Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
44300265 195979 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 195979 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 194854 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 194854 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 196400 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 196400 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 7997 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 7997 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 6349 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 6349 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 7721 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 7721 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 8277 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 8277 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 60491 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 60491 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 60513 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 60513 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 60513 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 60513 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 8479 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 8479 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 8480 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 8480 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 8484 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 8484 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 8485 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 8485 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 8554 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 8554 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 8569 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 8569 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 8572 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 8572 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 8592 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 8592 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 8683 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 8683 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 8684 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 8684 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 8688 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 8688 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 8689 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 8689 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 8690 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 8690 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 8717 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 8717 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 8780 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 8780 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 8800 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 8800 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 8850 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 8850 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 8851 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 8851 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 8867 5 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 8867 5 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 8868 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 8868 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 8897 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 8897 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 8926 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 8926 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 14100 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 14100 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 8479 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 8479 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 8484 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 8484 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 8683 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 8683 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 8684 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 8684 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 8689 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 8689 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 8690 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 8690 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 8867 5 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 8867 5 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 8868 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 8868 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 8897 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 8897 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 6221 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 6221 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 6899 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 6899 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 1014 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 1014 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 1014 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 8082 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 8082 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 8320 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 8320 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 81446 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 81446 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 7505 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 7505 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 8216 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 8216 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 8012 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 8012 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 8081 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 8081 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 8320 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 8320 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 7720 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 7720 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 8082 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 8082 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 8280 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 8280 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 8717 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 8717 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 7724 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 7724 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 8082 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 8082 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 7685 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 7685 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 7721 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 7721 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 8074 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 8074 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 82362 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 82362 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 7720 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 7720 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 7720 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 7720 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 7721 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 7721 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 8277 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 8277 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 7436 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 7436 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 7071 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 7071 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 82358 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 82358 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 82361 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 82361 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 60489 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 60489 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 7726 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 7726 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 7724 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 7724 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 81447 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 81447 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 8279 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 8279 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 81447 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 81447 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 5514 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 5514 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 6349 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 6349 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 8154 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 8154 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 7997 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 7997 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 7725 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 7725 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 7388 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 7388 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 7561 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 7561 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 82355 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 82355 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 60499 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 60499 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 60511 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 60511 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 106295 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 106295 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 7725 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 7725 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 82240 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 82240 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 8987 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 8987 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 8959 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 8959 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 8002 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 8002 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 6368 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 6368 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 7388 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 7388 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 82362 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 82362 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 8986 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 8986 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 7563 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 7563 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 7573 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 7573 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 60490 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 60490 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 2515 11 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 2515 11 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 2515 11 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 2515 11 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 2515 11 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 2515 11 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 60498 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 60498 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 8013 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 8013 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 82242 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 82242 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 7123 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 7123 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 7587 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 7587 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 8074 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 8074 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 564 10 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 564 10 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 564 10 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 564 10 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 81361 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 81361 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 82359 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 82359 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 7724 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 7724 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 2510 32 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 2510 32 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 2510 32 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 57522 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 57522 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 8002 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 8002 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 8767 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 8767 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 106281 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 106281 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 106290 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 106290 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 42611 123 None - 1 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 42611 123 None - 1 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 8592 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 8592 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 81363 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 81363 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 82238 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 82238 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 8003 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 8003 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 7562 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 7562 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 1115 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 1115 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 1115 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 73831 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 73831 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 8081 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 8081 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 195119 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 195119 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 96098 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 96098 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 82233 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 82233 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 82239 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 82239 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 8958 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 8958 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 82356 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 82356 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 82239 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 82239 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 7580 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 7580 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 57625 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 57625 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 8280 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 8280 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 7562 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 7562 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 8973 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 8973 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 60488 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 60488 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 60507 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 60507 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 60500 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 60500 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 186099 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 186099 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 7237 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 7237 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 82358 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 82358 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 7369 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 7369 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 6669 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 6669 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 5514 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 5514 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 8277 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 8277 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 195928 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 195928 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 60511 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 60511 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 60494 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 60494 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 60512 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 60512 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 8074 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 8074 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 82361 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 82361 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 7345 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 7345 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 6669 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 6669 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 7123 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 7123 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 5799 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 5799 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 7588 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 7588 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 7518 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 7518 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 60504 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 60504 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 7959 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 7959 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 5799 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 5799 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 8082 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 8082 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 60170 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 60170 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 60512 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 60512 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 5799 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 5799 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 8279 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 8279 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 82357 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 82357 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 106293 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 106293 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 2510 32 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 2510 32 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 2510 32 