765 0 None - 1 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 176765 0 None - 1 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 107008 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 107008 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 206270 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 206270 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 99520 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 99520 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 78746 0 None - 1 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 78746 0 None - 1 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 138011 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 138011 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 138011 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 138011 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 882 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 882 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
583 882 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 882 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 882 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 156027 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 156027 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 97359 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 97359 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
44380625 58726 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 58726 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 120314 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 120314 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 161165 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 161165 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 161165 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 161165 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 161935 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 161935 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 57591 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 57591 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 58755 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 58755 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 162659 0 None - 1 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 162659 0 None - 1 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 189022 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 189022 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 167113 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 167113 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
44293376 101675 0 None - 1 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 101675 0 None - 1 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
11583756 189654 0 None - 1 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 189654 0 None - 1 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
11532637 7714 0 None - 1 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 7714 0 None - 1 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
44577103 178745 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 178745 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 87202 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 87202 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 128667 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 128667 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
44380192 57447 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 57447 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 187366 0 None - 1 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 187366 0 None - 1 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 59138 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 59138 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
11604354 187524 0 None - 1 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 187524 0 None - 1 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
44359458 12147 0 None - 1 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 12147 0 None - 1 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 12147 0 None - 1 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
44451342 96465 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 96465 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
44444630 154823 0 None - 1 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 154823 0 None - 1 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
145951481 162955 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 162955 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 189665 0 None - 1 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 189665 0 None - 1 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 189379 0 None - 1 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 189379 0 None - 1 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 94145 0 None - 1 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 94145 0 None - 1 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 58750 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 58750 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 96175 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 96175 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 156673 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 156673 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 161914 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 161914 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 86963 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 86963 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
44434431 88511 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 88511 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 189022 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 189022 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
44432635 86783 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 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 86783 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 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 114534 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 114534 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 156292 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 156292 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
44358962 12143 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 12143 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 12143 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 124346 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 124346 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 210771 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 8107 0 None - 1 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 8107 0 None - 1 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 193121 0 None - 1 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 193121 0 None - 1 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 193121 0 None - 1 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 120191 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 120191 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 120278 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 120278 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 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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 167113 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 167113 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 96980 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 96980 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 155341 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 155341 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 155341 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 161459 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 161459 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 85433 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 85433 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 155682 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 155682 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 97117 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 97117 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 111481 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 111481 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 165296 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 165296 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 111481 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 111481 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 83392 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 83392 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 66798 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 66798 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 120311 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 120311 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 110453 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 110453 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 84406 0 None - 1 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 84406 0 None - 1 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 84406 0 None - 1 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 166832 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 166832 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
44398086 97035 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 97035 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 168980 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 168980 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
44434428 146754 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 146754 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
44293486 187417 0 None - 1 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 187417 0 None - 1 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
44432636 87385 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 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 87385 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 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 205345 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 205345 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
44293274 101256 0 None - 1 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 101256 0 None - 1 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 184266 0 None - 1 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 184266 0 None - 1 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
44293250 101733 0 None - 1 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 101733 0 None - 1 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
44359193 11638 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 11638 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 11638 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
16144515 156127 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 156127 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 99090 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 99090 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 85600 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 85600 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 162858 0 None - 1 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 162858 0 None - 1 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 168849 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 168849 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 9571 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 9571 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 206277 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 206277 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 12203 0 None - 1 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 12203 0 None - 1 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 12203 0 None - 1 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
44380514 120212 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 120212 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 210546 9 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 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 206286 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 206286 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 59292 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 59292 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 212741 8 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 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 212741 8 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 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 143596 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 143596 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 8296 0 None - 1 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 8296 0 None - 1 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 150227 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 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 150227 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 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
44293305 101461 0 None - 1 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 101461 0 None - 1 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
44293165 101693 0 None - 1 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 101693 0 None - 1 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 110578 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 110578 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 163111 0 None - 1 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 163111 0 None - 1 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 188675 0 None - 1 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 188675 0 None - 1 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 146767 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 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 146767 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 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
44561368 176814 0 None - 1 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 176814 0 None - 1 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
44432655 149486 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 149486 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 189654 0 None - 1 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 189654 0 None - 1 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 180226 0 None - 1 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 180226 0 None - 1 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 189010 0 None - 1 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 189010 0 None - 1 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
145952498 162876 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 162876 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 96808 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 96808 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 206189 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 206189 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
10187208 66748 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 66748 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 89808 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 89808 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 90088 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 90088 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
44451356 96363 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 96363 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
16148338 161948 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 161948 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 14566 0 None - 1 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 14566 0 None - 1 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 206406 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 206406 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 159795 0 None - 1 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 159795 0 None - 1 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 168479 0 None - 1 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 168479 0 None - 1 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 161779 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 161779 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 2020 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 2020 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 2020 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 189507 0 None - 1 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 189507 0 None - 1 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 110525 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 110525 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 58759 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 58759 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 58718 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 58718 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 161732 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 161732 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 161804 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 161804 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 96847 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 96847 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 160959 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 160959 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 161803 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 161803 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
9809394 120512 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 120512 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
9809382 100675 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 100675 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 90048 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 90048 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
44573791 187388 0 None - 1 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 187388 0 None - 1 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
44434415 88527 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 88527 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 88748 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 88748 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
44444663 94200 0 None - 1 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 94200 0 None - 1 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
44359287 11635 0 None - 1 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 11635 0 None - 1 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 11635 0 None - 1 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
44359303 11637 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 11637 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 11637 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
44576656 188246 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 188246 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 166754 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 166754 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 166934 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 166934 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 97014 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 97014 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 209946 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 161851 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 161851 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 161851 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 85433 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 85433 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 206242 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 206242 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 12199 0 None - 1 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 12199 0 None - 1 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 12199 0 None - 1 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 101634 0 None - 1 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 101634 0 None - 1 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 163085 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 163085 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 58721 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 58721 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 97022 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 97022 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 9921 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 9921 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 107009 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 107009 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 1359 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 1359 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 1359 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 1359 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 1359 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 1359 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 161311 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 161311 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
44321412 206252 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 206252 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 83440 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 83440 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 162843 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 162843 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 128656 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 128656 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 171415 0 None - 1 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 171415 0 None - 1 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
44432627 148128 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 148128 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
44321695 105981 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 105981 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
44434433 88749 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 88749 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 150972 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 150972 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 161931 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 161931 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 128659 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 128659 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 153594 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 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 153594 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 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 86699 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 86699 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
44185958 154998 0 None - 1 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 154998 0 None - 1 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 162073 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 162073 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 59016 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 59016 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 97141 0 None - 1 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 97141 0 None - 1 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 97170 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 97170 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 167297 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 167297 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 176133 0 None - 1 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 176133 0 None - 1 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 176133 0 None - 1 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 176133 0 None - 1 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 137101 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 137101 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 96875 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 96875 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 137101 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 137101 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 179369 0 None - 1 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 179369 0 None - 1 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 8220 0 None - 1 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 8220 0 None - 1 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 101515 0 None - 1 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 101515 0 None - 1 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
44293134 187401 0 None - 1 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 187401 0 None - 1 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 86771 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 86771 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
44560995 179153 0 None - 1 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 179153 0 None - 1 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 163480 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 163480 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
44293511 101286 0 None - 1 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 101286 0 None - 1 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 155000 0 None - 1 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 155000 0 None - 1 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
44434404 166568 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 166568 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
44359289 12151 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 12151 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 12151 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 160959 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 160959 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 156127 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 156127 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 208661 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 208661 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 209945 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 1359 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 1359 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 1359 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 1359 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 1359 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 1359 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 97170 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 97170 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 161311 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 161311 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 161459 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 161459 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 168849 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 168849 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 219 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 219 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
35 219 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 219 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 219 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 83392 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 83392 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 97014 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 97014 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 161803 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 161803 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 96847 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 96847 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 96875 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 96875 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 97022 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 97022 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 141776 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 141776 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 161732 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 161732 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 882 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 882 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
583 882 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 882 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 882 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 97117 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 97117 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 97359 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 97359 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 210771 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
16148338 161948 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 161948 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 170119 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 170119 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 210801 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 212741 8 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(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 212741 8 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(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 168498 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 168498 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 210546 9 None - 1 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
1184 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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 166832 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 166832 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 189654 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 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL515123 189654 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 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
138978204 166754 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 166754 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 166934 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 166934 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 167320 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 167320 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 961 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 961 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 961 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 166587 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 166587 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 166700 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 166700 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 167153 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 167153 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 166416 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 166416 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 744 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
NoneNone
Drug Central None None None None None
436 744 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
NoneNone
Drug Central None None None None None
50225 744 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
NoneNone
Drug Central None None None None None
CHEMBL2110824 744 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
NoneNone
Drug Central None None None None None
DB06719 744 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
NoneNone
Drug Central None None None None None
3860 744 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
436 744 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
50225 744 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
CHEMBL2110824 744 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
DB06719 744 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
1177 3867 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
25074470 3867 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
2968 3867 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
CHEMBL1201334 3867 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
DB06825 3867 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
1162 1831 0 None 16 3 Human 10.0 pEC50 = 10 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
16132914 1831 0 None 16 3 Human 10.0 pEC50 = 10 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
3860 744 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
436 744 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
50225 744 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
CHEMBL2110824 744 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
DB06719 744 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
1162 1831 0 None -16 3 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
16132914 1831 0 None -16 3 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
3860 744 0 None -2 2 Mouse 9.7 pEC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
436 744 0 None -2 2 Mouse 9.7 pEC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
50225 744 0 None -2 2 Mouse 9.7 pEC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
CHEMBL2110824 744 0 None -2 2 Mouse 9.7 pEC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
DB06719 744 0 None -2 2 Mouse 9.7 pEC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
11250647 1545 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 1545 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 1545 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 1545 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 1545 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
1175 2298 44 None -1 2 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
1559 2298 44 None -1 2 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
657181 2298 44 None -1 2 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
CHEMBL1201199 2298 44 None -1 2 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
DB00007 2298 44 None -1 2 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
10348973 3313 58 None -3 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 3313 58 None -3 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 3313 58 None -3 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 3313 58 None -3 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 3313 58 None -3 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 577 12 None 151 2 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 577 12 None 151 2 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 577 12 None 151 2 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 2323 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 2323 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 2323 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 4075 13 None -4 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 4075 13 None -4 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 4075 13 None -4 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 1832 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1164 1832 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17942747
1164 1832 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19638591
5581 1446 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19638591
11496610 4075 13 None 4 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 4075 13 None 4 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 4075 13 None 4 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 1831 0 None 16 3 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
16132914 1831 0 None 16 3 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1190 882 47 None 6025 3 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
25074887 882 47 None 6025 3 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
583 882 47 None 6025 3 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
CHEMBL1200490 882 47 None 6025 3 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
DB00050 882 47 None 6025 3 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
10231401 2020 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 2020 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 2020 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 2106 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
16130938 2106 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
3854 2106 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
73952264 2106 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
CHEMBL3989438 2106 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
1175 2298 44 None 1 2 Rat 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
1559 2298 44 None 1 2 Rat 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
657181 2298 44 None 1 2 Rat 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
CHEMBL1201199 2298 44 None 1 2 Rat 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
DB00007 2298 44 None 1 2 Rat 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
5583 248 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19638591
