Ligand source activities (1 row/activity)





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

44300265 200122 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 200122 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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
49871766 2557 None 36 Human Functional pEC50 = 9.7 9.7 -6 5
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by 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 10.1021/acs.jmedchem.3c00323
6170 2557 None 36 Human Functional pEC50 = 9.7 9.7 -6 5
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by 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 10.1021/acs.jmedchem.3c00323
CHEMBL1672354 2557 None 36 Human Functional pEC50 = 9.7 9.7 -6 5
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by 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 10.1021/acs.jmedchem.3c00323
49871766 2557 None 36 Human Functional pEC50 = 9.5 9.5 -6 5
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 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/acs.jmedchem.3c00323
6170 2557 None 36 Human Functional pEC50 = 9.5 9.5 -6 5
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 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/acs.jmedchem.3c00323
CHEMBL1672354 2557 None 36 Human Functional pEC50 = 9.5 9.5 -6 5
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 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/acs.jmedchem.3c00323
49871766 2557 None 36 Mouse Functional pEC50 = 9.4 9.4 -3 5
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in IP-1 accumulation incubated for 60 mins by 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 10.1021/acs.jmedchem.3c00323
6170 2557 None 36 Mouse Functional pEC50 = 9.4 9.4 -3 5
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in IP-1 accumulation incubated for 60 mins by 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 10.1021/acs.jmedchem.3c00323
CHEMBL1672354 2557 None 36 Mouse Functional pEC50 = 9.4 9.4 -3 5
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in IP-1 accumulation incubated for 60 mins by 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 10.1021/acs.jmedchem.3c00323
132427043 195579 None 3 Mouse Functional pEC50 = 9.4 9.4 -1 3
Agonist activity at endogenous mouse BB3 in mouse B16 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at endogenous mouse BB3 in mouse B16 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5406411 195579 None 3 Mouse Functional pEC50 = 9.4 9.4 -1 3
Agonist activity at endogenous mouse BB3 in mouse B16 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at endogenous mouse BB3 in mouse B16 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
44300355 198995 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 198995 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 200543 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 200543 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 8098 None 0 Mouse Functional pEC50 = 8 8.0 12 2
Agonistic activity 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 8098 None 0 Mouse Functional pEC50 = 8 8.0 12 2
Agonistic activity 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
132427043 195579 None 3 Human Functional pEC50 = 8.0 8.0 -2 3
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5406411 195579 None 3 Human Functional pEC50 = 8.0 8.0 -2 3
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
46884660 6444 None 0 Human Functional pEC50 = 7 7.0 -1 2
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 6444 None 0 Human Functional pEC50 = 7 7.0 -1 2
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 7820 None 0 Human Functional pEC50 = 7 7.0 -3 2
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 7820 None 0 Human Functional pEC50 = 7 7.0 -3 2
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 8379 None 0 Human Functional pEC50 = 7 7.0 -3 2
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 8379 None 0 Human Functional pEC50 = 7 7.0 -3 2
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 60851 None 0 Mouse Functional pEC50 = 7 7.0 4 2
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 60851 None 0 Mouse Functional pEC50 = 7 7.0 4 2
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 60873 None 0 Human Functional pEC50 = 5 5.0 - 1
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 60873 None 0 Human Functional pEC50 = 5 5.0 - 1
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 60873 None 0 Human Functional pEC50 = 5 5.0 - 1
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 60873 None 0 Human Functional pEC50 = 5 5.0 - 1
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 8582 None 0 Human Functional pEC50 = 5 5.0 1 2
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 8582 None 0 Human Functional pEC50 = 5 5.0 1 2
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 8583 None 0 Human Functional pEC50 = 5 5.0 -1 2
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 8583 None 0 Human Functional pEC50 = 5 5.0 -1 2
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 8587 None 0 Human Functional pEC50 = 5 5.0 1 2
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 8587 None 0 Human Functional pEC50 = 5 5.0 1 2
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 8588 None 0 Human Functional pEC50 = 5 5.0 -11 2
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 8588 None 0 Human Functional pEC50 = 5 5.0 -11 2
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 8659 None 0 Human Functional pEC50 = 5 5.0 -10 2
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 8659 None 0 Human Functional pEC50 = 5 5.0 -10 2
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 8674 None 0 Human Functional pEC50 = 5 5.0 -21 2
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 8674 None 0 Human Functional pEC50 = 5 5.0 -21 2
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 8677 None 0 Human Functional pEC50 = 5 5.0 -1 2
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 8677 None 0 Human Functional pEC50 = 5 5.0 -1 2
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 8697 None 0 Human Functional pEC50 = 5 5.0 -6 2
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 8697 None 0 Human Functional pEC50 = 5 5.0 -6 2
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 8788 None 0 Human Functional pEC50 = 5 5.0 1 2
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 8788 None 0 Human Functional pEC50 = 5 5.0 1 2
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 8789 None 0 Human Functional pEC50 = 5 5.0 1 2
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 8789 None 0 Human Functional pEC50 = 5 5.0 1 2
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 8793 None 0 Human Functional pEC50 = 5 5.0 -25 2
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 8793 None 0 Human Functional pEC50 = 5 5.0 -25 2
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 8794 None 0 Human Functional pEC50 = 5 5.0 1 2
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 8794 None 0 Human Functional pEC50 = 5 5.0 1 2
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 8795 None 0 Human Functional pEC50 = 5 5.0 1 2
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 8795 None 0 Human Functional pEC50 = 5 5.0 1 2
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 8822 None 0 Human Functional pEC50 = 5 5.0 -9 2
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 8822 None 0 Human Functional pEC50 = 5 5.0 -9 2
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 8885 None 0 Human Functional pEC50 = 5 5.0 -13 2
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 8885 None 0 Human Functional pEC50 = 5 5.0 -13 2
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 8905 None 0 Human Functional pEC50 = 5 5.0 -1 2
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 8905 None 0 Human Functional pEC50 = 5 5.0 -1 2
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 8955 None 0 Human Functional pEC50 = 5 5.0 -20 2
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 8955 None 0 Human Functional pEC50 = 5 5.0 -20 2
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 8956 None 5 Human Functional pEC50 = 5 5.0 -2 2
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 8956 None 5 Human Functional pEC50 = 5 5.0 -2 2
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 8972 None 3 Human Functional pEC50 = 5 5.0 1 2
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 8972 None 3 Human Functional pEC50 = 5 5.0 1 2
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 8973 None 0 Human Functional pEC50 = 5 5.0 1 2
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 8973 None 0 Human Functional pEC50 = 5 5.0 1 2
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 9002 None 0 Human Functional pEC50 = 5 5.0 1 2
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 9002 None 0 Human Functional pEC50 = 5 5.0 1 2
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 9031 None 0 Human Functional pEC50 = 5 5.0 -1 2
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 9031 None 0 Human Functional pEC50 = 5 5.0 -1 2
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 14235 None 0 Human Functional pEC50 = 5 5.0 -2 2
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 14235 None 0 Human Functional pEC50 = 5 5.0 -2 2
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 8582 None 0 Rat Functional pEC50 = 5 5.0 -1 2
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 8582 None 0 Rat Functional pEC50 = 5 5.0 -1 2
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 8587 None 0 Rat Functional pEC50 = 5 5.0 -1 2
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 8587 None 0 Rat Functional pEC50 = 5 5.0 -1 2
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 8788 None 0 Rat Functional pEC50 = 5 5.0 -1 2