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 100564 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 100564 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 563 26 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 563 26 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 563 26 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 8399 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 8399 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 195882 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 195882 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 6367 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 6367 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 60508 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 60508 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 82236 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 82236 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 7071 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 7071 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 82360 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 82360 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 73830 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 73830 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 2510 32 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 2510 32 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 2510 32 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 60487 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 60487 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 100168 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 100168 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 162568 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 162568 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 172144 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 172144 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 60508 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 60508 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 8993 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 8993 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 82238 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 82238 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 8012 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 8012 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 73830 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 73830 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 73831 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 73831 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 5970 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 5970 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 57623 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 57623 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 60492 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 60492 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 25010 8 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 25010 8 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 5830 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 5830 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 7505 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 7505 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 8768 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 8768 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 106294 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 106294 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 82242 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 82242 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 5799 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 5799 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 7561 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 7561 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 162624 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 162624 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 188835 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 188835 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 100087 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 100087 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 82241 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 82241 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 1014 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 1014 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 1014 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 1014 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 1014 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 1014 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 8073 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 8073 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 1014 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 1014 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 1014 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 106283 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 106283 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 73829 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 73829 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 8279 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 8279 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 60493 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 60493 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 60507 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 60507 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 5800 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 5800 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 7369 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 7369 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 7417 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 7417 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 73829 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 73829 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 60509 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 60509 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 195894 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 195894 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 5739 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 5739 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 8225 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 8225 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 7746 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 7746 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 7959 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 7959 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 82354 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 82354 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 8074 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 8074 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 60487 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 60487 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 7436 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 7436 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 5970 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 5970 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 8320 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 8320 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 196560 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 196560 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 8154 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 8154 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 213867 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 8399 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 8399 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 8262 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 8262 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 199846 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 199846 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 8081 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 8081 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 8003 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 8003 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 7370 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 7370 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 106288 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 106288 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 8986 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 8986 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 106292 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 106292 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 60499 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 60499 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 60500 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 60500 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 82241 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 82241 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 60495 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 60495 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 1115 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 1115 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 1115 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 9029 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 9029 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 7347 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 7347 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 8768 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 8768 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 7587 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 7587 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 60501 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 60501 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 8225 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 8225 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 8922 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 8922 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 8869 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 8869 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 8987 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 8987 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 60491 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 60491 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 187811 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 187811 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 8851 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 8851 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 8154 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 8154 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 82354 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 82354 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 8767 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 8767 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 82357 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 82357 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 82351 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 82351 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 60512 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 60512 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 8553 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 8553 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 192892 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 192892 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 5860 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 5860 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 14100 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 14100 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 60492 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 60492 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 7684 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 7684 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 204897 93 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 204897 93 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 7435 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 7435 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 106284 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 106284 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 8013 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 8013 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 7346 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 7346 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 8216 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 8216 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 81449 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 81449 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 60509 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 60509 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 60510 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 60510 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 8688 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 8688 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 7344 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 7344 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 8971 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 8971 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 60510 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 60510 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 6081 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 6081 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 8960 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 8960 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 8570 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 8570 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 81445 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 81445 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 7563 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 7563 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 7573 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 7573 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 8073 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 8073 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 8012 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 8012 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 82235 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 82235 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 60497 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 60497 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 7566 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 7566 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 7721 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 7721 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 8959 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 8959 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 7746 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 7746 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 6221 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 6221 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 6349 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 6349 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 60485 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 60485 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 60493 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 60493 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 60495 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 60495 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 210773 21 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 8553 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 8553 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 106287 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 106287 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 5830 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 5830 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 563 26 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 563 26 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 563 26 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 563 26 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 563 26 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 563 26 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 8569 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 8569 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 8641 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 8641 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 8850 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 8850 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 82232 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 82232 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 60488 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 60488 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 60502 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 60502 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 6258 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 6258 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 8972 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 8972 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 7344 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 7344 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 82350 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 82350 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 82355 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 82355 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 82350 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 82350 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 7237 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 7237 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 60490 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 60490 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 60512 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 60512 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 178240 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 178240 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 6082 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 6082 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 81362 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 81362 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 81451 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 81451 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 8003 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 8003 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 5800 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 5800 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 6082 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 6082 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 7720 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 7720 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 7589 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 7589 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 82234 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 82234 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 8993 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 8993 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 6765 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 6765 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 60487 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 60487 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 8922 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 8922 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 5860 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 5860 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 81450 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 81450 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 7417 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 7417 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 8973 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 8973 