10231401 2020 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 2020 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 2020 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 2020 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 2020 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 2020 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 3313 58 None -3 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 3313 58 None 3 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 3313 58 None -3 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 3313 58 None 3 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 3313 58 None -3 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 3313 58 None 3 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 3313 58 None -3 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 3313 58 None 3 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 3313 58 None -3 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 3313 58 None 3 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 2490 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 2490 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 147 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 147 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 147 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 1626 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 1626 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 3589 0 None - 1 Human 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
118856782 3589 0 None - 1 Human 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1173 3898 0 None - 1 Human 6.7 pIC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1172 3874 0 None - 1 Human 7.0 pIC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
16130930 3874 0 None - 1 Human 7.0 pIC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1169 1808 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
123777 1808 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1162 1831 0 None -39 3 Rat 7.7 pIC50 None 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
16132914 1831 0 None -39 3 Rat 7.7 pIC50 None 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
1179 961 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 961 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 961 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 1831 0 None -16 3 Mouse 8.3 pIC50 None 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1328228
16132914 1831 0 None -16 3 Mouse 8.3 pIC50 None 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1328228
1184 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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 1386 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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11563584 139548 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 139548 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 63518 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 63518 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 63568 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 63568 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 78114 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 78114 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 3313 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 3313 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 3313 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 3313 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 3313 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 63520 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 63520 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
53388958 63566 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 63566 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 63571 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 63571 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
10258719 153241 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 153241 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 3701 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 3701 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 3701 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 3701 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 77850 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 77850 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 168479 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 168479 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 3701 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 3701 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 3701 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 3701 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 169321 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 169321 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 3701 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 3701 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 3701 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 3701 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 63516 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 63516 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 63569 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 63569 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 63573 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 63573 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
11700433 77610 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 77610 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 78272 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 78272 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 79613 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 79613 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 138418 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 138418 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 170881 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 170881 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 63521 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 63521 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
67143119 175854 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 175854 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 172252 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 172252 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 172932 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 172932 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 174997 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 174997 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 63515 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 63515 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 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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 75929 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 75929 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 79841 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 79841 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 99017 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 99017 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 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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
44321964 96419 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 96419 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 63515 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 63515 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 63517 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 63517 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 63519 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 63519 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 63567 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 63567 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 63572 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 63572 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 63574 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 63574 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 63575 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 63575 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
1184 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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 13064 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 13064 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 13064 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 79637 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 79637 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 79829 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 79829 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 138225 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 138225 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 138418 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 138418 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 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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 175717 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 175717 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
53387071 63520 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 63520 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
1175 2298 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 2298 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 2298 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 2298 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 2298 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 161981 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 161981 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 63518 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 63518 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 78746 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 78746 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 99049 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 99049 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 124657 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 124657 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 183999 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 183999 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 206271 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 206271 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 9571 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 9571 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 110453 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 110453 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 3701 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 3701 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 3701 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 3701 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 63513 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 63513 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 63514 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 63514 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 63570 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 63570 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 63515 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 63515 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 63516 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 63516 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 100919 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 100919 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 58718 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 58718 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 58726 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 58726 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 58734 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 58734 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 59016 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 59016 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 120314 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 120314 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
1175 2298 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 2298 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 2298 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 2298 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 2298 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
10053165 183999 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 183999 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 183999 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 183999 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 168479 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 168479 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 2298 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 2298 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 2298 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 2298 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 2298 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 173886 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 173886 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 168479 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 168479 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 123812 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 123812 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 170336 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 170336 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
87285473 174090 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 174090 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 162659 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 162659 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 3313 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 3313 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 3313 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 3313 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 3313 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 172223 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 172223 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 162408 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 162408 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
67143773 170505 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 170505 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 171303 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 171303 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 173330 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 173330 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 98642 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 98642 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 99030 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 99030 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 105941 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 105941 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 107009 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 107009 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 206242 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 206242 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
44341082 9777 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 9777 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 10076 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 10076 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 110525 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 110525 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 203438 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 203438 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 57576 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 57576 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 57591 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 57591 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 58727 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 58727 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 96561 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 96561 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 119948 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 119948 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 120212 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 120212 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 120512 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 120512 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
11614283 78125 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 78125 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 139253 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 139253 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 139300 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 139300 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 117299 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 117299 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 170065 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 170065 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
44309572 204339 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 204339 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 14566 0 None - 1 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 14566 0 None - 1 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 170495 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 170495 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 14566 0 None - 1 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 14566 0 None - 1 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 14566 0 None - 1 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 14566 0 None - 1 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 169623 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 169623 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 162858 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 162858 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
44460342 167922 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 167922 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 210989 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 3701 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 3701 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 3701 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 3701 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 63573 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 63573 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 3701 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 3701 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 3701 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 3701 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 14566 0 None - 1 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 14566 0 None - 1 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 100675 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 100675 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 59085 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 59085 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
44293205 183961 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 183961 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 101221 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 101221 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 101825 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 101825 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
44395462 168223 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 168223 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 63521 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 63521 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 176191 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 176191 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 161990 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 161990 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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
9896737 83367 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 83367 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 66296 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 66296 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 66748 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 66748 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 66798 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 66798 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 2020 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 2020 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 2020 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 96808 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 96808 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 164262 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 164262 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 206270 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 206270 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 9744 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 9744 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 113502 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 113502 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 210989 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 170295 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 170295 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 50542 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 50542 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 57433 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 57433 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 58721 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 58721 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 59203 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 59203 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 59326 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 59326 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 120391 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 120391 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
44412890 78310 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 78310 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 186746 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 186746 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 3701 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 3701 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 3701 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 3701 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
87285708 173905 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 173905 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 170163 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 170163 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 165898 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 165898 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 111481 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 111481 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 206305 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 206305 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 109035 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 109035 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 113058 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 113058 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 205345 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 205345 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 100618 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 100618 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 58755 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 58755 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 59075 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 59075 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 111481 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 111481 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 120191 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 120191 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
44293045 185824 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 185824 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 187189 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 187189 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 162692 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 162692 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
44395491 123850 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 123850 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 206252 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 206252 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 206406 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 206406 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 9564 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 9564 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 114534 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 114534 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 213689 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 63519 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 63519 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 84406 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 84406 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 84406 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 57595 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 57595 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
1175 2298 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 2298 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 2298 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 2298 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 2298 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
44395583 124346 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 124346 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 9921 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 9921 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 113059 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 113059 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 168479 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 168479 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 193121 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 193121 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 193121 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 58774 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 58774 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 120278 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 120278 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 79613 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 79613 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
44293222 175960 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 175960 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 175960 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 193121 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 193121 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 193121 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 174874 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 174874 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 171467 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 171467 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 99021 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 99021 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 99029 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 99029 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 96848 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 96848 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 106939 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 106939 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 107008 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 107008 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 210989 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 170269 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 170269 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 175426 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 175426 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 168479 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 168479 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
44412945 96706 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 96706 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 175532 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 175532 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 171026 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 171026 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
11167850 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 213689 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 3701 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 3701 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 3701 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 3701 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 170742 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 170742 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 173196 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 173196 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 174877 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 174877 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 168479 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 168479 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 120277 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 120277 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 120379 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 120379 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 167579 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 167579 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 162445 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 162445 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 176907 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 176907 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 171516 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 171516 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 107169 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 107169 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 210989 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 3701 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 3701 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 3701 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 3701 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 210989 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 171361 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 171361 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 174328 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 174328 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 3701 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 3701 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 3701 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 3701 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
145953172 162472 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 162472 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 213189 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 172230 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 172230 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 106405 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 106405 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 210989 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 210989 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 210989 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 3701 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 3701 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 3701 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 3701 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 210989 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
CHEMBL415547 213189 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 66738 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 66738 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 185443 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 185443 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 206189 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 206189 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 3701 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 3701 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 3701 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 3701 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 11627 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 11627 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 11627 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
67143570 171757 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 171757 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 161683 0 None - 0 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 161683 0 None - 0 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 213689 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 174576 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 174576 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 59292 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 59292 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
44593425 176765 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 176765 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 210989 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 210989 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 3701 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 3701 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 3701 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 3701 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 77626 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 77626 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 77626 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 176191 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 176191 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
44593425 176765 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 176765 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 176765 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 176765 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 210989 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 210989 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 210989 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 210989 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 174615 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 174615 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
44402640 161830 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 161830 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 210989 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 210989 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 3701 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 3701 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 3701 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 3701 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 210989 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 176044 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 176044 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 179369 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 179369 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 11628 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 11628 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 11628 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
44293081 182704 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 182704 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 155229 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 155229 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 186312 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 186312 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 213689 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 210989 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 213689 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 210989 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 3701 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 3701 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 3701 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 3701 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 101182 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 101182 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 58750 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 58750 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
67143612 171050 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 171050 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 155229 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 155229 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 158526 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 158526 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 161830 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 161830 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 179578 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 179578 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 180015 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 180015 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
