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 204445 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 204445 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 203318 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 203318 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 204866 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 204866 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 14868 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 14868 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 13214 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 13214 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 14590 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 14590 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 15149 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 15149 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 67605 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 67605 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 67627 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 67627 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 67627 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 67627 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 15352 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 15352 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 15353 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 15353 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 15357 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 15357 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 15358 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 15358 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 15429 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 15429 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 15444 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 15444 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 15447 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 15447 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 15467 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 15467 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 15558 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 15558 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 15559 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 15559 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 15563 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 15563 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 15564 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 15564 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 15565 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 15565 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 15592 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 15592 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 15655 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 15655 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 15675 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 15675 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 15725 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 15725 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 15726 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 15726 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 15742 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 15742 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 15743 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 15743 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 15772 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 15772 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 15801 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 15801 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 21002 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 21002 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 15352 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 15352 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 15357 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 15357 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 15558 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 15558 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 15559 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 15559 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 15564 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 15564 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 15565 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 15565 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 15742 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 15742 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 15743 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 15743 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 15772 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 15772 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 13085 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 13085 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 13764 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 13764 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 7819 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 7819 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 7819 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 14953 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 14953 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 15192 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 15192 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 88647 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 88647 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 14373 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 14373 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 15087 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 15087 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 14883 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 14883 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 14952 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 14952 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 15192 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 15192 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 14589 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 14589 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 14953 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 14953 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 15152 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 15152 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 15592 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 15592 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 14593 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 14593 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 14953 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 14953 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 14554 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 14554 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 14590 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 14590 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 14945 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 14945 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 89563 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 89563 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 14589 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 14589 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 14589 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 14589 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 14590 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 14590 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 15149 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 15149 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 14304 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 14304 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 13937 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 13937 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 89559 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 89559 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 89562 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 89562 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 67603 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 67603 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 14595 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 14595 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 14593 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 14593 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 88648 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 88648 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 15151 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 15151 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 88648 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 88648 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 12377 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 12377 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 13214 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 13214 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 15025 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 15025 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 14868 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 14868 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 14594 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 14594 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 14256 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 14256 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 14429 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 14429 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 89556 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 89556 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 67613 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 67613 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 67625 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 67625 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 113568 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 113568 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 14594 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 14594 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 89441 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 89441 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 15862 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 15862 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 15834 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 15834 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 14873 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 14873 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 13233 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 13233 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 14256 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 14256 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 89563 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 89563 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 15861 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 15861 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 14431 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 14431 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 14441 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 14441 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 67604 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 67604 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 9340 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 9340 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 9340 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 9340 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 9340 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 9340 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 67612 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 67612 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 14884 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 14884 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 89443 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 89443 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 13989 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 13989 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 14455 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 14455 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 14945 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 14945 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 7358 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 7358 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 7358 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 7358 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 88562 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 88562 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 89560 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 89560 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 14593 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 14593 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 9335 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 9335 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 9335 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 64616 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 64616 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 14873 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 14873 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 15642 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 15642 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 113554 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 113554 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 113563 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 113563 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 49646 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 49646 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 15467 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 15467 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 88564 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 88564 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 89439 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 89439 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 14874 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 14874 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 14430 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 14430 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 7924 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 7924 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 7924 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 80969 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 80969 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 14952 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 14952 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 203583 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 203583 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 103334 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 103334 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 89434 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 89434 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 89440 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 89440 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 15833 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 15833 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 89557 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 89557 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 89440 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 89440 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 14448 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 14448 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 64720 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 64720 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 15152 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 15152 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 14430 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 14430 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 15848 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 15848 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 67602 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 67602 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 67621 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 67621 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 67614 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 67614 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 193470 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 193470 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 14105 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 14105 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 89559 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 89559 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 14237 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 14237 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 13534 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 13534 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 12377 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 12377 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 15149 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 15149 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 204394 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 204394 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 67625 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 67625 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 67608 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 67608 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 67626 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 67626 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 14945 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 14945 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 89562 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 89562 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 14213 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 14213 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 13534 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 13534 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 13989 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 13989 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 12663 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 12663 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 14456 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 14456 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 14386 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 14386 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 67618 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 67618 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 14829 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 14829 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 12663 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 12663 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 14953 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 14953 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 67283 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 67283 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 67626 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 67626 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 12663 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 12663 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 15151 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 15151 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 