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 82234 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 82234 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 7726 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 7726 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 81449 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 81449 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 106291 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 106291 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 7725 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 7725 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 178416 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 178416 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 81445 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 81445 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 6900 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 6900 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 6083 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 6083 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 60503 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 60503 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 195237 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 195237 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 7684 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 7684 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 7685 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 7685 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 6349 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 6349 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 82237 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 82237 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 8572 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 8572 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 8216 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 8216 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 8320 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 8320 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 81446 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 81446 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 82356 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 82356 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 8958 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 8958 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 73827 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 73827 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 60504 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 60504 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 60501 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 60501 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 106286 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 106286 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 212053 15 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 7726 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 7726 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 9029 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 9029 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 6765 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 6765 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 60506 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 60506 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 8280 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 8280 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 8280 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 8280 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 57624 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 57624 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 73827 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 73827 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 8869 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 8869 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 8570 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 8570 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 60498 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 60498 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 81361 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 81361 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 82236 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 82236 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 60496 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 60496 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 6900 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 6900 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 8971 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 8971 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 106285 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 106285 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 564 10 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 564 10 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 564 10 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 564 10 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 7580 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 7580 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 100420 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 100420 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 60505 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 60505 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 8960 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 8960 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 106289 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 106289 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 6899 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 6899 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 60489 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 60489 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 6083 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 6083 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 2515 11 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 2515 11 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 2515 11 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 7566 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 7566 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 60496 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 60496 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 8780 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 8780 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 81448 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 81448 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 73828 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 73828 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 8262 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 8262 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 8800 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 8800 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 81448 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 81448 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 82359 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 82359 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 7346 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 7346 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 563 26 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 563 26 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 563 26 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 82233 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 82233 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 82237 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 82237 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 6081 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 6081 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 106282 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 106282 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 197004 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 197004 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 8926 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 8926 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 6898 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 6898 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 82235 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 82235 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 60487 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 60487 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 60497 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 60497 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 6367 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 6367 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 73828 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 73828 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 60503 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 60503 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 7370 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 7370 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 81362 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 81362 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 60502 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 60502 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 60506 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 60506 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 82232 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 82232 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 8485 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 8485 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 60485 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 60485 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 6898 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 6898 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 6258 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 6258 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 82360 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 82360 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 8972 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 8972 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 7725 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 7725 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 8073 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 8073 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 81451 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 81451 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 8480 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 8480 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 7724 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 7724 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 6368 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 6368 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 100246 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 100246 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 7518 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 7518 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 1014 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 1014 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 1014 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 1014 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 1014 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 1014 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 1014 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 1014 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 1014 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 8003 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 8003 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 60494 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 60494 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 8277 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 8277 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 7726 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 7726 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 81450 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 81450 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 5739 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 5739 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 1014 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 1014 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 1014 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 60486 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 60486 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 8002 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 8002 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 8081 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 8081 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 8279 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 8279 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 81364 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 81364 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 8216 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 8216 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 82240 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 82240 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 8554 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 8554 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 8154 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 8154 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 8280 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 8280 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 1115 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 1115 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 1115 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 8002 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 8002 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 8013 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 8013 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 8012 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 8012 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 8013 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 8013 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 60486 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 60486 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 82351 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 82351 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 563 26 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 563 26 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 563 26 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 8073 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 8073 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 81365 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 81365 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 8641 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 8641 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 1129 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 1129 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 1129 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 1129 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 2785 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 31675498
145996512 2785 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 31675498
6192 3036 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 3036 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 262 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15635635
6191 262 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18006692
6191 262 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20438784
6192 3036 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 3036 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 2510 32 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 2510 32 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 2510 32 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 1124 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 1124 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 985 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 985 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 985 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 3036 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 3036 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 3036 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 3036 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 1125 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 1125 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 1125 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 1125 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 1125 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 1125 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 1125 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 1125 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 1125 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 1008 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 1008 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 3036 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 3036 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 2520 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 2520 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 262 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18006692
6191 262 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20438784
25025654 564 10 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 564 10 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 564 10 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 564 10 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 2510 32 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 2510 32 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 2510 32 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 2510 32 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 2510 32 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 2510 32 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 1014 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 1014 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 1014 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 563 26 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 563 26 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 563 26 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 1472 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18006692
633 1472 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20438784
25025654 564 10 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 564 10 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 564 10 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 564 10 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 567 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 567 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 1470 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18006692
3946 1470 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20438784
25025860 563 26 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 563 26 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 563 26 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 564 10 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 564 10 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 564 10 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 564 10 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 2515 11 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 2515 11 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 2515 11 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 563 26 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 563 26 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 563 26 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 567 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 567 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 567 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 567 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 567 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 567 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 567 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 567 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 1115 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 1115 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 1115 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 1417 0 None -6 4 Human 5.6 pIC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9325344