44573110 187194 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 187194 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 193238 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 193238 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 3701 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 3701 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 3701 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 3701 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 134342 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 134342 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 178746 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 178746 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 170289 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 170289 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 172504 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 172504 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 3701 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 3701 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 3701 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 3701 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 203331 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 203331 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 122195 0 None - 1 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 122195 0 None - 1 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 213785 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 101218 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 101218 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
11980076 208453 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 208453 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 213689 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 213689 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 213955 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 213689 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 134342 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 134342 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 134342 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 134342 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 12204 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 12204 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 12204 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
10930638 99029 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 99029 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
11599857 76878 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 76878 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 79725 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 79725 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
10837806 78026 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 78026 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 180543 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 180543 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 134342 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 134342 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
67142732 169623 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 169623 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 141923 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 141923 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 171540 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 171540 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 172932 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 172932 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 180825 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 180825 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
162673323 183116 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 183116 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 116187 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 116187 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 3701 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 3701 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 3701 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 3701 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 173116 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 173116 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 3701 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 3701 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 3701 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 3701 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 134342 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 134342 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
67143633 173310 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 173310 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
44573275 187415 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 187415 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 134342 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 134342 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 134342 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 134342 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 101174 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 101174 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
44406776 134342 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 134342 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 210989 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 134342 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 134342 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 163022 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 163022 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 134342 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 134342 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
44346397 114498 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 114498 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 3701 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 3701 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 3701 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 3701 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 11638 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 11638 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 11638 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
70697569 77974 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 77974 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
44346398 14538 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 14538 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 141618 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 141618 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 113743 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 113743 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 96502 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 96502 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 65591 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 65591 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 166366 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 166366 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
11619758 173214 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 173214 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
67144335 169838 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 169838 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 3701 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 3701 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 3701 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 3701 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 183214 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 183214 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
67143413 169617 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 169617 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
44573789 187340 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 187340 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 4075 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 4075 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 4075 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
53238728 170674 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 170674 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 4075 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 4075 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 4075 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 3701 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 3701 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 3701 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 3701 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
1185 3701 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 3701 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 3701 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 3701 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 213689 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 171467 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 171467 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 213689 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
25194091 189010 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 189010 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 189665 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 189665 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 3701 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 3701 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 3701 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 3701 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
44402647 69829 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 69829 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
11237922 65520 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 65520 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 65520 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 65520 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 189876 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 189876 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 141618 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 141618 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
87285767 174877 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 174877 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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
162652474 180451 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 180451 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 169862 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 169862 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 170495 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 170495 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 180229 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 180229 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 99029 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 99029 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 134342 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 134342 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 210989 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 210989 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 171170 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 171170 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 134342 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 134342 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 210989 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 173027 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 173027 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
44402467 170656 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 170656 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
25194090 188928 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 188928 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 14538 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 14538 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
123549935 179434 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 179434 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 179859 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 179859 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 94201 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 94201 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 210460 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 180513 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 180513 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 183431 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 183431 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 134342 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 134342 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
53238731 170976 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 170976 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
67144408 175909 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 175909 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 171105 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 171105 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 134342 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 134342 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 174129 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 174129 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 183007 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 183007 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
15462666 96502 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 96502 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 141618 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 141618 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 141923 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 141923 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
44391574 66090 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 66090 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 182525 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 182525 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
71666542 180347 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 180347 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 171361 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 171361 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 3701 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 3701 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 3701 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 3701 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 180218 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 180218 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
CHEMBL436874 213689 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
10930638 99029 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 99029 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 11631 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 11631 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 11631 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
44406776 134342 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 134342 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 210989 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 134342 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 134342 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 134342 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 134342 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 210989 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 57447 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 57447 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 134342 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 134342 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 134342 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 134342 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 74188 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 74188 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 134342 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 134342 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 134342 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 134342 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
44391718 65605 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 65605 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
162645007 179461 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 179461 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
44560995 179153 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 179153 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 113519 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 113519 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 99029 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 99029 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 71411 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 71411 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
67143374 171741 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 171741 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 179461 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 179461 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 183408 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 183408 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
71668147 179990 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 179990 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 116186 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 116186 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
145957339 162309 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 162309 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 180801 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 180801 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
44406776 134342 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 134342 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 172252 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 172252 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 213689 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 59138 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 59138 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 74187 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 74187 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 77626 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 77626 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 77626 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 213689 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 134342 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 134342 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 113743 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 113743 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
44402560 71436 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 71436 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 132820 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 132820 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
11330164 65203 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 65203 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 14538 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 14538 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 113743 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 113743 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 113519 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 113519 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 96502 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 96502 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
162673323 183116 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 183116 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 154702 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 154702 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 134342 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 134342 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 174522 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 174522 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 94479 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 94479 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 171105 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 171105 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
145955182 162412 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 162412 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
44406776 134342 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 134342 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 174522 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 174522 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 134342 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 134342 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 134342 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 134342 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
67143397 172146 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 172146 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
44444642 94370 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 94370 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 9388 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 9388 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 9388 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 9388 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 71678 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 71678 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
11720984 63479 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 63479 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
44346667 113743 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 113743 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
118167818 179432 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 179432 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
44444672 169402 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 169402 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 182199 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 182199 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 154967 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 154967 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 170505 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 170505 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 94502 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 94502 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 180336 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 180336 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 181300 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 181300 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 180015 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 180015 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
11634198 187366 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 187366 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 187597 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 187597 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
11634198 187366 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 187366 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 101596 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 101596 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
11525693 69830 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 69830 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 213689 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 171540 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 171540 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 74188 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 74188 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 210989 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 71616 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 71616 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 140273 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 140273 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 166022 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 166022 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
44417615 141923 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 141923 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 180543 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 180543 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 180451 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 180451 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 176044 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 176044 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 94283 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 94283 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 213689 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 193262 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 193262 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
67142711 172023 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 172023 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 162097 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 162097 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 134342 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 134342 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 3701 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 3701 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 3701 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 3701 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 141618 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 141618 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 12205 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 12205 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 12205 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 60475 0 None - 1 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 60475 0 None - 1 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 98186 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 98186 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 167486 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 167486 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
15462666 96502 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 96502 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 14538 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 14538 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 14538 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 14538 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 132757 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 132757 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 122954 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 122954 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
1185 3701 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 3701 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 3701 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 3701 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 213689 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 171026 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 171026 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 3701 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 3701 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 3701 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 3701 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 154998 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 154998 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 122714 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 122714 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 126775 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 126775 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 57433 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 57433 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
CHEMBL3085508 210989 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 3701 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 3701 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 3701 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 3701 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 94320 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 94320 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 171741 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 171741 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 175780 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 175780 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 12203 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 12203 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 12203 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
44413066 78404 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 78404 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 96761 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 96761 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 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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
44292869 177022 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 177022 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 101625 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 101625 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 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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 107093 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 107093 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 210989 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 210989 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 210989 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 210989 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 168479 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 168479 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 58759 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 58759 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 168489 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 168489 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 210989 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 213689 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
44402518 158526 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 158526 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 3701 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 3701 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 3701 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 3701 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 8107 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 8107 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 162256 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 162256 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 11635 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 11635 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 11635 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 100492 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 100492 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
44292939 101402 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 101402 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 169092 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 169092 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 176208 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 176208 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 213689 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 210989 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 213689 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 213689 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 210989 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 57618 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 57618 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
CHEMBL407619 212671 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 3701 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 3701 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 3701 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 3701 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 213689 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 210989 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 169092 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 169092 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 212671 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 175019 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 175019 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 163480 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 163480 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 210989 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 213689 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 210989 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 210989 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 175865 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 175865 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 210989 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 213689 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 12147 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 12147 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 12147 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 122557 0 None - 1 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 122557 0 None - 1 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 122557 0 None - 1 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 172627 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 172627 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
44402398 96979 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 96979 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 170495 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 170495 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 210989 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 213689 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 213689 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 162908 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 162908 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 12198 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 12198 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 12198 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 180020 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 180020 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 182070 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 182070 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 79775 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 79775 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 98893 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 98893 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 99394 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 99394 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
44573628 193217 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 193217 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 141618 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 141618 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 170360 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 170360 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 99029 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 99029 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 100617 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 100617 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 110501 0 None - 1 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 110501 0 None - 1 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 161662 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 161662 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 162183 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 162183 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 134342 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 134342 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
44274228 98674 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 98674 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 98706 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 98706 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 99152 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 99152 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 114498 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 114498 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
11692806 79816 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 79816 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 79850 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 79850 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
44346667 113743 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 113743 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 114498 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 114498 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 21613 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 21613 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 78034 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 78034 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
10624976 21613 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 21613 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
