Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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DOI

44300265 197666 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 517 9 5 3 3.7 O=C(Cc1ccc(Cl)cc1)NNC(=O)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL57104 197666 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 517 9 5 3 3.7 O=C(Cc1ccc(Cl)cc1)NNC(=O)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
44300355 196539 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 484 9 5 4 2.4 O=C(Cc1cccnc1)NNC(=O)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL56369 196539 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 484 9 5 4 2.4 O=C(Cc1cccnc1)NNC(=O)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
44300451 198087 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 443 9 4 4 3.4 O=C(N/N=C/c1ccco1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL57438 198087 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 443 9 4 4 3.4 O=C(N/N=C/c1ccco1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
46881642 8096 0 None 12 2 Mouse 8.0 pEC50 = 8 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 362 8 2 2 5.1 CC(C)CCc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1091468 8096 0 None 12 2 Mouse 8.0 pEC50 = 8 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 362 8 2 2 5.1 CC(C)CCc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46884660 6442 0 None -1 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 339 7 1 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cnsc3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1082471 6442 0 None -1 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 339 7 1 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cnsc3)cc2)n1 10.1016/j.bmcl.2010.02.076
46884661 7818 0 None -3 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 334 7 1 3 4.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cnccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089512 7818 0 None -3 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 334 7 1 3 4.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cnccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
46884627 8377 0 None -3 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 349 7 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(O)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1093170 8377 0 None -3 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 349 7 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(O)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
54580462 60831 0 None 4 2 Mouse 7.0 pEC50 = 7 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 422 6 3 5 3.9 CC(C)(C)CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762251 60831 0 None 4 2 Mouse 7.0 pEC50 = 7 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 422 6 3 5 3.9 CC(C)(C)CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
54581475 60853 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 by cell-based GRPR assayAgonist activity at human BRS3 by cell-based GRPR assay
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC1CC2CCC1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762275 60853 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 by cell-based GRPR assayAgonist activity at human BRS3 by cell-based GRPR assay
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC1CC2CCC1C2 10.1016/j.bmcl.2011.02.011
54581475 60853 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 by cell-based NMBR assayAgonist activity at human BRS3 by cell-based NMBR assay
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC1CC2CCC1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762275 60853 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 by cell-based NMBR assayAgonist activity at human BRS3 by cell-based NMBR assay
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC1CC2CCC1C2 10.1016/j.bmcl.2011.02.011
4900723 8580 1 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 377 3 2 6 1.9 CN1CCN(c2nc3[nH]nc(N)c3c3c2CN(Cc2ccccc2)CC3)CC1 10.1016/j.bmcl.2010.03.065
CHEMBL1094727 8580 1 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 377 3 2 6 1.9 CN1CCN(c2nc3[nH]nc(N)c3c3c2CN(Cc2ccccc2)CC3)CC1 10.1016/j.bmcl.2010.03.065
46887826 8581 0 None -1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 322 3 2 5 2.2 CN(C)c1nc2[nH]nc(N)c2c2c1CN(Cc1ccccc1)CC2 10.1016/j.bmcl.2010.03.065
CHEMBL1094728 8581 0 None -1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 322 3 2 5 2.2 CN(C)c1nc2[nH]nc(N)c2c2c1CN(Cc1ccccc1)CC2 10.1016/j.bmcl.2010.03.065
46887767 8585 0 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 390 3 2 5 3.9 Nc1n[nH]c2nc(N3CCCCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1094771 8585 0 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 390 3 2 5 3.9 Nc1n[nH]c2nc(N3CCCCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
46887768 8586 0 None -11 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 376 3 2 5 3.3 CC1CCN(c2nc3[nH]nc(N)c3c3c2CN(Cc2ccccc2)CC3)CC1 10.1016/j.bmcl.2010.03.065
CHEMBL1094772 8586 0 None -11 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 376 3 2 5 3.3 CC1CCN(c2nc3[nH]nc(N)c3c3c2CN(Cc2ccccc2)CC3)CC1 10.1016/j.bmcl.2010.03.065
46887765 8657 0 None -10 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 348 3 2 5 2.7 Nc1n[nH]c2nc(N3CCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1095424 8657 0 None -10 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 348 3 2 5 2.7 Nc1n[nH]c2nc(N3CCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
46888066 8672 0 None -21 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 390 5 2 5 3.9 CCNc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1095528 8672 0 None -21 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 390 5 2 5 3.9 CCNc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
46888068 8675 0 None -1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 376 3 1 6 3.1 Cn1nc(N)c2c3c(c(N4CCCCC4)nc21)CN(Cc1ccccc1)CC3 10.1016/j.bmcl.2010.03.065
CHEMBL1095530 8675 0 None -1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 376 3 1 6 3.1 Cn1nc(N)c2c3c(c(N4CCCCC4)nc21)CN(Cc1ccccc1)CC3 10.1016/j.bmcl.2010.03.065
46887766 8695 0 None -6 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 376 3 2 5 3.5 Nc1n[nH]c2nc(N3CCCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1095741 8695 0 None -6 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 376 3 2 5 3.5 Nc1n[nH]c2nc(N3CCCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
46887915 8786 0 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 392 4 2 6 3.1 COc1ccc(CN2CCc3c(c(N4CCCCC4)nc4[nH]nc(N)c34)C2)cc1 10.1016/j.bmcl.2010.03.065
CHEMBL1096531 8786 0 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 392 4 2 6 3.1 COc1ccc(CN2CCc3c(c(N4CCCCC4)nc4[nH]nc(N)c34)C2)cc1 10.1016/j.bmcl.2010.03.065
46887916 8787 0 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 430 3 2 5 4.1 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1cccc(C(F)(F)F)c1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1096532 8787 0 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 430 3 2 5 4.1 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1cccc(C(F)(F)F)c1)C3 10.1016/j.bmcl.2010.03.065
46887946 8791 0 None -25 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 406 3 2 7 2.8 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccc2c(c1)OCO2)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1096546 8791 0 None -25 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 406 3 2 7 2.8 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccc2c(c1)OCO2)C3 10.1016/j.bmcl.2010.03.065
46887947 8792 0 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 368 3 2 5 3.5 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(CC1CCCCC1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1096547 8792 0 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 368 3 2 5 3.5 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(CC1CCCCC1)C3 10.1016/j.bmcl.2010.03.065
46887948 8793 0 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 328 3 2 5 2.5 CC(C)CN1CCc2c(c(N3CCCCC3)nc3[nH]nc(N)c23)C1 10.1016/j.bmcl.2010.03.065
CHEMBL1096548 8793 0 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 328 3 2 5 2.5 CC(C)CN1CCc2c(c(N3CCCCC3)nc3[nH]nc(N)c23)C1 10.1016/j.bmcl.2010.03.065
46887949 8820 0 None -9 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 342 2 2 5 2.9 CC(C)(C)CN1CCc2c(c(N3CCCCC3)nc3[nH]nc(N)c23)C1 10.1016/j.bmcl.2010.03.065
CHEMBL1096819 8820 0 None -9 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 342 2 2 5 2.9 CC(C)(C)CN1CCc2c(c(N3CCCCC3)nc3[nH]nc(N)c23)C1 10.1016/j.bmcl.2010.03.065
46888069 8883 0 None -13 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 404 3 1 7 3.2 CC(=O)n1nc(N)c2c3c(c(N4CCCCC4)nc21)CN(Cc1ccccc1)CC3 10.1016/j.bmcl.2010.03.065
CHEMBL1097471 8883 0 None -13 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 404 3 1 7 3.2 CC(=O)n1nc(N)c2c3c(c(N4CCCCC4)nc21)CN(Cc1ccccc1)CC3 10.1016/j.bmcl.2010.03.065
46887875 8903 0 None -1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 336 4 3 5 2.9 CC(C)Nc1nc2[nH]nc(N)c2c2c1CN(Cc1ccccc1)CC2 10.1016/j.bmcl.2010.03.065
CHEMBL1097551 8903 0 None -1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 336 4 3 5 2.9 CC(C)Nc1nc2[nH]nc(N)c2c2c1CN(Cc1ccccc1)CC2 10.1016/j.bmcl.2010.03.065
46887824 8953 0 None -20 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 380 3 2 5 3.0 Nc1n[nH]c2nc(N3CCC(F)CC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1098097 8953 0 None -20 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 380 3 2 5 3.0 Nc1n[nH]c2nc(N3CCC(F)CC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
3288900 8954 8 None -2 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 364 3 2 6 1.9 Nc1n[nH]c2nc(N3CCOCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1098098 8954 8 None -2 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 364 3 2 6 1.9 Nc1n[nH]c2nc(N3CCOCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
25249151 8970 4 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 376 4 3 5 3.8 Nc1n[nH]c2nc(NC3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1098185 8970 4 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 376 4 3 5 3.8 Nc1n[nH]c2nc(NC3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
4899895 8971 1 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 370 4 3 5 3.8 Nc1n[nH]c2nc(Nc3ccccc3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1098186 8971 1 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 370 4 3 5 3.8 Nc1n[nH]c2nc(Nc3ccccc3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
46887825 9000 0 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 363 3 3 6 1.5 Nc1n[nH]c2nc(N3CCNCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1098433 9000 0 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 363 3 3 6 1.5 Nc1n[nH]c2nc(N3CCNCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
46887950 9029 0 None -1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 376 4 2 5 3.1 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(CCc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1098535 9029 0 None -1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 376 4 2 5 3.1 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(CCc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
46887914 14230 0 None -2 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 380 3 2 5 3.2 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccc(F)cc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1199153 14230 0 None -2 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 380 3 2 5 3.2 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccc(F)cc1)C3 10.1016/j.bmcl.2010.03.065
4900723 8580 1 None -1 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 377 3 2 6 1.9 CN1CCN(c2nc3[nH]nc(N)c3c3c2CN(Cc2ccccc2)CC3)CC1 10.1016/j.bmcl.2010.03.065
CHEMBL1094727 8580 1 None -1 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 377 3 2 6 1.9 CN1CCN(c2nc3[nH]nc(N)c3c3c2CN(Cc2ccccc2)CC3)CC1 10.1016/j.bmcl.2010.03.065
46887767 8585 0 None -1 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 390 3 2 5 3.9 Nc1n[nH]c2nc(N3CCCCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1094771 8585 0 None -1 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 390 3 2 5 3.9 Nc1n[nH]c2nc(N3CCCCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
46887915 8786 0 None -1 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 392 4 2 6 3.1 COc1ccc(CN2CCc3c(c(N4CCCCC4)nc4[nH]nc(N)c34)C2)cc1 10.1016/j.bmcl.2010.03.065
CHEMBL1096531 8786 0 None -1 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 392 4 2 6 3.1 COc1ccc(CN2CCc3c(c(N4CCCCC4)nc4[nH]nc(N)c34)C2)cc1 10.1016/j.bmcl.2010.03.065
46887916 8787 0 None -1 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 430 3 2 5 4.1 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1cccc(C(F)(F)F)c1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1096532 8787 0 None -1 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 430 3 2 5 4.1 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1cccc(C(F)(F)F)c1)C3 10.1016/j.bmcl.2010.03.065
46887947 8792 0 None -1 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 368 3 2 5 3.5 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(CC1CCCCC1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1096547 8792 0 None -1 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 368 3 2 5 3.5 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(CC1CCCCC1)C3 10.1016/j.bmcl.2010.03.065
46887948 8793 0 None -1 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 328 3 2 5 2.5 CC(C)CN1CCc2c(c(N3CCCCC3)nc3[nH]nc(N)c23)C1 10.1016/j.bmcl.2010.03.065
CHEMBL1096548 8793 0 None -1 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 328 3 2 5 2.5 CC(C)CN1CCc2c(c(N3CCCCC3)nc3[nH]nc(N)c23)C1 10.1016/j.bmcl.2010.03.065
25249151 8970 4 None -1 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 376 4 3 5 3.8 Nc1n[nH]c2nc(NC3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1098185 8970 4 None -1 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 376 4 3 5 3.8 Nc1n[nH]c2nc(NC3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
4899895 8971 1 None -1 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 370 4 3 5 3.8 Nc1n[nH]c2nc(Nc3ccccc3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1098186 8971 1 None -1 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 370 4 3 5 3.8 Nc1n[nH]c2nc(Nc3ccccc3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
46887825 9000 0 None -1 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 363 3 3 6 1.5 Nc1n[nH]c2nc(N3CCNCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1098433 9000 0 None -1 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 363 3 3 6 1.5 Nc1n[nH]c2nc(N3CCNCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
46882060 6313 0 None -2 2 Mouse 5.0 pEC50 = 5 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 346 7 2 2 5.3 CCCCc1cnc(/C=C/c2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1081866 6313 0 None -2 2 Mouse 5.0 pEC50 = 5 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 346 7 2 2 5.3 CCCCc1cnc(/C=C/c2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46881560 6992 0 None -13 2 Human 6.0 pEC50 = 6 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 346 7 2 2 4.5 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1084697 6992 0 None -13 2 Human 6.0 pEC50 = 6 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 346 7 2 2 4.5 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46845425 1032 2 None 1 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
8504 1032 2 None 1 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1089721 1032 2 None 1 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
25026056 8181 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 347 7 1 2 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091985 8181 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 347 7 1 2 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
46884630 8420 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 339 7 1 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccns3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1093459 8420 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 339 7 1 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccns3)cc2)n1 10.1016/j.bmcl.2010.02.076
62707362 81872 0 None -14 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 541 3 1 6 6.3 Cn1cc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(C)(C)C)cc2)Cc2ccc(C(F)(F)F)nc2N3)cn1 10.1021/ml200304j
CHEMBL2164577 81872 0 None -14 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 541 3 1 6 6.3 Cn1cc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(C)(C)C)cc2)Cc2ccc(C(F)(F)F)nc2N3)cn1 10.1021/ml200304j
46881509 7601 0 None 22 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 416 7 2 2 5.8 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccc(Cl)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1087933 7601 0 None 22 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 416 7 2 2 5.8 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccc(Cl)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46885311 8315 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 424 7 2 2 6.0 O=C(O)c1cc(F)c(F)cc1-c1ccc(CCc2nc(CC3CCCCC3)c[nH]2)cc1 10.1016/j.bmcl.2010.02.076
CHEMBL1092730 8315 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 424 7 2 2 6.0 O=C(O)c1cc(F)c(F)cc1-c1ccc(CCc2nc(CC3CCCCC3)c[nH]2)cc1 10.1016/j.bmcl.2010.02.076
46884576 8111 0 None 4 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 331 6 1 2 5.0 c1ccc(-c2ccc(CCc3nc(CC4CCCC4)c[nH]3)cc2)nc1 10.1016/j.bmcl.2010.02.076
CHEMBL1091598 8111 0 None 4 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 331 6 1 2 5.0 c1ccc(-c2ccc(CCc3nc(CC4CCCC4)c[nH]3)cc2)nc1 10.1016/j.bmcl.2010.02.076
46884578 8180 0 None 3 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 333 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccncc3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091984 8180 0 None 3 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 333 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccncc3)cc2)n1 10.1016/j.bmcl.2010.02.076
46884630 8420 0 None 2 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 339 7 1 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccns3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1093459 8420 0 None 2 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 339 7 1 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccns3)cc2)n1 10.1016/j.bmcl.2010.02.076
46884659 7817 0 None -3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 340 7 1 4 4.7 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3csnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089511 7817 0 None -3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 340 7 1 4 4.7 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3csnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
25026056 8181 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 347 7 1 2 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091985 8181 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 347 7 1 2 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
25025861 8380 0 None -1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 351 7 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccc(F)cn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1093184 8380 0 None -1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 351 7 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccc(F)cn3)cc2)n1 10.1016/j.bmcl.2010.02.076
46887949 8820 0 None 9 2 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 342 2 2 5 2.9 CC(C)(C)CN1CCc2c(c(N3CCCCC3)nc3[nH]nc(N)c23)C1 10.1016/j.bmcl.2010.03.065
CHEMBL1096819 8820 0 None 9 2 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 342 2 2 5 2.9 CC(C)(C)CN1CCc2c(c(N3CCCCC3)nc3[nH]nc(N)c23)C1 10.1016/j.bmcl.2010.03.065
25025862 7821 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 322 7 1 3 4.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089521 7821 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 322 7 1 3 4.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
25026056 8181 0 None -1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 347 7 1 2 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091985 8181 0 None -1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 347 7 1 2 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
25025858 7782 0 None -16 2 Human 7.0 pEC50 = 7.0 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 362 6 2 2 5.1 CC(C)(C)Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1089383 7782 0 None -16 2 Human 7.0 pEC50 = 7.0 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 362 6 2 2 5.1 CC(C)(C)Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46884661 7818 0 None 3 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 334 7 1 3 4.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cnccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089512 7818 0 None 3 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 334 7 1 3 4.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cnccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
46884688 8173 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 339 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCCC3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091918 8173 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 339 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCCC3)cc2)n1 10.1016/j.bmcl.2010.02.076
59618681 82788 0 None 14 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 512 2 1 5 6.4 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccc4ncccc4c32)cc1 10.1021/ml200207w
CHEMBL2179918 82788 0 None 14 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 512 2 1 5 6.4 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccc4ncccc4c32)cc1 10.1021/ml200207w
46884659 7817 0 None 3 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 340 7 1 4 4.7 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3csnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089511 7817 0 None 3 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 340 7 1 4 4.7 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3csnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
46884659 7817 0 None 3 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 340 7 1 4 4.7 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3csnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089511 7817 0 None 3 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 340 7 1 4 4.7 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3csnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
46884661 7818 0 None 3 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 334 7 1 3 4.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cnccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089512 7818 0 None 3 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 334 7 1 3 4.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cnccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
46884627 8377 0 None 3 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 349 7 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(O)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1093170 8377 0 None 3 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 349 7 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(O)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
46889210 7532 0 None 1 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 387 6 2 2 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc3c(c2)CNC(=O)c2ccccc2-3)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1087443 7532 0 None 1 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 387 6 2 2 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc3c(c2)CNC(=O)c2ccccc2-3)n1 10.1016/j.bmcl.2010.03.028
46881416 7165 0 None 18 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 382 7 2 2 5.2 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccccc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1085434 7165 0 None 18 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 382 7 2 2 5.2 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccccc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
59618811 82784 0 None 6 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 461 2 1 4 5.9 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccccc32)cc1 10.1021/ml200207w
CHEMBL2179914 82784 0 None 6 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 461 2 1 4 5.9 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccccc32)cc1 10.1021/ml200207w
59618620 82787 0 None 7 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 476 2 1 5 5.6 Cc1ccc2c(n1)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179917 82787 0 None 7 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 476 2 1 5 5.6 Cc1ccc2c(n1)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
54584418 60829 0 None 6 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@@H]2CC[C@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762249 60829 0 None 6 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@@H]2CC[C@H]1C2 10.1016/j.bmcl.2011.02.011
46884663 7823 0 None 3 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 323 7 1 4 3.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ccnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089523 7823 0 None 3 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 323 7 1 4 3.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ccnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
25025862 7821 0 None 2 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 322 7 1 3 4.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089521 7821 0 None 2 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 322 7 1 3 4.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
62707363 81873 0 None 8 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 544 3 2 5 6.3 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(C4CCNCC4)c32)cc1 10.1021/ml200304j
CHEMBL2164578 81873 0 None 8 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 544 3 2 5 6.3 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(C4CCNCC4)c32)cc1 10.1021/ml200304j
46884629 8379 0 None 2 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 358 7 1 3 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C#N)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1093183 8379 0 None 2 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 358 7 1 3 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C#N)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
62707363 81873 0 None -8 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 544 3 2 5 6.3 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(C4CCNCC4)c32)cc1 10.1021/ml200304j
CHEMBL2164578 81873 0 None -8 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 544 3 2 5 6.3 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(C4CCNCC4)c32)cc1 10.1021/ml200304j
46882013 5605 0 None -7 2 Human 5.9 pEC50 = 5.9 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 390 10 2 2 6.2 CCCCc1cnc(C(CCC)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1077345 5605 0 None -7 2 Human 5.9 pEC50 = 5.9 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 390 10 2 2 6.2 CCCCc1cnc(C(CCC)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46884660 6442 0 None 1 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 339 7 1 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cnsc3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1082471 6442 0 None 1 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 339 7 1 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cnsc3)cc2)n1 10.1016/j.bmcl.2010.02.076
46884628 8253 0 None 1 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 348 7 2 3 4.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(N)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1092381 8253 0 None 1 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 348 7 2 3 4.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(N)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
46881642 8096 0 None -12 2 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 362 8 2 2 5.1 CC(C)CCc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1091468 8096 0 None -12 2 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 362 8 2 2 5.1 CC(C)CCc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46884662 7822 0 None 6 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 323 7 1 4 3.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cncn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089522 7822 0 None 6 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 323 7 1 4 3.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cncn3)cc2)n1 10.1016/j.bmcl.2010.02.076
46889177 7484 0 None 10 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 497 10 2 4 6.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(C(F)(F)F)n[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1087066 7484 0 None 10 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 497 10 2 4 6.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(C(F)(F)F)n[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
46889233 7657 0 None -1 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 383 8 2 3 4.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCC[C@@H]3C(=O)O)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1088409 7657 0 None -1 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 383 8 2 3 4.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCC[C@@H]3C(=O)O)cc2)n1 10.1016/j.bmcl.2010.03.028
66901749 82781 0 None -18 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 475 2 1 4 6.2 Cc1cccc2c1N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179911 82781 0 None -18 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 475 2 1 4 6.2 Cc1cccc2c1N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
54585379 60839 0 None -3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 367 4 2 5 2.4 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1O[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762261 60839 0 None -3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 367 4 2 5 2.4 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1O[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
54583454 60851 0 None -3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 388 6 3 6 2.9 O=S(=O)(Nc1nc(C2CCC2)n[nH]1)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762273 60851 0 None -3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 388 6 3 6 2.9 O=S(=O)(Nc1nc(C2CCC2)n[nH]1)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
90663970 106791 0 None 12 3 Human 5.9 pEC50 = 5.9 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 553 14 5 4 2.5 NC(=O)CC[C@H](NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL3144503 106791 0 None 12 3 Human 5.9 pEC50 = 5.9 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 553 14 5 4 2.5 NC(=O)CC[C@H](NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
46884662 7822 0 None 6 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 323 7 1 4 3.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cncn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089522 7822 0 None 6 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 323 7 1 4 3.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cncn3)cc2)n1 10.1016/j.bmcl.2010.02.076
59618658 82666 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 507 2 1 5 6.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1csc(C(F)(F)F)c1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179481 82666 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 507 2 1 5 6.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1csc(C(F)(F)F)c1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
46887981 9090 0 None 28 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 418 5 2 5 3.9 CCC(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1099123 9090 0 None 28 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 418 5 2 5 3.9 CCC(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
46888018 9062 0 None -2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 460 5 2 5 4.9 CC(C)(C)CC(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1098837 9062 0 None -2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 460 5 2 5 4.9 CC(C)(C)CC(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
46885312 8101 0 None -10 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 377 8 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccnc3C(=O)O)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091553 8101 0 None -10 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 377 8 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccnc3C(=O)O)cc2)n1 10.1016/j.bmcl.2010.02.076
46881471 6461 0 None -13 2 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 396 7 2 2 5.5 Cc1ccccc1Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1082543 6461 0 None -13 2 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 396 7 2 2 5.5 Cc1ccccc1Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46889177 7484 0 None -10 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 497 10 2 4 6.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(C(F)(F)F)n[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1087066 7484 0 None -10 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 497 10 2 4 6.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(C(F)(F)F)n[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
59618681 82788 0 None -14 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 512 2 1 5 6.4 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccc4ncccc4c32)cc1 10.1021/ml200207w
CHEMBL2179918 82788 0 None -14 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 512 2 1 5 6.4 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccc4ncccc4c32)cc1 10.1021/ml200207w
46887980 9089 0 None 24 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 404 4 2 5 3.5 CC(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1099122 9089 0 None 24 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 404 4 2 5 3.5 CC(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
46889235 7659 0 None 2 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 406 8 2 4 5.0 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCC[C@@H]3c3ncn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1088411 7659 0 None 2 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 406 8 2 4 5.0 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCC[C@@H]3c3ncn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
25026058 7669 0 None 2 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 377 7 2 3 5.0 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCc4cn[nH]c43)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1088553 7669 0 None 2 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 377 7 2 3 5.0 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCc4cn[nH]c43)cc2)n1 10.1016/j.bmcl.2010.03.028
54580461 60830 0 None 4 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 380 6 3 5 2.9 CCC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762250 60830 0 None 4 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 380 6 3 5 2.9 CCC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
46200989 2562 15 None -9 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1021/ml200304j
8502 2562 15 None -9 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1021/ml200304j
CHEMBL2023109 2562 15 None -9 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1021/ml200304j
46200989 2562 15 None -9 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2012.03.029
8502 2562 15 None -9 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2012.03.029
CHEMBL2023109 2562 15 None -9 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2012.03.029