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 8788 None 0 Rat Functional pEC50 = 5 5.0 -1 2
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 8789 None 0 Rat Functional pEC50 = 5 5.0 -1 2
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 8789 None 0 Rat Functional pEC50 = 5 5.0 -1 2
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 8794 None 0 Rat Functional pEC50 = 5 5.0 -1 2
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 8794 None 0 Rat Functional pEC50 = 5 5.0 -1 2
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 8795 None 0 Rat Functional pEC50 = 5 5.0 -1 2
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 8795 None 0 Rat Functional pEC50 = 5 5.0 -1 2
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 8972 None 3 Rat Functional pEC50 = 5 5.0 -1 2
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 8972 None 3 Rat Functional pEC50 = 5 5.0 -1 2
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 8973 None 0 Rat Functional pEC50 = 5 5.0 -1 2
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 8973 None 0 Rat Functional pEC50 = 5 5.0 -1 2
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 9002 None 0 Rat Functional pEC50 = 5 5.0 -1 2
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 9002 None 0 Rat Functional pEC50 = 5 5.0 -1 2
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 6315 None 0 Mouse Functional pEC50 = 5 5.0 -2 2
Agonistic activity 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 6315 None 0 Mouse Functional pEC50 = 5 5.0 -2 2
Agonistic activity 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 6994 None 0 Human Functional pEC50 = 6 6.0 -13 2
Agonistic activity 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 6994 None 0 Human Functional pEC50 = 6 6.0 -13 2
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 346 7 2 2 4.5 O=C(O)c1ccccc1-c1ccc(CCc2ncc(CC3CC3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46845425 1032 None 2 Human Functional pEC50 = 7 7.0 1 2
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
8504 1032 None 2 Human Functional pEC50 = 7 7.0 1 2
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1089721 1032 None 2 Human Functional pEC50 = 7 7.0 1 2
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
172446140 195510 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 529 7 2 9 4.9 C=CC(C)(C)C(OC(=O)c1cccnc1Br)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5405083 195510 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 529 7 2 9 4.9 C=CC(C)(C)C(OC(=O)c1cccnc1Br)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
25026056 8183 None 0 Human Functional pEC50 = 7.0 7.0 1 2
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 8183 None 0 Human Functional pEC50 = 7.0 7.0 1 2
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 8422 None 0 Human Functional pEC50 = 7.0 7.0 -2 2
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 8422 None 0 Human Functional pEC50 = 7.0 7.0 -2 2
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 81903 None 0 Mouse Functional pEC50 = 7.0 7.0 -14 2
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 81903 None 0 Mouse Functional pEC50 = 7.0 7.0 -14 2
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 7603 None 0 Mouse Functional pEC50 = 7.0 7.0 22 2
Agonistic activity 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 7603 None 0 Mouse Functional pEC50 = 7.0 7.0 22 2
Agonistic activity 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 8317 None 0 Human Functional pEC50 = 7.0 7.0 -2 2
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 8317 None 0 Human Functional pEC50 = 7.0 7.0 -2 2
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 8113 None 0 Mouse Functional pEC50 = 7.0 7.0 4 2
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 8113 None 0 Mouse Functional pEC50 = 7.0 7.0 4 2
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 8182 None 0 Mouse Functional pEC50 = 7.0 7.0 3 2
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 8182 None 0 Mouse Functional pEC50 = 7.0 7.0 3 2
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 8422 None 0 Mouse Functional pEC50 = 7.0 7.0 2 2
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 8422 None 0 Mouse Functional pEC50 = 7.0 7.0 2 2
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 7819 None 0 Human Functional pEC50 = 7.0 7.0 -3 2
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 7819 None 0 Human Functional pEC50 = 7.0 7.0 -3 2
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 8183 None 0 Human Functional pEC50 = 7.0 7.0 1 2
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 8183 None 0 Human Functional pEC50 = 7.0 7.0 1 2
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 8382 None 0 Mouse Functional pEC50 = 7.0 7.0 -1 2
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 8382 None 0 Mouse Functional pEC50 = 7.0 7.0 -1 2
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 8822 None 0 Rat Functional pEC50 = 6.0 6.0 9 2
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 8822 None 0 Rat Functional pEC50 = 6.0 6.0 9 2
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 7823 None 0 Human Functional pEC50 = 7.0 7.0 -2 2
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 7823 None 0 Human Functional pEC50 = 7.0 7.0 -2 2
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 8183 None 0 Mouse Functional pEC50 = 7.0 7.0 -1 2
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 8183 None 0 Mouse Functional pEC50 = 7.0 7.0 -1 2
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 7784 None 0 Human Functional pEC50 = 7.0 7.0 -16 2
Agonistic activity 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 7784 None 0 Human Functional pEC50 = 7.0 7.0 -16 2
Agonistic activity 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 7820 None 0 Mouse Functional pEC50 = 7.0 7.0 3 2
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 7820 None 0 Mouse Functional pEC50 = 7.0 7.0 3 2
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 8175 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
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 8175 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
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 82820 None 0 Human Functional pEC50 = 7.0 7.0 14 2
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 82820 None 0 Human Functional pEC50 = 7.0 7.0 14 2
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 7819 None 0 Mouse Functional pEC50 = 7.0 7.0 3 2
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 7819 None 0 Mouse Functional pEC50 = 7.0 7.0 3 2
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 7819 None 0 Mouse Functional pEC50 = 8.0 8.0 3 2
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 7819 None 0 Mouse Functional pEC50 = 8.0 8.0 3 2
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 7820 None 0 Mouse Functional pEC50 = 8.0 8.0 3 2
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 7820 None 0 Mouse Functional pEC50 = 8.0 8.0 3 2
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 8379 None 0 Mouse Functional pEC50 = 8.0 8.0 3 2
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 8379 None 0 Mouse Functional pEC50 = 8.0 8.0 3 2
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 7534 None 0 Mouse Functional pEC50 = 8.0 8.0 1 2
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 7534 None 0 Mouse Functional pEC50 = 8.0 8.0 1 2
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 7167 None 0 Mouse Functional pEC50 = 8.0 8.0 18 2
Agonistic activity 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 7167 None 0 Mouse Functional pEC50 = 8.0 8.0 18 2
Agonistic activity 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 82816 None 0 Human Functional pEC50 = 7.0 7.0 6 2
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 82816 None 0 Human Functional pEC50 = 7.0 7.0 6 2
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 82819 None 0 Human Functional pEC50 = 7.0 7.0 7 2
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 82819 None 0 Human Functional pEC50 = 7.0 7.0 7 2
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 60849 None 0 Mouse Functional pEC50 = 7.0 7.0 6 2
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 60849 None 0 Mouse Functional pEC50 = 7.0 7.0 6 2
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 7825 None 0 Mouse Functional pEC50 = 7.0 7.0 3 2
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 7825 None 0 Mouse Functional pEC50 = 7.0 7.0 3 2
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 7823 None 0 Mouse Functional pEC50 = 7.0 7.0 2 2
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 7823 None 0 Mouse Functional pEC50 = 7.0 7.0 2 2
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 81904 None 0 Human Functional pEC50 = 6.9 6.9 8 2
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 81904 None 0 Human Functional pEC50 = 6.9 6.9 8 2
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 8381 None 0 Mouse Functional pEC50 = 6.9 6.9 2 2
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 8381 None 0 Mouse Functional pEC50 = 6.9 6.9 2 2
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 81904 None 0 Mouse Functional pEC50 = 6.9 6.9 -8 2
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 81904 None 0 Mouse Functional pEC50 = 6.9 6.9 -8 2
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 5607 None 0 Human Functional pEC50 = 5.9 5.9 -7 2
Agonistic activity 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 5607 None 0 Human Functional pEC50 = 5.9 5.9 -7 2
Agonistic activity 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 6444 None 0 Mouse Functional pEC50 = 6.9 6.9 1 2
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 6444 None 0 Mouse Functional pEC50 = 6.9 6.9 1 2