635 1417 0 None -6 4 Human 5.6 pIC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9593699
635 1417 0 None -6 4 Human 5.6 pIC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9765358




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
155511392 168970 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 168970 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 168970 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 168970 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 170751 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 170751 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 104801 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 104801 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 104801 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 104801 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 104801 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 104801 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 104801 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 104801 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 2515 11 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 2515 11 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 2515 11 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 104787 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 104787 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 104787 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 104787 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 1125 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 1125 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 1125 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 104789 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 104789 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 1125 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 1125 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 1125 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 104789 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 104789 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 104781 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 104781 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 104772 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 104772 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 104785 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 104785 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 170073 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 170073 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 170958 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 170958 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 104785 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 104785 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 104783 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 104783 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 985 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 985 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 985 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 172622 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 172622 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 104795 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 104795 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 104795 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 104795 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 104776 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 104776 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 104780 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 104780 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 104780 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 104780 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 175459 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 175459 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 104786 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 104786 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 104786 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 104786 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 174041 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 174041 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 172622 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 172622 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 2515 11 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 2515 11 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 2515 11 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 104770 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 104770 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 104770 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 104770 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 104796 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 104796 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 2510 32 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 2510 32 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 2510 32 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 171790 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 171790 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 104786 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 104786 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 104786 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 104786 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 104772 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 104772 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 104784 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 104784 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 104790 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 104790 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 104790 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 104790 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 104775 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 104775 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 115559 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 115559 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 104783 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 104783 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 172421 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 172421 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 104780 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 104780 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 104780 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 104780 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 169860 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 169860 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 175047 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 175047 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 104789 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 104789 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 104799 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 104799 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 104789 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 104789 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 104799 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 104799 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 104774 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 104774 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 104774 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 104774 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 115561 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 115561 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 104775 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 104775 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 104776 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 104776 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 104788 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 104788 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 104788 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 104788 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 171905 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 171905 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 2510 32 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 2510 32 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 2510 32 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 2515 11 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 2515 11 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 2515 11 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 169864 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 169864 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 104784 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 104784 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 104792 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 104792 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 104792 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 104792 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 171905 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 171905 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 104802 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 104802 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 104794 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 104794 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 104794 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 104794 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 174041 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 174041 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 104802 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 104802 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 104771 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 104771 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 104771 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 104771 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 169918 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 169918 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 115558 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 115558 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 175047 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 175047 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 175598 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 175598 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 170751 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 170751 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 115565 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 115565 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 104787 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 104787 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 104787 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 104787 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 1125 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 1125 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 1125 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 104797 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 104797 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 1125 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 1125 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 1125 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 104799 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 104799 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 104799 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 104799 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 115565 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 115565 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 104788 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 104788 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 104788 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 104788 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 1115 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 1115 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 1115 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 1115 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 1115 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 1115 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 104770 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 104770 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 104770 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 104770 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 115559 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 115559 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 104793 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 104793 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 104793 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 104793 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 104777 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 104777 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 104777 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 104777 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 172251 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 172251 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 115564 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 115564 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 169860 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 169860 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 115563 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 115563 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 115562 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 115562 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 172421 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 172421 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 104781 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 104781 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 115560 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 115560 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 169918 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 169918 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 985 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 985 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 985 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 104796 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 104796 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 172251 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 172251 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 115562 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 115562 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 104794 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 104794 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 104794 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 104794 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 104792 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 104792 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 104792 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 104792 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 173499 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 173499 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 175598 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 175598 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 115563 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 115563 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 115566 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 115566 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 115564 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 115564 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 104778 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 104778 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 104778 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 104778 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 104777 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 104777 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 104777 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 104777 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 104778 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 104778 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 104778 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 104778 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 104798 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 104798 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 104797 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 104797 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 170073 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 170073 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 104779 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 104779 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 104790 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 104790 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 104779 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 104779 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 104790 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 104790 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 104773 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 104773 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 169422 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 169422 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 173499 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 173499 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 115558 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 115558 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 171790 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 171790 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 172634 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 172634 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 170958 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 170958 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 104779 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 104779 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 104779 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 104779 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 2515 11 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 2515 11 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 2515 11 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 104782 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 104782 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 115566 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 115566 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 104795 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 104795 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 104795 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 104795 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 115561 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 115561 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 104782 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 104782 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 104798 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 104798 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 115560 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 115560 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 175459 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 175459 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 104774 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 104774 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 104774 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 104774 