54583450 60838 0 None 3 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 388 4 3 5 3.0 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC1CCc2ccccc21 10.1016/j.bmcl.2011.02.011
CHEMBL1762259 60838 0 None 3 2 Mouse 5.9 pEC50 = 5.9 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 388 4 3 5 3.0 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC1CCc2ccccc21 10.1016/j.bmcl.2011.02.011
46884577 8112 0 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccnc3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091599 8112 0 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccnc3)cc2)n1 10.1016/j.bmcl.2010.02.076
59618635 82668 0 None 6 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 435 2 1 4 5.8 Cc1ccc2c(n1)Nc1ccc(C)c(C)c1N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)C2 10.1021/ml200207w
CHEMBL2179484 82668 0 None 6 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 435 2 1 4 5.8 Cc1ccc2c(n1)Nc1ccc(C)c(C)c1N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)C2 10.1021/ml200207w
46881417 7217 0 None -7 2 Human 5.9 pEC50 = 5.9 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 396 8 2 2 5.3 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CCc3ccccc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1085670 7217 0 None -7 2 Human 5.9 pEC50 = 5.9 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 396 8 2 2 5.3 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CCc3ccccc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46889146 7683 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 348 7 2 2 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3O)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1088684 7683 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 348 7 2 2 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3O)cc2)n1 10.1016/j.bmcl.2010.03.028
46884688 8173 0 None 1 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 339 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCCC3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091918 8173 0 None 1 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 339 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCCC3)cc2)n1 10.1016/j.bmcl.2010.02.076
25025654 570 13 None -15 3 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 10.1016/j.bmcl.2010.01.154
6189 570 13 None -15 3 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 10.1016/j.bmcl.2010.01.154
8506 570 13 None -15 3 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 10.1016/j.bmcl.2010.01.154
CHEMBL1084942 570 13 None -15 3 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 10.1016/j.bmcl.2010.01.154
62707528 81787 0 None -11 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 573 4 2 8 6.0 C[C@@H](O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(C)(C)C)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
CHEMBL2164222 81787 0 None -11 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 573 4 2 8 6.0 C[C@@H](O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(C)(C)C)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
71451990 82785 0 None -6 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 537 3 2 5 6.2 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccc(C(C)(C)O)c(F)c32)cc1 10.1021/ml200207w
CHEMBL2179915 82785 0 None -6 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 537 3 2 5 6.2 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccc(C(C)(C)O)c(F)c32)cc1 10.1021/ml200207w
25025862 7821 0 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 322 7 1 3 4.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089521 7821 0 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 322 7 1 3 4.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
49871766 2557 40 None -17 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
6170 2557 40 None -17 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
CHEMBL1672354 2557 40 None -17 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
25026044 57842 1 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 390 6 2 4 3.9 CC(O)(Cc1nc(CC2(C(F)(F)F)CC2)c[nH]1)c1ccc(-n2cccn2)cc1 10.1021/ml100196d
CHEMBL1671874 57842 1 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 390 6 2 4 3.9 CC(O)(Cc1nc(CC2(C(F)(F)F)CC2)c[nH]1)c1ccc(-n2cccn2)cc1 10.1021/ml100196d
46885312 8101 0 None 10 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 377 8 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccnc3C(=O)O)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091553 8101 0 None 10 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 377 8 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccnc3C(=O)O)cc2)n1 10.1016/j.bmcl.2010.02.076
46881604 8870 0 None 25 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 374 6 2 2 5.6 O=C(O)c1ccccc1-c1ccc(CCc2ncc(C3CCCCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1097362 8870 0 None 25 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 374 6 2 2 5.6 O=C(O)c1ccccc1-c1ccc(CCc2ncc(C3CCCCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
90663956 106777 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 530 11 4 3 4.0 C[C@H](NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL3144489 106777 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 530 11 4 3 4.0 C[C@H](NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
90663965 106786 0 None 8 3 Human 5.9 pEC50 = 5.9 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 587 14 5 4 3.2 NC(=O)CC[C@H](NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL3144498 106786 0 None 8 3 Human 5.9 pEC50 = 5.9 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 587 14 5 4 3.2 NC(=O)CC[C@H](NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
4594 42872 127 None -4 6 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 345 5 1 5 2.9 COc1ccc2[nH]c([S+]([O-])Cc3ncc(C)c(OC)c3C)nc2c1 10.1016/j.bmcl.2008.09.033
CHEMBL1503 42872 127 None -4 6 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 345 5 1 5 2.9 COc1ccc2[nH]c([S+]([O-])Cc3ncc(C)c(OC)c3C)nc2c1 10.1016/j.bmcl.2008.09.033
46887766 8695 0 None 6 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 376 3 2 5 3.5 Nc1n[nH]c2nc(N3CCCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1095741 8695 0 None 6 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 376 3 2 5 3.5 Nc1n[nH]c2nc(N3CCCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
25134007 81789 0 None -87 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 573 5 2 8 6.0 CC(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(C(C)(C)O)n4)c32)cc1 10.1021/ml200304j
CHEMBL2164224 81789 0 None -87 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 573 5 2 8 6.0 CC(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(C(C)(C)O)n4)c32)cc1 10.1021/ml200304j
59618675 82664 0 None -2 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 497 1 1 5 4.8 Cc1ccc2c(c1C)N(S(=O)(=O)C1=NC(C(C)(C)C)C=[S+]1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179479 82664 0 None -2 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 497 1 1 5 4.8 Cc1ccc2c(c1C)N(S(=O)(=O)C1=NC(C(C)(C)C)C=[S+]1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
46885313 8102 0 None -3 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 377 8 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C(=O)O)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091554 8102 0 None -3 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 377 8 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C(=O)O)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
46889234 7658 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 407 8 2 5 4.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCC[C@@H]3c3nnn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1088410 7658 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 407 8 2 5 4.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCC[C@@H]3c3nnn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
56840673 1141 0 None 2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 10 mins by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 10 mins by bioluminescence assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
8503 1141 0 None 2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 10 mins by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 10 mins by bioluminescence assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
CHEMBL2164575 1141 0 None 2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 10 mins by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 10 mins by bioluminescence assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
59618711 74194 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 600 5 2 6 5.6 CNC(=O)C1(c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)CCC1 10.1016/j.bmc.2012.03.029
CHEMBL2023114 74194 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 600 5 2 6 5.6 CNC(=O)C1(c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)CCC1 10.1016/j.bmc.2012.03.029
46884578 8180 0 None 3 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccncc3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091984 8180 0 None 3 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccncc3)cc2)n1 10.1016/j.bmcl.2010.02.076
44300408 196804 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 455 10 5 3 3.4 O=C(NNCc1ccccc1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL56562 196804 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 455 10 5 3 3.4 O=C(NNCc1ccccc1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
44300286 96559 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 1106 31 11 12 2.1 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CCNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)O 10.1021/jm0210921
CHEMBL262992 96559 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 1106 31 11 12 2.1 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CCNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)O 10.1021/jm0210921
59618623 82659 0 None 2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 501 2 1 4 6.2 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(F)(F)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179474 82659 0 None 2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 501 2 1 4 6.2 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(F)(F)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
59618785 82665 0 None -3 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 507 2 1 5 6.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(F)(F)F)s1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179480 82665 0 None -3 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 507 2 1 5 6.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(F)(F)F)s1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
46888017 9061 0 None -24 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 446 4 2 5 4.5 CC(C)(C)C(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1098836 9061 0 None -24 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 446 4 2 5 4.5 CC(C)(C)C(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
66901760 82782 0 None -10 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 495 2 1 4 6.5 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(Cl)c32)cc1 10.1021/ml200207w
CHEMBL2179912 82782 0 None -10 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 495 2 1 4 6.5 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(Cl)c32)cc1 10.1021/ml200207w
59618785 82665 0 None 3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 507 2 1 5 6.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(F)(F)F)s1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179480 82665 0 None 3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 507 2 1 5 6.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(F)(F)F)s1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
46881473 7676 0 None -19 2 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 400 7 2 2 5.3 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3cccc(F)c3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1088614 7676 0 None -19 2 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 400 7 2 2 5.3 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3cccc(F)c3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
25026446 57946 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 338 5 2 4 3.6 CC(C)(C)Cc1c[nH]c(CC(C)(O)c2ccc(-n3cccn3)cc2)n1 10.1021/ml100196d
CHEMBL1672353 57946 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 338 5 2 4 3.6 CC(C)(C)Cc1c[nH]c(CC(C)(O)c2ccc(-n3cccn3)cc2)n1 10.1021/ml100196d
25025861 8380 0 None -1 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 351 7 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccc(F)cn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1093184 8380 0 None -1 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 351 7 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccc(F)cn3)cc2)n1 10.1016/j.bmcl.2010.02.076
46889234 7658 0 None -1 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 407 8 2 5 4.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCC[C@@H]3c3nnn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1088410 7658 0 None -1 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 407 8 2 5 4.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCC[C@@H]3c3nnn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
46889145 9076 0 None 1 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 398 7 2 4 4.8 c1ccc(-c2nnn[nH]2)c(-c2ccc(CCc3nc(CC4CCCC4)c[nH]3)cc2)c1 10.1016/j.bmcl.2010.03.028
CHEMBL1099034 9076 0 None 1 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 398 7 2 4 4.8 c1ccc(-c2nnn[nH]2)c(-c2ccc(CCc3nc(CC4CCCC4)c[nH]3)cc2)c1 10.1016/j.bmcl.2010.03.028
54581470 60828 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762248 60828 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
54583452 60847 0 None 7 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 399 5 2 4 4.8 CC(C)(C)c1cccc(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)c1 10.1016/j.bmcl.2011.02.011
CHEMBL1762269 60847 0 None 7 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 399 5 2 4 4.8 CC(C)(C)c1cccc(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)c1 10.1016/j.bmcl.2011.02.011
54586337 60840 0 None -3 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 367 4 2 5 2.4 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1O[C@@H]1C[C@@H]2CC[C@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762262 60840 0 None -3 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 367 4 2 5 2.4 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1O[C@@H]1C[C@@H]2CC[C@H]1C2 10.1016/j.bmcl.2011.02.011
44589824 186691 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 330 6 1 5 3.9 COc1cc(CSc2nc3ccc(OC)cc3[nH]2)cc(OC)c1 10.1016/j.bmcl.2008.09.033
CHEMBL488400 186691 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 330 6 1 5 3.9 COc1cc(CSc2nc3ccc(OC)cc3[nH]2)cc(OC)c1 10.1016/j.bmcl.2008.09.033
46881558 7333 0 None -31 2 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 400 7 2 2 5.3 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccc(F)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1086177 7333 0 None -31 2 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 400 7 2 2 5.3 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccc(F)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
59618811 82784 0 None -6 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 461 2 1 4 5.9 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccccc32)cc1 10.1021/ml200207w
CHEMBL2179914 82784 0 None -6 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 461 2 1 4 5.9 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccccc32)cc1 10.1021/ml200207w
46881507 7465 0 None 16 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 396 7 2 2 5.5 Cc1ccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1086912 7465 0 None 16 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 396 7 2 2 5.5 Cc1ccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46881418 6762 0 None 10 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 412 8 2 3 5.2 COc1ccccc1Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1083825 6762 0 None 10 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 412 8 2 3 5.2 COc1ccccc1Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46882013 5605 0 None 7 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 390 10 2 2 6.2 CCCCc1cnc(C(CCC)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1077345 5605 0 None 7 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 390 10 2 2 6.2 CCCCc1cnc(C(CCC)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46884627 8377 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 349 7 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(O)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1093170 8377 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 349 7 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(O)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
44300427 197615 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 468 12 4 3 3.4 O=C(CNCCc1ccccc1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL57068 197615 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 468 12 4 3 3.4 O=C(CNCCc1ccccc1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
54583454 60851 0 None 3 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 388 6 3 6 2.9 O=S(=O)(Nc1nc(C2CCC2)n[nH]1)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762273 60851 0 None 3 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 388 6 3 6 2.9 O=S(=O)(Nc1nc(C2CCC2)n[nH]1)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
54586335 60834 0 None -12 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 408 4 3 5 3.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@]1(C)C2(C)C 10.1016/j.bmcl.2011.02.011
CHEMBL1762254 60834 0 None -12 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 408 4 3 5 3.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@]1(C)C2(C)C 10.1016/j.bmcl.2011.02.011
54582478 60852 0 None -3 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 388 6 3 6 2.9 O=S(=O)(Nc1nc(C2CCC2)n[nH]1)c1cnccc1NC1CC2CCC1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762274 60852 0 None -3 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 388 6 3 6 2.9 O=S(=O)(Nc1nc(C2CCC2)n[nH]1)c1cnccc1NC1CC2CCC1C2 10.1016/j.bmcl.2011.02.011
46884688 8173 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 339 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCCC3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091918 8173 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 339 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCCC3)cc2)n1 10.1016/j.bmcl.2010.02.076
59618620 82787 0 None -7 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 476 2 1 5 5.6 Cc1ccc2c(n1)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179917 82787 0 None -7 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 476 2 1 5 5.6 Cc1ccc2c(n1)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
46889175 7441 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 429 10 2 4 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3ncn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1086673 7441 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 429 10 2 4 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3ncn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
46881418 6762 0 None -10 2 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 412 8 2 3 5.2 COc1ccccc1Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1083825 6762 0 None -10 2 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 412 8 2 3 5.2 COc1ccccc1Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46881417 7217 0 None 7 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 396 8 2 2 5.3 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CCc3ccccc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1085670 7217 0 None 7 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 396 8 2 2 5.3 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CCc3ccccc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46882011 5891 0 None 1 3 Rat 6.8 pEC50 = 6.8 Functional
Agonistic activity at rat BRS3 expressed in HEK293AEO at 10 uM by aequorin bioluminescence assayAgonistic activity at rat BRS3 expressed in HEK293AEO at 10 uM by aequorin bioluminescence assay
ChEMBL 406 11 3 3 5.2 CCCCc1cnc(C(CCCO)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1079517 5891 0 None 1 3 Rat 6.8 pEC50 = 6.8 Functional
Agonistic activity at rat BRS3 expressed in HEK293AEO at 10 uM by aequorin bioluminescence assayAgonistic activity at rat BRS3 expressed in HEK293AEO at 10 uM by aequorin bioluminescence assay
ChEMBL 406 11 3 3 5.2 CCCCc1cnc(C(CCCO)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46889147 7684 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 445 7 1 5 5.7 O=C1NC(=O)C(c2ccccc2-c2ccc(CCC3N=CC(CC4CCCC4)=N3)cc2)S1 10.1016/j.bmcl.2010.03.028
CHEMBL1088685 7684 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 445 7 1 5 5.7 O=C1NC(=O)C(c2ccccc2-c2ccc(CCC3N=CC(CC4CCCC4)=N3)cc2)S1 10.1016/j.bmcl.2010.03.028
46881510 7614 0 None -18 2 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 400 7 2 2 5.3 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccccc3F)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1088062 7614 0 None -18 2 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 400 7 2 2 5.3 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccccc3F)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
54585380 60844 0 None 3 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 380 4 2 5 2.8 CN(C(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2)C(C)(C)C 10.1016/j.bmcl.2011.02.011
CHEMBL1762266 60844 0 None 3 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 380 4 2 5 2.8 CN(C(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2)C(C)(C)C 10.1016/j.bmcl.2011.02.011
46881921 8057 0 None 15 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 362 8 2 2 5.5 CCCCc1cnc(C(C)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1091087 8057 0 None 15 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 362 8 2 2 5.5 CCCCc1cnc(C(C)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46882011 5891 0 None -15 3 Human 5.7 pEC50 = 5.7 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 406 11 3 3 5.2 CCCCc1cnc(C(CCCO)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1079517 5891 0 None -15 3 Human 5.7 pEC50 = 5.7 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 406 11 3 3 5.2 CCCCc1cnc(C(CCCO)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
25026056 8181 0 None -1 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 347 7 1 2 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091985 8181 0 None -1 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 347 7 1 2 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
44387452 60509 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 538 9 6 4 3.0 O=C(CC1NCCc2ccccc21)NNC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL175651 60509 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 538 9 6 4 3.0 O=C(CC1NCCc2ccccc21)NNC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
54582478 60852 0 None 3 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 388 6 3 6 2.9 O=S(=O)(Nc1nc(C2CCC2)n[nH]1)c1cnccc1NC1CC2CCC1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762274 60852 0 None 3 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 388 6 3 6 2.9 O=S(=O)(Nc1nc(C2CCC2)n[nH]1)c1cnccc1NC1CC2CCC1C2 10.1016/j.bmcl.2011.02.011
46882011 5891 0 None -15 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 406 11 3 3 5.2 CCCCc1cnc(C(CCCO)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1021/ml100196d
CHEMBL1079517 5891 0 None -15 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 406 11 3 3 5.2 CCCCc1cnc(C(CCCO)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1021/ml100196d
46884629 8379 0 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 358 7 1 3 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C#N)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1093183 8379 0 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 358 7 1 3 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C#N)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
71460964 82783 0 None 11 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 475 2 1 4 6.2 Cc1ccc2c(c1)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179913 82783 0 None 11 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 475 2 1 4 6.2 Cc1ccc2c(c1)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
90663968 106789 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 496 11 4 3 3.3 C[C@H](NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL3144501 106789 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 496 11 4 3 3.3 C[C@H](NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
49871766 2557 40 None 6 5 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at rat BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
6170 2557 40 None 6 5 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at rat BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
CHEMBL1672354 2557 40 None 6 5 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at rat BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
44300379 101046 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 522 9 6 3 3.5 O=C(Cc1cc2ccccc2[nH]1)NNC(=O)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL294647 101046 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 522 9 6 3 3.5 O=C(Cc1cc2ccccc2[nH]1)NNC(=O)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
25025860 569 32 None -4 5 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
6188 569 32 None -4 5 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1091720 569 32 None -4 5 Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
25025863 8499 0 None 4 2 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 430 10 2 5 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nnn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1094054 8499 0 None 4 2 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 430 10 2 5 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nnn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
44300436 197569 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 488 11 4 3 4.0 O=C(CNCc1ccc(Cl)cc1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL57039 197569 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 488 11 4 3 4.0 O=C(CNCc1ccc(Cl)cc1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
46881470 6460 0 None 40 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 407 7 2 3 5.0 N#Cc1cccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)c1 10.1016/j.bmcl.2010.01.154
CHEMBL1082542 6460 0 None 40 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 407 7 2 3 5.0 N#Cc1cccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)c1 10.1016/j.bmcl.2010.01.154
54582477 60848 0 None 11 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 406 5 2 6 4.2 CC(C)(C)c1csc(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)n1 10.1016/j.bmcl.2011.02.011
CHEMBL1762270 60848 0 None 11 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 406 5 2 6 4.2 CC(C)(C)c1csc(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)n1 10.1016/j.bmcl.2011.02.011
71460937 82662 0 None -10 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 493 3 1 4 6.4 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179477 82662 0 None -10 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 493 3 1 4 6.4 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
46881416 7165 0 None -18 2 Human 6.7 pEC50 = 6.7 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 382 7 2 2 5.2 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccccc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1085434 7165 0 None -18 2 Human 6.7 pEC50 = 6.7 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 382 7 2 2 5.2 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccccc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
71451991 82786 0 None -15 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 477 2 2 5 5.6 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(O)c32)cc1 10.1021/ml200207w
CHEMBL2179916 82786 0 None -15 2 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 477 2 2 5 5.6 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(O)c32)cc1 10.1021/ml200207w
59618746 74193 0 None 6 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 586 5 2 6 5.4 NC(=O)C1(c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)CCC1 10.1016/j.bmc.2012.03.029
CHEMBL2023113 74193 0 None 6 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 586 5 2 6 5.4 NC(=O)C1(c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)CCC1 10.1016/j.bmc.2012.03.029
49871766 2557 40 None -6 5 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
6170 2557 40 None -6 5 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
CHEMBL1672354 2557 40 None -6 5 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
53242205 60827 0 None 3 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762247 60827 0 None 3 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
44300429 100648 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 455 11 4 4 2.7 O=C(CNCc1cccnc1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL292176 100648 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 455 11 4 4 2.7 O=C(CNCc1cccnc1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
44300505 163130 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 454 11 4 3 3.3 O=C(CNCc1ccccc1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL417767 163130 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 454 11 4 3 3.3 O=C(CNCc1ccccc1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
44589872 172723 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 330 4 1 4 3.7 COc1ccc2nc(CCc3cc4c(cc3Cl)OCO4)[nH]c2c1 10.1016/j.bmcl.2008.09.033
CHEMBL450593 172723 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 330 4 1 4 3.7 COc1ccc2nc(CCc3cc4c(cc3Cl)OCO4)[nH]c2c1 10.1016/j.bmcl.2008.09.033
54582477 60848 0 None -11 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 406 5 2 6 4.2 CC(C)(C)c1csc(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)n1 10.1016/j.bmcl.2011.02.011
CHEMBL1762270 60848 0 None -11 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 406 5 2 6 4.2 CC(C)(C)c1csc(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)n1 10.1016/j.bmcl.2011.02.011
46888020 9096 0 None 2 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 460 6 2 5 4.9 CCC(C)(C)C(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1099135 9096 0 None 2 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 460 6 2 5 4.9 CCC(C)(C)C(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
59618675 82664 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 497 1 1 5 4.8 Cc1ccc2c(c1C)N(S(=O)(=O)C1=NC(C(C)(C)C)C=[S+]1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179479 82664 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 497 1 1 5 4.8 Cc1ccc2c(c1C)N(S(=O)(=O)C1=NC(C(C)(C)C)C=[S+]1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
46884576 8111 0 None 4 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 331 6 1 2 5.0 c1ccc(-c2ccc(CCc3nc(CC4CCCC4)c[nH]3)cc2)nc1 10.1016/j.bmcl.2010.02.076
CHEMBL1091598 8111 0 None 4 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 331 6 1 2 5.0 c1ccc(-c2ccc(CCc3nc(CC4CCCC4)c[nH]3)cc2)nc1 10.1016/j.bmcl.2010.02.076
59618746 74193 0 None -6 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 586 5 2 6 5.4 NC(=O)C1(c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)CCC1 10.1016/j.bmc.2012.03.029
CHEMBL2023113 74193 0 None -6 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 586 5 2 6 5.4 NC(=O)C1(c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)CCC1 10.1016/j.bmc.2012.03.029
59618711 74194 0 None -3 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 600 5 2 6 5.6 CNC(=O)C1(c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)CCC1 10.1016/j.bmc.2012.03.029
CHEMBL2023114 74194 0 None -3 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 600 5 2 6 5.6 CNC(=O)C1(c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)CCC1 10.1016/j.bmc.2012.03.029
46882010 6062 0 None 13 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 416 7 2 2 5.8 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccccc3Cl)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1080581 6062 0 None 13 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 416 7 2 2 5.8 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccccc3Cl)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
25055504 57944 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 367 5 2 3 4.7 CC(C)(C)Cc1c[nH]c(C(C)(O)Cc2ccc(-c3ccc(F)cn3)cc2)n1 10.1021/ml100196d
CHEMBL1672351 57944 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 367 5 2 3 4.7 CC(C)(C)Cc1c[nH]c(C(C)(O)Cc2ccc(-c3ccc(F)cn3)cc2)n1 10.1021/ml100196d
54581471 60832 0 None -6 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 444 5 3 5 3.6 O=C(NC12CC3CC(CC(C3)C1)C2)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762252 60832 0 None -6 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 444 5 3 5 3.6 O=C(NC12CC3CC(CC(C3)C1)C2)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
4157547 25229 9 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells using 10 uM dy-peptide by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells using 10 uM dy-peptide by bioluminescence assay
ChEMBL 352 5 3 5 2.1 CC(C)NC(=O)NS(=O)(=O)c1cnccc1NC1CC2CCC1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1348293 25229 9 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells using 10 uM dy-peptide by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells using 10 uM dy-peptide by bioluminescence assay
ChEMBL 352 5 3 5 2.1 CC(C)NC(=O)NS(=O)(=O)c1cnccc1NC1CC2CCC1C2 10.1016/j.bmcl.2011.02.011
46882057 5922 0 None 2 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 390 9 2 2 6.1 CCCCc1cnc(C(Cc2ccc(-c3ccccc3C(=O)O)cc2)C(C)C)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1079696 5922 0 None 2 2 Mouse 5.7 pEC50 = 5.7 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 390 9 2 2 6.1 CCCCc1cnc(C(Cc2ccc(-c3ccccc3C(=O)O)cc2)C(C)C)[nH]1 10.1016/j.bmcl.2010.01.154
46881509 7601 0 None -22 2 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 416 7 2 2 5.8 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccc(Cl)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1087933 7601 0 None -22 2 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 416 7 2 2 5.8 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccc(Cl)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46881605 8871 0 None 14 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 390 7 2 3 4.5 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CCOCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1097363 8871 0 None 14 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 390 7 2 3 4.5 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CCOCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
90663969 106790 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 601 15 5 4 3.6 NC(=O)CC[C@H](NC(=O)CCc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL3144502 106790 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 601 15 5 4 3.6 NC(=O)CC[C@H](NC(=O)CCc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
59618635 82668 0 None -6 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 435 2 1 4 5.8 Cc1ccc2c(n1)Nc1ccc(C)c(C)c1N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)C2 10.1021/ml200207w
CHEMBL2179484 82668 0 None -6 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 435 2 1 4 5.8 Cc1ccc2c(n1)Nc1ccc(C)c(C)c1N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)C2 10.1021/ml200207w