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 8255 None 0 Mouse Functional pEC50 = 6.9 6.9 1 2
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 8255 None 0 Mouse Functional pEC50 = 6.9 6.9 1 2
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 8098 None 0 Human Functional pEC50 = 6.9 6.9 -12 2
Agonistic activity 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 8098 None 0 Human Functional pEC50 = 6.9 6.9 -12 2
Agonistic activity 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 7824 None 0 Mouse Functional pEC50 = 7.9 7.9 6 2
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 7824 None 0 Mouse Functional pEC50 = 7.9 7.9 6 2
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 7486 None 0 Mouse Functional pEC50 = 7.9 7.9 10 2
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 7486 None 0 Mouse Functional pEC50 = 7.9 7.9 10 2
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 7659 None 0 Mouse Functional pEC50 = 7.9 7.9 -1 2
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 7659 None 0 Mouse Functional pEC50 = 7.9 7.9 -1 2
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 82813 None 0 Mouse Functional pEC50 = 6.9 6.9 -18 2
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 82813 None 0 Mouse Functional pEC50 = 6.9 6.9 -18 2
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 60859 None 0 Human Functional pEC50 = 5.9 5.9 -3 2
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 60859 None 0 Human Functional pEC50 = 5.9 5.9 -3 2
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 60871 None 0 Human Functional pEC50 = 5.9 5.9 -3 2
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 60871 None 0 Human Functional pEC50 = 5.9 5.9 -3 2
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 106847 None 0 Human Functional pEC50 = 5.9 5.9 12 3
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 106847 None 0 Human Functional pEC50 = 5.9 5.9 12 3
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 7824 None 0 Mouse Functional pEC50 = 6.9 6.9 6 2
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 7824 None 0 Mouse Functional pEC50 = 6.9 6.9 6 2
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 82698 None 0 Human Functional pEC50 = 6.9 6.9 2 2
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 82698 None 0 Human Functional pEC50 = 6.9 6.9 2 2
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 9092 None 0 Rat Functional pEC50 = 6.9 6.9 28 2
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 9092 None 0 Rat Functional pEC50 = 6.9 6.9 28 2
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 9064 None 0 Human Functional pEC50 = 5.9 5.9 -2 2
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 9064 None 0 Human Functional pEC50 = 5.9 5.9 -2 2
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 8103 None 0 Human Functional pEC50 = 5.9 5.9 -10 2
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 8103 None 0 Human Functional pEC50 = 5.9 5.9 -10 2
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 6463 None 0 Human Functional pEC50 = 6.9 6.9 -13 2
Agonistic activity 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 6463 None 0 Human Functional pEC50 = 6.9 6.9 -13 2
Agonistic activity 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 7486 None 0 Human Functional pEC50 = 6.9 6.9 -10 2
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 7486 None 0 Human Functional pEC50 = 6.9 6.9 -10 2
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 82820 None 0 Mouse Functional pEC50 = 6.9 6.9 -14 2
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 82820 None 0 Mouse Functional pEC50 = 6.9 6.9 -14 2
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 9091 None 0 Rat Functional pEC50 = 6.9 6.9 24 2
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 9091 None 0 Rat Functional pEC50 = 6.9 6.9 24 2
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 7661 None 0 Mouse Functional pEC50 = 7.9 7.9 2 2
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 7661 None 0 Mouse Functional pEC50 = 7.9 7.9 2 2
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 7671 None 0 Mouse Functional pEC50 = 7.9 7.9 2 2
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 7671 None 0 Mouse Functional pEC50 = 7.9 7.9 2 2
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 60850 None 0 Mouse Functional pEC50 = 7.9 7.9 4 2
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 60850 None 0 Mouse Functional pEC50 = 7.9 7.9 4 2
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
49871766 2557 None 36 Mouse Functional pEC50 = 7.9 7.9 -3 5
Agonist activity at endogenous mouse BB3 in mouse B16 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at endogenous mouse BB3 in mouse B16 cells assessed as increase in IP-1 accumulation incubated for 60 mins by 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 10.1021/acs.jmedchem.3c00323
6170 2557 None 36 Mouse Functional pEC50 = 7.9 7.9 -3 5
Agonist activity at endogenous mouse BB3 in mouse B16 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at endogenous mouse BB3 in mouse B16 cells assessed as increase in IP-1 accumulation incubated for 60 mins by 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 10.1021/acs.jmedchem.3c00323
CHEMBL1672354 2557 None 36 Mouse Functional pEC50 = 7.9 7.9 -3 5
Agonist activity at endogenous mouse BB3 in mouse B16 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at endogenous mouse BB3 in mouse B16 cells assessed as increase in IP-1 accumulation incubated for 60 mins by 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 10.1021/acs.jmedchem.3c00323
46200989 2562 None 14 Mouse Functional pEC50 = 6.9 6.9 -9 2
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1021/ml200304j
8502 2562 None 14 Mouse Functional pEC50 = 6.9 6.9 -9 2
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1021/ml200304j
CHEMBL2023109 2562 None 14 Mouse Functional pEC50 = 6.9 6.9 -9 2
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1021/ml200304j
46200989 2562 None 14 Mouse Functional pEC50 = 6.9 6.9 -9 2
Agonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2012.03.029
8502 2562 None 14 Mouse Functional pEC50 = 6.9 6.9 -9 2
Agonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2012.03.029
CHEMBL2023109 2562 None 14 Mouse Functional pEC50 = 6.9 6.9 -9 2
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 60858 None 0 Mouse Functional pEC50 = 5.9 5.9 3 2
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 60858 None 0 Mouse Functional pEC50 = 5.9 5.9 3 2
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 8114 None 0 Human Functional pEC50 = 6.9 6.9 -2 2
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 8114 None 0 Human Functional pEC50 = 6.9 6.9 -2 2
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 82700 None 0 Human Functional pEC50 = 6.9 6.9 6 2
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 82700 None 0 Human Functional pEC50 = 6.9 6.9 6 2
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 7219 None 0 Human Functional pEC50 = 5.9 5.9 -7 2
Agonistic activity 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 7219 None 0 Human Functional pEC50 = 5.9 5.9 -7 2
Agonistic activity 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 7685 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
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 7685 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
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 8175 None 0 Mouse Functional pEC50 = 6.9 6.9 1 2
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 8175 None 0 Mouse Functional pEC50 = 6.9 6.9 1 2
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 339 7 1 2 5.2 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCCC3)cc2)n1 10.1016/j.bmcl.2010.02.076
25025654 570 None 12 Human Functional pEC50 = 6.9 6.9 -15 3
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 10.1016/j.bmcl.2010.01.154
6189 570 None 12 Human Functional pEC50 = 6.9 6.9 -15 3
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 10.1016/j.bmcl.2010.01.154
8506 570 None 12 Human Functional pEC50 = 6.9 6.9 -15 3
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 10.1016/j.bmcl.2010.01.154
CHEMBL1084942 570 None 12 Human Functional pEC50 = 6.9 6.9 -15 3
Agonistic activity 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 81818 None 0 Mouse Functional pEC50 = 6.9 6.9 -11 2
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 81818 None 0 Mouse Functional pEC50 = 6.9 6.9 -11 2
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 82817 None 0 Mouse Functional pEC50 = 6.9 6.9 -6 2
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 82817 None 0 Mouse Functional pEC50 = 6.9 6.9 -6 2
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
172444284 195042 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 444 7 2 9 3.6 C=CC(C)(C)C(OC(=O)C1CCCO1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5395420 195042 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 444 7 2 9 3.6 C=CC(C)(C)C(OC(=O)C1CCCO1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
25025862 7823 None 0 Human Functional pEC50 = 6.9 6.9 -2 2
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 7823 None 0 Human Functional pEC50 = 6.9 6.9 -2 2
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 322 7 1 3 4.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3cccn3)cc2)n1 10.1016/j.bmcl.2010.02.076
49871766 2557 None 36 Human Functional pEC50 = 7.9 7.9 -6 5
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
6170 2557 None 36 Human Functional pEC50 = 7.9 7.9 -6 5
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
CHEMBL1672354 2557 None 36 Human Functional pEC50 = 7.9 7.9 -6 5