89558 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 89558 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 113566 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 113566 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 9335 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 9335 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 9335 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 107823 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 107823 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 7357 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 7357 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 7357 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 15271 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 15271 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 204348 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 204348 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 13232 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 13232 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 67622 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 67622 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 89437 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 89437 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 13937 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 13937 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 89561 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 89561 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 80968 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 80968 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 9335 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 9335 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 9335 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 67601 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 67601 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 107424 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 107424 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 169909 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 169909 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 179502 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 179502 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 67622 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 67622 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 15868 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 15868 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 89439 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 89439 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 14883 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 14883 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 80968 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 80968 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 80969 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 80969 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 12834 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 12834 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 64718 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 64718 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 67606 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 67606 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 32001 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 32001 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 12694 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 12694 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 14373 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 14373 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 15643 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 15643 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 113567 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 113567 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 89443 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 89443 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 12663 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 12663 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 14429 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 14429 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 169966 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 169966 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 196214 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 196214 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 107342 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 107342 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 89442 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 89442 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 7819 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 7819 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 7819 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 7819 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 7819 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 7819 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 14944 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 14944 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 7819 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 7819 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 7819 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 113556 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 113556 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 80967 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 80967 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 15151 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 15151 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 67607 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 67607 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 67621 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 67621 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 12664 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 12664 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 14237 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 14237 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 14285 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 14285 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 80967 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 80967 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 67623 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 67623 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 204360 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 204360 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 12603 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 12603 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 15096 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 15096 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 14615 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 14615 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 14829 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 14829 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 89555 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 89555 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 14945 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 14945 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 67601 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 67601 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 14304 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 14304 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 12834 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 12834 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 15192 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 15192 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 205026 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 205026 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 15025 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 15025 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 222432 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 15271 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 15271 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 15134 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 15134 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 208320 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 208320 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 14952 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 14952 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 14874 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 14874 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 14238 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 14238 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 113561 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 113561 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 15861 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 15861 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 113565 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 113565 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 67613 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 67613 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 67614 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 67614 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 89442 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 89442 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 67609 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 67609 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 7924 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 7924 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 7924 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 15904 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 15904 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 14215 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 14215 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 15643 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 15643 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 14455 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 14455 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 67615 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 67615 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 15096 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 15096 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 15797 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 15797 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 15744 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 15744 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 15862 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 15862 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 67605 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 67605 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 195184 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 195184 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 15726 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 15726 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 15025 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 15025 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 89555 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 89555 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 15642 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 15642 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 89558 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 89558 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 89552 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 89552 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 67626 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 67626 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 15428 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 15428 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 200680 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 200680 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 12724 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 12724 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 21002 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 21002 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 67606 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 67606 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 14553 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 14553 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 213412 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 213412 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 14303 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 14303 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 113557 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 113557 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 14884 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 14884 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 14214 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 14214 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 15087 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 15087 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 88650 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 88650 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 67623 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 67623 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 67624 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 67624 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 15563 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 15563 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 14212 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 14212 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 15846 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 15846 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 67624 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 67624 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 12945 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 12945 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 15835 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 15835 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 15445 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 15445 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 88646 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 88646 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 14431 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 14431 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 14441 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 14441 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 14944 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 14944 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 14883 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 14883 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 89436 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 89436 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 67611 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 67611 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 14434 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 14434 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 14590 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 14590 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 15834 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 15834 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 14615 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 14615 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 13085 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 13085 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 13214 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 13214 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 67599 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 67599 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 67607 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 67607 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 67609 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 67609 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 219309 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 15428 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 15428 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 113560 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 113560 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 12694 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 12694 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 7357 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 7357 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 7357 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 7357 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 7357 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 7357 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 15444 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 15444 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 15516 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 15516 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 15725 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 15725 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 89433 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 89433 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 67602 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 67602 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 67616 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 67616 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 13122 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 13122 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 15847 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 15847 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 14212 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 14212 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 89551 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 89551 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 89556 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 89556 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 89551 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 89551 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 14105 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 14105 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 67604 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 67604 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 67626 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 67626 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 185607 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 185607 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 12946 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 12946 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 88563 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 88563 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 88652 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 88652 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 14874 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 14874 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 12664 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 12664 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 12946 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 12946 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 14589 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 14589 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 14457 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 14457 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 89435 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 89435 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 15868 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 15868 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 13630 