46882011 5891 0 None -1 3 Mouse 6.6 pEC50 = 6.6 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 406 11 3 3 5.2 CCCCc1cnc(C(CCCO)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1079517 5891 0 None -1 3 Mouse 6.6 pEC50 = 6.6 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 406 11 3 3 5.2 CCCCc1cnc(C(CCCO)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46889233 7657 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 383 8 2 3 4.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCC[C@@H]3C(=O)O)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1088409 7657 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 383 8 2 3 4.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCC[C@@H]3C(=O)O)cc2)n1 10.1016/j.bmcl.2010.03.028
44300796 163187 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 445 10 5 4 3.0 O=C(NNCc1ccco1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL418147 163187 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 445 10 5 4 3.0 O=C(NNCc1ccco1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
44589929 189435 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 370 3 1 4 4.5 FC(F)(F)c1ccc2nc(COc3cc4c(cc3Cl)OCO4)[nH]c2c1 10.1016/j.bmcl.2008.09.033
CHEMBL513374 189435 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 370 3 1 4 4.5 FC(F)(F)c1ccc2nc(COc3cc4c(cc3Cl)OCO4)[nH]c2c1 10.1016/j.bmcl.2008.09.033
44300456 100566 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 453 9 4 3 3.8 O=C(N/N=C/c1ccccc1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL291549 100566 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 453 9 4 3 3.8 O=C(N/N=C/c1ccccc1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
59618646 82667 0 None -2 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 421 2 1 4 5.4 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1cccnc1N2 10.1021/ml200207w
CHEMBL2179482 82667 0 None -2 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 421 2 1 4 5.4 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1cccnc1N2 10.1021/ml200207w
46845425 1032 2 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
8504 1032 2 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1089721 1032 2 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
46845425 1032 2 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.03.028
8504 1032 2 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.03.028
CHEMBL1089721 1032 2 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.03.028
46884687 8172 0 None 3 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 324 7 1 5 3.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ncnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091917 8172 0 None 3 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 324 7 1 5 3.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ncnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
46845425 1032 2 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.01.154
8504 1032 2 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.01.154
CHEMBL1089721 1032 2 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.01.154
90663958 106779 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 482 12 4 3 3.8 C[C@H](NCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL3144491 106779 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 482 12 4 3 3.8 C[C@H](NCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
25129212 74192 0 None 7 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 574 5 2 6 5.2 CC(C)(C(N)=O)c1cccc2c1N(S(=O)(=O)c1ccc(OC(F)(F)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1016/j.bmc.2012.03.029
CHEMBL2023112 74192 0 None 7 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 574 5 2 6 5.2 CC(C)(C(N)=O)c1cccc2c1N(S(=O)(=O)c1ccc(OC(F)(F)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1016/j.bmc.2012.03.029
46884629 8379 0 None 2 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 358 7 1 3 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C#N)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1093183 8379 0 None 2 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 358 7 1 3 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C#N)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
54587369 60833 0 None 1 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 354 4 3 5 2.6 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC1CCCCC1 10.1016/j.bmcl.2011.02.011
CHEMBL1762253 60833 0 None 1 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 354 4 3 5 2.6 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC1CCCCC1 10.1016/j.bmcl.2011.02.011
54583452 60847 0 None -7 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 399 5 2 4 4.8 CC(C)(C)c1cccc(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)c1 10.1016/j.bmcl.2011.02.011
CHEMBL1762269 60847 0 None -7 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 399 5 2 4 4.8 CC(C)(C)c1cccc(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)c1 10.1016/j.bmcl.2011.02.011
46882012 5892 0 None -5 2 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 404 11 2 2 6.6 CCCCc1cnc(C(CCCC)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1079518 5892 0 None -5 2 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 404 11 2 2 6.6 CCCCc1cnc(C(CCCC)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46881507 7465 0 None -16 2 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 396 7 2 2 5.5 Cc1ccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1086912 7465 0 None -16 2 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 396 7 2 2 5.5 Cc1ccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46889232 7513 0 None 1 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 401 6 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc3c(c2)CN(C)C(=O)c2ccccc2-3)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1087200 7513 0 None 1 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 401 6 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc3c(c2)CN(C)C(=O)c2ccccc2-3)n1 10.1016/j.bmcl.2010.03.028
25129212 74192 0 None -7 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 574 5 2 6 5.2 CC(C)(C(N)=O)c1cccc2c1N(S(=O)(=O)c1ccc(OC(F)(F)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1016/j.bmc.2012.03.029
CHEMBL2023112 74192 0 None -7 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 574 5 2 6 5.2 CC(C)(C(N)=O)c1cccc2c1N(S(=O)(=O)c1ccc(OC(F)(F)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1016/j.bmc.2012.03.029
54583453 60849 0 None 3 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 389 5 3 5 3.5 CC(C)(C)c1cc(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)[nH]n1 10.1016/j.bmcl.2011.02.011
CHEMBL1762271 60849 0 None 3 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 389 5 3 5 3.5 CC(C)(C)c1cc(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)[nH]n1 10.1016/j.bmcl.2011.02.011
44300482 197581 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 487 9 4 3 4.4 O=C(N/N=C/c1ccc(Cl)cc1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL57046 197581 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 487 9 4 3 4.4 O=C(N/N=C/c1ccc(Cl)cc1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
46881961 5831 0 None -28 2 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 348 8 2 2 4.9 CCCCc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1079114 5831 0 None -28 2 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 348 8 2 2 4.9 CCCCc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46881920 8324 0 None -7 2 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 376 9 2 2 5.9 CCCCc1cnc(C(CC)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1092798 8324 0 None -7 2 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 376 9 2 2 5.9 CCCCc1cnc(C(CC)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46881644 7843 0 None 1 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 348 5 2 2 4.9 CC(C)(C)c1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1089720 7843 0 None 1 2 Mouse 5.6 pEC50 = 5.6 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 348 5 2 2 4.9 CC(C)(C)c1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46881921 8057 0 None -15 2 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 362 8 2 2 5.5 CCCCc1cnc(C(C)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1091087 8057 0 None -15 2 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 362 8 2 2 5.5 CCCCc1cnc(C(C)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
59618710 82780 0 None 7 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 473 2 1 4 6.2 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1cc(F)c(Cl)nc1N2 10.1021/ml200207w
CHEMBL2179910 82780 0 None 7 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 473 2 1 4 6.2 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1cc(F)c(Cl)nc1N2 10.1021/ml200207w
46884688 8173 0 None 1 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 339 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCCC3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091918 8173 0 None 1 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 339 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCCC3)cc2)n1 10.1016/j.bmcl.2010.02.076
53242205 60827 0 None 3 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762247 60827 0 None 3 2 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
46889210 7532 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 387 6 2 2 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc3c(c2)CNC(=O)c2ccccc2-3)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1087443 7532 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 387 6 2 2 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc3c(c2)CNC(=O)c2ccccc2-3)n1 10.1016/j.bmcl.2010.03.028
46882010 6062 0 None -13 2 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 416 7 2 2 5.8 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccccc3Cl)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1080581 6062 0 None -13 2 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 416 7 2 2 5.8 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccccc3Cl)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46884630 8420 0 None 2 2 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 339 7 1 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccns3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1093459 8420 0 None 2 2 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 339 7 1 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccns3)cc2)n1 10.1016/j.bmcl.2010.02.076
44300356 198247 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 483 9 5 3 3.0 O=C(Cc1ccccc1)NNC(=O)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL57559 198247 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 483 9 5 3 3.0 O=C(Cc1ccccc1)NNC(=O)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
46884628 8253 0 None 1 2 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 348 7 2 3 4.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(N)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1092381 8253 0 None 1 2 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 348 7 2 3 4.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(N)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL525577 215653 0 None -64 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](N)Cc1ccccc1)C(C)C)C(N)=O 10.1016/j.bmcl.2008.09.033
25025863 8499 0 None -4 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 430 10 2 5 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nnn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1094054 8499 0 None -4 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 430 10 2 5 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nnn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
46881683 8362 0 None 2 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 390 9 2 2 5.9 CCC(C)(CC)Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1093080 8362 0 None 2 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 390 9 2 2 5.9 CCC(C)(CC)Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
44300275 201541 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 522 11 3 3 4.5 O=C(CN1CCC(Cc2ccccc2)CC1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL60537 201541 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 522 11 3 3 4.5 O=C(CN1CCC(Cc2ccccc2)CC1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
46884578 8180 0 None -3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccncc3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091984 8180 0 None -3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccncc3)cc2)n1 10.1016/j.bmcl.2010.02.076
46885313 8102 0 None 3 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 377 8 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C(=O)O)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091554 8102 0 None 3 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 377 8 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C(=O)O)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
46881508 7466 0 None 26 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 416 7 2 2 5.8 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3cccc(Cl)c3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1086913 7466 0 None 26 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 416 7 2 2 5.8 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3cccc(Cl)c3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
90663963 106784 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 551 11 5 4 3.3 C[C@H](NC(=O)CC1NCCc2ccccc21)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL3144496 106784 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 551 11 5 4 3.3 C[C@H](NC(=O)CC1NCCc2ccccc21)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
46887980 9089 0 None -24 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 404 4 2 5 3.5 CC(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1099122 9089 0 None -24 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 404 4 2 5 3.5 CC(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
90663967 106788 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 497 11 4 4 2.7 C[C@H](NC(=O)Cc1cccnc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL3144500 106788 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 497 11 4 4 2.7 C[C@H](NC(=O)Cc1cccnc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
54585379 60839 0 None 3 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 367 4 2 5 2.4 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1O[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762261 60839 0 None 3 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 367 4 2 5 2.4 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1O[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
54586337 60840 0 None 3 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 367 4 2 5 2.4 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1O[C@@H]1C[C@@H]2CC[C@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762262 60840 0 None 3 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 367 4 2 5 2.4 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1O[C@@H]1C[C@@H]2CC[C@H]1C2 10.1016/j.bmcl.2011.02.011
59618646 82667 0 None 2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 421 2 1 4 5.4 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1cccnc1N2 10.1021/ml200207w
CHEMBL2179482 82667 0 None 2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 421 2 1 4 5.4 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1cccnc1N2 10.1021/ml200207w
54580463 60835 0 None 11 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 408 4 3 5 3.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@H]2CC[C@]1(C)C2(C)C 10.1016/j.bmcl.2011.02.011
CHEMBL1762255 60835 0 None 11 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 408 4 3 5 3.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@H]2CC[C@]1(C)C2(C)C 10.1016/j.bmcl.2011.02.011
56840673 1141 0 None -2 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
8503 1141 0 None -2 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
CHEMBL2164575 1141 0 None -2 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
46881603 9132 0 None 19 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 402 8 2 2 6.1 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CCC3CCCCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1099370 9132 0 None 19 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 402 8 2 2 6.1 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CCC3CCCCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
136086809 7443 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 445 10 3 4 4.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(=O)[nH][nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1086684 7443 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 445 10 3 4 4.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(=O)[nH][nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
46881605 8871 0 None -14 2 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 390 7 2 3 4.5 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CCOCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1097363 8871 0 None -14 2 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 390 7 2 3 4.5 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CCOCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46889146 7683 0 None 1 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 348 7 2 2 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3O)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1088684 7683 0 None 1 2 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 348 7 2 2 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3O)cc2)n1 10.1016/j.bmcl.2010.03.028
54581472 60841 0 None 18 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 365 4 3 4 3.1 CC(C)(C)NC(=O)NS(=O)(=O)c1ccccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762263 60841 0 None 18 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 365 4 3 4 3.1 CC(C)(C)NC(=O)NS(=O)(=O)c1ccccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
46881920 8324 0 None 7 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 376 9 2 2 5.9 CCCCc1cnc(C(CC)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1092798 8324 0 None 7 2 Mouse 6.5 pEC50 = 6.5 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 376 9 2 2 5.9 CCCCc1cnc(C(CC)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46887912 9025 0 None 16 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 396 3 2 5 3.7 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1Cl)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1098513 9025 0 None 16 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 396 3 2 5 3.7 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1Cl)C3 10.1016/j.bmcl.2010.03.065
46887877 8972 0 None 19 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 363 3 2 6 2.5 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccn1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1098188 8972 0 None 19 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 363 3 2 6 2.5 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccn1)C3 10.1016/j.bmcl.2010.03.065
46887981 9090 0 None -28 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 418 5 2 5 3.9 CCC(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1099123 9090 0 None -28 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 418 5 2 5 3.9 CCC(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
54580462 60831 0 None -4 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 422 6 3 5 3.9 CC(C)(C)CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762251 60831 0 None -4 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 422 6 3 5 3.9 CC(C)(C)CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
44589874 188405 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 344 4 1 4 4.3 COc1ccc2nc(C(C)Cc3cc4c(cc3Cl)OCO4)[nH]c2c1 10.1016/j.bmcl.2008.09.033
CHEMBL501895 188405 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 344 4 1 4 4.3 COc1ccc2nc(C(C)Cc3cc4c(cc3Cl)OCO4)[nH]c2c1 10.1016/j.bmcl.2008.09.033
3288900 8954 8 None 2 2 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 364 3 2 6 1.9 Nc1n[nH]c2nc(N3CCOCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1098098 8954 8 None 2 2 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 364 3 2 6 1.9 Nc1n[nH]c2nc(N3CCOCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
46884628 8253 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 348 7 2 3 4.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(N)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1092381 8253 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 348 7 2 3 4.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(N)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
59618710 82780 0 None -7 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 473 2 1 4 6.2 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1cc(F)c(Cl)nc1N2 10.1021/ml200207w
CHEMBL2179910 82780 0 None -7 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 473 2 1 4 6.2 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1cc(F)c(Cl)nc1N2 10.1021/ml200207w
46881604 8870 0 None -25 2 Human 6.4 pEC50 = 6.4 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 374 6 2 2 5.6 O=C(O)c1ccccc1-c1ccc(CCc2ncc(C3CCCCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1097362 8870 0 None -25 2 Human 6.4 pEC50 = 6.4 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 374 6 2 2 5.6 O=C(O)c1ccccc1-c1ccc(CCc2ncc(C3CCCCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
71460964 82783 0 None -11 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 475 2 1 4 6.2 Cc1ccc2c(c1)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179913 82783 0 None -11 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 475 2 1 4 6.2 Cc1ccc2c(c1)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
59618709 82777 1 None 14 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 455 2 1 4 6.1 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(Cl)nc1N2 10.1021/ml200207w
CHEMBL2179908 82777 1 None 14 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 455 2 1 4 6.1 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(Cl)nc1N2 10.1021/ml200207w
54582478 60852 0 None -3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 388 6 3 6 2.9 O=S(=O)(Nc1nc(C2CCC2)n[nH]1)c1cnccc1NC1CC2CCC1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762274 60852 0 None -3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 388 6 3 6 2.9 O=S(=O)(Nc1nc(C2CCC2)n[nH]1)c1cnccc1NC1CC2CCC1C2 10.1016/j.bmcl.2011.02.011
4254919 8656 9 None 12 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 362 3 2 5 3.1 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1095423 8656 9 None 12 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 362 3 2 5 3.1 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
4581089 193901 5 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 348 4 1 5 4.2 COc1ccc2nc(SCc3cc4c(cc3Cl)OCO4)[nH]c2c1 10.1016/j.bmcl.2008.09.033
CHEMBL527650 193901 5 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 348 4 1 5 4.2 COc1ccc2nc(SCc3cc4c(cc3Cl)OCO4)[nH]c2c1 10.1016/j.bmcl.2008.09.033
46882059 5952 0 None 14 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 362 9 2 2 5.3 CCCCc1cnc(CCCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1079869 5952 0 None 14 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 362 9 2 2 5.3 CCCCc1cnc(CCCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46887914 14230 0 None 2 2 Rat 5.4 pEC50 = 5.4 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 380 3 2 5 3.2 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccc(F)cc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1199153 14230 0 None 2 2 Rat 5.4 pEC50 = 5.4 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 380 3 2 5 3.2 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccc(F)cc1)C3 10.1016/j.bmcl.2010.03.065
54581471 60832 0 None 6 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 444 5 3 5 3.6 O=C(NC12CC3CC(CC(C3)C1)C2)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762252 60832 0 None 6 2 Mouse 7.4 pEC50 = 7.4 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 444 5 3 5 3.6 O=C(NC12CC3CC(CC(C3)C1)C2)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
46881643 7781 0 None -6 2 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 376 7 2 2 5.5 CC(C)(C)CCc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1089382 7781 0 None -6 2 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 376 7 2 2 5.5 CC(C)(C)CCc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
155794 206633 97 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 329 5 1 5 3.9 COc1ccc2nc(SCc3ncc(C)c(OC)c3C)[nH]c2c1 10.1016/j.bmcl.2008.09.033
CHEMBL892 206633 97 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 329 5 1 5 3.9 COc1ccc2nc(SCc3ncc(C)c(OC)c3C)[nH]c2c1 10.1016/j.bmcl.2008.09.033
46889209 7531 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 429 10 2 4 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3cnn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1087442 7531 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 429 10 2 4 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3cnn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
90663959 106780 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 502 11 4 3 4.4 C[C@H](NCc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL3144492 106780 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 502 11 4 3 4.4 C[C@H](NCc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
46884577 8112 0 None 2 2 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccnc3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091599 8112 0 None 2 2 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccnc3)cc2)n1 10.1016/j.bmcl.2010.02.076
46889176 7442 0 None 10 2 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 444 10 3 5 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(N)n[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1086674 7442 0 None 10 2 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 444 10 3 5 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(N)n[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
46885311 8315 0 None 2 2 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 424 7 2 2 6.0 O=C(O)c1cc(F)c(F)cc1-c1ccc(CCc2nc(CC3CCCCC3)c[nH]2)cc1 10.1016/j.bmcl.2010.02.076
CHEMBL1092730 8315 0 None 2 2 Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 424 7 2 2 6.0 O=C(O)c1cc(F)c(F)cc1-c1ccc(CCc2nc(CC3CCCCC3)c[nH]2)cc1 10.1016/j.bmcl.2010.02.076
62707364 81875 0 None 8 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 529 3 1 7 5.9 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4ncon4)c32)cc1 10.1021/ml200304j
CHEMBL2164580 81875 0 None 8 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 529 3 1 7 5.9 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4ncon4)c32)cc1 10.1021/ml200304j
54583453 60849 0 None -3 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 389 5 3 5 3.5 CC(C)(C)c1cc(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)[nH]n1 10.1016/j.bmcl.2011.02.011
CHEMBL1762271 60849 0 None -3 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 389 5 3 5 3.5 CC(C)(C)c1cc(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)[nH]n1 10.1016/j.bmcl.2011.02.011
54581474 60850 0 None -4 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 376 6 3 6 2.7 CC(C)c1n[nH]c(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)n1 10.1016/j.bmcl.2011.02.011
CHEMBL1762272 60850 0 None -4 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 376 6 3 6 2.7 CC(C)c1n[nH]c(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)n1 10.1016/j.bmcl.2011.02.011
46887946 8791 0 None 25 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 406 3 2 7 2.8 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccc2c(c1)OCO2)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1096546 8791 0 None 25 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 406 3 2 7 2.8 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccc2c(c1)OCO2)C3 10.1016/j.bmcl.2010.03.065
46861857 7440 0 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 461 10 3 4 6.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(=S)[nH][nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1086672 7440 0 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 461 10 3 4 6.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(=S)[nH][nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
46881601 9074 0 None -5 2 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 388 7 2 2 5.7 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CCCCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1099032 9074 0 None -5 2 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 388 7 2 2 5.7 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CCCCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
54581474 60850 0 None 4 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 376 6 3 6 2.7 CC(C)c1n[nH]c(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)n1 10.1016/j.bmcl.2011.02.011
CHEMBL1762272 60850 0 None 4 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 376 6 3 6 2.7 CC(C)c1n[nH]c(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)n1 10.1016/j.bmcl.2011.02.011
46881962 6173 0 None -52 2 Human 5.4 pEC50 = 5.4 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 412 8 2 3 5.2 COc1cccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)c1 10.1016/j.bmcl.2010.01.154
CHEMBL1081130 6173 0 None -52 2 Human 5.4 pEC50 = 5.4 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 412 8 2 3 5.2 COc1cccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)c1 10.1016/j.bmcl.2010.01.154
46888019 9063 0 None 1 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 458 5 2 5 4.6 O=C(Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3)C1CCCC1 10.1016/j.bmcl.2010.03.065
CHEMBL1098838 9063 0 None 1 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 458 5 2 5 4.6 O=C(Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3)C1CCCC1 10.1016/j.bmcl.2010.03.065
46888067 8673 0 None -6 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 432 5 2 5 5.0 CC(C)(C)CNc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1095529 8673 0 None -6 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 432 5 2 5 5.0 CC(C)(C)CNc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
59618747 81871 0 None 6 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 538 3 1 5 6.9 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4cccnc4)c32)cc1 10.1021/ml200304j
CHEMBL2164576 81871 0 None 6 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 538 3 1 5 6.9 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4cccnc4)c32)cc1 10.1021/ml200304j
46889235 7659 0 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 406 8 2 4 5.0 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCC[C@@H]3c3ncn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1088411 7659 0 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 406 8 2 4 5.0 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCC[C@@H]3c3ncn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
25026058 7669 0 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 377 7 2 3 5.0 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCc4cn[nH]c43)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1088553 7669 0 None -2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 377 7 2 3 5.0 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCc4cn[nH]c43)cc2)n1 10.1016/j.bmcl.2010.03.028
46884687 8172 0 None -3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 324 7 1 5 3.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ncnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091917 8172 0 None -3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 324 7 1 5 3.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ncnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
46884576 8111 0 None -4 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 331 6 1 2 5.0 c1ccc(-c2ccc(CCc3nc(CC4CCCC4)c[nH]3)cc2)nc1 10.1016/j.bmcl.2010.02.076
CHEMBL1091598 8111 0 None -4 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 331 6 1 2 5.0 c1ccc(-c2ccc(CCc3nc(CC4CCCC4)c[nH]3)cc2)nc1 10.1016/j.bmcl.2010.02.076
59618698 82661 0 None 6 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 517 3 1 5 6.1 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(OC(F)(F)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179476 82661 0 None 6 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 517 3 1 5 6.1 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(OC(F)(F)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
54580465 60837 0 None 1 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 390 5 3 5 3.2 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC(C)(C)c1ccccc1 10.1016/j.bmcl.2011.02.011
CHEMBL1762258 60837 0 None 1 2 Mouse 5.4 pEC50 = 5.4 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 390 5 3 5 3.2 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC(C)(C)c1ccccc1 10.1016/j.bmcl.2011.02.011
46881472 7662 0 None -56 2 Human 5.4 pEC50 = 5.4 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 396 7 2 2 5.5 Cc1cccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)c1 10.1016/j.bmcl.2010.01.154
CHEMBL1088468 7662 0 None -56 2 Human 5.4 pEC50 = 5.4 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 396 7 2 2 5.5 Cc1cccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)c1 10.1016/j.bmcl.2010.01.154
46884661 7818 0 None -3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 334 7 1 3 4.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cnccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089512 7818 0 None -3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 334 7 1 3 4.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cnccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
46888018 9062 0 None 2 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 460 5 2 5 4.9 CC(C)(C)CC(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1098837 9062 0 None 2 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 460 5 2 5 4.9 CC(C)(C)CC(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
46881644 7843 0 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 348 5 2 2 4.9 CC(C)(C)c1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1089720 7843 0 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 348 5 2 2 4.9 CC(C)(C)c1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46882060 6313 0 None 2 2 Human 5.4 pEC50 = 5.4 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 346 7 2 2 5.3 CCCCc1cnc(/C=C/c2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1081866 6313 0 None 2 2 Human 5.4 pEC50 = 5.4 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 346 7 2 2 5.3 CCCCc1cnc(/C=C/c2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46884660 6442 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 339 7 1 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cnsc3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1082471 6442 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 339 7 1 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cnsc3)cc2)n1 10.1016/j.bmcl.2010.02.076
1214469 60825 1 None -5 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 352 5 3 5 2.1 CC(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762245 60825 1 None -5 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 352 5 3 5 2.1 CC(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
54587369 60833 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 354 4 3 5 2.6 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC1CCCCC1 10.1016/j.bmcl.2011.02.011
CHEMBL1762253 60833 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 354 4 3 5 2.6 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC1CCCCC1 10.1016/j.bmcl.2011.02.011
54580463 60835 0 None -11 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 408 4 3 5 3.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@H]2CC[C@]1(C)C2(C)C 10.1016/j.bmcl.2011.02.011