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 57859 None 1 Human Functional pEC50 = 7.9 7.9 - 1
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 57859 None 1 Human Functional pEC50 = 7.9 7.9 - 1
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 8103 None 0 Mouse Functional pEC50 = 7.9 7.9 10 2
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 8103 None 0 Mouse Functional pEC50 = 7.9 7.9 10 2
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
172443644 195475 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 451 7 2 9 4.1 C=CC(C)(C)C(OC(=O)c1ccccn1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5404444 195475 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 451 7 2 9 4.1 C=CC(C)(C)C(OC(=O)c1ccccn1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
46881604 8872 None 0 Mouse Functional pEC50 = 7.8 7.8 25 2
Agonistic activity 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 8872 None 0 Mouse Functional pEC50 = 7.8 7.8 25 2
Agonistic activity 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 106833 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 106833 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 106842 None 0 Human Functional pEC50 = 5.9 5.9 8 3
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 106842 None 0 Human Functional pEC50 = 5.9 5.9 8 3
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 42886 None 68 Human Functional pEC50 = 4.9 4.9 -4 6
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 42886 None 68 Human Functional pEC50 = 4.9 4.9 -4 6
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 8697 None 0 Rat Functional pEC50 = 5.8 5.8 6 2
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 8697 None 0 Rat Functional pEC50 = 5.8 5.8 6 2
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 81820 None 0 Mouse Functional pEC50 = 6.8 6.8 -87 2
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 81820 None 0 Mouse Functional pEC50 = 6.8 6.8 -87 2
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 82696 None 0 Mouse Functional pEC50 = 6.8 6.8 -2 2
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 82696 None 0 Mouse Functional pEC50 = 6.8 6.8 -2 2
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
132427043 195579 None 3 Human Functional pEC50 = 6.8 6.8 -2 3
Agonist activity at human BB3 transiently expressed in human HEK293T cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 transiently expressed in human HEK293T cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5406411 195579 None 3 Human Functional pEC50 = 6.8 6.8 -2 3
Agonist activity at human BB3 transiently expressed in human HEK293T cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 transiently expressed in human HEK293T cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
46885313 8104 None 0 Human Functional pEC50 = 7.8 7.8 -3 2
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 8104 None 0 Human Functional pEC50 = 7.8 7.8 -3 2
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 7660 None 0 Human Functional pEC50 = 7.8 7.8 1 2
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 7660 None 0 Human Functional pEC50 = 7.8 7.8 1 2
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 407 8 2 5 4.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(N3CCCC[C@@H]3c3nnn[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
56840673 1141 None 0 Human Functional pEC50 = 7.8 7.8 2 2
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 10 mins by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 10 mins by bioluminescence assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
8503 1141 None 0 Human Functional pEC50 = 7.8 7.8 2 2
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 10 mins by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 10 mins by bioluminescence assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
CHEMBL2164575 1141 None 0 Human Functional pEC50 = 7.8 7.8 2 2
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 74220 None 0 Human Functional pEC50 = 7.8 7.8 3 2
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 74220 None 0 Human Functional pEC50 = 7.8 7.8 3 2
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 8182 None 0 Mouse Functional pEC50 = 7.8 7.8 3 2
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 8182 None 0 Mouse Functional pEC50 = 7.8 7.8 3 2
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 199260 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 199260 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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
172460636 196513 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 451 7 2 9 4.1 C=CC(C)(C)C(OC(=O)c1cccnc1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5425677 196513 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 451 7 2 9 4.1 C=CC(C)(C)C(OC(=O)c1cccnc1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
44300286 96612 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 96612 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 82691 None 0 Human Functional pEC50 = 6.8 6.8 2 2
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 82691 None 0 Human Functional pEC50 = 6.8 6.8 2 2
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 82697 None 0 Mouse Functional pEC50 = 6.8 6.8 -3 2
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 82697 None 0 Mouse Functional pEC50 = 6.8 6.8 -3 2
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 9063 None 0 Human Functional pEC50 = 5.8 5.8 -24 2
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 9063 None 0 Human Functional pEC50 = 5.8 5.8 -24 2
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 82814 None 0 Mouse Functional pEC50 = 6.8 6.8 -10 2
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 82814 None 0 Mouse Functional pEC50 = 6.8 6.8 -10 2
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 82697 None 0 Human Functional pEC50 = 6.8 6.8 3 2
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 82697 None 0 Human Functional pEC50 = 6.8 6.8 3 2
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 7678 None 0 Human Functional pEC50 = 6.8 6.8 -19 2
Agonistic activity 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 7678 None 0 Human Functional pEC50 = 6.8 6.8 -19 2
Agonistic activity 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 57963 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 57963 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 8382 None 0 Mouse Functional pEC50 = 7.8 7.8 -1 2
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 8382 None 0 Mouse Functional pEC50 = 7.8 7.8 -1 2
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 7660 None 0 Mouse Functional pEC50 = 7.8 7.8 -1 2
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 7660 None 0 Mouse Functional pEC50 = 7.8 7.8 -1 2
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 9078 None 0 Mouse Functional pEC50 = 7.8 7.8 1 2
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 9078 None 0 Mouse Functional pEC50 = 7.8 7.8 1 2
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 60848 None 0 Human Functional pEC50 = 6.8 6.8 -3 2
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 60848 None 0 Human Functional pEC50 = 6.8 6.8 -3 2
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 60867 None 0 Mouse Functional pEC50 = 6.8 6.8 7 2
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 60867 None 0 Mouse Functional pEC50 = 6.8 6.8 7 2
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 60860 None 0 Human Functional pEC50 = 5.8 5.8 -3 2
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 60860 None 0 Human Functional pEC50 = 5.8 5.8 -3 2
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 186797 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 186797 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 7335 None 0 Human Functional pEC50 = 5.8 5.8 -31 2
Agonistic activity 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 7335 None 0 Human Functional pEC50 = 5.8 5.8 -31 2
Agonistic activity 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 82816 None 0 Mouse Functional pEC50 = 6.8 6.8 -6 2
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 82816 None 0 Mouse Functional pEC50 = 6.8 6.8 -6 2
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 7467 None 0 Mouse Functional pEC50 = 6.8 6.8 16 2
Agonistic activity 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 7467 None 0 Mouse Functional pEC50 = 6.8 6.8 16 2
Agonistic activity 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 6764 None 0 Mouse Functional pEC50 = 6.8 6.8 10 2
Agonistic activity 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 6764 None 0 Mouse Functional pEC50 = 6.8 6.8 10 2
Agonistic activity 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 5607 None 0 Mouse Functional pEC50 = 6.8 6.8 7 2
Agonistic activity 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 5607 None 0 Mouse Functional pEC50 = 6.8 6.8 7 2
Agonistic activity 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 8379 None 0 Human Functional pEC50 = 6.8 6.8 -3 2
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 8379 None 0 Human Functional pEC50 = 6.8 6.8 -3 2
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 200071 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 200071 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 60871 None 0 Mouse Functional pEC50 = 6.8 6.8 3 2
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 60871 None 0 Mouse Functional pEC50 = 6.8 6.8 3 2
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 60854 None 0 Human Functional pEC50 = 5.8 5.8 -12 2
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 60854 None 0 Human Functional pEC50 = 5.8 5.8 -12 2
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 60872 None 0 Human Functional pEC50 = 5.8 5.8 -3 2