44406776 134342 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 134342 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 170360 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 170360 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 182476 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 182476 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 577 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 577 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 577 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 182018 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 182018 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 577 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 577 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 577 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 105965 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 105965 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 187556 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 187556 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 187683 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 187683 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 180226 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 180226 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 71529 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 71529 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
44406776 134342 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 134342 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 113519 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 113519 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 113743 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 113743 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
44402670 71958 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 71958 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 133268 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 133268 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
44417615 141923 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 141923 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 141317 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 141317 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 168275 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 168275 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
67143509 170065 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 170065 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 171609 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 171609 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 172223 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 172223 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 172152 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 172152 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
91810333 179578 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 179578 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 187685 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 187685 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 99029 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 99029 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 65595 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 65595 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 134342 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 134342 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 210458 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 74187 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 74187 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 173282 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 173282 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 99029 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 99029 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
44391516 64373 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 64373 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
71623059 180825 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 180825 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 134342 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 134342 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 172378 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 172378 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 180874 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 180874 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 134342 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 134342 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
44573713 192889 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 192889 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 168479 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 168479 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 12211 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 12211 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 12211 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 162890 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 162890 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 135221 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 135221 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
44406776 134342 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 134342 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 171303 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 171303 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 134342 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 134342 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 3701 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 3701 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 3701 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 3701 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
44346667 113743 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 113743 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 65675 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 65675 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
44346667 113743 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 113743 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 116187 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 116187 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 94229 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 94229 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 181181 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 181181 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
44572287 180803 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 180803 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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 3701 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
44406776 134342 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 134342 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 175706 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 175706 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 3701 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 3701 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 3701 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 3701 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 134342 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 134342 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 141923 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 141923 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 3701 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 3701 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 3701 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 3701 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 114498 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 114498 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 113743 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 113743 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
CHEMBL4564312 214012 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 113743 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 113743 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 3701 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 3701 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 3701 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 3701 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 66682 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 66682 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 182070 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 182070 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 94145 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 94145 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 182714 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 182714 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 183491 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 183491 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
87285565 170269 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 170269 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
44402072 71739 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 71739 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 65611 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 65611 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
162670223 182571 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 182571 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 180229 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 180229 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 187598 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 187598 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 189654 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 189654 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 168479 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 168479 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 99029 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 99029 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 213689 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 210459 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 175854 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 175854 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 141131 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 141131 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 166304 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 166304 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 114498 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 114498 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 173330 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 173330 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 213689 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 183431 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 183431 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 577 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 577 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 577 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
44573626 187532 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 187532 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 192862 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 192862 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 134342 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 134342 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
12784 577 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 577 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 577 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
44402472 132821 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 132821 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 134342 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 134342 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 134342 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 134342 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 57447 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 57447 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 175717 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 175717 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 174090 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 174090 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
44402589 125172 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 125172 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 63498 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 63498 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 94200 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 94200 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 134342 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 134342 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 134342 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 134342 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
118179051 180218 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 180218 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
9961721 168479 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 168479 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 12141 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 12141 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 12141 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
44402256 136279 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 136279 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 173310 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 173310 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 134342 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 134342 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
44402431 71413 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 71413 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
44391548 66033 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 66033 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
145948856 167482 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 167482 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
44573277 187446 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 187446 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 113743 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 113743 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
44406776 134342 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 134342 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 175780 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 175780 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
44359312 12201 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 12201 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 12201 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 3701 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 3701 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 3701 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 3701 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 210989 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 100749 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 100749 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 102684 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 102684 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 58758 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 58758 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
CHEMBL436874 213689 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 213689 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 213689 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 213689 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 172878 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 172878 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
44402398 96979 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 96979 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 161258 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 161258 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 210989 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 210989 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 12199 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 12199 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 12199 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
86275342 116186 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 116186 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 168064 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 168064 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 210989 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 213689 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 210989 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 210989 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 210989 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 213689 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
11167850 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 213689 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 189507 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 189507 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 161258 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 161258 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 213689 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 213689 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 11630 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 11630 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 11630 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 188675 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 188675 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 120311 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 120311 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 134342 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 134342 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 213689 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 210989 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 134342 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 134342 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 134342 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 134342 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 213689 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 172952 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 172952 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 210989 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 210989 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 213689 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 210989 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 213689 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 170641 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 170641 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 12206 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 12206 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 12206 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 213689 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 184085 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 184085 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
15462663 99047 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 99047 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
44417614 141618 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 141618 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 203408 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 203408 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 78110 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 78110 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 78115 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 78115 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
9873394 79919 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 79919 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 139088 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 139088 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 139229 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 139229 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
44391499 65933 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 65933 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
15462666 96502 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 96502 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
162667361 182525 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 182525 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 183408 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 183408 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
44573586 187501 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 187501 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 113743 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 113743 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 99029 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 99029 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 71885 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 71885 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
CHEMBL436874 213689 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 180229 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 180229 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
44359301 11636 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 11636 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 11636 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 12144 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 12144 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 12144 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 181892 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 181892 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 188839 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 188839 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
44406776 134342 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 134342 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
44359303 11637 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 11637 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 11637 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 122135 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 122135 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 124953 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 124953 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
67144370 174615 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 174615 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 171516 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 171516 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 187270 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 187270 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 154939 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 154939 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
11671279 130884 0 None - 1 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 130884 0 None - 1 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 126184 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 126184 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
44561105 186751 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 186751 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 141923 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 141923 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 14538 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 14538 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 71194 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 71194 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 155001 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 155001 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 154938 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 154938 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 181935 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 181935 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
11294792 63288 0 None - 1 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 63288 0 None - 1 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 174161 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 174161 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 175426 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 175426 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 64882 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 64882 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 155000 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 155000 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 182136 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 182136 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 154883 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 154883 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
CHEMBL436874 213689 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 170146 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 170146 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 171609 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 171609 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
44417615 141923 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 141923 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 133443 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 133443 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 170336 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 170336 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 8364 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 8364 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 8364 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 8364 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 181300 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 181300 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
44293274 101256 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 101256 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 101567 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 101567 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 187401 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 187401 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
CHEMBL2430900 210461 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 175069 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 175069 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 124803 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 124803 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 114498 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 114498 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 179461 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 179461 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 187531 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 187531 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
44402553 71433 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 71433 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 213689 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
10919052 113519 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 113519 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 154279 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 154279 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 173196 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 173196 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 179926 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 179926 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
11518185 187688 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 187688 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 99029 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 99029 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
44406776 134342 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 134342 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 113519 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 113519 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 141618 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 141618 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 113519 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 113519 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 64300 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 64300 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
CHEMBL436874 213689 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
1184 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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 168602 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 168602 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
CHEMBL3085508 210989 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 210989 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 213689 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 213689 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 174047 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 174047 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 66076 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 66076 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 3701 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 3701 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 3701 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 3701 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 8081 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 8081 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 105963 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 105963 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 213689 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 210989 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 110578 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 110578 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 213689 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 210989 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 213689 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 206277 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 206277 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 206286 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 206286 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 213689 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 134342 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 134342 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
44593424 176133 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 176133 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 213689 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 176133 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 176133 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
44346397 114498 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 114498 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 168479 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 168479 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 168479 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 168479 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 12143 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 12143 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 12143 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
44413009 79765 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 79765 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
44274327 82183 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 82183 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 82826 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 82826 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 99029 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 99029 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 99029 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 99029 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 114498 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 114498 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 77490 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 77490 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 77668 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 77668 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
44391784 122326 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 122326 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
44417614 141618 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 141618 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 113519 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 113519 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
67143420 162908 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 162908 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 167484 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 167484 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 116186 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 116186 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 180218 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 180218 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
44402645 169124 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 169124 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 213689 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 134342 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 134342 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 133434 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 133434 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 174328 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 174328 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 179990 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 179990 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 175399 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 175399 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
44402463 127524 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 127524 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 213689 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 182199 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 182199 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 116188 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 116188 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 187342 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 187342 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
44402293 71428 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 71428 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 182070 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 182070 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 8109 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 8109 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 141923 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 141923 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 113743 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 113743 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 180020 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 180020 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
44359224 11629 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 11629 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 11629 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 101693 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 101693 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
44346397 114498 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 114498 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
44561142 186703 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 186703 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 114498 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 114498 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
44573791 187388 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 187388 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 162802 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 162802 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 134342 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 134342 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 134342 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 134342 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 181181 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 181181 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
15602807 8220 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 8220 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
44402499 69823 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 69823 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 134342 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 134342 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 3701 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 3701 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 3701 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 3701 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
162647697 179859 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 179859 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 169601 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 169601 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
67144478 170351 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 170351 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 134342 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 134342 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 213689 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
44417615 141923 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 141923 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 166021 0 None - 1 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 166021 0 None - 1 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 122939 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 122939 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
11226753 63344 0 None - 1 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 63344 0 None - 1 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 134342 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 134342 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 173905 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 173905 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 162305 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 162305 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