CHEMBL1762255 60835 0 None -11 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 408 4 3 5 3.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@H]2CC[C@]1(C)C2(C)C 10.1016/j.bmcl.2011.02.011
CHEMBL403317 212530 27 None -6309 4 Human 5.4 pEC50 = 5.4 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)CN)[C@@H](C)O)C(N)=O 10.1021/jm0210921
4254919 8656 9 None -12 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 362 3 2 5 3.1 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1095423 8656 9 None -12 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 362 3 2 5 3.1 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
90663962 106783 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 468 11 4 3 3.7 C[C@H](NCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL3144495 106783 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 468 11 4 3 3.7 C[C@H](NCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
46882057 5922 0 None -2 2 Human 5.3 pEC50 = 5.3 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 390 9 2 2 6.1 CCCCc1cnc(C(Cc2ccc(-c3ccccc3C(=O)O)cc2)C(C)C)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1079696 5922 0 None -2 2 Human 5.3 pEC50 = 5.3 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 390 9 2 2 6.1 CCCCc1cnc(C(Cc2ccc(-c3ccccc3C(=O)O)cc2)C(C)C)[nH]1 10.1016/j.bmcl.2010.01.154
25025860 569 32 None -14 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
6188 569 32 None -14 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1091720 569 32 None -14 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
25025860 569 32 None -14 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1021/ml100196d
6188 569 32 None -14 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1021/ml100196d
CHEMBL1091720 569 32 None -14 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1021/ml100196d
46888066 8672 0 None 21 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 390 5 2 5 3.9 CCNc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1095528 8672 0 None 21 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 390 5 2 5 3.9 CCNc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
46887982 8744 0 None -47 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 432 5 2 5 4.1 CC(C)C(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1096193 8744 0 None -47 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 432 5 2 5 4.1 CC(C)C(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
46887824 8953 0 None 20 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 380 3 2 5 3.0 Nc1n[nH]c2nc(N3CCC(F)CC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1098097 8953 0 None 20 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 380 3 2 5 3.0 Nc1n[nH]c2nc(N3CCC(F)CC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
25128865 82658 0 None 9 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 475 3 1 4 6.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179473 82658 0 None 9 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 475 3 1 4 6.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
54581470 60828 0 None 3 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762248 60828 0 None 3 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
54584420 60842 0 None 1 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 365 5 2 5 2.9 CC(C)(C)CC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762264 60842 0 None 1 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 365 5 2 5 2.9 CC(C)(C)CC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
46882061 6350 0 None -5 2 Human 5.3 pEC50 = 5.3 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 368 6 2 2 5.2 O=C(O)c1ccccc1-c1ccc(CCc2ncc(-c3ccccc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1082041 6350 0 None -5 2 Human 5.3 pEC50 = 5.3 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 368 6 2 2 5.2 O=C(O)c1ccccc1-c1ccc(CCc2ncc(-c3ccccc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46881602 9075 0 None 15 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 402 7 2 2 6.1 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CCCCCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1099033 9075 0 None 15 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 402 7 2 2 6.1 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CCCCCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46861857 7440 0 None 2 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 461 10 3 4 6.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(=S)[nH][nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1086672 7440 0 None 2 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 461 10 3 4 6.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(=S)[nH][nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
59618678 82776 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 446 2 1 5 5.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C#N)nc1N2 10.1021/ml200207w
CHEMBL2179907 82776 0 None 3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 446 2 1 5 5.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C#N)nc1N2 10.1021/ml200207w
66901749 82781 0 None 18 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 475 2 1 4 6.2 Cc1cccc2c1N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179911 82781 0 None 18 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 475 2 1 4 6.2 Cc1cccc2c1N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
59618678 82776 0 None -3 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 446 2 1 5 5.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C#N)nc1N2 10.1021/ml200207w
CHEMBL2179907 82776 0 None -3 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 446 2 1 5 5.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C#N)nc1N2 10.1021/ml200207w
46881558 7333 0 None 31 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 400 7 2 2 5.3 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccc(F)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1086177 7333 0 None 31 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 400 7 2 2 5.3 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccc(F)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
54580461 60830 0 None -4 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 380 6 3 5 2.9 CCC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762250 60830 0 None -4 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 380 6 3 5 2.9 CCC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
54582478 60852 0 None 3 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 388 6 3 6 2.9 O=S(=O)(Nc1nc(C2CCC2)n[nH]1)c1cnccc1NC1CC2CCC1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762274 60852 0 None 3 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 388 6 3 6 2.9 O=S(=O)(Nc1nc(C2CCC2)n[nH]1)c1cnccc1NC1CC2CCC1C2 10.1016/j.bmcl.2011.02.011
25110720 178828 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 332 4 1 5 3.5 COc1ccc2nc(COc3cc4c(cc3Cl)OCO4)[nH]c2c1 10.1016/j.bmcl.2008.09.033
CHEMBL469313 178828 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 332 4 1 5 3.5 COc1ccc2nc(COc3cc4c(cc3Cl)OCO4)[nH]c2c1 10.1016/j.bmcl.2008.09.033
46881963 6174 0 None 10 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 412 8 2 3 5.2 COc1ccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1081131 6174 0 None 10 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 412 8 2 3 5.2 COc1ccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
59618790 81788 0 None 12 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 587 4 2 8 6.1 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(C(C)(C)O)n4)c32)cc1 10.1021/ml200304j
CHEMBL2164223 81788 0 None 12 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 587 4 2 8 6.1 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(C(C)(C)O)n4)c32)cc1 10.1021/ml200304j
62707365 81877 0 None 11 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 573 4 2 8 6.0 C[C@H](O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(C)(C)C)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
CHEMBL2164582 81877 0 None 11 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 573 4 2 8 6.0 C[C@H](O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(C)(C)C)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
46885313 8102 0 None -3 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 377 8 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C(=O)O)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091554 8102 0 None -3 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 377 8 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C(=O)O)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
46882012 5892 0 None 5 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 404 11 2 2 6.6 CCCCc1cnc(C(CCCC)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1079518 5892 0 None 5 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 404 11 2 2 6.6 CCCCc1cnc(C(CCCC)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46881963 6174 0 None -10 2 Human 5.3 pEC50 = 5.3 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 412 8 2 3 5.2 COc1ccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1081131 6174 0 None -10 2 Human 5.3 pEC50 = 5.3 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 412 8 2 3 5.2 COc1ccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46884659 7817 0 None -3 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 340 7 1 4 4.7 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3csnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089511 7817 0 None -3 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 340 7 1 4 4.7 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3csnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
46889148 7685 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 406 10 2 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCC(=O)O)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1088686 7685 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 406 10 2 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCC(=O)O)cc2)n1 10.1016/j.bmcl.2010.03.028
59618778 82660 0 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 511 3 1 6 4.6 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(S(C)(=O)=O)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179475 82660 0 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 511 3 1 6 4.6 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(S(C)(=O)=O)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
46888020 9096 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 460 6 2 5 4.9 CCC(C)(C)C(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1099135 9096 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 460 6 2 5 4.9 CCC(C)(C)C(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
46881419 6858 0 None -8 2 Human 5.3 pEC50 = 5.3 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 407 7 2 3 5.0 N#Cc1ccccc1Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1084130 6858 0 None -8 2 Human 5.3 pEC50 = 5.3 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 407 7 2 3 5.0 N#Cc1ccccc1Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
53242205 60827 0 None -3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762247 60827 0 None -3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
46887912 9025 0 None -16 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 396 3 2 5 3.7 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1Cl)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1098513 9025 0 None -16 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 396 3 2 5 3.7 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1Cl)C3 10.1016/j.bmcl.2010.03.065
46882059 5952 0 None -14 2 Human 5.3 pEC50 = 5.3 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 362 9 2 2 5.3 CCCCc1cnc(CCCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1079869 5952 0 None -14 2 Human 5.3 pEC50 = 5.3 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 362 9 2 2 5.3 CCCCc1cnc(CCCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
59618753 81876 0 None 14 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 559 4 2 8 5.4 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(CO)n4)c32)cc1 10.1021/ml200304j
CHEMBL2164581 81876 0 None 14 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 559 4 2 8 5.4 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(CO)n4)c32)cc1 10.1021/ml200304j
46889232 7513 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 401 6 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc3c(c2)CN(C)C(=O)c2ccccc2-3)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1087200 7513 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 401 6 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc3c(c2)CN(C)C(=O)c2ccccc2-3)n1 10.1016/j.bmcl.2010.03.028
46889145 9076 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 398 7 2 4 4.8 c1ccc(-c2nnn[nH]2)c(-c2ccc(CCc3nc(CC4CCCC4)c[nH]3)cc2)c1 10.1016/j.bmcl.2010.03.028
CHEMBL1099034 9076 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 398 7 2 4 4.8 c1ccc(-c2nnn[nH]2)c(-c2ccc(CCc3nc(CC4CCCC4)c[nH]3)cc2)c1 10.1016/j.bmcl.2010.03.028
59618778 82660 0 None -2 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 511 3 1 6 4.6 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(S(C)(=O)=O)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179475 82660 0 None -2 2 Mouse 6.3 pEC50 = 6.3 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 511 3 1 6 4.6 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(S(C)(=O)=O)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
46884663 7823 0 None 3 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 323 7 1 4 3.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ccnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089523 7823 0 None 3 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 323 7 1 4 3.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ccnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
62707364 81875 0 None -8 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 529 3 1 7 5.9 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4ncon4)c32)cc1 10.1021/ml200304j
CHEMBL2164580 81875 0 None -8 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 529 3 1 7 5.9 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4ncon4)c32)cc1 10.1021/ml200304j
90663966 106787 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 592 14 6 4 3.0 NC(=O)CC[C@H](NC(=O)Cc1cc2ccccc2[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL3144499 106787 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 592 14 6 4 3.0 NC(=O)CC[C@H](NC(=O)Cc1cc2ccccc2[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
46884662 7822 0 None -6 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 323 7 1 4 3.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cncn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089522 7822 0 None -6 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 323 7 1 4 3.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cncn3)cc2)n1 10.1016/j.bmcl.2010.02.076
44589928 179004 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 336 3 1 4 4.2 Clc1ccc2nc(COc3cc4c(cc3Cl)OCO4)[nH]c2c1 10.1016/j.bmcl.2008.09.033
CHEMBL471016 179004 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay
ChEMBL 336 3 1 4 4.2 Clc1ccc2nc(COc3cc4c(cc3Cl)OCO4)[nH]c2c1 10.1016/j.bmcl.2008.09.033
59618747 81871 0 None -6 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 538 3 1 5 6.9 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4cccnc4)c32)cc1 10.1021/ml200304j
CHEMBL2164576 81871 0 None -6 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 538 3 1 5 6.9 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4cccnc4)c32)cc1 10.1021/ml200304j
46881561 6993 0 None -83 2 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 360 7 2 2 4.9 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1084698 6993 0 None -83 2 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 360 7 2 2 4.9 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46881964 6175 0 None -8 2 Human 5.2 pEC50 = 5.2 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 407 7 2 3 5.0 N#Cc1ccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1081132 6175 0 None -8 2 Human 5.2 pEC50 = 5.2 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 407 7 2 3 5.0 N#Cc1ccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
54584421 60843 0 None 13 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 367 4 2 6 2.9 CC(C)(C)OC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762265 60843 0 None 13 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 367 4 2 6 2.9 CC(C)(C)OC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
44300407 196922 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 489 10 5 3 4.1 O=C(NNCc1ccc(Cl)cc1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL56626 196922 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 489 10 5 3 4.1 O=C(NNCc1ccc(Cl)cc1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
46881643 7781 0 None 6 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 376 7 2 2 5.5 CC(C)(C)CCc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1089382 7781 0 None 6 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 376 7 2 2 5.5 CC(C)(C)CCc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
25025858 7782 0 None 16 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 362 6 2 2 5.1 CC(C)(C)Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1089383 7782 0 None 16 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 362 6 2 2 5.1 CC(C)(C)Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46884660 6442 0 None 1 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 339 7 1 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cnsc3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1082471 6442 0 None 1 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 339 7 1 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cnsc3)cc2)n1 10.1016/j.bmcl.2010.02.076
59618730 82663 0 None 4 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 500 3 1 5 6.0 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C#N)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179478 82663 0 None 4 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 500 3 1 5 6.0 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C#N)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
46888068 8675 0 None 1 2 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 376 3 1 6 3.1 Cn1nc(N)c2c3c(c(N4CCCCC4)nc21)CN(Cc1ccccc1)CC3 10.1016/j.bmcl.2010.03.065
CHEMBL1095530 8675 0 None 1 2 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 376 3 1 6 3.1 Cn1nc(N)c2c3c(c(N4CCCCC4)nc21)CN(Cc1ccccc1)CC3 10.1016/j.bmcl.2010.03.065
46885311 8315 0 None -2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 424 7 2 2 6.0 O=C(O)c1cc(F)c(F)cc1-c1ccc(CCc2nc(CC3CCCCC3)c[nH]2)cc1 10.1016/j.bmcl.2010.02.076
CHEMBL1092730 8315 0 None -2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 424 7 2 2 6.0 O=C(O)c1cc(F)c(F)cc1-c1ccc(CCc2nc(CC3CCCCC3)c[nH]2)cc1 10.1016/j.bmcl.2010.02.076
46884630 8420 0 None -2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 339 7 1 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccns3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1093459 8420 0 None -2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 339 7 1 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccns3)cc2)n1 10.1016/j.bmcl.2010.02.076
62707362 81872 0 None 14 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 541 3 1 6 6.3 Cn1cc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(C)(C)C)cc2)Cc2ccc(C(F)(F)F)nc2N3)cn1 10.1021/ml200304j
CHEMBL2164577 81872 0 None 14 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 541 3 1 6 6.3 Cn1cc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(C)(C)C)cc2)Cc2ccc(C(F)(F)F)nc2N3)cn1 10.1021/ml200304j
66901760 82782 0 None 10 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 495 2 1 4 6.5 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(Cl)c32)cc1 10.1021/ml200207w
CHEMBL2179912 82782 0 None 10 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 495 2 1 4 6.5 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(Cl)c32)cc1 10.1021/ml200207w
46888017 9061 0 None 24 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 446 4 2 5 4.5 CC(C)(C)C(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1098836 9061 0 None 24 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 446 4 2 5 4.5 CC(C)(C)C(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
59618821 74190 0 None 7 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 657 6 2 9 6.4 CC(C)(O)c1nc(C(C)(C)c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1016/j.bmc.2012.03.029
CHEMBL2023110 74190 0 None 7 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 657 6 2 9 6.4 CC(C)(O)c1nc(C(C)(C)c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1016/j.bmc.2012.03.029
54585380 60844 0 None -3 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 380 4 2 5 2.8 CN(C(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2)C(C)(C)C 10.1016/j.bmcl.2011.02.011
CHEMBL1762266 60844 0 None -3 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 380 4 2 5 2.8 CN(C(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2)C(C)(C)C 10.1016/j.bmcl.2011.02.011
54581472 60841 0 None -18 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 365 4 3 4 3.1 CC(C)(C)NC(=O)NS(=O)(=O)c1ccccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762263 60841 0 None -18 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 365 4 3 4 3.1 CC(C)(C)NC(=O)NS(=O)(=O)c1ccccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
90663961 106782 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 544 12 4 3 4.3 C[C@H](NC(=O)CCc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL3144494 106782 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 544 12 4 3 4.3 C[C@H](NC(=O)CCc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL438926 213811 19 None -190 3 Human 5.2 pEC50 = 5.2 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)CNC(=O)CNC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)[C@@H](C)O)C(C)C)[C@@H](C)O)C(C)C)C(N)=O 10.1021/jm0210921
46884663 7823 0 None -3 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 323 7 1 4 3.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ccnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089523 7823 0 None -3 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 323 7 1 4 3.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ccnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
46881603 9132 0 None -19 2 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 402 8 2 2 6.1 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CCC3CCCCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1099370 9132 0 None -19 2 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 402 8 2 2 6.1 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CCC3CCCCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46881419 6858 0 None 8 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 407 7 2 3 5.0 N#Cc1ccccc1Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1084130 6858 0 None 8 2 Mouse 6.2 pEC50 = 6.2 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 407 7 2 3 5.0 N#Cc1ccccc1Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
54583451 60846 0 None 1 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 380 4 2 5 2.8 CN(C(=O)NC(C)(C)C)S(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762268 60846 0 None 1 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 380 4 2 5 2.8 CN(C(=O)NC(C)(C)C)S(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
25025861 8380 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 351 7 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccc(F)cn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1093184 8380 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 351 7 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccc(F)cn3)cc2)n1 10.1016/j.bmcl.2010.02.076
25025861 8380 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 351 7 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccc(F)cn3)cc2)n1 10.1021/ml100196d
CHEMBL1093184 8380 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 351 7 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccc(F)cn3)cc2)n1 10.1021/ml100196d
25026445 57945 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 367 5 2 3 4.7 CC(C)(C)Cc1c[nH]c(CC(C)(O)c2ccc(-c3ccc(F)cn3)cc2)n1 10.1021/ml100196d
CHEMBL1672352 57945 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 367 5 2 3 4.7 CC(C)(C)Cc1c[nH]c(CC(C)(O)c2ccc(-c3ccc(F)cn3)cc2)n1 10.1021/ml100196d
59618821 74190 0 None -7 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 657 6 2 9 6.4 CC(C)(O)c1nc(C(C)(C)c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1016/j.bmc.2012.03.029
CHEMBL2023110 74190 0 None -7 2 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 657 6 2 9 6.4 CC(C)(O)c1nc(C(C)(C)c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1016/j.bmc.2012.03.029
46887877 8972 0 None -19 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 363 3 2 6 2.5 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccn1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1098188 8972 0 None -19 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 363 3 2 6 2.5 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccn1)C3 10.1016/j.bmcl.2010.03.065
46888067 8673 0 None 6 2 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 432 5 2 5 5.0 CC(C)(C)CNc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1095529 8673 0 None 6 2 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 432 5 2 5 5.0 CC(C)(C)CNc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
54583450 60838 0 None -3 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 388 4 3 5 3.0 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC1CCc2ccccc21 10.1016/j.bmcl.2011.02.011
CHEMBL1762259 60838 0 None -3 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 388 4 3 5 3.0 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC1CCc2ccccc21 10.1016/j.bmcl.2011.02.011
62707528 81787 0 None 11 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 573 4 2 8 6.0 C[C@@H](O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(C)(C)C)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
CHEMBL2164222 81787 0 None 11 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 573 4 2 8 6.0 C[C@@H](O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(C)(C)C)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
71460937 82662 0 None 10 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 493 3 1 4 6.4 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179477 82662 0 None 10 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 493 3 1 4 6.4 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
54586336 60836 0 None 1 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 362 5 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NCc1ccccc1 10.1016/j.bmcl.2011.02.011
CHEMBL1762257 60836 0 None 1 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 362 5 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NCc1ccccc1 10.1016/j.bmcl.2011.02.011
46881561 6993 0 None 83 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 360 7 2 2 4.9 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1084698 6993 0 None 83 2 Mouse 8.2 pEC50 = 8.2 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 360 7 2 2 4.9 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46881601 9074 0 None 5 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 388 7 2 2 5.7 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CCCCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1099032 9074 0 None 5 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 388 7 2 2 5.7 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CCCCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
90663960 106781 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 540 11 4 5 3.0 C[C@H](NC(=O)Cc1ccc2c(c1)OCO2)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL3144493 106781 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 540 11 4 5 3.0 C[C@H](NC(=O)Cc1ccc2c(c1)OCO2)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
25025654 570 13 None 1 3 Mouse 8.1 pEC50 = 8.1 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 10.1016/j.bmcl.2010.01.154
6189 570 13 None 1 3 Mouse 8.1 pEC50 = 8.1 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 10.1016/j.bmcl.2010.01.154
8506 570 13 None 1 3 Mouse 8.1 pEC50 = 8.1 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 10.1016/j.bmcl.2010.01.154
CHEMBL1084942 570 13 None 1 3 Mouse 8.1 pEC50 = 8.1 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 10.1016/j.bmcl.2010.01.154
46881473 7676 0 None 19 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 400 7 2 2 5.3 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3cccc(F)c3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1088614 7676 0 None 19 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 400 7 2 2 5.3 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3cccc(F)c3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
44300503 100900 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 523 11 3 4 3.4 O=C(CN1CCN(Cc2ccccc2)CC1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL293820 100900 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 523 11 3 4 3.4 O=C(CN1CCN(Cc2ccccc2)CC1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
54581473 60845 0 None 1 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 365 4 4 5 2.3 CC(C)(C)NC(=N)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762267 60845 0 None 1 2 Mouse 5.2 pEC50 = 5.2 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 365 4 4 5 2.3 CC(C)(C)NC(=N)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
46888019 9063 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 458 5 2 5 4.6 O=C(Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3)C1CCCC1 10.1016/j.bmcl.2010.03.065
CHEMBL1098838 9063 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 458 5 2 5 4.6 O=C(Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3)C1CCCC1 10.1016/j.bmcl.2010.03.065
90663964 106785 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 582 15 6 5 1.9 NC(=O)CC[C@H](NC(=O)[C@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL3144497 106785 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 582 15 6 5 1.9 NC(=O)CC[C@H](NC(=O)[C@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
46881560 6992 0 None 13 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 346 7 2 2 4.5 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1084697 6992 0 None 13 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 346 7 2 2 4.5 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
54584418 60829 0 None -6 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@@H]2CC[C@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762249 60829 0 None -6 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@@H]2CC[C@H]1C2 10.1016/j.bmcl.2011.02.011
46881964 6175 0 None 8 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 407 7 2 3 5.0 N#Cc1ccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1081132 6175 0 None 8 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 407 7 2 3 5.0 N#Cc1ccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46200989 2562 15 None 9 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2012.03.029
8502 2562 15 None 9 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2012.03.029
CHEMBL2023109 2562 15 None 9 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2012.03.029
46881472 7662 0 None 56 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 396 7 2 2 5.5 Cc1cccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)c1 10.1016/j.bmcl.2010.01.154
CHEMBL1088468 7662 0 None 56 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 396 7 2 2 5.5 Cc1cccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)c1 10.1016/j.bmcl.2010.01.154
54586336 60836 0 None -1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 362 5 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NCc1ccccc1 10.1016/j.bmcl.2011.02.011
CHEMBL1762257 60836 0 None -1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 362 5 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NCc1ccccc1 10.1016/j.bmcl.2011.02.011
46888069 8883 0 None 13 2 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 404 3 1 7 3.2 CC(=O)n1nc(N)c2c3c(c(N4CCCCC4)nc21)CN(Cc1ccccc1)CC3 10.1016/j.bmcl.2010.03.065
CHEMBL1097471 8883 0 None 13 2 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 404 3 1 7 3.2 CC(=O)n1nc(N)c2c3c(c(N4CCCCC4)nc21)CN(Cc1ccccc1)CC3 10.1016/j.bmcl.2010.03.065
136118727 81874 0 None -1 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 545 3 2 7 5.2 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(=O)[nH]4)c32)cc1 10.1021/ml200304j
CHEMBL2164579 81874 0 None -1 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 545 3 2 7 5.2 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(=O)[nH]4)c32)cc1 10.1021/ml200304j
25128867 74191 0 None -10 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 669 6 2 9 6.5 CC(C)(O)c1nc(C2(c3cccc4c3N(S(=O)(=O)c3ccc(OC(F)(F)F)cc3)Cc3ccc(C(F)(F)F)nc3N4)CCC2)no1 10.1016/j.bmc.2012.03.029
CHEMBL2023111 74191 0 None -10 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 669 6 2 9 6.5 CC(C)(O)c1nc(C2(c3cccc4c3N(S(=O)(=O)c3ccc(OC(F)(F)F)cc3)Cc3ccc(C(F)(F)F)nc3N4)CCC2)no1 10.1016/j.bmc.2012.03.029
46881683 8362 0 None -2 2 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 390 9 2 2 5.9 CCC(C)(CC)Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1093080 8362 0 None -2 2 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 390 9 2 2 5.9 CCC(C)(CC)Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46887875 8903 0 None 1 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 336 4 3 5 2.9 CC(C)Nc1nc2[nH]nc(N)c2c2c1CN(Cc1ccccc1)CC2 10.1016/j.bmcl.2010.03.065
CHEMBL1097551 8903 0 None 1 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 336 4 3 5 2.9 CC(C)Nc1nc2[nH]nc(N)c2c2c1CN(Cc1ccccc1)CC2 10.1016/j.bmcl.2010.03.065
136118727 81874 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 545 3 2 7 5.2 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(=O)[nH]4)c32)cc1 10.1021/ml200304j
CHEMBL2164579 81874 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 545 3 2 7 5.2 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(=O)[nH]4)c32)cc1 10.1021/ml200304j
71451990 82785 0 None 6 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 537 3 2 5 6.2 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccc(C(C)(C)O)c(F)c32)cc1 10.1021/ml200207w
CHEMBL2179915 82785 0 None 6 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 537 3 2 5 6.2 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccc(C(C)(C)O)c(F)c32)cc1 10.1021/ml200207w
46889176 7442 0 None -10 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 444 10 3 5 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(N)n[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1086674 7442 0 None -10 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 444 10 3 5 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(N)n[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
25025860 569 32 None -4 5 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
6188 569 32 None -4 5 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1091720 569 32 None -4 5 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
59618623 82659 0 None -2 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 501 2 1 4 6.2 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(F)(F)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179474 82659 0 None -2 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 501 2 1 4 6.2 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(F)(F)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