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 13630 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 67601 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 67601 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 15797 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 15797 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 12724 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 12724 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 88651 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 88651 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 14285 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 14285 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 15848 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 15848 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 89435 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 89435 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 14595 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 14595 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 88650 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 88650 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 113564 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 113564 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 14594 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 14594 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 185783 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 185783 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 88646 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 88646 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 13765 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 13765 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 12947 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 12947 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 67617 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 67617 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 203701 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 203701 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 14553 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 14553 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 14554 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 14554 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 13214 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 13214 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 89438 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 89438 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 15447 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 15447 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 15087 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 15087 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 15192 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 15192 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 88647 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 88647 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 89557 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 89557 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 15833 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 15833 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 80965 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 80965 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 67618 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 67618 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 67615 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 67615 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 113559 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 113559 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 220590 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 14595 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 14595 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 15904 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 15904 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 13630 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 13630 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 67620 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 67620 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 15152 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 15152 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 15152 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 15152 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 64719 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 64719 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 80965 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 80965 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 15744 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 15744 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 15445 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 15445 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 67612 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 67612 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 88562 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 88562 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 89437 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 89437 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 67610 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 67610 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 13765 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 13765 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 15846 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 15846 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 113558 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 113558 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 7358 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 7358 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 7358 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 7358 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 14448 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 14448 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 107677 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 107677 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 67619 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 67619 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 15835 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 15835 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 113562 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 113562 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 13764 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 13764 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 67603 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 67603 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 12947 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 12947 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 9340 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 9340 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 9340 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 14434 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 14434 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 67610 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 67610 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 15655 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 15655 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 88649 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 88649 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 80966 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 80966 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 15134 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 15134 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 15675 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 15675 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 88649 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 88649 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 89560 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 89560 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 14214 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 14214 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 7357 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 7357 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 7357 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 89434 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 89434 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 89438 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 89438 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 12945 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 12945 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 113555 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 113555 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 205470 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 205470 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 15801 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 15801 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 13763 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 13763 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 89436 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 89436 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 67601 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 67601 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 67611 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 67611 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 13232 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 13232 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 80966 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 80966 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 67617 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 67617 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 14238 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 14238 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 88563 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 88563 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 67616 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 67616 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 67620 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 67620 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 89433 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 89433 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 15358 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 15358 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 67599 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 67599 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 13763 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 13763 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 13122 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 13122 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 89561 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 89561 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 15847 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 15847 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 14594 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 14594 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 14944 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 14944 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 88652 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 88652 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 15353 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 15353 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 14593 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 14593 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 13233 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 13233 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 107502 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 107502 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 14386 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 14386 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 7819 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 7819 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 7819 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 7819 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 7819 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 7819 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 7819 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 7819 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 7819 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 14874 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 14874 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 67608 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 67608 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 15149 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 15149 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 14595 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 14595 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 88651 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 88651 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 12603 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 12603 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 7819 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 7819 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 7819 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 67600 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 67600 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 14873 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 14873 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 14952 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 14952 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 15151 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 15151 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 88565 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 88565 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 15087 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 15087 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 89441 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 89441 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 15429 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 15429 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 15025 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 15025 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 15152 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 15152 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 7924 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 7924 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 7924 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 14873 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 14873 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 14884 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 14884 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 14883 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 14883 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 14884 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 14884 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 67600 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 67600 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 89552 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 89552 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 7357 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 7357 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 7357 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 14944 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 14944 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 88566 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 88566 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 15516 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 15516 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 7938 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 7938 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 7938 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 7938 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 9613 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 31675498
145996512 9613 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 31675498
6192 9871 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 9871 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 7052 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15635635
6191 7052 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18006692
6191 7052 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20438784
6192 9871 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 9871 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 9335 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 9335 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 9335 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 7933 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 7933 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 7789 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 7789 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 7789 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 9871 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 9871 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 9871 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 9871 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 7934 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 7934 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 7934 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 7934 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 7934 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 7934 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 7934 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 7934 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 7934 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 7813 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 7813 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 9871 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 9871 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 9345 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 9345 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 7052 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18006692
6191 7052 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20438784
25025654 7358 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 7358 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 7358 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 7358 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 9335 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 9335 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 9335 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 9335 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 9335 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 9335 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 7819 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 7819 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 7819 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 7357 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 7357 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 7357 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 8287 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18006692
633 8287 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20438784
25025654 7358 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 7358 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 7358 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 7358 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 7361 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 7361 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 8285 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18006692
3946 8285 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20438784