44391628 65872 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 65872 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 168673 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 168673 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 169601 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 169601 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 154969 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 154969 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 173488 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 173488 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 203415 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 203415 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 122333 1 None - 1 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 122333 1 None - 1 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 101145 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 101145 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
67143432 172127 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 172127 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 187613 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 187613 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 210989 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 210989 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 210989 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 3701 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 3701 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 3701 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 3701 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 105981 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 105981 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 210989 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
155531714 176191 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 176191 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 134342 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 134342 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 213689 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 162905 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 162905 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 116189 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 116189 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 189824 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 189824 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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
44321510 107139 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 107139 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 213689 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 171899 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 171899 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 190468 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 190468 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 213689 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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
44295630 190828 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 190828 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 213689 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 192627 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 192627 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 213689 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
15462657 80223 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 80223 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
25193798 170198 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 170198 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 168479 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 168479 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
CHEMBL436874 213689 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 210989 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
44417614 141618 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 141618 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 113519 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 113519 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
11570616 78306 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 78306 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 79758 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 79758 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
11167850 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 14538 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 14538 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 141923 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 141923 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 139334 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 139334 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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
67144162 175053 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 175053 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
44346397 114498 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 114498 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 113743 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 113743 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 213689 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
11167850 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 141923 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 141923 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 175019 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 175019 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
67143487 170763 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 170763 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 179434 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 179434 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 183007 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 183007 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
162665107 182136 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 182136 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 113519 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 113519 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
86275342 116186 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 116186 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
67143432 172127 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 172127 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 137465 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 137465 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 154721 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 154721 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
44293164 167831 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 167831 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
118179174 182476 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 182476 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 172952 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 172952 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 181154 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 181154 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 154704 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 154704 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
44406776 134342 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 134342 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 179461 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 179461 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 187447 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 187447 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
44293285 162775 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 162775 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 71938 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 71938 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 63767 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 63767 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 134342 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 134342 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 179461 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 179461 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 71635 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 71635 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
11583388 8290 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 8290 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 114498 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 114498 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 180229 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 180229 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 193802 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 193802 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 166120 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 166120 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 183214 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 183214 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 137542 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 137542 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
10930638 99029 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 99029 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 134342 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 134342 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 3701 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 3701 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 3701 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 3701 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
10674894 25540 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 25540 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 213785 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 25540 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 25540 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
44321497 98093 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 98093 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 213689 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 176475 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 176475 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 162070 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 162070 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 62888 0 None - 1 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 62888 0 None - 1 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 3701 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 3701 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 3701 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 3701 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 161679 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 161679 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 161867 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 161867 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 170495 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 170495 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 161867 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 161867 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 210989 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 213689 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 111221 0 None - 1 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 111221 0 None - 1 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 170327 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 170327 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 178746 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 178746 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 213689 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 7714 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 7714 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 134342 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 134342 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 172309 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 172309 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 161679 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 161679 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 171757 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 171757 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 180825 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 180825 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
9961721 168479 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 168479 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 168479 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 168479 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 14566 0 None - 1 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 14566 0 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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
44406776 134342 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 134342 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 213689 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
15462666 96502 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 96502 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 141618 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 141618 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
44402378 69676 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 69676 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
44417614 141618 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 141618 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 173153 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 173153 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 182571 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 182571 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
44402464 169089 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 169089 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 133564 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 133564 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 173719 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 173719 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
44402538 168435 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 168435 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
145954593 162533 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 162533 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 134342 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 134342 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
44406776 134342 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 134342 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
44561265 173108 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 173108 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
44402462 69905 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 69905 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 173886 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 173886 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
71666542 180347 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 180347 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 213689 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 171305 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 171305 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 171239 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 171239 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 170768 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 170768 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 133439 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 133439 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 168503 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 168503 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 213689 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 179461 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 179461 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
44391526 122606 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 122606 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 116188 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 116188 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 181935 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 181935 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 187686 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 187686 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
44402465 135235 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 135235 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 162714 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 162714 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 210989 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 122618 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 122618 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
44444644 154999 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 154999 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
24825725 192627 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 192627 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 102769 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 102769 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 175960 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 175960 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 175960 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 187342 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 187342 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 9388 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 9388 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
67144646 173137 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 173137 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 174883 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 174883 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 171415 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 171415 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 169617 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 169617 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 210989 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 77653 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 77653 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 187524 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 187524 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 2741 28 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 495 7 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 2741 28 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 495 7 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 2741 28 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 495 7 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 2741 28 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 495 7 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 162597 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 162597 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 210989 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 134342 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 134342 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 210989 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 210989 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
44417614 141618 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 141618 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 141618 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 141618 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 116553 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 116553 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
10722009 116553 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 116553 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
15462665 168659 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 168659 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 77910 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 77910 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
11512807 140136 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 140136 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 187554 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 187554 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
10919052 113519 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 113519 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
44346398 14538 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 14538 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
127036774 137509 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 137509 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
145949556 162933 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 162933 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 174123 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 174123 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
44444649 155005 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 155005 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
44391821 65581 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 65581 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 171269 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 171269 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
11318649 64354 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 64354 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
118179169 179926 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 179926 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 180874 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 180874 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
44444628 94319 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 94319 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 71136 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 71136 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
44593415 189379 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 189379 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 187416 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 187416 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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
11592658 79751 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 79751 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 213689 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 10044 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 10044 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 213689 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
1185 3701 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 3701 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 3701 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 3701 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 210989 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 176814 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 176814 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 134342 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 134342 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 134342 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 134342 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 169834 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 169834 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 98673 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 98673 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 173401 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 173401 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 189379 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 189379 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 99029 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 99029 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 141923 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 141923 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
44406776 134342 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 134342 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 65227 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 65227 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 187471 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 187471 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 122337 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 122337 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
86275343 183491 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 183491 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
67143612 171050 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 171050 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 12151 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 12151 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 12151 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
11167850 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 182018 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 182018 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
44406776 134342 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 134342 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
44444675 154722 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 154722 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 70207 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 70207 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
44391670 64692 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 64692 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 170295 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 170295 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 174997 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 174997 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
145949399 162734 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 162734 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 168479 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 168479 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 11632 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 11632 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 11632 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 138946 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 138946 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 78746 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 78746 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 77653 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 77653 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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
CHEMBL3085508 210989 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 134342 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 134342 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 210989 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 3701 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 3701 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 3701 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 3701 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 210989 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 8296 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 8296 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 180825 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 180825 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 182018 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 182018 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 187240 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 187240 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
44417614 141618 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 141618 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 114498 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 114498 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
118178989 181154 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 181154 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 182714 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 182714 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 169834 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 169834 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 116189 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 116189 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
1185 3701 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 3701 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 3701 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 3701 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
10919052 113519 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 113519 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 186430 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 186430 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 213689 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 154823 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 154823 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
11167850 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 71297 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 71297 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 179432 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 179432 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 180218 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 180218 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
1190 882 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 882 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
583 882 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 882 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 882 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
CHEMBL2370807 209923 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
CHEMBL266716 210694 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
CHEMBL2370809 209925 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 3313 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 3313 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 3313 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 3313 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 3313 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
CHEMBL2370818 209927 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
CHEMBL2370808 209924 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
10348973 3313 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 3313 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 3313 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 3313 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 3313 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 209922 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 209926 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
11250647 1545 46 None - 1 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 1545 46 None - 1 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 1545 46 None - 1 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 1545 46 None - 1 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 1545 46 None - 1 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
11250647 1545 46 None - 1 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 1545 46 None - 1 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 1545 46 None - 1 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 1545 46 None - 1 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 1545 46 None - 1 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
12784 577 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 577 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 577 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
12784 577 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 577 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 577 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
CHEMBL405548 212565 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
11364940 178525 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 178525 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 3701 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 3701 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 3701 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 3701 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 3733 36 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 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 3733 36 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 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 3733 36 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 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
1184 3733 36 None - 1 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 3733 36 None - 1 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 3733 36 None - 1 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
CHEMBL438897 213804 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)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
CHEMBL269726 210804 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
44449120 95233 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 95233 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
CHEMBL441208 213886 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
44267907 16331 0 None 1 2 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 16331 0 None 1 2 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 16331 0 None 1 2 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 16331 0 None 1 2 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
44448991 155341 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 155341 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 155341 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
9872676 78195 0 None 1479 16 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 78195 0 None 1479 16 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
10649568 14566 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 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 14566 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 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 168479 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 168479 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
11376252 69370 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 69370 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 69370 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 69370 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
11421412 178741 15 None - 1 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 178741 15 None - 1 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 166240 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 166240 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 178741 15 None - 1 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 178741 15 None - 1 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
11167850 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 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 495 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 2741 28 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 495 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 2741 28 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 495 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 2741 28 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 495 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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
11443711 10132 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 10132 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 114498 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 114498 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
44400235 168431 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 168431 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 122557 0 None - 1 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 122557 0 None - 1 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 122557 0 None - 1 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 96045 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 96045 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
44400235 168431 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 168431 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 168431 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 168431 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 168431 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 168431 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 168431 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 168431 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
10345138 122557 0 None - 1 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 122557 0 None - 1 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 122557 0 None - 1 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 155341 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 155341 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 155341 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 122557 0 None - 1 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 122557 0 None - 1 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 122557 0 None - 1 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
44451355 158166 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 158166 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