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 60872 None 0 Human Functional pEC50 = 5.8 5.8 -3 2
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 8175 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
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 8175 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
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 82819 None 0 Mouse Functional pEC50 = 6.8 6.8 -7 2
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 82819 None 0 Mouse Functional pEC50 = 6.8 6.8 -7 2
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 7443 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 7443 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 6764 None 0 Human Functional pEC50 = 5.8 5.8 -10 2
Agonistic activity 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 6764 None 0 Human Functional pEC50 = 5.8 5.8 -10 2
Agonistic activity 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 7219 None 0 Mouse Functional pEC50 = 6.8 6.8 7 2
Agonistic activity 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 7219 None 0 Mouse Functional pEC50 = 6.8 6.8 7 2
Agonistic activity 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 5893 None 0 Rat Functional pEC50 = 6.8 6.8 1 3
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 5893 None 0 Rat Functional pEC50 = 6.8 6.8 1 3
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 7686 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 7686 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 7616 None 0 Human Functional pEC50 = 6.8 6.8 -18 2
Agonistic activity 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 7616 None 0 Human Functional pEC50 = 6.8 6.8 -18 2
Agonistic activity 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 60864 None 0 Mouse Functional pEC50 = 6.8 6.8 3 2
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 60864 None 0 Mouse Functional pEC50 = 6.8 6.8 3 2
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 8059 None 0 Mouse Functional pEC50 = 6.7 6.7 15 2
Agonistic activity 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 8059 None 0 Mouse Functional pEC50 = 6.7 6.7 15 2
Agonistic activity 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 5893 None 0 Human Functional pEC50 = 5.7 5.7 -15 3
Agonistic activity 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 5893 None 0 Human Functional pEC50 = 5.7 5.7 -15 3
Agonistic activity 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 8183 None 0 Mouse Functional pEC50 = 7.7 7.7 -1 2
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 8183 None 0 Mouse Functional pEC50 = 7.7 7.7 -1 2
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 60529 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 60529 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 60872 None 0 Mouse Functional pEC50 = 6.7 6.7 3 2
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 60872 None 0 Mouse Functional pEC50 = 6.7 6.7 3 2
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 5893 None 0 Human Functional pEC50 = 5.7 5.7 -15 3
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 5893 None 0 Human Functional pEC50 = 5.7 5.7 -15 3
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 8381 None 0 Human Functional pEC50 = 6.7 6.7 -2 2
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 8381 None 0 Human Functional pEC50 = 6.7 6.7 -2 2
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 82815 None 0 Human Functional pEC50 = 6.7 6.7 11 2
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 82815 None 0 Human Functional pEC50 = 6.7 6.7 11 2
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 106845 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 106845 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 496 11 4 3 3.3 C[C@H](NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
49871766 2557 None 36 Rat Functional pEC50 = 8.7 8.7 3 5
Agonist activity at rat BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at rat BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
6170 2557 None 36 Rat Functional pEC50 = 8.7 8.7 3 5
Agonist activity at rat BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at rat BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
CHEMBL1672354 2557 None 36 Rat Functional pEC50 = 8.7 8.7 3 5
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 101100 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 101100 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 522 9 6 3 3.5 O=C(Cc1cc2ccccc2[nH]1)NNC(=O)NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
25025860 569 None 23 Mouse Functional pEC50 = 8.6 8.6 -4 5
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
6188 569 None 23 Mouse Functional pEC50 = 8.6 8.6 -4 5
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1091720 569 None 23 Mouse Functional pEC50 = 8.6 8.6 -4 5
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 8501 None 0 Mouse Functional pEC50 = 8.5 8.5 4 2
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 8501 None 0 Mouse Functional pEC50 = 8.5 8.5 4 2
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 200025 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 200025 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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
49871766 2557 None 36 Mouse Functional pEC50 = 8.5 8.5 -3 5
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 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/acs.jmedchem.3c00323
6170 2557 None 36 Mouse Functional pEC50 = 8.5 8.5 -3 5
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 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/acs.jmedchem.3c00323
CHEMBL1672354 2557 None 36 Mouse Functional pEC50 = 8.5 8.5 -3 5
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 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/acs.jmedchem.3c00323
46881470 6462 None 0 Mouse Functional pEC50 = 7.7 7.7 40 2
Agonistic activity 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 6462 None 0 Mouse Functional pEC50 = 7.7 7.7 40 2
Agonistic activity 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 60868 None 0 Mouse Functional pEC50 = 6.7 6.7 11 2
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 60868 None 0 Mouse Functional pEC50 = 6.7 6.7 11 2
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 82694 None 0 Mouse Functional pEC50 = 6.7 6.7 -10 2
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 82694 None 0 Mouse Functional pEC50 = 6.7 6.7 -10 2
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 7167 None 0 Human Functional pEC50 = 6.7 6.7 -18 2
Agonistic activity 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 7167 None 0 Human Functional pEC50 = 6.7 6.7 -18 2
Agonistic activity 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 82818 None 0 Mouse Functional pEC50 = 6.7 6.7 -15 2
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 82818 None 0 Mouse Functional pEC50 = 6.7 6.7 -15 2
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 74219 None 0 Human Functional pEC50 = 7.7 7.7 6 2
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 74219 None 0 Human Functional pEC50 = 7.7 7.7 6 2
Agonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 586 5 2 6 5.4 NC(=O)C1(c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)CCC1 10.1016/j.bmc.2012.03.029
49871766 2557 None 36 Mouse Functional pEC50 = 7.7 7.7 -3 5
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
6170 2557 None 36 Mouse Functional pEC50 = 7.7 7.7 -3 5
Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
CHEMBL1672354 2557 None 36 Mouse Functional pEC50 = 7.7 7.7 -3 5
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 60847 None 0 Mouse Functional pEC50 = 7.7 7.7 3 2
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 60847 None 0 Mouse Functional pEC50 = 7.7 7.7 3 2
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 100702 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 100702 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 163225 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 163225 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 172826 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 172826 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 60868 None 0 Human Functional pEC50 = 5.7 5.7 -11 2
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 60868 None 0 Human Functional pEC50 = 5.7 5.7 -11 2
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 9098 None 0 Rat Functional pEC50 = 6.7 6.7 2 2
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 9098 None 0 Rat Functional pEC50 = 6.7 6.7 2 2
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 82696 None 0 Human Functional pEC50 = 6.7 6.7 2 2
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 82696 None 0 Human Functional pEC50 = 6.7 6.7 2 2
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 8113 None 0 Mouse Functional pEC50 = 7.7 7.7 4 2
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 8113 None 0 Mouse Functional pEC50 = 7.7 7.7 4 2
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 74219 None 0 Mouse Functional pEC50 = 7.7 7.7 -6 2
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 74219 None 0 Mouse Functional pEC50 = 7.7 7.7 -6 2
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 74220 None 0 Mouse Functional pEC50 = 7.7 7.7 -3 2
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 74220 None 0 Mouse Functional pEC50 = 7.7 7.7 -3 2
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 6064 None 0 Mouse Functional pEC50 = 7.7 7.7 13 2
Agonistic activity 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 6064 None 0 Mouse Functional pEC50 = 7.7 7.7 13 2