25025860 7357 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 7357 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 7357 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 7358 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 7358 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 7358 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 7358 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 9340 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 9340 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 9340 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 7357 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 7357 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 7357 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 7361 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 7361 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 7361 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 7361 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 7361 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 7361 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 7361 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 7361 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 7924 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 7924 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 7924 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 8232 0 None -6 4 Human 5.6 pIC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9325344
635 8232 0 None -6 4 Human 5.6 pIC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9593699
635 8232 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 176327 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 176327 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 176327 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 176327 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 178106 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 178106 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 112070 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 112070 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 112070 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 112070 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 112070 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 112070 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 112070 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 112070 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 9340 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 9340 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 9340 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 112056 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 112056 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 112056 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 112056 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 7934 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 7934 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 7934 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 112058 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 112058 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 7934 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 7934 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 7934 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 112058 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 112058 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 112050 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 112050 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 112041 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 112041 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 112054 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 112054 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 177429 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 177429 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 178313 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 178313 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 112054 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 112054 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 112052 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 112052 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 7789 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 7789 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 7789 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 179982 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 179982 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 112064 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 112064 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 112064 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 112064 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 112045 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 112045 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 112049 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 112049 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 112049 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 112049 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 182822 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 182822 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 112055 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 112055 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 112055 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 112055 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 181402 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 181402 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 179982 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 179982 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 9340 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 9340 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 9340 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 112039 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 112039 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 112039 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 112039 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 112065 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 112065 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 9335 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 9335 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 9335 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 179145 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 179145 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 112055 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 112055 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 112055 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 112055 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 112041 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 112041 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 112053 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 112053 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 112059 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 112059 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 112059 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 112059 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 112044 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 112044 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 122850 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 122850 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 112052 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 112052 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 179779 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 179779 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 112049 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 112049 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 112049 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 112049 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 177218 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 177218 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 182409 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 182409 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 112058 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 112058 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 112068 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 112068 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 112058 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 112058 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 112068 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 112068 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 112043 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 112043 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 112043 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 112043 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 122852 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 122852 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 112044 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 112044 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 112045 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 112045 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 112057 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 112057 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 112057 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 112057 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 179261 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 179261 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 9335 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 9335 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 9335 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 9340 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 9340 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 9340 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 177221 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 177221 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 112053 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 112053 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 112061 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 112061 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 112061 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 112061 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 179261 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 179261 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 112071 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 112071 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 112063 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 112063 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 112063 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 112063 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 181402 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 181402 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 112071 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 112071 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 112040 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 112040 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 112040 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 112040 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 177275 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 177275 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 122849 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 122849 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 182409 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 182409 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 182961 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 182961 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 178106 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 178106 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 122856 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 122856 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 112056 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 112056 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 112056 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 112056 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 7934 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 7934 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 7934 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 112066 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 112066 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 7934 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 7934 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 7934 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 112068 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 112068 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 112068 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 112068 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 122856 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 122856 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 112057 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 112057 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 112057 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 112057 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 7924 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 7924 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 7924 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 7924 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 7924 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 7924 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 112039 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 112039 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 112039 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 112039 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 122850 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 122850 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 112062 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 112062 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 112062 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 112062 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 112046 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 112046 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 112046 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 112046 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 179609 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 179609 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 122855 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 122855 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 177218 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 177218 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 122854 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 122854 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 122853 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 122853 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 179779 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 179779 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 112050 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 112050 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 122851 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 122851 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 177275 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 177275 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 7789 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 7789 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 7789 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 112065 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 112065 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 179609 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 179609 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 122853 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 122853 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 112063 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 112063 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 112063 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 112063 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 112061 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 112061 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 112061 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 112061 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 180860 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 180860 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 182961 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 182961 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 122854 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 122854 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 122857 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 122857 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 122855 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 122855 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 112047 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 112047 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 112047 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 112047 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 112046 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 112046 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 112046 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 112046 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 112047 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 112047 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 112047 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 112047 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 112067 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 112067 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 112066 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 112066 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 177429 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 177429 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 112048 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 112048 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 112059 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 112059 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 112048 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 112048 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 112059 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 112059 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 112042 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 112042 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 176779 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 176779 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 180860 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 180860 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 122849 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 122849 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 179145 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 179145 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 179994 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 179994 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 178313 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 178313 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 112048 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 112048 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 112048 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 112048 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 9340 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 9340 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 9340 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 112051 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 112051 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 