59618730 82663 0 None -4 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 500 3 1 5 6.0 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C#N)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179478 82663 0 None -4 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 500 3 1 5 6.0 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C#N)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
46881962 6173 0 None 52 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 412 8 2 3 5.2 COc1cccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)c1 10.1016/j.bmcl.2010.01.154
CHEMBL1081130 6173 0 None 52 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 412 8 2 3 5.2 COc1cccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)c1 10.1016/j.bmcl.2010.01.154
90663957 106778 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 535 11 5 3 3.8 C[C@H](NC(=O)Cc1cc2ccccc2[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL3144490 106778 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 535 11 5 3 3.8 C[C@H](NC(=O)Cc1cc2ccccc2[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
44300383 198691 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 535 10 4 4 5.5 O=C(N/N=C/c1ccc(-c2cccs2)cc1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL58097 198691 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 535 10 4 4 5.5 O=C(N/N=C/c1ccc(-c2cccs2)cc1)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
46887950 9029 0 None 1 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 376 4 2 5 3.1 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(CCc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1098535 9029 0 None 1 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 376 4 2 5 3.1 Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(CCc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
46881559 6991 0 None 10 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 418 7 2 2 5.4 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3cccc(F)c3F)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1084696 6991 0 None 10 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 418 7 2 2 5.4 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3cccc(F)c3F)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
59618698 82661 0 None -6 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 517 3 1 5 6.1 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(OC(F)(F)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179476 82661 0 None -6 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 517 3 1 5 6.1 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(OC(F)(F)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
53242205 60827 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762247 60827 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
54580465 60837 0 None -1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 390 5 3 5 3.2 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC(C)(C)c1ccccc1 10.1016/j.bmcl.2011.02.011
CHEMBL1762258 60837 0 None -1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 390 5 3 5 3.2 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC(C)(C)c1ccccc1 10.1016/j.bmcl.2011.02.011
46881470 6460 0 None -40 2 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 407 7 2 3 5.0 N#Cc1cccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)c1 10.1016/j.bmcl.2010.01.154
CHEMBL1082542 6460 0 None -40 2 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 407 7 2 3 5.0 N#Cc1cccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)c1 10.1016/j.bmcl.2010.01.154
25128867 74191 0 None 10 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 669 6 2 9 6.5 CC(C)(O)c1nc(C2(c3cccc4c3N(S(=O)(=O)c3ccc(OC(F)(F)F)cc3)Cc3ccc(C(F)(F)F)nc3N4)CCC2)no1 10.1016/j.bmc.2012.03.029
CHEMBL2023111 74191 0 None 10 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 669 6 2 9 6.5 CC(C)(O)c1nc(C2(c3cccc4c3N(S(=O)(=O)c3ccc(OC(F)(F)F)cc3)Cc3ccc(C(F)(F)F)nc3N4)CCC2)no1 10.1016/j.bmc.2012.03.029
54584421 60843 0 None -13 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 367 4 2 6 2.9 CC(C)(C)OC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762265 60843 0 None -13 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 367 4 2 6 2.9 CC(C)(C)OC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
46881508 7466 0 None -26 2 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 416 7 2 2 5.8 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3cccc(Cl)c3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1086913 7466 0 None -26 2 Human 6.1 pEC50 = 6.1 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 416 7 2 2 5.8 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3cccc(Cl)c3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
59618790 81788 0 None -12 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 587 4 2 8 6.1 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(C(C)(C)O)n4)c32)cc1 10.1021/ml200304j
CHEMBL2164223 81788 0 None -12 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 587 4 2 8 6.1 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(C(C)(C)O)n4)c32)cc1 10.1021/ml200304j
54584420 60842 0 None -1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 365 5 2 5 2.9 CC(C)(C)CC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762264 60842 0 None -1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 365 5 2 5 2.9 CC(C)(C)CC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
54583451 60846 0 None -1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 380 4 2 5 2.8 CN(C(=O)NC(C)(C)C)S(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762268 60846 0 None -1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 380 4 2 5 2.8 CN(C(=O)NC(C)(C)C)S(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
25128865 82658 0 None -9 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 475 3 1 4 6.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179473 82658 0 None -9 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 475 3 1 4 6.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
46887768 8586 0 None 11 2 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 376 3 2 5 3.3 CC1CCN(c2nc3[nH]nc(N)c3c3c2CN(Cc2ccccc2)CC3)CC1 10.1016/j.bmcl.2010.03.065
CHEMBL1094772 8586 0 None 11 2 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 376 3 2 5 3.3 CC1CCN(c2nc3[nH]nc(N)c3c3c2CN(Cc2ccccc2)CC3)CC1 10.1016/j.bmcl.2010.03.065
1214469 60825 1 None 5 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 352 5 3 5 2.1 CC(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762245 60825 1 None 5 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 352 5 3 5 2.1 CC(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
46881559 6991 0 None -10 2 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 418 7 2 2 5.4 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3cccc(F)c3F)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1084696 6991 0 None -10 2 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 418 7 2 2 5.4 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3cccc(F)c3F)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46882061 6350 0 None 5 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 368 6 2 2 5.2 O=C(O)c1ccccc1-c1ccc(CCc2ncc(-c3ccccc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1082041 6350 0 None 5 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 368 6 2 2 5.2 O=C(O)c1ccccc1-c1ccc(CCc2ncc(-c3ccccc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
71451991 82786 0 None 15 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 477 2 2 5 5.6 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(O)c32)cc1 10.1021/ml200207w
CHEMBL2179916 82786 0 None 15 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 477 2 2 5 5.6 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(O)c32)cc1 10.1021/ml200207w
46881602 9075 0 None -15 2 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 402 7 2 2 6.1 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CCCCCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1099033 9075 0 None -15 2 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 402 7 2 2 6.1 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CCCCCC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46884662 7822 0 None -6 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 323 7 1 4 3.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cncn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089522 7822 0 None -6 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 323 7 1 4 3.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cncn3)cc2)n1 10.1016/j.bmcl.2010.02.076
46884687 8172 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 324 7 1 5 3.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ncnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091917 8172 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 324 7 1 5 3.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ncnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
62707365 81877 0 None -11 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 573 4 2 8 6.0 C[C@H](O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(C)(C)C)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
CHEMBL2164582 81877 0 None -11 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 573 4 2 8 6.0 C[C@H](O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(C)(C)C)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
46887826 8581 0 None 1 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 322 3 2 5 2.2 CN(C)c1nc2[nH]nc(N)c2c2c1CN(Cc1ccccc1)CC2 10.1016/j.bmcl.2010.03.065
CHEMBL1094728 8581 0 None 1 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 322 3 2 5 2.2 CN(C)c1nc2[nH]nc(N)c2c2c1CN(Cc1ccccc1)CC2 10.1016/j.bmcl.2010.03.065
25025862 7821 0 None 2 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 322 7 1 3 4.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089521 7821 0 None 2 2 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 322 7 1 3 4.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
46881471 6461 0 None 13 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 396 7 2 2 5.5 Cc1ccccc1Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1082543 6461 0 None 13 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 396 7 2 2 5.5 Cc1ccccc1Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
44300413 100726 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 538 9 6 4 3.0 O=C(CC1NCCc2ccccc21)NNC(=O)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
CHEMBL292646 100726 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 538 9 6 4 3.0 O=C(CC1NCCc2ccccc21)NNC(=O)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
46881510 7614 0 None 18 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 400 7 2 2 5.3 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccccc3F)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
CHEMBL1088062 7614 0 None 18 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 400 7 2 2 5.3 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccccc3F)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46845425 1032 2 None -1 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
8504 1032 2 None -1 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1089721 1032 2 None -1 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
46845425 1032 2 None -1 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.03.028
8504 1032 2 None -1 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.03.028
CHEMBL1089721 1032 2 None -1 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.03.028
46845425 1032 2 None -1 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.01.154
8504 1032 2 None -1 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.01.154
CHEMBL1089721 1032 2 None -1 2 Mouse 8.0 pEC50 = 8.0 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.01.154
46885313 8102 0 None 3 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 377 8 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C(=O)O)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091554 8102 0 None 3 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 377 8 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C(=O)O)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
54586335 60834 0 None 12 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 408 4 3 5 3.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@]1(C)C2(C)C 10.1016/j.bmcl.2011.02.011
CHEMBL1762254 60834 0 None 12 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 408 4 3 5 3.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@]1(C)C2(C)C 10.1016/j.bmcl.2011.02.011
46884627 8377 0 None 3 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 349 7 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(O)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1093170 8377 0 None 3 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 349 7 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(O)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
46884663 7823 0 None -3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 323 7 1 4 3.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ccnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089523 7823 0 None -3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 323 7 1 4 3.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ccnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
59618753 81876 0 None -14 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 559 4 2 8 5.4 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(CO)n4)c32)cc1 10.1021/ml200304j
CHEMBL2164581 81876 0 None -14 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 559 4 2 8 5.4 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(CO)n4)c32)cc1 10.1021/ml200304j
46881961 5831 0 None 28 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 348 8 2 2 4.9 CCCCc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1079114 5831 0 None 28 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 348 8 2 2 4.9 CCCCc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46845425 1032 2 None -1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
8504 1032 2 None -1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1089721 1032 2 None -1 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
11891917 60826 1 None -8 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 352 5 3 5 2.1 CC(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762246 60826 1 None -8 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human BRS3 by functional assayAgonist activity at human BRS3 by functional assay
ChEMBL 352 5 3 5 2.1 CC(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
46885312 8101 0 None -10 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 377 8 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccnc3C(=O)O)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091553 8101 0 None -10 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 377 8 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccnc3C(=O)O)cc2)n1 10.1016/j.bmcl.2010.02.076
46884578 8180 0 None -3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 333 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccncc3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091984 8180 0 None -3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 333 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccncc3)cc2)n1 10.1016/j.bmcl.2010.02.076
46884629 8379 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 358 7 1 3 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C#N)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1093183 8379 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 358 7 1 3 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C#N)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
25134006 81790 0 None -11 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 599 4 2 8 5.8 CC(C)(O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
CHEMBL2164225 81790 0 None -11 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 599 4 2 8 5.8 CC(C)(O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
46885311 8315 0 None 2 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 424 7 2 2 6.0 O=C(O)c1cc(F)c(F)cc1-c1ccc(CCc2nc(CC3CCCCC3)c[nH]2)cc1 10.1016/j.bmcl.2010.02.076
CHEMBL1092730 8315 0 None 2 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 424 7 2 2 6.0 O=C(O)c1cc(F)c(F)cc1-c1ccc(CCc2nc(CC3CCCCC3)c[nH]2)cc1 10.1016/j.bmcl.2010.02.076
59618658 82666 0 None -2 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 507 2 1 5 6.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1csc(C(F)(F)F)c1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179481 82666 0 None -2 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 507 2 1 5 6.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1csc(C(F)(F)F)c1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
46887765 8657 0 None 10 2 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 348 3 2 5 2.7 Nc1n[nH]c2nc(N3CCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1095424 8657 0 None 10 2 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 348 3 2 5 2.7 Nc1n[nH]c2nc(N3CCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
46884628 8253 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 348 7 2 3 4.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(N)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1092381 8253 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 348 7 2 3 4.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(N)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
25025861 8380 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 351 7 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccc(F)cn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1093184 8380 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 351 7 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccc(F)cn3)cc2)n1 10.1016/j.bmcl.2010.02.076
56840673 1141 0 None 2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
8503 1141 0 None 2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
CHEMBL2164575 1141 0 None 2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
46885312 8101 0 None 10 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 377 8 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccnc3C(=O)O)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091553 8101 0 None 10 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 377 8 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccnc3C(=O)O)cc2)n1 10.1016/j.bmcl.2010.02.076
46884577 8112 0 None 2 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 333 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccnc3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091599 8112 0 None 2 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 333 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccnc3)cc2)n1 10.1016/j.bmcl.2010.02.076
46884576 8111 0 None -4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 331 6 1 2 5.0 c1ccc(-c2ccc(CCc3nc(CC4CCCC4)c[nH]3)cc2)nc1 10.1016/j.bmcl.2010.02.076
CHEMBL1091598 8111 0 None -4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 331 6 1 2 5.0 c1ccc(-c2ccc(CCc3nc(CC4CCCC4)c[nH]3)cc2)nc1 10.1016/j.bmcl.2010.02.076
46884577 8112 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 333 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccnc3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091599 8112 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 333 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccnc3)cc2)n1 10.1016/j.bmcl.2010.02.076
11891917 60826 1 None 8 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 352 5 3 5 2.1 CC(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762246 60826 1 None 8 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 352 5 3 5 2.1 CC(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
59618709 82777 1 None -14 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 455 2 1 4 6.1 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(Cl)nc1N2 10.1021/ml200207w
CHEMBL2179908 82777 1 None -14 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 455 2 1 4 6.1 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(Cl)nc1N2 10.1021/ml200207w
25025860 569 32 None -14 5 Human 7.0 pEC50 = 7 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
6188 569 32 None -14 5 Human 7.0 pEC50 = 7 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1091720 569 32 None -14 5 Human 7.0 pEC50 = 7 Functional
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
46884687 8172 0 None 3 2 Mouse 7.0 pEC50 = 7 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 324 7 1 5 3.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ncnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091917 8172 0 None 3 2 Mouse 7.0 pEC50 = 7 Functional
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 324 7 1 5 3.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ncnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
62707207 81791 0 None -5 2 Mouse 7.0 pEC50 = 7 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 597 6 2 9 5.4 CC(C)(O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
CHEMBL2164226 81791 0 None -5 2 Mouse 7.0 pEC50 = 7 Functional
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 597 6 2 9 5.4 CC(C)(O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
46887982 8744 0 None 47 2 Rat 7.0 pEC50 = 7 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 432 5 2 5 4.1 CC(C)C(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
CHEMBL1096193 8744 0 None 47 2 Rat 7.0 pEC50 = 7 Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assayAgonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
ChEMBL 432 5 2 5 4.1 CC(C)C(=O)Nc1n[nH]c2nc(N3CCCCC3)c3c(c12)CCN(Cc1ccccc1)C3 10.1016/j.bmcl.2010.03.065
11261 1155 0 None -2 2 Human 6.6 pEC50 = 6.6 Functional
In a Ca aequorin assay.In a Ca aequorin assay.
Guide to Pharmacology 428 4 1 3 5.0 COc1ccc2c(c1)C(=O)N(Cc1ccccc1)C(c1c2cccc1)C(=O)NC(C)(C)C 28324017
154733031 1155 0 None -2 2 Human 6.6 pEC50 = 6.6 Functional
In a Ca aequorin assay.In a Ca aequorin assay.
Guide to Pharmacology 428 4 1 3 5.0 COc1ccc2c(c1)C(=O)N(Cc1ccccc1)C(c1c2cccc1)C(=O)NC(C)(C)C 28324017
11261 1155 0 None 2 2 Rat 7.0 pEC50 = 7 Functional
In a Ca aequorin assay.In a Ca aequorin assay.
Guide to Pharmacology 428 4 1 3 5.0 COc1ccc2c(c1)C(=O)N(Cc1ccccc1)C(c1c2cccc1)C(=O)NC(C)(C)C 28324017
154733031 1155 0 None 2 2 Rat 7.0 pEC50 = 7 Functional
In a Ca aequorin assay.In a Ca aequorin assay.
Guide to Pharmacology 428 4 1 3 5.0 COc1ccc2c(c1)C(=O)N(Cc1ccccc1)C(c1c2cccc1)C(=O)NC(C)(C)C 28324017
10569 2837 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 31675498
145996512 2837 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 31675498
6192 3097 0 None -3 3 Rat 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 482 10 4 3 3.4 CC(C(=O)NC(C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NC(=O)c1ccccc1 19580790
73755184 3097 0 None -3 3 Rat 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 482 10 4 3 3.4 CC(C(=O)NC(C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NC(=O)c1ccccc1 19580790
6191 264 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15635635
6191 264 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18006692
6191 264 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20438784
6192 3097 0 None 3 3 Mouse 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 482 10 4 3 3.4 CC(C(=O)NC(C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NC(=O)c1ccccc1 19580790
73755184 3097 0 None 3 3 Mouse 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 482 10 4 3 3.4 CC(C(=O)NC(C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NC(=O)c1ccccc1 19580790
49871766 2557 40 None -17 5 Human 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 24900253
6170 2557 40 None -17 5 Human 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 24900253
CHEMBL1672354 2557 40 None -17 5 Human 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 24900253
8508 1150 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 479 8 2 5 4.5 CC(CCOc1cccc(c1)CC(=O)N1CCNc2c([C@H]1CC(=O)O)ccc(n2)C(F)(F)F)C 24412111
91827365 1150 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 479 8 2 5 4.5 CC(CCOc1cccc(c1)CC(=O)N1CCNc2c([C@H]1CC(=O)O)ccc(n2)C(F)(F)F)C 24412111
8507 1002 0 None 3 2 Human 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 493 7 2 6 4.1 CC(CC(=O)Oc1cccc(c1)CC(=O)N1CCNc2c([C@H]1CC(=O)O)ccc(n2)C(F)(F)F)C 25497965
91827364 1002 0 None 3 2 Human 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 493 7 2 6 4.1 CC(CC(=O)Oc1cccc(c1)CC(=O)N1CCNc2c([C@H]1CC(=O)O)ccc(n2)C(F)(F)F)C 25497965
CHEMBL3356404 1002 0 None 3 2 Human 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 493 7 2 6 4.1 CC(CC(=O)Oc1cccc(c1)CC(=O)N1CCNc2c([C@H]1CC(=O)O)ccc(n2)C(F)(F)F)C 25497965
6192 3097 0 None -4 3 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 482 10 4 3 3.4 CC(C(=O)NC(C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NC(=O)c1ccccc1 12212809
6192 3097 0 None -4 3 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 482 10 4 3 3.4 CC(C(=O)NC(C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NC(=O)c1ccccc1 19580790
73755184 3097 0 None -4 3 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 482 10 4 3 3.4 CC(C(=O)NC(C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NC(=O)c1ccccc1 12212809
73755184 3097 0 None -4 3 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 482 10 4 3 3.4 CC(C(=O)NC(C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NC(=O)c1ccccc1 19580790
72944991 1151 0 None 2 2 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 24412111
72944991 1151 0 None 2 2 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 26524625
72944991 1151 0 None 2 2 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 35644465
8509 1151 0 None 2 2 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 24412111
8509 1151 0 None 2 2 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 26524625
8509 1151 0 None 2 2 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 35644465
CHEMBL3115390 1151 0 None 2 2 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 24412111
CHEMBL3115390 1151 0 None 2 2 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 26524625
CHEMBL3115390 1151 0 None 2 2 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 35644465
10254379 1026 0 None - 1 Human 9.7 pEC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 475 9 5 3 4.4 O=C(N[C@@H](C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NNc1ccc(cc1)Cl 12723954
630 1026 0 None - 1 Human 9.7 pEC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 475 9 5 3 4.4 O=C(N[C@@H](C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NNc1ccc(cc1)Cl 12723954
6192 3097 0 None -4 3 Human 5.3 pIC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 482 10 4 3 3.4 CC(C(=O)NC(C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NC(=O)c1ccccc1 20438784
73755184 3097 0 None -4 3 Human 5.3 pIC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 482 10 4 3 3.4 CC(C(=O)NC(C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NC(=O)c1ccccc1 20438784
8505 2567 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 569 10 4 5 5.8 COc1ccc(cc1)C1(CCCCC1)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)Nc1ccc(cc1)[N+](=O)[O-] 25554218
91827363 2567 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 569 10 4 5 5.8 COc1ccc(cc1)C1(CCCCC1)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)Nc1ccc(cc1)[N+](=O)[O-] 25554218
6191 264 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18006692
6191 264 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20438784
25025654 570 13 None -15 3 Human 7.0 pIC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
6189 570 13 None -15 3 Human 7.0 pIC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
8506 570 13 None -15 3 Human 7.0 pIC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
CHEMBL1084942 570 13 None -15 3 Human 7.0 pIC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
49871766 2557 40 None -17 5 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 23892571
49871766 2557 40 None -17 5 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 24900253
6170 2557 40 None -17 5 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 23892571
6170 2557 40 None -17 5 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 24900253
CHEMBL1672354 2557 40 None -17 5 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 23892571
CHEMBL1672354 2557 40 None -17 5 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 24900253
46845425 1032 2 None 1 2 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 20167483
8504 1032 2 None 1 2 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 20167483
CHEMBL1089721 1032 2 None 1 2 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 20167483
25025860 569 32 None -14 5 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 20096642
6188 569 32 None -14 5 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 20096642
CHEMBL1091720 569 32 None -14 5 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 20096642
633 1505 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18006692
633 1505 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20438784
25025654 570 13 None -1 3 Rat 8.0 pIC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
6189 570 13 None -1 3 Rat 8.0 pIC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
8506 570 13 None -1 3 Rat 8.0 pIC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
CHEMBL1084942 570 13 None -1 3 Rat 8.0 pIC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
6176 573 0 None -4 5 Mouse 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 895 23 7 8 4.8 CC(C[C@@H](C(=O)NCC1=CCCC(=C1)C[N+](C)(C)C)NC(=O)C[C@@H]([C@@H](NC([C@@H](N(C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C)Cc1c[nH]c[nH+]1)O)CC1CCCCC1)O)C 20096642
73755180 573 0 None -4 5 Mouse 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 895 23 7 8 4.8 CC(C[C@@H](C(=O)NCC1=CCCC(=C1)C[N+](C)(C)C)NC(=O)C[C@@H]([C@@H](NC([C@@H](N(C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C)Cc1c[nH]c[nH+]1)O)CC1CCCCC1)O)C 20096642
3946 1503 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18006692
3946 1503 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20438784
25025860 569 32 None -4 5 Mouse 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 20096642
6188 569 32 None -4 5 Mouse 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 20096642
CHEMBL1091720 569 32 None -4 5 Mouse 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 20096642
25025654 570 13 None 1 3 Mouse 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
6189 570 13 None 1 3 Mouse 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
8506 570 13 None 1 3 Mouse 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
CHEMBL1084942 570 13 None 1 3 Mouse 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
46200989 2562 15 None 9 2 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 24900461
8502 2562 15 None 9 2 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 24900461
CHEMBL2023109 2562 15 None 9 2 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 24900461
25025860 569 32 None 4 5 Rat 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 20096642
6188 569 32 None 4 5 Rat 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 20096642
CHEMBL1091720 569 32 None 4 5 Rat 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 20096642
6176 573 0 None -1 5 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 895 23 7 8 4.8 CC(C[C@@H](C(=O)NCC1=CCCC(=C1)C[N+](C)(C)C)NC(=O)C[C@@H]([C@@H](NC([C@@H](N(C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C)Cc1c[nH]c[nH+]1)O)CC1CCCCC1)O)C 20096642
6176 573 0 None -1 5 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 895 23 7 8 4.8 CC(C[C@@H](C(=O)NCC1=CCCC(=C1)C[N+](C)(C)C)NC(=O)C[C@@H]([C@@H](NC([C@@H](N(C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C)Cc1c[nH]c[nH+]1)O)CC1CCCCC1)O)C 23892571
6176 573 0 None -1 5 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 895 23 7 8 4.8 CC(C[C@@H](C(=O)NCC1=CCCC(=C1)C[N+](C)(C)C)NC(=O)C[C@@H]([C@@H](NC([C@@H](N(C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C)Cc1c[nH]c[nH+]1)O)CC1CCCCC1)O)C 30971479
73755180 573 0 None -1 5 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 895 23 7 8 4.8 CC(C[C@@H](C(=O)NCC1=CCCC(=C1)C[N+](C)(C)C)NC(=O)C[C@@H]([C@@H](NC([C@@H](N(C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C)Cc1c[nH]c[nH+]1)O)CC1CCCCC1)O)C 20096642
73755180 573 0 None -1 5 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 895 23 7 8 4.8 CC(C[C@@H](C(=O)NCC1=CCCC(=C1)C[N+](C)(C)C)NC(=O)C[C@@H]([C@@H](NC([C@@H](N(C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C)Cc1c[nH]c[nH+]1)O)CC1CCCCC1)O)C 23892571
73755180 573 0 None -1 5 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 895 23 7 8 4.8 CC(C[C@@H](C(=O)NCC1=CCCC(=C1)C[N+](C)(C)C)NC(=O)C[C@@H]([C@@H](NC([C@@H](N(C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C)Cc1c[nH]c[nH+]1)O)CC1CCCCC1)O)C 30971479
6176 573 0 None 1 5 Rat 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 895 23 7 8 4.8 CC(C[C@@H](C(=O)NCC1=CCCC(=C1)C[N+](C)(C)C)NC(=O)C[C@@H]([C@@H](NC([C@@H](N(C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C)Cc1c[nH]c[nH+]1)O)CC1CCCCC1)O)C 20096642
73755180 573 0 None 1 5 Rat 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 895 23 7 8 4.8 CC(C[C@@H](C(=O)NCC1=CCCC(=C1)C[N+](C)(C)C)NC(=O)C[C@@H]([C@@H](NC([C@@H](N(C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C)Cc1c[nH]c[nH+]1)O)CC1CCCCC1)O)C 20096642
56840673 1141 0 None 2 2 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 24900283
8503 1141 0 None 2 2 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 24900283
CHEMBL2164575 1141 0 None 2 2 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 24900283
635 1450 0 None -6 4 Human 5.6 pIC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9325344
635 1450 0 None -6 4 Human 5.6 pIC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9593699
635 1450 0 None -6 4 Human 5.6 pIC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9765358




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DOI

155511392 169548 0 None - 0 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 516 10 2 5 6.5 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1CCOc1cccc(O)c1 10.1016/j.bmcl.2016.07.056
CHEMBL4435571 169548 0 None - 0 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 516 10 2 5 6.5 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1CCOc1cccc(O)c1 10.1016/j.bmcl.2016.07.056
155511392 169548 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 516 10 2 5 6.5 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1CCOc1cccc(O)c1 10.1016/j.bmcl.2016.07.056
CHEMBL4435571 169548 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 516 10 2 5 6.5 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1CCOc1cccc(O)c1 10.1016/j.bmcl.2016.07.056
155528415 171327 0 None - 0 Human 9.0 pEC50 = 9 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 466 9 1 5 5.3 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CCC(=O)O)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4461212 171327 0 None - 0 Human 9.0 pEC50 = 9 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 466 9 1 5 5.3 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CCC(=O)O)cc1 10.1016/j.bmcl.2016.07.056
76314247 105293 0 None - 0 Mouse 9.0 pEC50 = 9 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 441 4 1 4 5.2 Cc1ccc(Oc2cccc(CC(=O)N3CCNc4nc(C(F)(F)F)ccc4C3)c2)cc1 10.1016/j.bmcl.2013.12.106
CHEMBL3115400 105293 0 None - 0 Mouse 9.0 pEC50 = 9 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 441 4 1 4 5.2 Cc1ccc(Oc2cccc(CC(=O)N3CCNc4nc(C(F)(F)F)ccc4C3)c2)cc1 10.1016/j.bmcl.2013.12.106
76314247 105293 0 None - 0 Mouse 9.0 pEC50 = 9 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 441 4 1 4 5.2 Cc1ccc(Oc2cccc(CC(=O)N3CCNc4nc(C(F)(F)F)ccc4C3)c2)cc1 10.1016/j.bmc.2014.11.018
CHEMBL3115400 105293 0 None - 0 Mouse 9.0 pEC50 = 9 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 441 4 1 4 5.2 Cc1ccc(Oc2cccc(CC(=O)N3CCNc4nc(C(F)(F)F)ccc4C3)c2)cc1 10.1016/j.bmc.2014.11.018