10985312 78746 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 78746 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 78746 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 78746 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
44288080 160188 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 160188 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
44400245 126081 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 126081 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 126081 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 126081 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 1545 46 None - 1 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 1545 46 None - 1 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 1545 46 None - 1 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 1545 46 None - 1 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 1545 46 None - 1 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 69328 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 69328 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
11365653 174190 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 174190 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 160908 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 160908 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
11477988 91010 0 None - 1 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 91010 0 None - 1 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 91010 0 None - 1 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 91010 0 None - 1 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 67462 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 67462 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 20270 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 20270 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 188437 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 188437 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 173650 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 173650 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 109118 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 109118 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
9809065 101631 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 101631 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 10231 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 10231 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 19752 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 19752 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 10231 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 10231 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 67462 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 67462 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
11331001 189022 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 189022 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 173046 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 173046 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 174190 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 174190 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 189022 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 189022 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 188738 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 188738 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 158324 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 158324 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 134014 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 134014 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 134014 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 134014 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
11262242 188738 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 188738 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 89808 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 89808 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
44400229 68683 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 68683 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
44287759 96697 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 96697 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
11168776 63610 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 63610 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 67801 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 67801 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
9854500 102272 0 None -1 2 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 102272 0 None -1 2 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 102272 0 None -1 2 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 102272 0 None -1 2 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 102272 0 None -1 2 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 102272 0 None -1 2 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 189022 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 189022 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 188196 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 188196 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 21047 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 21047 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 66920 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 66920 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 14138 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 14138 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
44435979 88541 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 88541 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 88732 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 88732 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 161681 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 161681 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 15252 0 None - 1 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 15252 0 None - 1 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 173256 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 173256 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 114809 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 114809 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 128678 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 128678 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 128678 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 62593 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 62593 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 20190 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 20190 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 114809 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 114809 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 102669 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 102669 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 88497 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 88497 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 61017 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 61017 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 61017 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 95844 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 95844 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 16313 0 None - 1 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 16313 0 None - 1 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
44340637 9579 0 None - 1 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 9579 0 None - 1 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 111096 0 None - 1 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 111096 0 None - 1 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 15459 0 None - 1 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 15459 0 None - 1 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 85665 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 85665 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
9807700 187302 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 187302 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 113806 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 113806 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 102634 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 102634 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 60479 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 60479 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 16441 0 None - 1 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 16441 0 None - 1 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
12986401 187641 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 187641 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 189408 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 189408 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 84400 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 84400 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 188659 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 188659 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 63246 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 63246 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 203874 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 203874 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 203906 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 203906 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 188659 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 188659 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 16445 0 None - 1 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 16445 0 None - 1 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 59666 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 59666 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 203141 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 203141 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 63838 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 63838 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 188053 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 188053 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 63024 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 63024 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 63024 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 203175 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 203175 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 158175 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 158175 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
44267876 98106 0 None - 1 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 98106 0 None - 1 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 204256 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 204256 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 9542 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 9542 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 10572 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 10572 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 11022 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 11022 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
25156946 188369 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 188369 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 85088 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 85088 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 63344 0 None - 1 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 63344 0 None - 1 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 111221 0 None - 1 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 111221 0 None - 1 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 124344 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 124344 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 67573 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 67573 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
44387880 60538 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 60538 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 60602 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 60602 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 132407 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 132407 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
44352734 18515 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 18515 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 164812 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 164812 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 123022 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 123022 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 123022 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
44340631 9508 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 9508 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
11763365 101203 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 101203 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
44309440 102634 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 102634 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
44389652 166024 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 166024 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
44435817 89104 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 89104 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
44577101 178527 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 178527 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 99090 0 None - 1 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 99090 0 None - 1 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 63349 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 63349 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 166086 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 166086 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 60475 0 None - 1 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 60475 0 None - 1 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 11182 0 None - 1 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 11182 0 None - 1 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 100228 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 100228 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 89712 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 89712 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 101959 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 101959 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 89712 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 89712 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 21808 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 21808 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 122925 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 122925 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 127505 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 127505 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 102248 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 102248 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 203665 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 203665 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
21045818 113096 0 None - 1 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 113096 0 None - 1 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
44436014 88586 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 88586 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 147573 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 147573 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 102990 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 102990 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
44577097 178491 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 178491 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 63408 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 63408 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 63408 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 115215 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 115215 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 116786 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 116786 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 96785 0 None - 1 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 96785 0 None - 1 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 66182 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 66182 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 114530 0 None - 1 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 114530 0 None - 1 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
11283517 95454 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 95454 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 95454 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 95454 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 123052 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 123052 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 123052 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
44312724 12400 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 12400 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 12400 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 203743 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 203743 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 161914 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 161914 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 14163 0 None - 1 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 14163 0 None - 1 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 167139 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 167139 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 67658 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 67658 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 203905 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 203905 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 147043 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 147043 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
11249167 90300 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 90300 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
44435979 88541 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 88541 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 90300 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 90300 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 84771 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 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 84771 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 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 90300 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 90300 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 123119 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 123119 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 63610 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 63610 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 66110 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 66110 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 58097 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 58097 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 96505 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 96505 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 189035 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 189035 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 84771 0 None - 1 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 84771 0 None - 1 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 98103 0 None -8 2 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 98103 0 None -8 2 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 123302 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 123302 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 113869 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 113869 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 9708 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 9708 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 203581 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 203581 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 113691 0 None - 1 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 113691 0 None - 1 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 86937 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 86937 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 122633 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 122633 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 132296 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 132296 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 9908 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 9908 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 117088 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 117088 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
44587401 188233 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 188233 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
44435819 89195 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 89195 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 11009 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 11009 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 11009 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 11009 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 15363 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 15363 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 10095 1 None - 1 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 10095 1 None - 1 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 101956 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 101956 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 122628 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 122628 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 89510 0 None - 1 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 89510 0 None - 1 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 89361 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 89361 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 9870 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 9870 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
44451397 95903 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 95903 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 90048 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 90048 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 18073 0 None - 1 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 18073 0 None - 1 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
44353276 117227 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 117227 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 114125 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 114125 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 88726 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 88726 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 10781 0 None - 1 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 10781 0 None - 1 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 114803 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 114803 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 86744 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 86744 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 14538 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 14538 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 114815 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 114815 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 156673 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 156673 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 14948 0 None - 1 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 14948 0 None - 1 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 186845 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 186845 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 123022 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 123022 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 123022 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 100818 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 100818 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 146295 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 146295 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 10960 0 None - 1 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 10960 0 None - 1 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 113070 0 None - 1 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 113070 0 None - 1 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
11318370 9702 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 9702 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 124358 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 124358 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 168558 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 168558 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 168121 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 168121 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
44387961 166021 0 None - 1 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 166021 0 None - 1 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
44267902 98404 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 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 98404 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 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 163205 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 163205 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 98404 0 None - 1 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 98404 0 None - 1 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 118274 0 None - 1 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 118274 0 None - 1 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 123095 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 123095 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 96502 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 96502 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 88785 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 88785 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 130615 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 130615 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 110403 0 None - 1 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 110403 0 None - 1 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 167710 0 None - 1 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 167710 0 None - 1 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 116684 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 116684 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 163357 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 163357 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 88729 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 88729 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 109635 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 109635 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
11467134 123553 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 123553 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 123553 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 127426 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 127426 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 101795 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 101795 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 155341 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 155341 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 155341 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 20221 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 20221 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 9690 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 9690 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 157081 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 157081 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
44451349 96152 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 96152 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 146195 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 146195 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 15570 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 15570 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 124364 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 124364 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 124364 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 124364 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
11671279 130884 0 None - 1 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 130884 0 None - 1 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 116815 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 116815 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 188859 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 188859 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 173650 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 173650 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
11331001 189022 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 189022 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 961 36 None 4 2 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 961 36 None 4 2 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 961 36 None 4 2 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
11282957 122333 1 None - 1 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 122333 1 None - 1 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 194819 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 194819 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 122333 1 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 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 122333 1 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 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 122333 1 None - 1 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 122333 1 None - 1 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
71459935 78958 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 78958 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 114736 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 114736 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
44400350 126996 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 126996 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
9831160 163470 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 163470 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 163470 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 163470 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
11168311 166242 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 166242 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 103784 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 103784 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
10919567 99030 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 99030 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 89510 0 None - 1 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 89510 0 None - 1 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 123553 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 123553 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 123553 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 131787 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 131787 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 131787 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 95552 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 95552 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 125885 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 125885 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 9602 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 9602 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 89510 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(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23730 89510 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(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
10098618 111330 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 111330 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 123553 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 123553 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 123553 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
44435975 92179 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 92179 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 147571 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 147571 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 60681 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 60681 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 62525 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 62525 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 170602 0 None - 1 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 170602 0 None - 1 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
9984259 110501 0 None - 1 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 110501 0 None - 1 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 10577 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 10577 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 67572 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 67572 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 123052 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 123052 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 123052 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 98982 0 None - 1 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 98982 0 None - 1 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 110501 0 None - 1 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 110501 0 None - 1 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 20343 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 20343 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 9641 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 9641 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
44287779 141574 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 141574 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
44267885 17821 0 None - 1 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 17821 0 None - 1 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 97215 0 None - 1 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 97215 0 None - 1 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
11490288 168647 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 168647 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 168647 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 19016 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 19016 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
11354193 96214 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 96214 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 167899 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 167899 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 123222 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 123222 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 118100 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 118100 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
44267874 97214 0 None - 1 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 97214 0 None - 1 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
11191153 194870 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 194870 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 193438 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 193438 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
44267810 98091 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 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 98091 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 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 98091 0 None - 1 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 98091 0 None - 1 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 193237 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 193237 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 88708 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 88708 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 123790 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 123790 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 163008 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 163008 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 203853 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 203853 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 10576 0 None - 1 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 10576 0 None - 1 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 14558 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 14558 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 64871 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 64871 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 204048 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 204048 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 118447 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 118447 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 102454 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 102454 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 161341 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 161341 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 156448 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 156448 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