122857 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 122857 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 112064 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 112064 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 112064 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 112064 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 122852 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 122852 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 112051 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 112051 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 112067 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 112067 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 122851 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 122851 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 182822 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 182822 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 112043 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 112043 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 112043 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 112043 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 112040 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 112040 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 112040 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 112040 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 179994 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 179994 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 7924 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 7924 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 7924 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 7924 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 7924 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 7924 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 112042 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 112042 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 177221 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 177221 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 80967 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 80967 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 80968 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 80968 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 80966 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 80966 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 89563 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 89563 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 88651 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 88651 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 88647 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 88647 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 89556 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 89556 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 88563 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 88563 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 88650 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 88650 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 219878 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 89552 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 89552 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 88652 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 88652 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 9335 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 9335 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 9335 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 80965 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 80965 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 7924 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 7924 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 7924 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 88648 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 88648 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 89433 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 89433 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 88564 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 88564 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 88646 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 88646 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 88562 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 88562 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 14304 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 14304 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 89440 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 89440 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 89443 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 89443 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 13214 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 13214 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 67601 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 67601 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 14952 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 14952 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 14457 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 14457 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 7819 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 7819 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 7819 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 64616 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 64616 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 7819 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 7819 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 7819 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 15192 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 15192 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 14256 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 14256 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 89441 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 89441 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 15151 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 15151 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 15848 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 15848 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 15152 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 15152 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 7924 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 7924 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 7924 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 64719 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 64719 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 14883 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 14883 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 14441 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 14441 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 88566 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 88566 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 7357 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 7357 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 7357 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 15152 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 15152 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 80969 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 80969 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 89561 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 89561 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 7357 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 7357 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 7357 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 14285 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 14285 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 89439 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 89439 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 14944 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 14944 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 14213 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 14213 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 67602 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 67602 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 67623 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 67623 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 67622 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 67622 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 14431 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 14431 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 14214 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 14214 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 9335 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 9335 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 9335 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 14945 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 14945 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 14874 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 14874 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 14456 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 14456 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 88649 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 88649 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 67625 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 67625 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 89557 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 89557 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 89436 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 89436 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 9340 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 9340 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 9340 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 9340 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 9340 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 9340 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 67609 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 67609 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 67611 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 67611 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 14215 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 14215 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 14455 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 14455 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 67606 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 67606 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 67626 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 67626 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 14593 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 14593 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 14594 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 14594 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 15087 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 15087 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 12663 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 12663 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 168584 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 168584 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 67612 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 67612 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 14595 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 14595 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 89551 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 89551 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 89442 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 89442 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 67607 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 67607 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 89553 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 89553 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 14589 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 14589 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 64720 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 64720 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 89560 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 89560 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 14429 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 14429 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 15271 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 15271 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 89562 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 89562 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 9335 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 9335 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 9335 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 89559 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 89559 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 89437 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 89437 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 89438 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 89438 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 89558 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 89558 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 14590 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 14590 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 15149 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 15149 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 67599 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 67599 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 67621 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 67621 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 67605 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 67605 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 14873 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 14873 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 14212 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 14212 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 14430 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 14430 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 14953 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 14953 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 89434 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 89434 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 7357 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 7357 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 7357 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 32001 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 32001 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 67615 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 67615 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 67603 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 67603 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 67618 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 67618 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 67608 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 67608 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 67620 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 67620 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 67601 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 67601 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 67626 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 67626 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 15025 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 15025 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 14884 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 14884 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 89435 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 89435 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 67604 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 67604 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 67624 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 67624 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 88565 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 88565 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 89555 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 89555 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 64718 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 64718 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 67600 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 67600 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 14303 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 14303 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 67614 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 67614 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 67619 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 67619 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 67613 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 67613 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 222432 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 9335 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 9335 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 9335 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 9335 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 9335 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 9335 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 9335 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 9335 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 9335 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 125279 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 125279 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 125279 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 7358 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 7358 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 7358 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 7358 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 222728 0 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) -316 12 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 222866 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 222866 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 222867 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 222872 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 222870 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 222871 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 222869 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 222868 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 222728 0 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) -316 12 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 222874 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 10063 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 10063 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 222873 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 9335 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 9335 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 9335 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 9335 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 9335 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 9335 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 8285 0 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15102928
632 8260 0 None -6 5 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9325344
633 8287 0 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11112777
49871766 9335 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 9335 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 9335 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 8260 0 None -1 5 Mouse 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10454496
632 8260 0 None 1 5 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10454496