Agonistic activity 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 57961 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 57961 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 60852 None 0 Human Functional pEC50 = 6.7 6.7 -6 2
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 60852 None 0 Human Functional pEC50 = 6.7 6.7 -6 2
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 25237 None 9 Human Functional pEC50 = 6.7 6.7 - 1
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 25237 None 9 Human Functional pEC50 = 6.7 6.7 - 1
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 5924 None 0 Mouse Functional pEC50 = 5.7 5.7 2 2
Agonistic activity 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 5924 None 0 Mouse Functional pEC50 = 5.7 5.7 2 2
Agonistic activity 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
135398391 195996 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 418 10 3 8 3.7 C=CC(C)(C)C(OCCCCO)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5414856 195996 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 418 10 3 8 3.7 C=CC(C)(C)C(OCCCCO)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
46881509 7603 None 0 Human Functional pEC50 = 5.6 5.6 -22 2
Agonistic activity 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 7603 None 0 Human Functional pEC50 = 5.6 5.6 -22 2
Agonistic activity 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 8873 None 0 Mouse Functional pEC50 = 7.6 7.6 14 2
Agonistic activity 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 8873 None 0 Mouse Functional pEC50 = 7.6 7.6 14 2
Agonistic activity 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 106846 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 106846 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 82700 None 0 Mouse Functional pEC50 = 6.6 6.6 -6 2
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 82700 None 0 Mouse Functional pEC50 = 6.6 6.6 -6 2
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 5893 None 0 Mouse Functional pEC50 = 6.6 6.6 -1 3
Agonistic activity 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 5893 None 0 Mouse Functional pEC50 = 6.6 6.6 -1 3
Agonistic activity 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
123695309 196718 None 0 Human Functional pEC50 = 5.6 5.6 -4 2
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assay
ChEMBL 346 5 3 7 3.0 COc1cc(C(O)CC=C(C)C)c(OC)c2c1/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5430646 196718 None 0 Human Functional pEC50 = 5.6 5.6 -4 2
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assay
ChEMBL 346 5 3 7 3.0 COc1cc(C(O)CC=C(C)C)c(OC)c2c1/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
46889233 7659 None 0 Human Functional pEC50 = 7.6 7.6 1 2
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 7659 None 0 Human Functional pEC50 = 7.6 7.6 1 2
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 163282 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 163282 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 189544 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 189544 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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
65909 39640 None 17 Human Functional pEC50 = 6.6 6.6 - 1
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 428 3 1 5 4.2 CC1(CN2CCC(n3c(=O)[nH]c4ccccc43)CC2)OCc2ccccc2-n2cccc21 10.1021/jm0210921
CHEMBL1474352 39640 None 17 Human Functional pEC50 = 6.6 6.6 - 1
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 428 3 1 5 4.2 CC1(CN2CCC(n3c(=O)[nH]c4ccccc43)CC2)OCc2ccccc2-n2cccc21 10.1021/jm0210921
CHEMBL5483013 39640 None 17 Human Functional pEC50 = 6.6 6.6 - 1
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 428 3 1 5 4.2 CC1(CN2CCC(n3c(=O)[nH]c4ccccc43)CC2)OCc2ccccc2-n2cccc21 10.1021/jm0210921
59618646 82699 None 0 Mouse Functional pEC50 = 6.6 6.6 -2 2
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 82699 None 0 Mouse Functional pEC50 = 6.6 6.6 -2 2
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 421 2 1 4 5.4 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1cccnc1N2 10.1021/ml200207w
46845425 1032 None 2 Human Functional pEC50 = 7.6 7.6 1 2
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
8504 1032 None 2 Human Functional pEC50 = 7.6 7.6 1 2
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1089721 1032 None 2 Human Functional pEC50 = 7.6 7.6 1 2
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
46845425 1032 None 2 Human Functional pEC50 = 7.6 7.6 1 2
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.03.028
8504 1032 None 2 Human Functional pEC50 = 7.6 7.6 1 2
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.03.028
CHEMBL1089721 1032 None 2 Human Functional pEC50 = 7.6 7.6 1 2
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 8174 None 0 Mouse Functional pEC50 = 7.6 7.6 3 2
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 8174 None 0 Mouse Functional pEC50 = 7.6 7.6 3 2
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 324 7 1 5 3.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-n3ncnn3)cc2)n1 10.1016/j.bmcl.2010.02.076
46845425 1032 None 2 Human Functional pEC50 = 7.6 7.6 1 2
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.01.154
8504 1032 None 2 Human Functional pEC50 = 7.6 7.6 1 2
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.01.154
CHEMBL1089721 1032 None 2 Human Functional pEC50 = 7.6 7.6 1 2
Agonistic activity 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 106835 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 106835 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 74218 None 0 Human Functional pEC50 = 7.6 7.6 7 2
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 74218 None 0 Human Functional pEC50 = 7.6 7.6 7 2
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 8381 None 0 Mouse Functional pEC50 = 7.6 7.6 2 2
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 8381 None 0 Mouse Functional pEC50 = 7.6 7.6 2 2
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 60853 None 0 Mouse Functional pEC50 = 6.6 6.6 1 2
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 60853 None 0 Mouse Functional pEC50 = 6.6 6.6 1 2
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 60867 None 0 Human Functional pEC50 = 5.6 5.6 -7 2
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 60867 None 0 Human Functional pEC50 = 5.6 5.6 -7 2
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 5894 None 0 Human Functional pEC50 = 5.6 5.6 -5 2
Agonistic activity 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 5894 None 0 Human Functional pEC50 = 5.6 5.6 -5 2
Agonistic activity 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 7467 None 0 Human Functional pEC50 = 5.6 5.6 -16 2
Agonistic activity 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 7467 None 0 Human Functional pEC50 = 5.6 5.6 -16 2
Agonistic activity 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 7515 None 0 Mouse Functional pEC50 = 7.6 7.6 1 2
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 7515 None 0 Mouse Functional pEC50 = 7.6 7.6 1 2
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 74218 None 0 Mouse Functional pEC50 = 7.6 7.6 -7 2
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 74218 None 0 Mouse Functional pEC50 = 7.6 7.6 -7 2
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 60869 None 0 Mouse Functional pEC50 = 6.6 6.6 3 2
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 60869 None 0 Mouse Functional pEC50 = 6.6 6.6 3 2
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 200037 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 200037 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 5833 None 0 Human Functional pEC50 = 5.6 5.6 -28 2
Agonistic activity 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 5833 None 0 Human Functional pEC50 = 5.6 5.6 -28 2
Agonistic activity 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 8326 None 0 Human Functional pEC50 = 5.6 5.6 -7 2
Agonistic activity 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 8326 None 0 Human Functional pEC50 = 5.6 5.6 -7 2
Agonistic activity 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 7845 None 0 Mouse Functional pEC50 = 5.6 5.6 1 2
Agonistic activity 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 7845 None 0 Mouse Functional pEC50 = 5.6 5.6 1 2
Agonistic activity 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 8059 None 0 Human Functional pEC50 = 5.6 5.6 -15 2
Agonistic activity 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 8059 None 0 Human Functional pEC50 = 5.6 5.6 -15 2
Agonistic activity 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 82812 None 0 Human Functional pEC50 = 6.6 6.6 7 2
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 82812 None 0 Human Functional pEC50 = 6.6 6.6 7 2
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
172452178 195831 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 451 7 2 9 4.1 C=CC(C)(C)C(OC(=O)c1ccncc1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5411592 195831 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 451 7 2 9 4.1 C=CC(C)(C)C(OC(=O)c1ccncc1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
46884688 8175 None 0 Mouse Functional pEC50 = 7.6 7.6 1 2
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 8175 None 0 Mouse Functional pEC50 = 7.6 7.6 1 2
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 60847 None 0 Mouse Functional pEC50 = 7.6 7.6 3 2
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 60847 None 0 Mouse Functional pEC50 = 7.6 7.6 3 2
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 7534 None 0 Human Functional pEC50 = 7.5 7.5 -1 2
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 7534 None 0 Human Functional pEC50 = 7.5 7.5 -1 2