44577051 187430 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 187430 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 111376 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 111376 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 166568 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 166568 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 204202 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 204202 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 63246 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 63246 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 187576 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 187576 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 90648 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 90648 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 12063 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 12063 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 12063 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 128678 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 128678 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 128678 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 123656 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 123656 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 90648 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 90648 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 103274 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 103274 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
10929667 85772 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 85772 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 85772 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 85772 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 122387 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 122387 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 110637 0 None - 1 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 110637 0 None - 1 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 113087 0 None - 1 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 113087 0 None - 1 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 130884 0 None - 1 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 130884 0 None - 1 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 85772 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 85772 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 9749 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 9749 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 101134 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 101134 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 90660 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 90660 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
11123821 203307 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 203307 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 166021 0 None - 1 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 166021 0 None - 1 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 168574 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 168574 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 168572 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 168572 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 88746 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 88746 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 89115 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 89115 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 169480 0 None - 1 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 169480 0 None - 1 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 89499 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 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 89499 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 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 147096 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 147096 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 9503 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 9503 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
44340804 9149 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 9149 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 110158 0 None - 1 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 110158 0 None - 1 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 111241 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 111241 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 18877 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 18877 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 203834 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 203834 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 96077 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 96077 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
44435985 146950 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 146950 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 89360 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 89360 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 147098 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 147098 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 166119 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 166119 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
44352515 117071 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 117071 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 186641 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 186641 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 12069 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 12069 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 12069 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 96175 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 96175 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 22317 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 22317 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 10578 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 10578 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 122143 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 122143 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 63408 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 63408 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 63408 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 188622 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 188622 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 63189 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 63189 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 81580 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 81580 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 22251 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 22251 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
44394852 127165 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 127165 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 114429 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 114429 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
44267863 98518 0 None - 1 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 98518 0 None - 1 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 62099 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 62099 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 15449 0 None - 1 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 15449 0 None - 1 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 108787 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 108787 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
44340644 9914 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 9914 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 203903 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 203903 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 20658 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 20658 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 102735 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 102735 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 204378 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 204378 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 172240 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 172240 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 60660 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 60660 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 14422 0 None - 1 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 14422 0 None - 1 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 146753 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 146753 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 103617 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 103617 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
11226470 163069 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 163069 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 126271 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 126271 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 60520 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 60520 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
11375759 63835 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 63835 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 122630 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 122630 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 122630 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 172711 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 172711 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 122333 1 None - 1 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 122333 1 None - 1 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 188975 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 188975 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 117734 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 117734 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
11455317 62888 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 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 62888 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 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 172711 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 172711 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 173541 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 173541 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 63382 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 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 63382 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 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 63382 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 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 188934 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 188934 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
11421518 165296 0 None - 1 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 165296 0 None - 1 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 155509 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 155509 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 188667 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 188667 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
44353258 116080 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 116080 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
44267868 98075 0 None - 1 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 98075 0 None - 1 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 165296 0 None - 1 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 165296 0 None - 1 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 123667 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 123667 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 188278 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 188278 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 200907 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 200907 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 66362 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 66362 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 67656 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 67656 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 200907 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 200907 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 88730 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 88730 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 146947 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 146947 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 165296 0 None - 1 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 165296 0 None - 1 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 204105 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 204105 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 101937 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 101937 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 113970 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 113970 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 88496 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 88496 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 114450 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 114450 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
44394893 129670 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 129670 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 168717 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 168717 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 96526 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 96526 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 146955 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 146955 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 117484 0 None - 1 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 117484 0 None - 1 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
44340825 168081 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 168081 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 134730 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 134730 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 110567 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 110567 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 174621 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 174621 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 20969 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 20969 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 174621 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 174621 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 188170 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 188170 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 87039 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 87039 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 87039 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 87039 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
44451331 159881 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 159881 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
44352657 21551 0 None - 1 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 21551 0 None - 1 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 155320 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 155320 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 124383 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 124383 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 168647 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 168647 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 168647 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 170542 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 170542 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 13784 0 None - 1 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 13784 0 None - 1 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
44340771 9715 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 9715 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 168695 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 168695 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 90227 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 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 90227 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 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 178740 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 178740 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 90227 0 None - 1 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 90227 0 None - 1 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 130172 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 130172 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 90227 0 None - 1 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 90227 0 None - 1 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 90227 0 None - 1 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 90227 0 None - 1 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 203141 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 203141 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 172566 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 172566 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 90227 0 None - 1 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 90227 0 None - 1 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 89191 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 89191 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 66942 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 66942 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 131787 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 131787 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 131787 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 88587 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 88587 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 172705 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 172705 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 15450 0 None - 1 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 15450 0 None - 1 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 184000 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 184000 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
44309576 102268 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 102268 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 113519 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 113519 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 131845 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 131845 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 97112 0 None - 1 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 97112 0 None - 1 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 114824 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 114824 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 128505 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 128505 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 128505 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 128505 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 128505 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 128505 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 85223 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 85223 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 168037 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 168037 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 168037 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 168037 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 203863 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 203863 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
44352933 21493 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 21493 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 188247 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 188247 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 89923 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 89923 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 89923 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 89923 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 189040 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 189040 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 98075 0 None - 1 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 98075 0 None - 1 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 96506 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 96506 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 96465 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 96465 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
44390795 122178 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 122178 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 203122 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 203122 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
11178994 10402 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 10402 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 10402 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 10402 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 188262 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 188262 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 188262 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 188262 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 99520 0 None - 1 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 99520 0 None - 1 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 20089 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 20089 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 135283 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 135283 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 122630 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 122630 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 122630 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
9983568 98982 0 None - 1 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 98982 0 None - 1 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 14096 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 14096 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 113743 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 113743 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 172634 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 172634 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 101684 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 101684 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 155044 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 155044 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
25156944 189112 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 189112 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 178524 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 178524 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
11214614 189429 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 189429 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 85433 0 None - 1 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 85433 0 None - 1 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 85433 0 None - 1 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 85433 0 None - 1 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 96046 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 96046 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 85433 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 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 85433 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 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 122523 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 122523 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
11490509 63364 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 63364 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 101434 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 101434 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 101434 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 101434 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
44587395 172628 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 172628 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
9809382 100675 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 100675 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
44449683 157313 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 157313 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 178742 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 178742 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 96278 1 None - 1 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 96278 1 None - 1 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 123770 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 123770 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 11056 1 None - 1 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 11056 1 None - 1 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 96278 1 None - 1 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 96278 1 None - 1 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 113398 0 None - 1 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 113398 0 None - 1 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 96278 1 None - 1 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 96278 1 None - 1 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 20650 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 20650 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 115234 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 115234 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 184273 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 184273 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 85229 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 85229 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 99399 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 99399 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 18537 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 18537 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 99399 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 99399 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 85229 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 85229 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 168720 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 168720 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
44309357 98088 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 98088 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 63493 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 63493 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 62888 0 None - 1 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 62888 0 None - 1 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 193583 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 193583 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 22568 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 22568 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 126203 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 126203 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 168869 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 168869 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 11371 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 11371 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
21047858 10088 0 None - 1 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 10088 0 None - 1 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 63869 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 63869 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 22087 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 22087 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
44346348 114354 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 114354 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 91010 0 None - 1 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 91010 0 None - 1 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 101498 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 101498 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 101678 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 101678 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 9521 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 9521 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 11321 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 11321 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 11321 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 116061 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 116061 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 15346 0 None - 1 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 15346 0 None - 1 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 116061 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 116061 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 22325 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 22325 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
44451406 96582 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 96582 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 122333 1 None - 1 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 122333 1 None - 1 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 147065 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 147065 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 19824 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 19824 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
11261195 63706 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 63706 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 63706 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 63706 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 90194 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 90194 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 85781 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 85781 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 90194 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 90194 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 113566 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 113566 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 63149 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 63149 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 162233 0 None - 1 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 162233 0 None - 1 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 67068 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 67068 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 102962 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 102962 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 102962 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 102962 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 110477 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 110477 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 9455 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 9455 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 89540 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 89540 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
44267906 167492 0 None - 1 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 167492 0 None - 1 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 201673 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 201673 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 96041 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 96041 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 84755 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 84755 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 203161 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 203161 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 203184 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 203184 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 67063 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 67063 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 165962 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 165962 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
11124921 191800 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 191800 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 89362 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 89362 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 116732 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 116732 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
11191675 63382 0 None - 1 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 63382 0 None - 1 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 63382 0 None - 1 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 9579 0 None - 1 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 9579 0 None - 1 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 9455 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 9455 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 88542 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 88542 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 146954 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 146954 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 63876 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 63876 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 122195 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 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 122195 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 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 109118 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 109118 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 188767 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 188767 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 109118 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 109118 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 188767 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 188767 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
44434414 88526 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 88526 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
44399944 68635 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 68635 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 68635 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 68635 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 68635 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 68635 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 68635 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 68635 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 9579 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 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 9579 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 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 9579 0 None - 1 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 9579 0 None - 1 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 9579 0 None - 1 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 9579 0 None - 1 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 62593 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 62593 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 122295 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 122295 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 122295 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 68635 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 68635 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
44267887 98481 0 None -41 2 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 98481 0 None -41 2 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
44353249 168445 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 168445 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 85433 0 None - 1 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 85433 0 None - 1 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 96156 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 96156 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 155728 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 155728 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
9916573 157055 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 157055 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 130171 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 130171 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 63699 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 63699 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 63699 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 155621 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 155621 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
11202795 112833 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 112833 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 89499 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 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 89499 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 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 112833 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 112833 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 110652 0 None - 1 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 110652 0 None - 1 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 15570 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 15570 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 168864 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 168864 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 12008 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 12008 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