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 104771 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 104771 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 104771 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 104771 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 172634 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 172634 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 1115 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 1115 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 1115 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 1115 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 1115 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 1115 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 104773 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 104773 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 169864 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 169864 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 73829 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 73829 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 73830 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 73830 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 73828 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 73828 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 82362 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 82362 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 81450 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 81450 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 81446 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 81446 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 82355 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 82355 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 81362 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 81362 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 81449 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 81449 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 211341 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 82351 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 82351 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 81451 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 81451 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 2510 32 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 2510 32 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 2510 32 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 73827 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 73827 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 1115 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 1115 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 1115 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 81447 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 81447 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 82232 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 82232 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 81363 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 81363 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 81445 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 81445 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 81361 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 81361 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 7436 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 7436 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 82239 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 82239 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 82242 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 82242 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 6349 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 6349 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 60487 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 60487 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 8081 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 8081 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 7589 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 7589 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 1014 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 1014 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 1014 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 57522 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 57522 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 1014 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 1014 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 1014 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 8320 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 8320 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 7388 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 7388 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 82240 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 82240 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 8279 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 8279 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 8973 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 8973 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 8280 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 8280 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 1115 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 1115 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 1115 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 57624 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 57624 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 8012 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 8012 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 7573 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 7573 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 81365 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 81365 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 563 26 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 563 26 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 563 26 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 8280 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 8280 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 73831 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 73831 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 82360 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 82360 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 563 26 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 563 26 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 563 26 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 7417 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 7417 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 82238 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 82238 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 8073 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 8073 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 7345 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 7345 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 60488 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 60488 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 60509 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 60509 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 60508 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 60508 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 7563 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 7563 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 7346 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 7346 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 2510 32 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 2510 32 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 2510 32 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 8074 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 8074 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 8003 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 8003 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 7588 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 7588 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 81448 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 81448 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 60511 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 60511 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 82356 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 82356 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 82235 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 82235 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 2515 11 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 2515 11 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 2515 11 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 2515 11 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 2515 11 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 2515 11 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 60495 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 60495 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 60497 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 60497 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 7347 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 7347 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 7587 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 7587 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 60492 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 60492 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 60512 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 60512 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 7724 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 7724 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 7725 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 7725 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 8216 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 8216 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 5799 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 5799 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 161244 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 161244 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 60498 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 60498 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 7726 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 7726 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 82350 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 82350 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 82241 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 82241 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 60493 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 60493 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 82352 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 82352 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 7720 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 7720 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 57625 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 57625 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 82359 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 82359 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 7561 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 7561 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 8399 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 8399 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 82361 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 82361 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 2510 32 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 2510 32 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 2510 32 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 82358 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 82358 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 82236 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 82236 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 82237 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 82237 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 82357 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 82357 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 7721 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 7721 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 8277 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 8277 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 60485 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 60485 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 60507 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 60507 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 60491 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 60491 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 8002 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 8002 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 7344 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 7344 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 7562 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 7562 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 8082 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 8082 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 82233 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 82233 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 563 26 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 563 26 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 563 26 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 25010 8 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 25010 8 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 60501 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 60501 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 60489 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 60489 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 60504 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 60504 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 60494 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 60494 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 60506 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 60506 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 60487 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 60487 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 60512 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 60512 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 8154 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 8154 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 8013 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 8013 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 82234 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 82234 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 60490 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 60490 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 60510 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 60510 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 81364 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 81364 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 82354 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 82354 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 57623 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 57623 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 60486 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 60486 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 7435 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 7435 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 60500 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 60500 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 60505 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 60505 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 60499 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 60499 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 213867 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 2510 32 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 2510 32 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 2510 32 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 2510 32 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 2510 32 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 2510 32 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 2510 32 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 2510 32 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 2510 32 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
25025654 564 10 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 564 10 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 564 10 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 564 10 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
1577 3634 104 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3634 104 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3634 104 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3634 104 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3634 104 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3634 104 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3634 104 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3634 104 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3634 104 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3634 104 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3634 104 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3634 104 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3634 104 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3634 104 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
None 214306 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 214306 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 214307 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 214312 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 214310 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 214311 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 214309 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 214308 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
1577 3634 104 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3634 104 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3634 104 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3634 104 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3634 104 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3634 104 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3634 104 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3634 104 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3634 104 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3634 104 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3634 104 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3634 104 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3634 104 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3634 104 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) -269 26 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512399 214314 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 3226 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 3226 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 214313 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 2510 32 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 2510 32 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 2510 32 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 2510 32 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 2510 32 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 2510 32 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 1470 0 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15102928
632 1445 0 None -6 5 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9325344
633 1472 0 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11112777
49871766 2510 32 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 2510 32 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 2510 32 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 1445 0 None -1 5 Mouse 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10454496
632 1445 0 None 1 5 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10454496