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 6064 None 0 Human Functional pEC50 = 6.5 6.5 -13 2
Agonistic activity 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 6064 None 0 Human Functional pEC50 = 6.5 6.5 -13 2
Agonistic activity 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 8422 None 0 Mouse Functional pEC50 = 8.5 8.5 2 2
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 8422 None 0 Mouse Functional pEC50 = 8.5 8.5 2 2
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 200703 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 200703 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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
132427043 195579 None 3 Human Functional pEC50 = 8.4 8.4 -2 3
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5406411 195579 None 3 Human Functional pEC50 = 8.4 8.4 -2 3
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
46884628 8255 None 0 Mouse Functional pEC50 = 8.4 8.4 1 2
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 8255 None 0 Mouse Functional pEC50 = 8.4 8.4 1 2
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 218143 None 0 Human Functional pEC50 = 8.4 8.4 -64 3
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 8501 None 0 Human Functional pEC50 = 7.5 7.5 -4 2
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 8501 None 0 Human Functional pEC50 = 7.5 7.5 -4 2
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 8364 None 0 Mouse Functional pEC50 = 7.5 7.5 2 2
Agonistic activity 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 8364 None 0 Mouse Functional pEC50 = 7.5 7.5 2 2
Agonistic activity 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 203998 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 203998 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 8182 None 0 Human Functional pEC50 = 6.5 6.5 -3 2
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 8182 None 0 Human Functional pEC50 = 6.5 6.5 -3 2
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 8104 None 0 Mouse Functional pEC50 = 6.5 6.5 3 2
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 8104 None 0 Mouse Functional pEC50 = 6.5 6.5 3 2
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 7468 None 0 Mouse Functional pEC50 = 7.5 7.5 26 2
Agonistic activity 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 7468 None 0 Mouse Functional pEC50 = 7.5 7.5 26 2
Agonistic activity 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 106840 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 106840 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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
172465965 196684 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 478 8 2 9 4.6 C=CC(C)(C)C(OC(=O)c1ccc(C=O)cc1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5429857 196684 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 478 8 2 9 4.6 C=CC(C)(C)C(OC(=O)c1ccc(C=O)cc1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
46887980 9091 None 0 Human Functional pEC50 = 5.5 5.5 -24 2
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 9091 None 0 Human Functional pEC50 = 5.5 5.5 -24 2
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 106844 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 106844 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 60859 None 0 Mouse Functional pEC50 = 6.5 6.5 3 2
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 60859 None 0 Mouse Functional pEC50 = 6.5 6.5 3 2
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 60860 None 0 Mouse Functional pEC50 = 6.5 6.5 3 2
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 60860 None 0 Mouse Functional pEC50 = 6.5 6.5 3 2
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 82699 None 0 Human Functional pEC50 = 6.5 6.5 2 2
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 82699 None 0 Human Functional pEC50 = 6.5 6.5 2 2
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 60855 None 0 Mouse Functional pEC50 = 7.5 7.5 11 2
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 60855 None 0 Mouse Functional pEC50 = 7.5 7.5 11 2
Agonist activity at mouse BRS3 by functional assayAgonist activity at mouse BRS3 by functional assay
ChEMBL 408 4 3 5 3.5 CC(C)(C)NC(=O)NS(=O)(=O)c1cnccc1N[C@H]1C[C@H]2CC[C@]1(C)C2(C)C 10.1016/j.bmcl.2011.02.011
56840673 1141 None 0 Mouse Functional pEC50 = 7.5 7.5 -2 2
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
8503 1141 None 0 Mouse Functional pEC50 = 7.5 7.5 -2 2
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
CHEMBL2164575 1141 None 0 Mouse Functional pEC50 = 7.5 7.5 -2 2
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 9134 None 0 Mouse Functional pEC50 = 7.5 7.5 19 2
Agonistic activity 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 9134 None 0 Mouse Functional pEC50 = 7.5 7.5 19 2
Agonistic activity 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 7445 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 7445 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 8873 None 0 Human Functional pEC50 = 6.5 6.5 -14 2
Agonistic activity 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 8873 None 0 Human Functional pEC50 = 6.5 6.5 -14 2
Agonistic activity 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
123695309 196718 None 0 Human Functional pEC50 = 5.5 5.5 -4 2
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 346 5 3 7 3.0 COc1cc(C(O)CC=C(C)C)c(OC)c2c1/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5430646 196718 None 0 Human Functional pEC50 = 5.5 5.5 -4 2
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 346 5 3 7 3.0 COc1cc(C(O)CC=C(C)C)c(OC)c2c1/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
46889146 7685 None 0 Mouse Functional pEC50 = 7.5 7.5 1 2
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 7685 None 0 Mouse Functional pEC50 = 7.5 7.5 1 2
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 60861 None 0 Mouse Functional pEC50 = 6.5 6.5 18 2
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 60861 None 0 Mouse Functional pEC50 = 6.5 6.5 18 2
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 8326 None 0 Mouse Functional pEC50 = 6.5 6.5 7 2
Agonistic activity 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 8326 None 0 Mouse Functional pEC50 = 6.5 6.5 7 2
Agonistic activity 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 9027 None 0 Rat Functional pEC50 = 6.5 6.5 16 2
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 9027 None 0 Rat Functional pEC50 = 6.5 6.5 16 2
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 8974 None 0 Rat Functional pEC50 = 6.5 6.5 19 2
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 8974 None 0 Rat Functional pEC50 = 6.5 6.5 19 2
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 9092 None 0 Human Functional pEC50 = 5.5 5.5 -28 2
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 9092 None 0 Human Functional pEC50 = 5.5 5.5 -28 2
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 60851 None 0 Human Functional pEC50 = 6.5 6.5 -4 2
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 60851 None 0 Human Functional pEC50 = 6.5 6.5 -4 2
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 188512 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 188512 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 8956 None 5 Rat Functional pEC50 = 5.5 5.5 2 2
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 8956 None 5 Rat Functional pEC50 = 5.5 5.5 2 2
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 8255 None 0 Human Functional pEC50 = 7.4 7.4 -1 2
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 8255 None 0 Human Functional pEC50 = 7.4 7.4 -1 2
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 82812 None 0 Mouse Functional pEC50 = 6.4 6.4 -7 2
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 82812 None 0 Mouse Functional pEC50 = 6.4 6.4 -7 2
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 8872 None 0 Human Functional pEC50 = 6.4 6.4 -25 2
Agonistic activity 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 8872 None 0 Human Functional pEC50 = 6.4 6.4 -25 2
Agonistic activity 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 82815 None 0 Mouse Functional pEC50 = 6.4 6.4 -11 2
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 82815 None 0 Mouse Functional pEC50 = 6.4 6.4 -11 2
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 82809 None 0 Human Functional pEC50 = 7.4 7.4 14 2
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 82809 None 0 Human Functional pEC50 = 7.4 7.4 14 2
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 60872 None 0 Human Functional pEC50 = 6.4 6.4 -3 2
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 60872 None 0 Human Functional pEC50 = 6.4 6.4 -3 2
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 8658 None 6 Rat Functional pEC50 = 6.4 6.4 12 2
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 8658 None 6 Rat Functional pEC50 = 6.4 6.4 12 2
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 194010 None 2 Human Functional pEC50 = 6.4 6.4 - 1
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 194010 None 2 Human Functional pEC50 = 6.4 6.4 - 1
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 5954 None 0 Mouse Functional pEC50 = 6.4 6.4 14 2
Agonistic activity 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 5954 None 0 Mouse Functional pEC50 = 6.4 6.4 14 2
Agonistic activity 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 14235 None 0 Rat Functional pEC50 = 5.4 5.4 2 2
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 14235 None 0 Rat Functional pEC50 = 5.4 5.4 2 2
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 60852 None 0 Mouse Functional pEC50 = 7.4 7.4 6 2
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 60852 None 0 Mouse Functional pEC50 = 7.4 7.4 6 2