11050500 101848 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 101848 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 89106 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 89106 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 102609 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 102609 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 172353 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 172353 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
44436000 147202 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 147202 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
44340646 9689 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 9689 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 168421 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 168421 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 168421 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 102362 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 102362 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 96510 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 96510 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 168757 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 168757 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 110317 0 None - 1 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 110317 0 None - 1 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 150184 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 150184 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
44343931 110401 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 110401 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
44343931 110401 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 110401 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 69388 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 69388 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
44340697 110669 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 110669 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 9578 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 9578 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 89499 0 None - 1 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 89499 0 None - 1 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 102326 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 102326 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 10388 0 None - 1 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 10388 0 None - 1 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 14510 0 None - 1 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 14510 0 None - 1 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
44267864 167756 0 None - 1 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 167756 0 None - 1 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 98364 0 None - 1 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 98364 0 None - 1 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 168421 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 168421 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 168421 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 114464 0 None - 1 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 114464 0 None - 1 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 63699 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 63699 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 63699 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 124045 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 124045 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 14508 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 14508 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 150972 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 150972 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 178492 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 178492 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 96363 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 96363 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 122767 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 122767 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 188987 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 188987 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 110553 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 110553 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 13562 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 13562 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 122295 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 122295 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 122295 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 68684 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 68684 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 961 36 None -4 2 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 961 36 None -4 2 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 961 36 None -4 2 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 68684 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 68684 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 122295 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 122295 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 122295 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 961 36 None -4 2 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 961 36 None -4 2 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 961 36 None -4 2 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
44215933 96078 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 96078 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
44400354 133504 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 133504 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
11236870 11046 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 11046 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 63288 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 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 63288 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 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 122557 0 None - 1 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 122557 0 None - 1 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 122557 0 None - 1 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 11046 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 11046 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 63344 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 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 63344 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 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 111221 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 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 111221 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 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 111221 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 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 111221 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 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
11751752 13562 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 13562 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 88495 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 88495 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 156674 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 156674 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 116081 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 116081 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 63419 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 63419 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 63419 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 95233 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 95233 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 112838 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 112838 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 90227 0 None - 1 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 90227 0 None - 1 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
44353231 116809 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 116809 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 96213 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 96213 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 63274 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 63274 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 62500 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 62500 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 62500 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 112986 0 None - 1 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 112986 0 None - 1 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 168388 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 168388 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 128684 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 128684 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 166584 0 None - 1 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 166584 0 None - 1 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 62506 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 62506 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 62506 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 22248 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 22248 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 15574 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 15574 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 101681 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 101681 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
11294792 63288 0 None - 1 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 63288 0 None - 1 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 204305 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 204305 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 13260 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 13260 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 171048 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 171048 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 13260 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 13260 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 60485 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 60485 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 61762 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 61762 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 114142 0 None - 1 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 114142 0 None - 1 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 161384 0 None - 1 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 161384 0 None - 1 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 133361 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 133361 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
44352641 118163 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 118163 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
11444384 63419 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 63419 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 63419 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 102749 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 102749 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 114550 0 None - 1 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 114550 0 None - 1 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 95064 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 95064 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 99250 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 99250 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 187794 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 187794 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 150973 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 150973 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
11353175 99479 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 99479 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 66358 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 66358 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
44288082 163168 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 163168 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 155076 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 155076 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 102183 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 102183 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 102183 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 102183 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 122144 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 122144 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 102183 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 102183 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 172473 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 172473 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
44288073 169427 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 169427 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 189130 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 189130 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 127418 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 127418 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 127418 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 127418 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 193367 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 193367 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 10237 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 10237 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 10237 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 10237 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
11179922 87320 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 87320 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 66305 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 66305 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 87320 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 87320 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 167649 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 167649 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 122716 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 122716 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 122389 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 122389 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 122389 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 123323 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 123323 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 96116 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 96116 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 10495 0 None - 1 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 10495 0 None - 1 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
44340860 9615 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 9615 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 10175 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 10175 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 189048 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 189048 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 184190 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 184190 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 113324 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 113324 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
44451486 158177 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 158177 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 129818 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 129818 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
11214294 122195 0 None - 1 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 122195 0 None - 1 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 14564 0 None - 1 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 14564 0 None - 1 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 96196 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 96196 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 86990 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 86990 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 86990 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 86990 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 62500 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 62500 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 62500 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 61044 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 61044 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
44346662 114426 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 114426 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
44576655 188221 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 188221 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 62506 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 62506 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 62506 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 168980 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 168980 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
10875519 189313 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 189313 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
11455176 99059 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 99059 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 99059 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 99059 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 9943 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 9943 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 16314 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 16314 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 87450 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 87450 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 87450 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 87450 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 203957 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 203957 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 111297 0 None - 1 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 111297 0 None - 1 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 100213 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 100213 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 98120 0 None - 1 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 98120 0 None - 1 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
44267904 98416 0 None - 1 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 98416 0 None - 1 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 101794 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 101794 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 69380 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 69380 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 16599 0 None - 1 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 16599 0 None - 1 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 110501 0 None - 1 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 110501 0 None - 1 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 110501 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 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 110501 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 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 110501 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 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 110501 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 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 68674 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 68674 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 123053 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 123053 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
44309319 203714 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 203714 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 96507 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 96507 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 15301 0 None - 1 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 15301 0 None - 1 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 115501 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 115501 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 63884 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 63884 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
44435981 146949 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 146949 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 110577 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 110577 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 98675 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 98675 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 168716 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 168716 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 99090 0 None - 1 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 99090 0 None - 1 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 60546 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 60546 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 110481 0 None - 1 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 110481 0 None - 1 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
44340643 111344 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 111344 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 96466 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 96466 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 9472 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 9472 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 88780 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 88780 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 88779 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 88779 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 167426 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 167426 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 22611 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 22611 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 60475 0 None - 1 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 60475 0 None - 1 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
11191675 63382 0 None - 1 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 63382 0 None - 1 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 63382 0 None - 1 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 99520 0 None - 1 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 99520 0 None - 1 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 64574 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 64574 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 112837 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 112837 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 61017 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 61017 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 61017 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 63024 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 63024 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 63024 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
44390758 64946 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 64946 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 9455 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 9455 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
44387896 129674 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 129674 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 125887 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 125887 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 10689 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 10689 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 113372 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 113372 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 129674 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 129674 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
44400247 122042 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 122042 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 168357 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 168357 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 188827 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 188827 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 114448 0 None - 1 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 114448 0 None - 1 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
44340623 9480 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 9480 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 164474 0 None - 1 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 164474 0 None - 1 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 10979 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 10979 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 101759 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 101759 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 64779 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 64779 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 96948 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 96948 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 155914 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 155914 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
11431754 13298 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 13298 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
44436001 161682 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 161682 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 203857 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 203857 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 9669 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 9669 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 102546 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 102546 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 9609 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 9609 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 10493 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 10493 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 14041 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 14041 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 89105 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 89105 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 14041 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 14041 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 173173 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 173173 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 122389 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 122389 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 122389 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 154191 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 154191 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 88504 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 88504 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
11980076 208453 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 208453 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
25077405 2715 0 None - 1 Human 8.0 pKd = 8.0 Binding
NoneNone
Drug Central None None None None None
3902 2715 0 None - 1 Human 8.0 pKd = 8.0 Binding
NoneNone
Drug Central None None None None None
CHEMBL1201309 2715 0 None - 1 Human 8.0 pKd = 8.0 Binding
NoneNone
Drug Central None None None None None
DB00666 2715 0 None - 1 Human 8.0 pKd = 8.0 Binding
NoneNone
Drug Central None None None None None
1162 1831 0 None 16 2 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
16132914 1831 0 None 16 2 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
3878 1833 0 None - 1 Human 8.2 pKd = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17254668
188304 1631 0 None - 1 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9341 1631 0 None - 1 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL3272563 1631 0 None - 1 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9342 326 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9855027 326 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL3272561 326 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9344 1934 0 None - 1 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
25077495 1390 0 None - 1 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9343 1390 0 None - 1 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL2365665 1390 0 None - 1 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
DB11510 1390 0 None - 1 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
3860 744 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
3860 744 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
436 744 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
436 744 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
50225 744 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
50225 744 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
CHEMBL2110824 744 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL2110824 744 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
DB06719 744 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
DB06719 744 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
11167850 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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
101755083 1359 47 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
16136245 1359 47 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
4379 1359 47 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
5585 1359 47 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
CHEMBL415606 1359 47 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
DB06699 1359 47 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
1190 882 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 882 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
583 882 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 882 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 882 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
1188 219 48 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
16131215 219 48 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
35 219 48 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
CHEMBL1252 219 48 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
DB00106 219 48 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
11225 1116 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 1116 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 1831 0 None -16 2 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
16132914 1831 0 None -16 2 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
1162 1831 0 None 16 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
1162 1831 0 None 16 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
16132914 1831 0 None 16 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
16132914 1831 0 None 16 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
1162 1831 0 None 16 2 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
16132914 1831 0 None 16 2 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
101755083 1359 47 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
16136245 1359 47 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
4379 1359 47 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
5585 1359 47 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
CHEMBL415606 1359 47 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
DB06699 1359 47 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
1175 2298 44 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
1559 2298 44 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
657181 2298 44 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
CHEMBL1201199 2298 44 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
DB00007 2298 44 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
11250647 1545 46 None - 1 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 1545 46 None - 1 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 1545 46 None - 1 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 1545 46 None - 1 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 1545 46 None - 1 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 1545 46 None - 1 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 1545 46 None - 1 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 1545 46 None - 1 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 1545 46 None - 1 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 1545 46 None - 1 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 1631 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9341 1631 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL3272563 1631 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9342 326 0 None - 1 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9855027 326 0 None - 1 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL3272561 326 0 None - 1 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9344 1934 0 None - 1 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
1188 219 48 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
16131215 219 48 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
35 219 48 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
CHEMBL1252 219 48 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
DB00106 219 48 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
1177 3867 0 None 5 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
25074470 3867 0 None 5 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
2968 3867 0 None 5 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
CHEMBL1201334 3867 0 None 5 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
DB06825 3867 0 None 5 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
101827019 2106 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850267
16130938 2106 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850267
3854 2106 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850267
73952264 2106 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850267
CHEMBL3989438 2106 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850267
25077495 1390 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9343 1390 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL2365665 1390 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
DB11510 1390 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
1190 882 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
1190 882 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7649152
1190 882 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
25074887 882 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
25074887 882 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7649152
25074887 882 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
583 882 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
583 882 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7649152
583 882 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
CHEMBL1200490 882 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
CHEMBL1200490 882 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7649152
CHEMBL1200490 882 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
DB00050 882 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
DB00050 882 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7649152
DB00050 882 47 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
3860 744 0 None 57 2 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
436 744 0 None 57 2 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
50225 744 0 None 57 2 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL2110824 744 0 None 57 2 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
DB06719 744 0 None 57 2 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
1180 1303 0 None - 1 Human 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
1185 3701 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 3701 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 3701 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 3701 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 1288 0 None - 1 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
1170 1931 0 None - 1 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
1179 961 36 None -4 2 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 961 36 None -4 2 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 961 36 None -4 2 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 1626 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 1626 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 1304 0 None - 1 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
1177 3867 0 None -5 2 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
25074470 3867 0 None -5 2 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
2968 3867 0 None -5 2 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
CHEMBL1201334 3867 0 None -5 2 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
DB06825 3867 0 None -5 2 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
11167850 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 2741 28 None - 1 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 427 0 None - 1 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
16132443 427 0 None - 1 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077