76314247 105293 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 441 4 1 4 5.2 Cc1ccc(Oc2cccc(CC(=O)N3CCNc4nc(C(F)(F)F)ccc4C3)c2)cc1 10.1016/j.bmcl.2013.12.106
CHEMBL3115400 105293 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 441 4 1 4 5.2 Cc1ccc(Oc2cccc(CC(=O)N3CCNc4nc(C(F)(F)F)ccc4C3)c2)cc1 10.1016/j.bmcl.2013.12.106
76314247 105293 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 441 4 1 4 5.2 Cc1ccc(Oc2cccc(CC(=O)N3CCNc4nc(C(F)(F)F)ccc4C3)c2)cc1 10.1016/j.bmc.2014.11.018
CHEMBL3115400 105293 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 441 4 1 4 5.2 Cc1ccc(Oc2cccc(CC(=O)N3CCNc4nc(C(F)(F)F)ccc4C3)c2)cc1 10.1016/j.bmc.2014.11.018
46200989 2562 15 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmcl.2013.12.106
8502 2562 15 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmcl.2013.12.106
CHEMBL2023109 2562 15 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmcl.2013.12.106
76321532 105279 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115386 105279 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2013.12.106
76321532 105279 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3115386 105279 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmc.2014.11.018
72944991 1151 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 10.1016/j.bmcl.2013.12.106
8509 1151 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 10.1016/j.bmcl.2013.12.106
CHEMBL3115390 1151 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 10.1016/j.bmcl.2013.12.106
76328698 105281 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 503 6 2 5 5.0 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccc(F)cc2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115388 105281 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 503 6 2 5 5.0 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccc(F)cc2)c1 10.1016/j.bmcl.2013.12.106
72944991 1151 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 10.1016/j.bmc.2014.11.018
8509 1151 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 10.1016/j.bmc.2014.11.018
CHEMBL3115390 1151 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 10.1016/j.bmc.2014.11.018
76328698 105281 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 503 6 2 5 5.0 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccc(F)cc2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3115388 105281 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 503 6 2 5 5.0 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccc(F)cc2)c1 10.1016/j.bmc.2014.11.018
76317821 105273 0 None - 0 Mouse 7.0 pEC50 = 7 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 419 4 1 4 4.4 O=C(Cc1cccc(OC2CCCC2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
CHEMBL3115380 105273 0 None - 0 Mouse 7.0 pEC50 = 7 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 419 4 1 4 4.4 O=C(Cc1cccc(OC2CCCC2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
76336000 105264 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 428 4 1 5 4.3 O=C(Cc1cccc(Oc2cccnc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
CHEMBL3115371 105264 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 428 4 1 5 4.3 O=C(Cc1cccc(Oc2cccnc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
76328696 105277 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 471 6 2 5 4.8 O=C(Cc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1CCO 10.1016/j.bmcl.2013.12.106
CHEMBL3115384 105277 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 471 6 2 5 4.8 O=C(Cc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1CCO 10.1016/j.bmcl.2013.12.106
155521672 170650 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 452 9 2 4 5.2 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1CCC(=O)O 10.1016/j.bmcl.2016.07.056
CHEMBL4451347 170650 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 452 9 2 4 5.2 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1CCC(=O)O 10.1016/j.bmcl.2016.07.056
155530555 171534 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 515 10 1 6 4.4 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CCNS(C)(=O)=O)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4464287 171534 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 515 10 1 6 4.4 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CCNS(C)(=O)=O)cc1 10.1016/j.bmcl.2016.07.056
76328696 105277 0 None - 0 Mouse 8.0 pEC50 = 8.0 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 471 6 2 5 4.8 O=C(Cc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1CCO 10.1016/j.bmcl.2013.12.106
CHEMBL3115384 105277 0 None - 0 Mouse 8.0 pEC50 = 8.0 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 471 6 2 5 4.8 O=C(Cc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1CCO 10.1016/j.bmcl.2013.12.106
76325133 105275 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 457 5 2 5 4.4 O=C(Cc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1CO 10.1016/j.bmcl.2013.12.106
CHEMBL3115382 105275 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 457 5 2 5 4.4 O=C(Cc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1CO 10.1016/j.bmcl.2013.12.106
8507 1002 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 7 2 6 4.1 CC(CC(=O)Oc1cccc(c1)CC(=O)N1CCNc2c([C@H]1CC(=O)O)ccc(n2)C(F)(F)F)C 10.1016/j.bmc.2014.11.018
91827364 1002 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 7 2 6 4.1 CC(CC(=O)Oc1cccc(c1)CC(=O)N1CCNc2c([C@H]1CC(=O)O)ccc(n2)C(F)(F)F)C 10.1016/j.bmc.2014.11.018
CHEMBL3356404 1002 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 7 2 6 4.1 CC(CC(=O)Oc1cccc(c1)CC(=O)N1CCNc2c([C@H]1CC(=O)O)ccc(n2)C(F)(F)F)C 10.1016/j.bmc.2014.11.018
155543657 173203 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 514 9 2 4 6.5 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1Cc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4522752 173203 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 514 9 2 4 6.5 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1Cc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2016.07.056
76325135 105287 0 None - 0 Mouse 7.9 pEC50 = 7.9 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 427 4 1 4 4.9 O=C(Cc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
CHEMBL3115395 105287 0 None - 0 Mouse 7.9 pEC50 = 7.9 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 427 4 1 4 4.9 O=C(Cc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
76325135 105287 0 None - 0 Mouse 7.9 pEC50 = 7.9 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 427 4 1 4 4.9 O=C(Cc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmc.2014.11.018
CHEMBL3115395 105287 0 None - 0 Mouse 7.9 pEC50 = 7.9 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 427 4 1 4 4.9 O=C(Cc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmc.2014.11.018
76332372 105268 0 None - 0 Mouse 5.9 pEC50 = 5.9 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 379 4 1 4 3.5 CCOc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115375 105268 0 None - 0 Mouse 5.9 pEC50 = 5.9 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 379 4 1 4 3.5 CCOc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
76336002 105272 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 421 4 1 4 4.5 CC(C)(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115379 105272 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 421 4 1 4 4.5 CC(C)(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
76336002 105272 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 421 4 1 4 4.5 CC(C)(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3115379 105272 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 421 4 1 4 4.5 CC(C)(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmc.2014.11.018
155568183 176043 0 None - 0 Mouse 5.9 pEC50 = 5.9 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 420 8 2 4 4.7 CC(C)(C)Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)n1CC(=O)O 10.1016/j.bmcl.2016.07.056
CHEMBL4590481 176043 0 None - 0 Mouse 5.9 pEC50 = 5.9 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 420 8 2 4 4.7 CC(C)(C)Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)n1CC(=O)O 10.1016/j.bmcl.2016.07.056
76328697 105278 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)CC1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115385 105278 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)CC1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2013.12.106
76328697 105278 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)CC1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3115385 105278 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)CC1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmc.2014.11.018
155554592 174623 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 530 10 1 6 6.6 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CCOc2cccc(O)c2)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4557722 174623 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 530 10 1 6 6.6 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CCOc2cccc(O)c2)cc1 10.1016/j.bmcl.2016.07.056
155543657 173203 0 None - 0 Mouse 7.9 pEC50 = 7.9 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 514 9 2 4 6.5 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1Cc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4522752 173203 0 None - 0 Mouse 7.9 pEC50 = 7.9 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 514 9 2 4 6.5 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1Cc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2016.07.056
46200989 2562 15 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2014.11.018
8502 2562 15 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2014.11.018
CHEMBL2023109 2562 15 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2014.11.018
76332370 105262 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 484 5 1 4 5.6 CC(C)C1CN(Cc2ccccc2)c2ccccc2CN1C(=O)Nc1cccc(N2CCOCC2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115369 105262 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 484 5 1 4 5.6 CC(C)C1CN(Cc2ccccc2)c2ccccc2CN1C(=O)Nc1cccc(N2CCOCC2)c1 10.1016/j.bmcl.2013.12.106
76332370 105262 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 484 5 1 4 5.6 CC(C)C1CN(Cc2ccccc2)c2ccccc2CN1C(=O)Nc1cccc(N2CCOCC2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3115369 105262 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 484 5 1 4 5.6 CC(C)C1CN(Cc2ccccc2)c2ccccc2CN1C(=O)Nc1cccc(N2CCOCC2)c1 10.1016/j.bmc.2014.11.018
76336003 105288 0 None - 0 Mouse 5.9 pEC50 = 5.9 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 428 3 2 4 5.4 O=C(Nc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
CHEMBL3115396 105288 0 None - 0 Mouse 5.9 pEC50 = 5.9 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 428 3 2 4 5.4 O=C(Nc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
49871766 2557 40 None -9 3 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1016/j.bmc.2014.11.018
6170 2557 40 None -9 3 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1016/j.bmc.2014.11.018
CHEMBL1672354 2557 40 None -9 3 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1016/j.bmc.2014.11.018
155538227 172366 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 438 8 2 4 4.8 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1CC(=O)O 10.1016/j.bmcl.2016.07.056
CHEMBL4476111 172366 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 438 8 2 4 4.8 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1CC(=O)O 10.1016/j.bmcl.2016.07.056
76328697 105278 0 None - 0 Mouse 7.8 pEC50 = 7.8 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)CC1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115385 105278 0 None - 0 Mouse 7.8 pEC50 = 7.8 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)CC1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2013.12.106
76328697 105278 0 None - 0 Mouse 7.8 pEC50 = 7.8 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)CC1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3115385 105278 0 None - 0 Mouse 7.8 pEC50 = 7.8 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)CC1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmc.2014.11.018
76336000 105264 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 428 4 1 5 4.3 O=C(Cc1cccc(Oc2cccnc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
CHEMBL3115371 105264 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 428 4 1 5 4.3 O=C(Cc1cccc(Oc2cccnc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
76321531 105276 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 471 5 2 5 4.5 O=C(O)C1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115383 105276 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 471 5 2 5 4.5 O=C(O)C1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2013.12.106
76325134 105282 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 465 7 2 5 4.1 CC(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115389 105282 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 465 7 2 5 4.1 CC(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmcl.2013.12.106
76325134 105282 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 465 7 2 5 4.1 CC(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
CHEMBL3115389 105282 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 465 7 2 5 4.1 CC(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
76317820 105267 0 None - 0 Mouse 5.8 pEC50 = 5.8 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 365 3 1 4 3.1 COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115374 105267 0 None - 0 Mouse 5.8 pEC50 = 5.8 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 365 3 1 4 3.1 COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
118721523 116072 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 8 2 6 4.2 CCCCC(=O)Oc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
CHEMBL3356405 116072 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 8 2 6 4.2 CCCCC(=O)Oc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
76325133 105275 0 None - 0 Mouse 7.7 pEC50 = 7.7 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 457 5 2 5 4.4 O=C(Cc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1CO 10.1016/j.bmcl.2013.12.106
CHEMBL3115382 105275 0 None - 0 Mouse 7.7 pEC50 = 7.7 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 457 5 2 5 4.4 O=C(Cc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1CO 10.1016/j.bmcl.2013.12.106
155541223 173000 0 None - 0 Mouse 5.7 pEC50 = 5.7 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 391 9 1 4 4.8 CCC(C)(C)Cc1cn(CC(=O)O)c(CCc2ccc(-c3ccccn3)cc2)n1 10.1016/j.bmcl.2016.07.056
CHEMBL4518142 173000 0 None - 0 Mouse 5.7 pEC50 = 5.7 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 391 9 1 4 4.8 CCC(C)(C)Cc1cn(CC(=O)O)c(CCc2ccc(-c3ccccn3)cc2)n1 10.1016/j.bmcl.2016.07.056
76336002 105272 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 421 4 1 4 4.5 CC(C)(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115379 105272 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 421 4 1 4 4.5 CC(C)(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
76336002 105272 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 421 4 1 4 4.5 CC(C)(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3115379 105272 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 421 4 1 4 4.5 CC(C)(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmc.2014.11.018
155519281 170439 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 501 10 2 5 4.3 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1CCNS(C)(=O)=O 10.1016/j.bmcl.2016.07.056
CHEMBL4448589 170439 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 501 10 2 5 4.3 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1CCNS(C)(=O)=O 10.1016/j.bmcl.2016.07.056
155561529 175630 0 None - 0 Mouse 8.7 pEC50 = 8.7 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 424 8 2 4 4.8 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1CCO 10.1016/j.bmcl.2016.07.056
CHEMBL4580739 175630 0 None - 0 Mouse 8.7 pEC50 = 8.7 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 424 8 2 4 4.8 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1CCO 10.1016/j.bmcl.2016.07.056
76328698 105281 0 None - 0 Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 503 6 2 5 5.0 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccc(F)cc2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115388 105281 0 None - 0 Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 503 6 2 5 5.0 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccc(F)cc2)c1 10.1016/j.bmcl.2013.12.106
76336005 105291 0 None - 0 Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 445 4 1 4 5.0 O=C(Cc1cccc(Oc2ccc(F)cc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
CHEMBL3115399 105291 0 None - 0 Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 445 4 1 4 5.0 O=C(Cc1cccc(Oc2ccc(F)cc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
76328698 105281 0 None - 0 Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 503 6 2 5 5.0 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccc(F)cc2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3115388 105281 0 None - 0 Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 503 6 2 5 5.0 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccc(F)cc2)c1 10.1016/j.bmc.2014.11.018
76336005 105291 0 None - 0 Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 445 4 1 4 5.0 O=C(Cc1cccc(Oc2ccc(F)cc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmc.2014.11.018
CHEMBL3115399 105291 0 None - 0 Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 445 4 1 4 5.0 O=C(Cc1cccc(Oc2ccc(F)cc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmc.2014.11.018
76325132 105266 0 None - 0 Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 442 4 1 5 4.6 Cc1ccc(Oc2cccc(CC(=O)N3CCNc4nc(C(F)(F)F)ccc4C3)c2)cn1 10.1016/j.bmcl.2013.12.106
CHEMBL3115373 105266 0 None - 0 Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 442 4 1 5 4.6 Cc1ccc(Oc2cccc(CC(=O)N3CCNc4nc(C(F)(F)F)ccc4C3)c2)cn1 10.1016/j.bmcl.2013.12.106
76325132 105266 0 None - 0 Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 442 4 1 5 4.6 Cc1ccc(Oc2cccc(CC(=O)N3CCNc4nc(C(F)(F)F)ccc4C3)c2)cn1 10.1016/j.bmc.2014.11.018
CHEMBL3115373 105266 0 None - 0 Mouse 8.6 pEC50 = 8.6 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 442 4 1 5 4.6 Cc1ccc(Oc2cccc(CC(=O)N3CCNc4nc(C(F)(F)F)ccc4C3)c2)cn1 10.1016/j.bmc.2014.11.018
118721525 116074 0 None - 0 Mouse 7.7 pEC50 = 7.7 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 507 6 2 6 4.5 CC(C)(C)CC(=O)Oc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
CHEMBL3356407 116074 0 None - 0 Mouse 7.7 pEC50 = 7.7 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 507 6 2 6 4.5 CC(C)(C)CC(=O)Oc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
76317820 105267 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 365 3 1 4 3.1 COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115374 105267 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 365 3 1 4 3.1 COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
76332372 105268 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 379 4 1 4 3.5 CCOc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115375 105268 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 379 4 1 4 3.5 CCOc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
76332373 105280 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)C[C@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115387 105280 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)C[C@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2013.12.106
76332373 105280 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)C[C@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3115387 105280 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)C[C@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmc.2014.11.018
155539847 172482 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 438 8 1 5 4.8 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CCO)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4482945 172482 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 438 8 1 5 4.8 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CCO)cc1 10.1016/j.bmcl.2016.07.056
49871766 2557 40 None -2 3 Mouse 7.7 pEC50 = 7.7 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1016/j.bmc.2014.11.018
6170 2557 40 None -2 3 Mouse 7.7 pEC50 = 7.7 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1016/j.bmc.2014.11.018
CHEMBL1672354 2557 40 None -2 3 Mouse 7.7 pEC50 = 7.7 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1016/j.bmc.2014.11.018
46200989 2562 15 None - 0 Mouse 7.7 pEC50 = 7.7 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmcl.2013.12.106
8502 2562 15 None - 0 Mouse 7.7 pEC50 = 7.7 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmcl.2013.12.106
CHEMBL2023109 2562 15 None - 0 Mouse 7.7 pEC50 = 7.7 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmcl.2013.12.106
155519753 170442 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 342 6 1 3 4.2 COC(=O)C(C)(C)c1ccc(CCc2ncc(CC(C)(C)C)[nH]2)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4448645 170442 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 342 6 1 3 4.2 COC(=O)C(C)(C)c1ccc(CCc2ncc(CC(C)(C)C)[nH]2)cc1 10.1016/j.bmcl.2016.07.056
76321531 105276 0 None - 0 Mouse 5.7 pEC50 = 5.7 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 471 5 2 5 4.5 O=C(O)C1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115383 105276 0 None - 0 Mouse 5.7 pEC50 = 5.7 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 471 5 2 5 4.5 O=C(O)C1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2013.12.106
76317822 105284 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 439 2 1 3 6.2 CC(C)(C)c1ccc(CC(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccccc32)cc1 10.1016/j.bmcl.2013.12.106
CHEMBL3115392 105284 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 439 2 1 3 6.2 CC(C)(C)c1ccc(CC(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccccc32)cc1 10.1016/j.bmcl.2013.12.106
76317822 105284 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 439 2 1 3 6.2 CC(C)(C)c1ccc(CC(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccccc32)cc1 10.1016/j.bmc.2014.11.018
CHEMBL3115392 105284 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 439 2 1 3 6.2 CC(C)(C)c1ccc(CC(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccccc32)cc1 10.1016/j.bmc.2014.11.018
155539847 172482 0 None - 0 Mouse 7.6 pEC50 = 7.6 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 438 8 1 5 4.8 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CCO)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4482945 172482 0 None - 0 Mouse 7.6 pEC50 = 7.6 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 438 8 1 5 4.8 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CCO)cc1 10.1016/j.bmcl.2016.07.056
76317823 105294 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 428 4 1 5 4.3 O=C(Cc1cccc(Oc2ccccn2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
CHEMBL3115401 105294 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 428 4 1 5 4.3 O=C(Cc1cccc(Oc2ccccn2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
76310619 105286 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 475 4 1 4 6.7 O=C(Cc1cccc(Oc2ccccc2)c1)N1Cc2ccc(C(F)(F)F)nc2Nc2ccccc21 10.1016/j.bmcl.2013.12.106
CHEMBL3115394 105286 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 475 4 1 4 6.7 O=C(Cc1cccc(Oc2ccccc2)c1)N1Cc2ccc(C(F)(F)F)nc2Nc2ccccc21 10.1016/j.bmcl.2013.12.106
76310619 105286 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 475 4 1 4 6.7 O=C(Cc1cccc(Oc2ccccc2)c1)N1Cc2ccc(C(F)(F)F)nc2Nc2ccccc21 10.1016/j.bmc.2014.11.018
CHEMBL3115394 105286 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 475 4 1 4 6.7 O=C(Cc1cccc(Oc2ccccc2)c1)N1Cc2ccc(C(F)(F)F)nc2Nc2ccccc21 10.1016/j.bmc.2014.11.018
155554592 174623 0 None - 0 Mouse 7.6 pEC50 = 7.6 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 530 10 1 6 6.6 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CCOc2cccc(O)c2)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4557722 174623 0 None - 0 Mouse 7.6 pEC50 = 7.6 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 530 10 1 6 6.6 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CCOc2cccc(O)c2)cc1 10.1016/j.bmcl.2016.07.056
76317823 105294 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 428 4 1 5 4.3 O=C(Cc1cccc(Oc2ccccn2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
CHEMBL3115401 105294 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 428 4 1 5 4.3 O=C(Cc1cccc(Oc2ccccn2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
76328694 105263 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 322 3 0 2 4.1 CC(=O)N1Cc2ccccc2N(Cc2ccccc2)CC1C(C)C 10.1016/j.bmcl.2013.12.106
CHEMBL3115370 105263 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 322 3 0 2 4.1 CC(=O)N1Cc2ccccc2N(Cc2ccccc2)CC1C(C)C 10.1016/j.bmcl.2013.12.106
76328694 105263 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 322 3 0 2 4.1 CC(=O)N1Cc2ccccc2N(Cc2ccccc2)CC1C(C)C 10.1016/j.bmc.2014.11.018
CHEMBL3115370 105263 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 322 3 0 2 4.1 CC(=O)N1Cc2ccccc2N(Cc2ccccc2)CC1C(C)C 10.1016/j.bmc.2014.11.018
155520679 170496 0 None - 0 Mouse 7.6 pEC50 = 7.6 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 391 9 1 4 4.8 CCC(C)(C)Cc1cnc(CCc2ccc(-c3ccccn3)cc2)n1CC(=O)O 10.1016/j.bmcl.2016.07.056
CHEMBL4449347 170496 0 None - 0 Mouse 7.6 pEC50 = 7.6 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 391 9 1 4 4.8 CCC(C)(C)Cc1cnc(CCc2ccc(-c3ccccn3)cc2)n1CC(=O)O 10.1016/j.bmcl.2016.07.056
118721522 116071 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 479 6 2 6 3.7 CC(C)C(=O)Oc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
CHEMBL3356403 116071 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 479 6 2 6 3.7 CC(C)C(=O)Oc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
155561529 175630 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 424 8 2 4 4.8 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1CCO 10.1016/j.bmcl.2016.07.056
CHEMBL4580739 175630 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 424 8 2 4 4.8 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1CCO 10.1016/j.bmcl.2016.07.056
155568881 176182 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 528 9 1 5 6.6 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2Cc2ccc(C(=O)O)cc2)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4593256 176182 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 528 9 1 5 6.6 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2Cc2ccc(C(=O)O)cc2)cc1 10.1016/j.bmcl.2016.07.056
155528415 171327 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 466 9 1 5 5.3 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CCC(=O)O)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4461212 171327 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 466 9 1 5 5.3 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CCC(=O)O)cc1 10.1016/j.bmcl.2016.07.056
118721530 116078 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 491 7 2 6 3.7 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(C(=O)OCC2CC2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3356412 116078 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 491 7 2 6 3.7 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(C(=O)OCC2CC2)c1 10.1016/j.bmc.2014.11.018
76321532 105279 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115386 105279 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2013.12.106
76321532 105279 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3115386 105279 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmc.2014.11.018
72944991 1151 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 10.1016/j.bmcl.2013.12.106
8509 1151 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 10.1016/j.bmcl.2013.12.106
CHEMBL3115390 1151 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 10.1016/j.bmcl.2013.12.106
76328699 105289 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 445 4 1 4 5.0 O=C(Cc1cccc(Oc2ccccc2F)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
CHEMBL3115397 105289 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 445 4 1 4 5.0 O=C(Cc1cccc(Oc2ccccc2F)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
72944991 1151 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 10.1016/j.bmc.2014.11.018
8509 1151 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 10.1016/j.bmc.2014.11.018
CHEMBL3115390 1151 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 10.1016/j.bmc.2014.11.018
76336005 105291 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 445 4 1 4 5.0 O=C(Cc1cccc(Oc2ccc(F)cc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
CHEMBL3115399 105291 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 445 4 1 4 5.0 O=C(Cc1cccc(Oc2ccc(F)cc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
76336005 105291 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 445 4 1 4 5.0 O=C(Cc1cccc(Oc2ccc(F)cc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmc.2014.11.018
CHEMBL3115399 105291 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 445 4 1 4 5.0 O=C(Cc1cccc(Oc2ccc(F)cc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmc.2014.11.018
118721530 116078 0 None - 0 Mouse 8.4 pEC50 = 8.4 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 491 7 2 6 3.7 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(C(=O)OCC2CC2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3356412 116078 0 None - 0 Mouse 8.4 pEC50 = 8.4 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 491 7 2 6 3.7 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(C(=O)OCC2CC2)c1 10.1016/j.bmc.2014.11.018
76332373 105280 0 None - 0 Mouse 5.5 pEC50 = 5.5 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)C[C@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115387 105280 0 None - 0 Mouse 5.5 pEC50 = 5.5 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)C[C@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2013.12.106
76332373 105280 0 None - 0 Mouse 5.5 pEC50 = 5.5 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)C[C@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3115387 105280 0 None - 0 Mouse 5.5 pEC50 = 5.5 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)C[C@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmc.2014.11.018
56840673 1141 0 None - 0 Mouse 7.5 pEC50 = 7.5 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2013.12.106
8503 1141 0 None - 0 Mouse 7.5 pEC50 = 7.5 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2013.12.106
CHEMBL2164575 1141 0 None - 0 Mouse 7.5 pEC50 = 7.5 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2013.12.106
56840673 1141 0 None - 0 Mouse 7.5 pEC50 = 7.5 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmc.2014.11.018
8503 1141 0 None - 0 Mouse 7.5 pEC50 = 7.5 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmc.2014.11.018
CHEMBL2164575 1141 0 None - 0 Mouse 7.5 pEC50 = 7.5 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmc.2014.11.018
76332370 105262 0 None - 0 Mouse 7.5 pEC50 = 7.5 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 484 5 1 4 5.6 CC(C)C1CN(Cc2ccccc2)c2ccccc2CN1C(=O)Nc1cccc(N2CCOCC2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115369 105262 0 None - 0 Mouse 7.5 pEC50 = 7.5 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 484 5 1 4 5.6 CC(C)C1CN(Cc2ccccc2)c2ccccc2CN1C(=O)Nc1cccc(N2CCOCC2)c1 10.1016/j.bmcl.2013.12.106
76332370 105262 0 None - 0 Mouse 7.5 pEC50 = 7.5 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 484 5 1 4 5.6 CC(C)C1CN(Cc2ccccc2)c2ccccc2CN1C(=O)Nc1cccc(N2CCOCC2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3115369 105262 0 None - 0 Mouse 7.5 pEC50 = 7.5 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 484 5 1 4 5.6 CC(C)C1CN(Cc2ccccc2)c2ccccc2CN1C(=O)Nc1cccc(N2CCOCC2)c1 10.1016/j.bmc.2014.11.018
118721523 116072 0 None - 0 Mouse 7.5 pEC50 = 7.5 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 8 2 6 4.2 CCCCC(=O)Oc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
CHEMBL3356405 116072 0 None - 0 Mouse 7.5 pEC50 = 7.5 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 8 2 6 4.2 CCCCC(=O)Oc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
76314246 105285 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 475 4 1 4 6.7 O=C(Cc1ccc(Oc2ccccc2)cc1)N1Cc2ccc(C(F)(F)F)nc2Nc2ccccc21 10.1016/j.bmcl.2013.12.106
CHEMBL3115393 105285 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 475 4 1 4 6.7 O=C(Cc1ccc(Oc2ccccc2)cc1)N1Cc2ccc(C(F)(F)F)nc2Nc2ccccc21 10.1016/j.bmcl.2013.12.106
76314246 105285 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 475 4 1 4 6.7 O=C(Cc1ccc(Oc2ccccc2)cc1)N1Cc2ccc(C(F)(F)F)nc2Nc2ccccc21 10.1016/j.bmc.2014.11.018
CHEMBL3115393 105285 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 475 4 1 4 6.7 O=C(Cc1ccc(Oc2ccccc2)cc1)N1Cc2ccc(C(F)(F)F)nc2Nc2ccccc21 10.1016/j.bmc.2014.11.018
76328695 105269 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 393 4 1 4 3.9 CC(C)Oc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115376 105269 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 393 4 1 4 3.9 CC(C)Oc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
76328695 105269 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 393 4 1 4 3.9 CC(C)Oc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3115376 105269 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 393 4 1 4 3.9 CC(C)Oc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmc.2014.11.018
132538074 172830 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 452 8 1 5 4.9 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CC(=O)O)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4514194 172830 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 452 8 1 5 4.9 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CC(=O)O)cc1 10.1016/j.bmcl.2016.07.056
118721529 116077 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 8 2 6 4.1 CCCCOC(=O)c1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
CHEMBL3356411 116077 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 8 2 6 4.1 CCCCOC(=O)c1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
155519281 170439 0 None - 0 Mouse 8.4 pEC50 = 8.4 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 501 10 2 5 4.3 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1CCNS(C)(=O)=O 10.1016/j.bmcl.2016.07.056
CHEMBL4448589 170439 0 None - 0 Mouse 8.4 pEC50 = 8.4 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 501 10 2 5 4.3 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1CCNS(C)(=O)=O 10.1016/j.bmcl.2016.07.056
118721528 116076 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 7 2 6 3.9 CC(C)COC(=O)c1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
CHEMBL3356410 116076 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 7 2 6 3.9 CC(C)COC(=O)c1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
118721527 116075 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 479 6 2 6 3.7 CC(C)OC(=O)c1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
CHEMBL3356409 116075 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 479 6 2 6 3.7 CC(C)OC(=O)c1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
155541223 173000 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 391 9 1 4 4.8 CCC(C)(C)Cc1cn(CC(=O)O)c(CCc2ccc(-c3ccccn3)cc2)n1 10.1016/j.bmcl.2016.07.056
CHEMBL4518142 173000 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 391 9 1 4 4.8 CCC(C)(C)Cc1cn(CC(=O)O)c(CCc2ccc(-c3ccccn3)cc2)n1 10.1016/j.bmcl.2016.07.056
76317821 105273 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 419 4 1 4 4.4 O=C(Cc1cccc(OC2CCCC2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
CHEMBL3115380 105273 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 419 4 1 4 4.4 O=C(Cc1cccc(OC2CCCC2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
118721524 116073 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 491 7 2 6 3.8 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(OC(=O)CC2CC2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3356406 116073 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 491 7 2 6 3.8 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(OC(=O)CC2CC2)c1 10.1016/j.bmc.2014.11.018
155520679 170496 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 391 9 1 4 4.8 CCC(C)(C)Cc1cnc(CCc2ccc(-c3ccccn3)cc2)n1CC(=O)O 10.1016/j.bmcl.2016.07.056
CHEMBL4449347 170496 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 391 9 1 4 4.8 CCC(C)(C)Cc1cnc(CCc2ccc(-c3ccccn3)cc2)n1CC(=O)O 10.1016/j.bmcl.2016.07.056
8507 1002 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 7 2 6 4.1 CC(CC(=O)Oc1cccc(c1)CC(=O)N1CCNc2c([C@H]1CC(=O)O)ccc(n2)C(F)(F)F)C 10.1016/j.bmc.2014.11.018
91827364 1002 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 7 2 6 4.1 CC(CC(=O)Oc1cccc(c1)CC(=O)N1CCNc2c([C@H]1CC(=O)O)ccc(n2)C(F)(F)F)C 10.1016/j.bmc.2014.11.018
CHEMBL3356404 1002 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 7 2 6 4.1 CC(CC(=O)Oc1cccc(c1)CC(=O)N1CCNc2c([C@H]1CC(=O)O)ccc(n2)C(F)(F)F)C 10.1016/j.bmc.2014.11.018
76336003 105288 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 428 3 2 4 5.4 O=C(Nc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
CHEMBL3115396 105288 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 428 3 2 4 5.4 O=C(Nc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
132538074 172830 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 452 8 1 5 4.9 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CC(=O)O)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4514194 172830 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 452 8 1 5 4.9 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CC(=O)O)cc1 10.1016/j.bmcl.2016.07.056
118721527 116075 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 479 6 2 6 3.7 CC(C)OC(=O)c1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
CHEMBL3356409 116075 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 479 6 2 6 3.7 CC(C)OC(=O)c1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
76310619 105286 0 None - 0 Mouse 7.3 pEC50 = 7.3 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 475 4 1 4 6.7 O=C(Cc1cccc(Oc2ccccc2)c1)N1Cc2ccc(C(F)(F)F)nc2Nc2ccccc21 10.1016/j.bmcl.2013.12.106
CHEMBL3115394 105286 0 None - 0 Mouse 7.3 pEC50 = 7.3 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 475 4 1 4 6.7 O=C(Cc1cccc(Oc2ccccc2)c1)N1Cc2ccc(C(F)(F)F)nc2Nc2ccccc21 10.1016/j.bmcl.2013.12.106
76310619 105286 0 None - 0 Mouse 7.3 pEC50 = 7.3 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 475 4 1 4 6.7 O=C(Cc1cccc(Oc2ccccc2)c1)N1Cc2ccc(C(F)(F)F)nc2Nc2ccccc21 10.1016/j.bmc.2014.11.018
CHEMBL3115394 105286 0 None - 0 Mouse 7.3 pEC50 = 7.3 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 475 4 1 4 6.7 O=C(Cc1cccc(Oc2ccccc2)c1)N1Cc2ccc(C(F)(F)F)nc2Nc2ccccc21 10.1016/j.bmc.2014.11.018
76317822 105284 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 439 2 1 3 6.2 CC(C)(C)c1ccc(CC(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccccc32)cc1 10.1016/j.bmcl.2013.12.106
CHEMBL3115392 105284 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 439 2 1 3 6.2 CC(C)(C)c1ccc(CC(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccccc32)cc1 10.1016/j.bmcl.2013.12.106
76317822 105284 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 439 2 1 3 6.2 CC(C)(C)c1ccc(CC(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccccc32)cc1 10.1016/j.bmc.2014.11.018
CHEMBL3115392 105284 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 439 2 1 3 6.2 CC(C)(C)c1ccc(CC(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccccc32)cc1 10.1016/j.bmc.2014.11.018
155552947 174081 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 376 6 1 3 5.2 COC(=O)c1ccccc1-c1ccc(CCc2ncc(CC(C)(C)C)[nH]2)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4544477 174081 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 376 6 1 3 5.2 COC(=O)c1ccccc1-c1ccc(CCc2ncc(CC(C)(C)C)[nH]2)cc1 10.1016/j.bmcl.2016.07.056
155568881 176182 0 None - 0 Mouse 8.3 pEC50 = 8.3 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 528 9 1 5 6.6 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2Cc2ccc(C(=O)O)cc2)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4593256 176182 0 None - 0 Mouse 8.3 pEC50 = 8.3 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 528 9 1 5 6.6 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2Cc2ccc(C(=O)O)cc2)cc1 10.1016/j.bmcl.2016.07.056
118721528 116076 0 None - 0 Mouse 8.3 pEC50 = 8.3 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 7 2 6 3.9 CC(C)COC(=O)c1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
CHEMBL3356410 116076 0 None - 0 Mouse 8.3 pEC50 = 8.3 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 7 2 6 3.9 CC(C)COC(=O)c1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
118721531 116079 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 507 6 2 6 4.3 CC(C)(C)COC(=O)c1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
CHEMBL3356413 116079 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 507 6 2 6 4.3 CC(C)(C)COC(=O)c1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
118721529 116077 0 None - 0 Mouse 8.3 pEC50 = 8.3 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 8 2 6 4.1 CCCCOC(=O)c1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
CHEMBL3356411 116077 0 None - 0 Mouse 8.3 pEC50 = 8.3 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 8 2 6 4.1 CCCCOC(=O)c1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
76336001 105270 0 None - 0 Mouse 7.3 pEC50 = 7.3 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 407 6 1 4 4.3 CCCCOc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115377 105270 0 None - 0 Mouse 7.3 pEC50 = 7.3 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 407 6 1 4 4.3 CCCCOc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
76336001 105270 0 None - 0 Mouse 7.3 pEC50 = 7.3 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 407 6 1 4 4.3 CCCCOc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3115377 105270 0 None - 0 Mouse 7.3 pEC50 = 7.3 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 407 6 1 4 4.3 CCCCOc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmc.2014.11.018
76328695 105269 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 393 4 1 4 3.9 CC(C)Oc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115376 105269 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 393 4 1 4 3.9 CC(C)Oc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
76328695 105269 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 393 4 1 4 3.9 CC(C)Oc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3115376 105269 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 393 4 1 4 3.9 CC(C)Oc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmc.2014.11.018
76336001 105270 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 407 6 1 4 4.3 CCCCOc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115377 105270 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 407 6 1 4 4.3 CCCCOc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
76336001 105270 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 407 6 1 4 4.3 CCCCOc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3115377 105270 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 407 6 1 4 4.3 CCCCOc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmc.2014.11.018
76336004 105290 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 445 4 1 4 5.0 O=C(Cc1cccc(Oc2cccc(F)c2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
CHEMBL3115398 105290 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 445 4 1 4 5.0 O=C(Cc1cccc(Oc2cccc(F)c2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
76328699 105289 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 445 4 1 4 5.0 O=C(Cc1cccc(Oc2ccccc2F)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
CHEMBL3115397 105289 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 445 4 1 4 5.0 O=C(Cc1cccc(Oc2ccccc2F)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
155521672 170650 0 None - 0 Mouse 7.2 pEC50 = 7.2 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 452 9 2 4 5.2 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1CCC(=O)O 10.1016/j.bmcl.2016.07.056
CHEMBL4451347 170650 0 None - 0 Mouse 7.2 pEC50 = 7.2 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 452 9 2 4 5.2 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1CCC(=O)O 10.1016/j.bmcl.2016.07.056
76310617 105271 0 None - 0 Mouse 7.2 pEC50 = 7.2 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 407 5 1 4 4.1 CC(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115378 105271 0 None - 0 Mouse 7.2 pEC50 = 7.2 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 407 5 1 4 4.1 CC(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
76325134 105282 0 None - 0 Mouse 7.2 pEC50 = 7.2 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 465 7 2 5 4.1 CC(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115389 105282 0 None - 0 Mouse 7.2 pEC50 = 7.2 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 465 7 2 5 4.1 CC(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmcl.2013.12.106
76310617 105271 0 None - 0 Mouse 7.2 pEC50 = 7.2 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 407 5 1 4 4.1 CC(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3115378 105271 0 None - 0 Mouse 7.2 pEC50 = 7.2 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 407 5 1 4 4.1 CC(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmc.2014.11.018
76325134 105282 0 None - 0 Mouse 7.2 pEC50 = 7.2 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 465 7 2 5 4.1 CC(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
CHEMBL3115389 105282 0 None - 0 Mouse 7.2 pEC50 = 7.2 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 465 7 2 5 4.1 CC(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
76332371 105265 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 428 4 1 5 4.3 O=C(Cc1cccc(Oc2ccncc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
CHEMBL3115372 105265 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 428 4 1 5 4.3 O=C(Cc1cccc(Oc2ccncc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
155515849 170000 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 358 7 1 4 4.1 COC(=O)C(C)(C)Oc1ccc(CCc2ncc(CC(C)(C)C)[nH]2)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4442362 170000 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 358 7 1 4 4.1 COC(=O)C(C)(C)Oc1ccc(CCc2ncc(CC(C)(C)C)[nH]2)cc1 10.1016/j.bmcl.2016.07.056
155552947 174081 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 376 6 1 3 5.2 COC(=O)c1ccccc1-c1ccc(CCc2ncc(CC(C)(C)C)[nH]2)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4544477 174081 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 376 6 1 3 5.2 COC(=O)c1ccccc1-c1ccc(CCc2ncc(CC(C)(C)C)[nH]2)cc1 10.1016/j.bmcl.2016.07.056
118721522 116071 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 479 6 2 6 3.7 CC(C)C(=O)Oc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
CHEMBL3356403 116071 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 479 6 2 6 3.7 CC(C)C(=O)Oc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
155538227 172366 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 438 8 2 4 4.8 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1CC(=O)O 10.1016/j.bmcl.2016.07.056
CHEMBL4476111 172366 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 438 8 2 4 4.8 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1CC(=O)O 10.1016/j.bmcl.2016.07.056
155543793 173215 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 434 8 1 5 4.8 COC(=O)c1ccccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CC(=O)O)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4522974 173215 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 434 8 1 5 4.8 COC(=O)c1ccccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CC(=O)O)cc1 10.1016/j.bmcl.2016.07.056
155530555 171534 0 None - 0 Mouse 8.2 pEC50 = 8.2 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 515 10 1 6 4.4 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CCNS(C)(=O)=O)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4464287 171534 0 None - 0 Mouse 8.2 pEC50 = 8.2 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 515 10 1 6 4.4 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CCNS(C)(=O)=O)cc1 10.1016/j.bmcl.2016.07.056
76310617 105271 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 407 5 1 4 4.1 CC(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
CHEMBL3115378 105271 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 407 5 1 4 4.1 CC(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmcl.2013.12.106
76310617 105271 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 407 5 1 4 4.1 CC(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3115378 105271 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 407 5 1 4 4.1 CC(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmc.2014.11.018
46200989 2562 15 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2014.11.018
8502 2562 15 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2014.11.018
CHEMBL2023109 2562 15 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2014.11.018
76314245 105274 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 433 4 1 4 4.8 O=C(Cc1cccc(OC2CCCCC2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
CHEMBL3115381 105274 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 433 4 1 4 4.8 O=C(Cc1cccc(OC2CCCCC2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
118721531 116079 0 None - 0 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 507 6 2 6 4.3 CC(C)(C)COC(=O)c1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
CHEMBL3356413 116079 0 None - 0 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 507 6 2 6 4.3 CC(C)(C)COC(=O)c1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
76325135 105287 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 427 4 1 4 4.9 O=C(Cc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
CHEMBL3115395 105287 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 427 4 1 4 4.9 O=C(Cc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
76325135 105287 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 427 4 1 4 4.9 O=C(Cc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmc.2014.11.018
CHEMBL3115395 105287 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 427 4 1 4 4.9 O=C(Cc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmc.2014.11.018
118721525 116074 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 507 6 2 6 4.5 CC(C)(C)CC(=O)Oc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
CHEMBL3356407 116074 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 507 6 2 6 4.5 CC(C)(C)CC(=O)Oc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3[C@H]2CC(=O)O)c1 10.1016/j.bmc.2014.11.018
76314245 105274 0 None - 0 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 433 4 1 4 4.8 O=C(Cc1cccc(OC2CCCCC2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
CHEMBL3115381 105274 0 None - 0 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 433 4 1 4 4.8 O=C(Cc1cccc(OC2CCCCC2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
76336004 105290 0 None - 0 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 445 4 1 4 5.0 O=C(Cc1cccc(Oc2cccc(F)c2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
CHEMBL3115398 105290 0 None - 0 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 445 4 1 4 5.0 O=C(Cc1cccc(Oc2cccc(F)c2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
118721524 116073 0 None - 0 Mouse 7.1 pEC50 = 7.1 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 491 7 2 6 3.8 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(OC(=O)CC2CC2)c1 10.1016/j.bmc.2014.11.018
CHEMBL3356406 116073 0 None - 0 Mouse 7.1 pEC50 = 7.1 Binding
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 491 7 2 6 3.8 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(OC(=O)CC2CC2)c1 10.1016/j.bmc.2014.11.018
155568183 176043 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 420 8 2 4 4.7 CC(C)(C)Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)n1CC(=O)O 10.1016/j.bmcl.2016.07.056
CHEMBL4590481 176043 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 420 8 2 4 4.7 CC(C)(C)Cc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)n1CC(=O)O 10.1016/j.bmcl.2016.07.056
76325132 105266 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 442 4 1 5 4.6 Cc1ccc(Oc2cccc(CC(=O)N3CCNc4nc(C(F)(F)F)ccc4C3)c2)cn1 10.1016/j.bmcl.2013.12.106
CHEMBL3115373 105266 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 442 4 1 5 4.6 Cc1ccc(Oc2cccc(CC(=O)N3CCNc4nc(C(F)(F)F)ccc4C3)c2)cn1 10.1016/j.bmcl.2013.12.106
76325132 105266 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 442 4 1 5 4.6 Cc1ccc(Oc2cccc(CC(=O)N3CCNc4nc(C(F)(F)F)ccc4C3)c2)cn1 10.1016/j.bmc.2014.11.018
CHEMBL3115373 105266 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 442 4 1 5 4.6 Cc1ccc(Oc2cccc(CC(=O)N3CCNc4nc(C(F)(F)F)ccc4C3)c2)cn1 10.1016/j.bmc.2014.11.018
76328694 105263 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 322 3 0 2 4.1 CC(=O)N1Cc2ccccc2N(Cc2ccccc2)CC1C(C)C 10.1016/j.bmcl.2013.12.106
CHEMBL3115370 105263 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 322 3 0 2 4.1 CC(=O)N1Cc2ccccc2N(Cc2ccccc2)CC1C(C)C 10.1016/j.bmcl.2013.12.106
76328694 105263 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 322 3 0 2 4.1 CC(=O)N1Cc2ccccc2N(Cc2ccccc2)CC1C(C)C 10.1016/j.bmc.2014.11.018
CHEMBL3115370 105263 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 322 3 0 2 4.1 CC(=O)N1Cc2ccccc2N(Cc2ccccc2)CC1C(C)C 10.1016/j.bmc.2014.11.018
155543793 173215 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 434 8 1 5 4.8 COC(=O)c1ccccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CC(=O)O)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4522974 173215 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 434 8 1 5 4.8 COC(=O)c1ccccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CC(=O)O)cc1 10.1016/j.bmcl.2016.07.056
56840673 1141 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2013.12.106
8503 1141 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2013.12.106
CHEMBL2164575 1141 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2013.12.106
56840673 1141 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmc.2014.11.018
8503 1141 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmc.2014.11.018
CHEMBL2164575 1141 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmc.2014.11.018
76332371 105265 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 428 4 1 5 4.3 O=C(Cc1cccc(Oc2ccncc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
CHEMBL3115372 105265 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 428 4 1 5 4.3 O=C(Cc1cccc(Oc2ccncc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
155519753 170442 0 None - 0 Mouse 5.0 pEC50 = 5 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 342 6 1 3 4.2 COC(=O)C(C)(C)c1ccc(CCc2ncc(CC(C)(C)C)[nH]2)cc1 10.1016/j.bmcl.2016.07.056
CHEMBL4448645 170442 0 None - 0 Mouse 5.0 pEC50 = 5 Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 342 6 1 3 4.2 COC(=O)C(C)(C)c1ccc(CCc2ncc(CC(C)(C)C)[nH]2)cc1 10.1016/j.bmcl.2016.07.056
25129212 74192 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingDisplacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
ChEMBL 574 5 2 6 5.2 CC(C)(C(N)=O)c1cccc2c1N(S(=O)(=O)c1ccc(OC(F)(F)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1016/j.bmc.2012.03.029
CHEMBL2023112 74192 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingDisplacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
ChEMBL 574 5 2 6 5.2 CC(C)(C(N)=O)c1cccc2c1N(S(=O)(=O)c1ccc(OC(F)(F)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1016/j.bmc.2012.03.029
59618746 74193 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingDisplacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
ChEMBL 586 5 2 6 5.4 NC(=O)C1(c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)CCC1 10.1016/j.bmc.2012.03.029
CHEMBL2023113 74193 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingDisplacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
ChEMBL 586 5 2 6 5.4 NC(=O)C1(c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)CCC1 10.1016/j.bmc.2012.03.029
25128867 74191 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingDisplacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
ChEMBL 669 6 2 9 6.5 CC(C)(O)c1nc(C2(c3cccc4c3N(S(=O)(=O)c3ccc(OC(F)(F)F)cc3)Cc3ccc(C(F)(F)F)nc3N4)CCC2)no1 10.1016/j.bmc.2012.03.029
CHEMBL2023111 74191 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingDisplacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
ChEMBL 669 6 2 9 6.5 CC(C)(O)c1nc(C2(c3cccc4c3N(S(=O)(=O)c3ccc(OC(F)(F)F)cc3)Cc3ccc(C(F)(F)F)nc3N4)CCC2)no1 10.1016/j.bmc.2012.03.029
59618681 82788 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 512 2 1 5 6.4 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccc4ncccc4c32)cc1 10.1021/ml200207w
CHEMBL2179918 82788 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 512 2 1 5 6.4 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccc4ncccc4c32)cc1 10.1021/ml200207w
59618753 81876 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 559 4 2 8 5.4 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(CO)n4)c32)cc1 10.1021/ml200304j
CHEMBL2164581 81876 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 559 4 2 8 5.4 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(CO)n4)c32)cc1 10.1021/ml200304j
62707362 81872 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 541 3 1 6 6.3 Cn1cc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(C)(C)C)cc2)Cc2ccc(C(F)(F)F)nc2N3)cn1 10.1021/ml200304j
CHEMBL2164577 81872 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 541 3 1 6 6.3 Cn1cc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(C)(C)C)cc2)Cc2ccc(C(F)(F)F)nc2N3)cn1 10.1021/ml200304j
66901749 82781 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 475 2 1 4 6.2 Cc1cccc2c1N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179911 82781 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 475 2 1 4 6.2 Cc1cccc2c1N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
59618790 81788 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 587 4 2 8 6.1 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(C(C)(C)O)n4)c32)cc1 10.1021/ml200304j
CHEMBL2164223 81788 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 587 4 2 8 6.1 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(C(C)(C)O)n4)c32)cc1 10.1021/ml200304j
62707364 81875 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 529 3 1 7 5.9 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4ncon4)c32)cc1 10.1021/ml200304j
CHEMBL2164580 81875 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 529 3 1 7 5.9 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4ncon4)c32)cc1 10.1021/ml200304j
CHEMBL413893 213099 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of bombesin subtype 3 receptor expressed in human lung carcinoidsInhibition of bombesin subtype 3 receptor expressed in human lung carcinoids
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(N)=O 10.1021/jm049437y
59618709 82777 1 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 455 2 1 4 6.1 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(Cl)nc1N2 10.1021/ml200207w
CHEMBL2179908 82777 1 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 455 2 1 4 6.1 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(Cl)nc1N2 10.1021/ml200207w
62707365 81877 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 573 4 2 8 6.0 C[C@H](O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(C)(C)C)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
CHEMBL2164582 81877 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 573 4 2 8 6.0 C[C@H](O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(C)(C)C)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
49871766 2557 40 None 2 3 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [3H]Bag-3 from rat BRS-3Displacement of [3H]Bag-3 from rat BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
6170 2557 40 None 2 3 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [3H]Bag-3 from rat BRS-3Displacement of [3H]Bag-3 from rat BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
CHEMBL1672354 2557 40 None 2 3 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [3H]Bag-3 from rat BRS-3Displacement of [3H]Bag-3 from rat BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
59618821 74190 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingDisplacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
ChEMBL 657 6 2 9 6.4 CC(C)(O)c1nc(C(C)(C)c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1016/j.bmc.2012.03.029
CHEMBL2023110 74190 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingDisplacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
ChEMBL 657 6 2 9 6.4 CC(C)(O)c1nc(C(C)(C)c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1016/j.bmc.2012.03.029
56840673 1141 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
8503 1141 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
CHEMBL2164575 1141 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
62707363 81873 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 544 3 2 5 6.3 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(C4CCNCC4)c32)cc1 10.1021/ml200304j
CHEMBL2164578 81873 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 544 3 2 5 6.3 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(C4CCNCC4)c32)cc1 10.1021/ml200304j
25128865 82658 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 475 3 1 4 6.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179473 82658 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 475 3 1 4 6.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
25134007 81789 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 573 5 2 8 6.0 CC(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(C(C)(C)O)n4)c32)cc1 10.1021/ml200304j
CHEMBL2164224 81789 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 573 5 2 8 6.0 CC(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(C(C)(C)O)n4)c32)cc1 10.1021/ml200304j
59618747 81871 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 538 3 1 5 6.9 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4cccnc4)c32)cc1 10.1021/ml200304j
CHEMBL2164576 81871 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 538 3 1 5 6.9 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4cccnc4)c32)cc1 10.1021/ml200304j
62707528 81787 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 573 4 2 8 6.0 C[C@@H](O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(C)(C)C)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
CHEMBL2164222 81787 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 573 4 2 8 6.0 C[C@@H](O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(C)(C)C)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
46889210 7532 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 387 6 2 2 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc3c(c2)CNC(=O)c2ccccc2-3)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1087443 7532 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 387 6 2 2 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc3c(c2)CNC(=O)c2ccccc2-3)n1 10.1016/j.bmcl.2010.03.028
59618785 82665 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 507 2 1 5 6.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(F)(F)F)s1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179480 82665 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 507 2 1 5 6.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(F)(F)F)s1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
59618635 82668 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 435 2 1 4 5.8 Cc1ccc2c(n1)Nc1ccc(C)c(C)c1N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)C2 10.1021/ml200207w
CHEMBL2179484 82668 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 435 2 1 4 5.8 Cc1ccc2c(n1)Nc1ccc(C)c(C)c1N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)C2 10.1021/ml200207w
46884660 6442 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 339 7 1 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cnsc3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1082471 6442 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 339 7 1 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cnsc3)cc2)n1 10.1016/j.bmcl.2010.02.076
53242205 60827 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762247 60827 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
46884578 8180 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 333 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccncc3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091984 8180 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 333 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccncc3)cc2)n1 10.1016/j.bmcl.2010.02.076
46889148 7685 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 406 10 2 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCC(=O)O)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1088686 7685 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 406 10 2 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCC(=O)O)cc2)n1 10.1016/j.bmcl.2010.03.028
46845425 1032 2 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.03.028
8504 1032 2 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.03.028
CHEMBL1089721 1032 2 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.03.028
25026044 57842 1 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 390 6 2 4 3.9 CC(O)(Cc1nc(CC2(C(F)(F)F)CC2)c[nH]1)c1ccc(-n2cccn2)cc1 10.1021/ml100196d
CHEMBL1671874 57842 1 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 390 6 2 4 3.9 CC(O)(Cc1nc(CC2(C(F)(F)F)CC2)c[nH]1)c1ccc(-n2cccn2)cc1 10.1021/ml100196d
46845425 1032 2 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
8504 1032 2 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1089721 1032 2 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
46884630 8420 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 339 7 1 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccns3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1093459 8420 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 339 7 1 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccns3)cc2)n1 10.1016/j.bmcl.2010.02.076
46889177 7484 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 497 10 2 4 6.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(C(F)(F)F)n[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1087066 7484 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 497 10 2 4 6.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(C(F)(F)F)n[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
59618658 82666 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 507 2 1 5 6.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1csc(C(F)(F)F)c1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179481 82666 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 507 2 1 5 6.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1csc(C(F)(F)F)c1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
46884629 8379 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 358 7 1 3 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C#N)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1093183 8379 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 358 7 1 3 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C#N)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
46889145 9076 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 398 7 2 4 4.8 c1ccc(-c2nnn[nH]2)c(-c2ccc(CCc3nc(CC4CCCC4)c[nH]3)cc2)c1 10.1016/j.bmcl.2010.03.028
CHEMBL1099034 9076 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 398 7 2 4 4.8 c1ccc(-c2nnn[nH]2)c(-c2ccc(CCc3nc(CC4CCCC4)c[nH]3)cc2)c1 10.1016/j.bmcl.2010.03.028
25025861 8380 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 351 7 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccc(F)cn3)cc2)n1 10.1021/ml100196d
CHEMBL1093184 8380 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 351 7 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccc(F)cn3)cc2)n1 10.1021/ml100196d
56840673 1141 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
8503 1141 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
CHEMBL2164575 1141 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
25026445 57945 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 367 5 2 3 4.7 CC(C)(C)Cc1c[nH]c(CC(C)(O)c2ccc(-c3ccc(F)cn3)cc2)n1 10.1021/ml100196d
CHEMBL1672352 57945 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 367 5 2 3 4.7 CC(C)(C)Cc1c[nH]c(CC(C)(O)c2ccc(-c3ccc(F)cn3)cc2)n1 10.1021/ml100196d
46884576 8111 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 331 6 1 2 5.0 c1ccc(-c2ccc(CCc3nc(CC4CCCC4)c[nH]3)cc2)nc1 10.1016/j.bmcl.2010.02.076
CHEMBL1091598 8111 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 331 6 1 2 5.0 c1ccc(-c2ccc(CCc3nc(CC4CCCC4)c[nH]3)cc2)nc1 10.1016/j.bmcl.2010.02.076
25026058 7669 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 377 7 2 3 5.0 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCc4cn[nH]c43)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1088553 7669 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 377 7 2 3 5.0 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCc4cn[nH]c43)cc2)n1 10.1016/j.bmcl.2010.03.028
62707207 81791 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 597 6 2 9 5.4 CC(C)(O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
CHEMBL2164226 81791 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 597 6 2 9 5.4 CC(C)(O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
25025860 569 32 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
6188 569 32 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1091720 569 32 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
25025861 8380 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 351 7 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccc(F)cn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1093184 8380 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 351 7 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccc(F)cn3)cc2)n1 10.1016/j.bmcl.2010.02.076
59618711 74194 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingDisplacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
ChEMBL 600 5 2 6 5.6 CNC(=O)C1(c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)CCC1 10.1016/j.bmc.2012.03.029
CHEMBL2023114 74194 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingDisplacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
ChEMBL 600 5 2 6 5.6 CNC(=O)C1(c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)CCC1 10.1016/j.bmc.2012.03.029
71451991 82786 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 477 2 2 5 5.6 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(O)c32)cc1 10.1021/ml200207w
CHEMBL2179916 82786 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 477 2 2 5 5.6 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(O)c32)cc1 10.1021/ml200207w
25025860 569 32 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from rat BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from rat BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
6188 569 32 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from rat BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from rat BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1091720 569 32 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from rat BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from rat BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
46889232 7513 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 401 6 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc3c(c2)CN(C)C(=O)c2ccccc2-3)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1087200 7513 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 401 6 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc3c(c2)CN(C)C(=O)c2ccccc2-3)n1 10.1016/j.bmcl.2010.03.028
59618675 82664 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 497 1 1 5 4.8 Cc1ccc2c(c1C)N(S(=O)(=O)C1=NC(C(C)(C)C)C=[S+]1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179479 82664 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 497 1 1 5 4.8 Cc1ccc2c(c1C)N(S(=O)(=O)C1=NC(C(C)(C)C)C=[S+]1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
46884687 8172 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 324 7 1 5 3.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ncnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091917 8172 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 324 7 1 5 3.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ncnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
46889175 7441 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 429 10 2 4 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3ncn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1086673 7441 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 429 10 2 4 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3ncn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
54581470 60828 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762248 60828 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
54583453 60849 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 389 5 3 5 3.5 CC(C)(C)c1cc(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)[nH]n1 10.1016/j.bmcl.2011.02.011
CHEMBL1762271 60849 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 389 5 3 5 3.5 CC(C)(C)c1cc(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)[nH]n1 10.1016/j.bmcl.2011.02.011
54582477 60848 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 406 5 2 6 4.2 CC(C)(C)c1csc(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)n1 10.1016/j.bmcl.2011.02.011
CHEMBL1762270 60848 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 406 5 2 6 4.2 CC(C)(C)c1csc(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)n1 10.1016/j.bmcl.2011.02.011
46889235 7659 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 406 8 2 4 5.0 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCC[C@@H]3c3ncn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1088411 7659 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 406 8 2 4 5.0 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCC[C@@H]3c3ncn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
46889176 7442 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 444 10 3 5 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(N)n[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1086674 7442 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 444 10 3 5 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(N)n[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
49871766 2557 40 None -9 3 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
6170 2557 40 None -9 3 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
CHEMBL1672354 2557 40 None -9 3 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
46884688 8173 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 339 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCCC3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091918 8173 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 339 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCCC3)cc2)n1 10.1016/j.bmcl.2010.02.076
46885313 8102 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 377 8 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C(=O)O)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091554 8102 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 377 8 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C(=O)O)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
46889147 7684 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 445 7 1 5 5.7 O=C1NC(=O)C(c2ccccc2-c2ccc(CCC3N=CC(CC4CCCC4)=N3)cc2)S1 10.1016/j.bmcl.2010.03.028
CHEMBL1088685 7684 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 445 7 1 5 5.7 O=C1NC(=O)C(c2ccccc2-c2ccc(CCC3N=CC(CC4CCCC4)=N3)cc2)S1 10.1016/j.bmcl.2010.03.028
136118727 81874 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 545 3 2 7 5.2 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(=O)[nH]4)c32)cc1 10.1021/ml200304j
CHEMBL2164579 81874 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 545 3 2 7 5.2 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(-c4noc(=O)[nH]4)c32)cc1 10.1021/ml200304j
54583454 60851 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 388 6 3 6 2.9 O=S(=O)(Nc1nc(C2CCC2)n[nH]1)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762273 60851 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 388 6 3 6 2.9 O=S(=O)(Nc1nc(C2CCC2)n[nH]1)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
66901760 82782 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 495 2 1 4 6.5 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(Cl)c32)cc1 10.1021/ml200207w
CHEMBL2179912 82782 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 495 2 1 4 6.5 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(Cl)c32)cc1 10.1021/ml200207w
59618698 82661 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 517 3 1 5 6.1 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(OC(F)(F)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179476 82661 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 517 3 1 5 6.1 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(OC(F)(F)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
46200989 2562 15 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingDisplacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2012.03.029
8502 2562 15 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingDisplacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2012.03.029
CHEMBL2023109 2562 15 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingDisplacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2012.03.029
46200989 2562 15 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1021/ml200304j
8502 2562 15 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1021/ml200304j
CHEMBL2023109 2562 15 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1021/ml200304j
54580463 60835 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 408 4 3 5 3.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@H]2CC[C@]1(C)C2(C)C 10.1016/j.bmcl.2011.02.011
CHEMBL1762255 60835 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 408 4 3 5 3.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@H]2CC[C@]1(C)C2(C)C 10.1016/j.bmcl.2011.02.011
54580465 60837 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 390 5 3 5 3.2 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC(C)(C)c1ccccc1 10.1016/j.bmcl.2011.02.011
CHEMBL1762258 60837 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 390 5 3 5 3.2 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC(C)(C)c1ccccc1 10.1016/j.bmcl.2011.02.011
136086809 7443 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 445 10 3 4 4.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(=O)[nH][nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1086684 7443 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 445 10 3 4 4.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(=O)[nH][nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
46889146 7683 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 348 7 2 2 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3O)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1088684 7683 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 348 7 2 2 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3O)cc2)n1 10.1016/j.bmcl.2010.03.028
54581471 60832 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 444 5 3 5 3.6 O=C(NC12CC3CC(CC(C3)C1)C2)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762252 60832 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 444 5 3 5 3.6 O=C(NC12CC3CC(CC(C3)C1)C2)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
54582478 60852 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 388 6 3 6 2.9 O=S(=O)(Nc1nc(C2CCC2)n[nH]1)c1cnccc1NC1CC2CCC1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762274 60852 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 388 6 3 6 2.9 O=S(=O)(Nc1nc(C2CCC2)n[nH]1)c1cnccc1NC1CC2CCC1C2 10.1016/j.bmcl.2011.02.011
25025862 7821 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 322 7 1 3 4.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089521 7821 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 322 7 1 3 4.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
46884662 7822 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 323 7 1 4 3.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cncn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089522 7822 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 323 7 1 4 3.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cncn3)cc2)n1 10.1016/j.bmcl.2010.02.076
46885311 8315 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 424 7 2 2 6.0 O=C(O)c1cc(F)c(F)cc1-c1ccc(CCc2nc(CC3CCCCC3)c[nH]2)cc1 10.1016/j.bmcl.2010.02.076
CHEMBL1092730 8315 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 424 7 2 2 6.0 O=C(O)c1cc(F)c(F)cc1-c1ccc(CCc2nc(CC3CCCCC3)c[nH]2)cc1 10.1016/j.bmcl.2010.02.076
46882011 5891 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]bombesin from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]bombesin from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
ChEMBL 406 11 3 3 5.2 CCCCc1cnc(C(CCCO)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
CHEMBL1079517 5891 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]bombesin from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]bombesin from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
ChEMBL 406 11 3 3 5.2 CCCCc1cnc(C(CCCO)Cc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
11389266 161805 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of bombesin subtype 3 receptor expressed in human lung carcinoidsInhibition of bombesin subtype 3 receptor expressed in human lung carcinoids
ChEMBL 1303 44 17 18 -2.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)COCC(=O)Nc1ccc(CC(CNCCN)CNCCN)cc1)C(C)C)C(N)=O 10.1021/jm049437y
CHEMBL414307 161805 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of bombesin subtype 3 receptor expressed in human lung carcinoidsInhibition of bombesin subtype 3 receptor expressed in human lung carcinoids
ChEMBL 1303 44 17 18 -2.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)COCC(=O)Nc1ccc(CC(CNCCN)CNCCN)cc1)C(C)C)C(N)=O 10.1021/jm049437y
54583450 60838 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 388 4 3 5 3.0 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC1CCc2ccccc21 10.1016/j.bmcl.2011.02.011
CHEMBL1762259 60838 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 388 4 3 5 3.0 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC1CCc2ccccc21 10.1016/j.bmcl.2011.02.011
46884663 7823 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 323 7 1 4 3.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ccnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089523 7823 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 323 7 1 4 3.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ccnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
59618678 82776 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 446 2 1 5 5.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C#N)nc1N2 10.1021/ml200207w
CHEMBL2179907 82776 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 446 2 1 5 5.3 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C#N)nc1N2 10.1021/ml200207w
59618646 82667 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 421 2 1 4 5.4 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1cccnc1N2 10.1021/ml200207w
CHEMBL2179482 82667 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 421 2 1 4 5.4 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1cccnc1N2 10.1021/ml200207w
54587369 60833 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 354 4 3 5 2.6 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC1CCCCC1 10.1016/j.bmcl.2011.02.011
CHEMBL1762253 60833 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 354 4 3 5 2.6 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1NC1CCCCC1 10.1016/j.bmcl.2011.02.011
71462686 82778 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 455 2 1 4 6.1 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1cc(Cl)cnc1N2 10.1021/ml200207w
CHEMBL2179909 82778 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 455 2 1 4 6.1 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1cc(Cl)cnc1N2 10.1021/ml200207w
46884659 7817 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 340 7 1 4 4.7 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3csnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089511 7817 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 340 7 1 4 4.7 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3csnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
25026446 57946 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 338 5 2 4 3.6 CC(C)(C)Cc1c[nH]c(CC(C)(O)c2ccc(-n3cccn3)cc2)n1 10.1021/ml100196d
CHEMBL1672353 57946 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 338 5 2 4 3.6 CC(C)(C)Cc1c[nH]c(CC(C)(O)c2ccc(-n3cccn3)cc2)n1 10.1021/ml100196d
71451990 82785 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 537 3 2 5 6.2 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccc(C(C)(C)O)c(F)c32)cc1 10.1021/ml200207w
CHEMBL2179915 82785 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 537 3 2 5 6.2 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccc(C(C)(C)O)c(F)c32)cc1 10.1021/ml200207w
46889233 7657 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 383 8 2 3 4.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCC[C@@H]3C(=O)O)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1088409 7657 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 383 8 2 3 4.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCC[C@@H]3C(=O)O)cc2)n1 10.1016/j.bmcl.2010.03.028
25025863 8499 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 430 10 2 5 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nnn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1094054 8499 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 430 10 2 5 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nnn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
59618620 82787 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 476 2 1 5 5.6 Cc1ccc2c(n1)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179917 82787 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 476 2 1 5 5.6 Cc1ccc2c(n1)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
49871766 2557 40 None -2 3 Mouse 8.3 pIC50 = 8.3 Binding
Displacement of [3H]Bag-3 from mouse BRS-3Displacement of [3H]Bag-3 from mouse BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
6170 2557 40 None -2 3 Mouse 8.3 pIC50 = 8.3 Binding
Displacement of [3H]Bag-3 from mouse BRS-3Displacement of [3H]Bag-3 from mouse BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
CHEMBL1672354 2557 40 None -2 3 Mouse 8.3 pIC50 = 8.3 Binding
Displacement of [3H]Bag-3 from mouse BRS-3Displacement of [3H]Bag-3 from mouse BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
59618811 82784 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 461 2 1 4 5.9 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccccc32)cc1 10.1021/ml200207w
CHEMBL2179914 82784 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 461 2 1 4 5.9 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3ccccc32)cc1 10.1021/ml200207w
71460937 82662 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 493 3 1 4 6.4 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179477 82662 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 493 3 1 4 6.4 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
59618730 82663 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 500 3 1 5 6.0 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C#N)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179478 82663 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 500 3 1 5 6.0 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C#N)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
71460964 82783 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 475 2 1 4 6.2 Cc1ccc2c(c1)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179913 82783 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 475 2 1 4 6.2 Cc1ccc2c(c1)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
46884661 7818 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 334 7 1 3 4.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cnccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1089512 7818 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 334 7 1 3 4.6 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cnccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
46884627 8377 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 349 7 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(O)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1093170 8377 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 349 7 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(O)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
1214469 60825 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 352 5 3 5 2.1 CC(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762245 60825 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 352 5 3 5 2.1 CC(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
54583452 60847 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 399 5 2 4 4.8 CC(C)(C)c1cccc(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)c1 10.1016/j.bmcl.2011.02.011
CHEMBL1762269 60847 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 399 5 2 4 4.8 CC(C)(C)c1cccc(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)c1 10.1016/j.bmcl.2011.02.011
54580462 60831 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 422 6 3 5 3.9 CC(C)(C)CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762251 60831 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 422 6 3 5 3.9 CC(C)(C)CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
46885312 8101 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 377 8 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccnc3C(=O)O)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091553 8101 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 377 8 2 3 4.9 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccnc3C(=O)O)cc2)n1 10.1016/j.bmcl.2010.02.076
46861857 7440 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 461 10 3 4 6.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(=S)[nH][nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1086672 7440 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 461 10 3 4 6.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(=S)[nH][nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
46889234 7658 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 407 8 2 5 4.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCC[C@@H]3c3nnn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1088410 7658 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 407 8 2 5 4.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCC[C@@H]3c3nnn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
25026056 8181 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 347 7 1 2 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091985 8181 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 347 7 1 2 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(C)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
59618623 82659 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 501 2 1 4 6.2 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(F)(F)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179474 82659 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 501 2 1 4 6.2 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(F)(F)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
25025860 569 32 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from mouse BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from mouse BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
6188 569 32 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from mouse BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from mouse BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1091720 569 32 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from mouse BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from mouse BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
4157547 25229 9 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-[D-Tyr6, b-Ala11, Phe13, Nle14]-Bombesin (6-14) from human BRS3 by competitive binding assayDisplacement of [125I]-[D-Tyr6, b-Ala11, Phe13, Nle14]-Bombesin (6-14) from human BRS3 by competitive binding assay
ChEMBL 352 5 3 5 2.1 CC(C)NC(=O)NS(=O)(=O)c1cnccc1NC1CC2CCC1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1348293 25229 9 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-[D-Tyr6, b-Ala11, Phe13, Nle14]-Bombesin (6-14) from human BRS3 by competitive binding assayDisplacement of [125I]-[D-Tyr6, b-Ala11, Phe13, Nle14]-Bombesin (6-14) from human BRS3 by competitive binding assay
ChEMBL 352 5 3 5 2.1 CC(C)NC(=O)NS(=O)(=O)c1cnccc1NC1CC2CCC1C2 10.1016/j.bmcl.2011.02.011
54581472 60841 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 365 4 3 4 3.1 CC(C)(C)NC(=O)NS(=O)(=O)c1ccccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762263 60841 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 365 4 3 4 3.1 CC(C)(C)NC(=O)NS(=O)(=O)c1ccccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
54584418 60829 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@@H]2CC[C@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762249 60829 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@@H]2CC[C@H]1C2 10.1016/j.bmcl.2011.02.011
54585380 60844 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 380 4 2 5 2.8 CN(C(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2)C(C)(C)C 10.1016/j.bmcl.2011.02.011
CHEMBL1762266 60844 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 380 4 2 5 2.8 CN(C(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2)C(C)(C)C 10.1016/j.bmcl.2011.02.011
54586335 60834 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 408 4 3 5 3.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@]1(C)C2(C)C 10.1016/j.bmcl.2011.02.011
CHEMBL1762254 60834 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 408 4 3 5 3.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@]1(C)C2(C)C 10.1016/j.bmcl.2011.02.011
54583451 60846 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 380 4 2 5 2.8 CN(C(=O)NC(C)(C)C)S(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762268 60846 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 380 4 2 5 2.8 CN(C(=O)NC(C)(C)C)S(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
53242205 60827 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762247 60827 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 366 4 3 5 2.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
54582478 60852 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 388 6 3 6 2.9 O=S(=O)(Nc1nc(C2CCC2)n[nH]1)c1cnccc1NC1CC2CCC1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762274 60852 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 388 6 3 6 2.9 O=S(=O)(Nc1nc(C2CCC2)n[nH]1)c1cnccc1NC1CC2CCC1C2 10.1016/j.bmcl.2011.02.011
46884628 8253 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 348 7 2 3 4.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(N)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1092381 8253 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 348 7 2 3 4.8 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccc(N)n3)cc2)n1 10.1016/j.bmcl.2010.02.076
46884577 8112 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 333 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccnc3)cc2)n1 10.1016/j.bmcl.2010.02.076
CHEMBL1091599 8112 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 333 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3cccnc3)cc2)n1 10.1016/j.bmcl.2010.02.076
59618778 82660 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 511 3 1 6 4.6 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(S(C)(=O)=O)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
CHEMBL2179475 82660 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 511 3 1 6 4.6 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(S(C)(=O)=O)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
54580461 60830 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 380 6 3 5 2.9 CCC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762250 60830 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 380 6 3 5 2.9 CCC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
54581474 60850 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 376 6 3 6 2.7 CC(C)c1n[nH]c(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)n1 10.1016/j.bmcl.2011.02.011
CHEMBL1762272 60850 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 376 6 3 6 2.7 CC(C)c1n[nH]c(NS(=O)(=O)c2cnccc2N[C@@H]2C[C@H]3CC[C@@H]2C3)n1 10.1016/j.bmcl.2011.02.011
25134006 81790 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 599 4 2 8 5.8 CC(C)(O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
CHEMBL2164225 81790 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 599 4 2 8 5.8 CC(C)(O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
59618710 82780 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 473 2 1 4 6.2 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1cc(F)c(Cl)nc1N2 10.1021/ml200207w
CHEMBL2179910 82780 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 473 2 1 4 6.2 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1cc(F)c(Cl)nc1N2 10.1021/ml200207w
25055504 57944 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 367 5 2 3 4.7 CC(C)(C)Cc1c[nH]c(C(C)(O)Cc2ccc(-c3ccc(F)cn3)cc2)n1 10.1021/ml100196d
CHEMBL1672351 57944 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 367 5 2 3 4.7 CC(C)(C)Cc1c[nH]c(C(C)(O)Cc2ccc(-c3ccc(F)cn3)cc2)n1 10.1021/ml100196d
11891917 60826 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 352 5 3 5 2.1 CC(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762246 60826 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 352 5 3 5 2.1 CC(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
46889209 7531 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 429 10 2 4 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3cnn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
CHEMBL1087442 7531 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 429 10 2 4 5.5 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3cnn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
54586337 60840 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 367 4 2 5 2.4 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1O[C@@H]1C[C@@H]2CC[C@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762262 60840 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 367 4 2 5 2.4 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1O[C@@H]1C[C@@H]2CC[C@H]1C2 10.1016/j.bmcl.2011.02.011
54581473 60845 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 365 4 4 5 2.3 CC(C)(C)NC(=N)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762267 60845 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 365 4 4 5 2.3 CC(C)(C)NC(=N)NS(=O)(=O)c1cnccc1N[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
54585379 60839 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 367 4 2 5 2.4 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1O[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL1762261 60839 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 367 4 2 5 2.4 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1O[C@@H]1C[C@H]2CC[C@@H]1C2 10.1016/j.bmcl.2011.02.011
CHEMBL525577 215653 0 None 2 3 Human 9.4 pKi = 9.4 Binding
Binding affinity to BRS-3 receptorBinding affinity to BRS-3 receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](N)Cc1ccccc1)C(C)C)C(N)=O 10.1016/j.bmcl.2008.09.033
49871766 2557 40 None 2 3 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]Bag-3 from rat BRS-3Displacement of [3H]Bag-3 from rat BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
6170 2557 40 None 2 3 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]Bag-3 from rat BRS-3Displacement of [3H]Bag-3 from rat BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
CHEMBL1672354 2557 40 None 2 3 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]Bag-3 from rat BRS-3Displacement of [3H]Bag-3 from rat BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
49871766 2557 40 None -2 3 Mouse 8.8 pKi = 8.8 Binding
Displacement of [3H]Bag-3 from mouse BRS-3Displacement of [3H]Bag-3 from mouse BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
6170 2557 40 None -2 3 Mouse 8.8 pKi = 8.8 Binding
Displacement of [3H]Bag-3 from mouse BRS-3Displacement of [3H]Bag-3 from mouse BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
CHEMBL1672354 2557 40 None -2 3 Mouse 8.8 pKi = 8.8 Binding
Displacement of [3H]Bag-3 from mouse BRS-3Displacement of [3H]Bag-3 from mouse BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
49871766 2557 40 None -9 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
6170 2557 40 None -9 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
CHEMBL1672354 2557 40 None -9 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
71300326 118501 40 None -6 3 Human 5.1 pKi = 5.1 Binding
Selectivity interaction (Enzyme panel (ion channels, GPCRs, other targets)) EUB0000196bCl BRS3Selectivity interaction (Enzyme panel (ion channels, GPCRs, other targets)) EUB0000196bCl BRS3
ChEMBL 499 6 2 4 3.0 O=C([C@@H](Cc1cccc(C(F)(F)F)c1)NS(=O)(=O)c1cc(F)c2c(c1)CCNC2)N1CCCC1 10.6019/CHEMBL5212743
CHEMBL3414622 118501 40 None -6 3 Human 5.1 pKi = 5.1 Binding
Selectivity interaction (Enzyme panel (ion channels, GPCRs, other targets)) EUB0000196bCl BRS3Selectivity interaction (Enzyme panel (ion channels, GPCRs, other targets)) EUB0000196bCl BRS3
ChEMBL 499 6 2 4 3.0 O=C([C@@H](Cc1cccc(C(F)(F)F)c1)NS(=O)(=O)c1cc(F)c2c(c1)CCNC2)N1CCCC1 10.6019/CHEMBL5212743
CHEMBL4789678 118501 40 None -6 3 Human 5.1 pKi = 5.1 Binding
Selectivity interaction (Enzyme panel (ion channels, GPCRs, other targets)) EUB0000196bCl BRS3Selectivity interaction (Enzyme panel (ion channels, GPCRs, other targets)) EUB0000196bCl BRS3
ChEMBL 499 6 2 4 3.0 O=C([C@@H](Cc1cccc(C(F)(F)F)c1)NS(=O)(=O)c1cc(F)c2c(c1)CCNC2)N1CCCC1 10.6019/CHEMBL5212743
25025654 570 13 None - 1 Mouse 8.6 pKd = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
6189 570 13 None - 1 Mouse 8.6 pKd = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
8506 570 13 None - 1 Mouse 8.6 pKd = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
CHEMBL1084942 570 13 None - 1 Mouse 8.6 pKd = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
164512405 215949 0 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) -316 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
None 216087 0 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 1054 32 14 14 -3.4 CC(C)CC(C(=O)NC(CCSC)C(=O)N)NC(=O)C(CC1=CN=CN1)NC(=O)CNC(=O)C(C(C)C)NC(=O)C(C)NC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(CCC(=O)N)NC(=O)C(CC(=O)N)N None
None 216087 0 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 1054 32 14 14 -3.4 CC(C)CC(C(=O)NC(CCSC)C(=O)N)NC(=O)C(CC1=CN=CN1)NC(=O)CNC(=O)C(C(C)C)NC(=O)C(C)NC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(CCC(=O)N)NC(=O)C(CC(=O)N)N None
23185015 216088 0 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 2858 85 36 38 -8.6 CC(C)CC(C(=O)NC(CCSC)C(=O)N)NC(=O)C(CC1=CNC=N1)NC(=O)CNC(=O)C(C(C)C)NC(=O)C(C)NC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(CC4=CNC=N4)NC(=O)C(CC(=O)N)NC(=O)CNC(=O)C(CCCNC(=N)N)NC(=O)C5CCCN5C(=O)C(CC6=CC=C(C=C6)O)NC(=O)C(CCSC)NC(=O)C(CCCCN)NC(=O)C(C(C)O)NC(=O)C(CC(C)C)NC(=O)C(C(C)C)NC(=O)C(C(C)O)NC(=O)CNC(=O)CNC(=O)CNC(=O)C(C)NC(=O)C7CCCN7C(=O)C(CC(C)C)NC(=O)C8CCCN8C(=O)C(C(C)C)N None
None 216093 0 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 1120 33 15 15 -3.6 CC(C)CC(C(=O)NC(CCSC)C(=O)N)NC(=O)C(CC1=CN=CN1)NC(=O)CNC(=O)C(C(C)C)NC(=O)C(C)NC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(CC4=CN=CN4)NC(=O)C(CC(=O)N)NC(=O)CN None
None 216091 0 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) - 1 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 1019 28 12 12 -1.3 CC(C)CC(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(C)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCSC)C(=O)N)NC(=O)C4CCC(=O)N4 None
None 216092 0 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) - 1 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 1071 29 13 13 -1.6 CCC(C)C(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(C)C(=O)NC(C(C)O)C(=O)NCC(=O)NC(CC3=CN=CN3)C(=O)NC(CC4=CC=CC=C4)C(=O)NC(CCSC)C(=O)N)NC(=O)C5CCC(=O)N5 None
25078137 216090 0 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) - 1 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 1535 47 21 20 -6.1 C[C@H]([C@@H](C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@@H](C)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CC3=CN=CN3)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CNC(=O)[C@@H]4CCC(=O)N4)O None
None 216089 0 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) - 1 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 1084 30 13 13 -2.1 CC(C)C(C(=O)NCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCSC)C(=O)N)NC(=O)C(C)NC(=O)C(CC3=CNC4=CC=CC=C43)NC(=O)C(CCC(=O)N)NC(=O)C5CCC(=O)N5 None
164512405 215949 0 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) -316 13 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
164512399 216095 0 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) - 1 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 304 7 4 9 -10.5 C(C(C(C(C(=O)COP(=O)([O-])[O-])O)O)O)O.[Na+].[Na+] None
22146595 3290 0 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) -3467 3 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase None None None None None
618 3290 0 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) -3467 3 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216094 0 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) - 1 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase None None None None None
49871766 2557 40 None -9 3 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 23892571
49871766 2557 40 None -9 3 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 24900253
6170 2557 40 None -9 3 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 23892571
6170 2557 40 None -9 3 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 24900253
CHEMBL1672354 2557 40 None -9 3 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 23892571
CHEMBL1672354 2557 40 None -9 3 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 24900253
3946 1503 0 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15102928
632 1478 0 None -6 5 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9325344
633 1505 0 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11112777
49871766 2557 40 None -2 3 Mouse 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 21036912
6170 2557 40 None -2 3 Mouse 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 21036912
CHEMBL1672354 2557 40 None -2 3 Mouse 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 21036912
632 1478 0 None -1 5 Mouse 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10454496
632 1478 0 None 1 5 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10454496