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 7783 None 0 Human Functional pEC50 = 7.4 7.4 -6 2
Agonistic activity 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 7783 None 0 Human Functional pEC50 = 7.4 7.4 -6 2
Agonistic activity 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 209091 None 60 Human Functional pEC50 = 5.4 5.4 - 1
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 209091 None 60 Human Functional pEC50 = 5.4 5.4 - 1
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 7533 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 7533 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 106836 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 106836 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 8114 None 0 Mouse Functional pEC50 = 8.4 8.4 2 2
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 8114 None 0 Mouse Functional pEC50 = 8.4 8.4 2 2
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 7444 None 0 Mouse Functional pEC50 = 8.3 8.3 10 2
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 7444 None 0 Mouse Functional pEC50 = 8.3 8.3 10 2
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 8317 None 0 Mouse Functional pEC50 = 8.3 8.3 2 2
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 8317 None 0 Mouse Functional pEC50 = 8.3 8.3 2 2
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
132427046 195173 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 450 7 2 8 4.7 C=CC(C)(C)C(OC(=O)c1ccccc1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5398098 195173 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 450 7 2 8 4.7 C=CC(C)(C)C(OC(=O)c1ccccc1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
62707364 81906 None 0 Human Functional pEC50 = 7.4 7.4 8 2
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 81906 None 0 Human Functional pEC50 = 7.4 7.4 8 2
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 60869 None 0 Human Functional pEC50 = 5.4 5.4 -3 2
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 60869 None 0 Human Functional pEC50 = 5.4 5.4 -3 2
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 60870 None 0 Human Functional pEC50 = 5.4 5.4 -4 2
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 60870 None 0 Human Functional pEC50 = 5.4 5.4 -4 2
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 8793 None 0 Rat Functional pEC50 = 6.4 6.4 25 2
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 8793 None 0 Rat Functional pEC50 = 6.4 6.4 25 2
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 7442 None 0 Human Functional pEC50 = 7.4 7.4 -2 2
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 7442 None 0 Human Functional pEC50 = 7.4 7.4 -2 2
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 9076 None 0 Human Functional pEC50 = 7.4 7.4 -5 2
Agonistic activity 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 9076 None 0 Human Functional pEC50 = 7.4 7.4 -5 2
Agonistic activity 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 60870 None 0 Mouse Functional pEC50 = 6.4 6.4 4 2
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 60870 None 0 Mouse Functional pEC50 = 6.4 6.4 4 2
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 6175 None 0 Human Functional pEC50 = 5.4 5.4 -52 2
Agonistic activity 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 6175 None 0 Human Functional pEC50 = 5.4 5.4 -52 2
Agonistic activity 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 9065 None 0 Rat Functional pEC50 = 6.4 6.4 1 2
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 9065 None 0 Rat Functional pEC50 = 6.4 6.4 1 2
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 8675 None 0 Human Functional pEC50 = 5.4 5.4 -6 2
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 8675 None 0 Human Functional pEC50 = 5.4 5.4 -6 2
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 81902 None 0 Human Functional pEC50 = 7.4 7.4 6 2
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 81902 None 0 Human Functional pEC50 = 7.4 7.4 6 2
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 7661 None 0 Human Functional pEC50 = 7.4 7.4 -2 2
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 7661 None 0 Human Functional pEC50 = 7.4 7.4 -2 2
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 7671 None 0 Human Functional pEC50 = 7.4 7.4 -2 2
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 7671 None 0 Human Functional pEC50 = 7.4 7.4 -2 2
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 8174 None 0 Human Functional pEC50 = 6.4 6.4 -3 2
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 8174 None 0 Human Functional pEC50 = 6.4 6.4 -3 2
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 8113 None 0 Human Functional pEC50 = 6.4 6.4 -4 2
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 8113 None 0 Human Functional pEC50 = 6.4 6.4 -4 2
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 82693 None 0 Human Functional pEC50 = 7.4 7.4 6 2
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 82693 None 0 Human Functional pEC50 = 7.4 7.4 6 2
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 60857 None 0 Mouse Functional pEC50 = 5.4 5.4 1 2
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 60857 None 0 Mouse Functional pEC50 = 5.4 5.4 1 2
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 7664 None 0 Human Functional pEC50 = 5.4 5.4 -56 2
Agonistic activity 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 7664 None 0 Human Functional pEC50 = 5.4 5.4 -56 2
Agonistic activity 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 7820 None 0 Human Functional pEC50 = 6.4 6.4 -3 2
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 7820 None 0 Human Functional pEC50 = 6.4 6.4 -3 2
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 9064 None 0 Rat Functional pEC50 = 6.4 6.4 2 2
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 9064 None 0 Rat Functional pEC50 = 6.4 6.4 2 2
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 7845 None 0 Human Functional pEC50 = 5.4 5.4 -1 2
Agonistic activity 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 7845 None 0 Human Functional pEC50 = 5.4 5.4 -1 2
Agonistic activity 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 6315 None 0 Human Functional pEC50 = 5.4 5.4 2 2
Agonistic activity 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 6315 None 0 Human Functional pEC50 = 5.4 5.4 2 2
Agonistic activity 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 6444 None 0 Human Functional pEC50 = 7.4 7.4 -1 2
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 6444 None 0 Human Functional pEC50 = 7.4 7.4 -1 2
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 60845 None 0 Human Functional pEC50 = 6.4 6.4 -5 2
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 60845 None 0 Human Functional pEC50 = 6.4 6.4 -5 2
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 60853 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
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 60853 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
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 60855 None 0 Human Functional pEC50 = 6.4 6.4 -11 2
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 60855 None 0 Human Functional pEC50 = 6.4 6.4 -11 2
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 214990 None 22 Human Functional pEC50 = 5.4 5.4 -6309 4
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 8658 None 6 Human Functional pEC50 = 5.3 5.3 -12 2
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 8658 None 6 Human Functional pEC50 = 5.3 5.3 -12 2
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 106839 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 106839 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 5924 None 0 Human Functional pEC50 = 5.3 5.3 -2 2
Agonistic activity 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 5924 None 0 Human Functional pEC50 = 5.3 5.3 -2 2
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 390 9 2 2 6.1 CCCCc1cnc(C(Cc2ccc(-c3ccccc3C(=O)O)cc2)C(C)C)[nH]1 10.1016/j.bmcl.2010.01.154
25025860 569 None 23 Human Functional pEC50 = 7.3 7.3 -14 5
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
6188 569 None 23 Human Functional pEC50 = 7.3 7.3 -14 5
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1091720 569 None 23 Human Functional pEC50 = 7.3 7.3 -14 5
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
25025860 569 None 23 Human Functional pEC50 = 7.3 7.3 -14 5
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1021/ml100196d
6188 569 None 23 Human Functional pEC50 = 7.3 7.3 -14 5
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assayAgonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1021/ml100196d
CHEMBL1091720 569 None 23 Human Functional pEC50 = 7.3 7.3 -14 5
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 8674 None 0 Rat Functional pEC50 = 6.3 6.3 21 2
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 8674 None 0 Rat Functional pEC50 = 6.3 6.3 21 2
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 8746 None 0 Human Functional pEC50 = 5.3 5.3 -47 2
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 8746 None 0 Human Functional pEC50 = 5.3 5.3 -47 2
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 8955 None 0 Rat Functional pEC50 = 6.3 6.3 20 2
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 8955 None 0 Rat Functional pEC50 = 6.3 6.3 20 2
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 82690 None 0 Human Functional pEC50 = 7.3 7.3 9 2
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 82690 None 0 Human Functional pEC50 = 7.3 7.3 9 2
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 60848 None 0 Mouse Functional pEC50 = 7.3 7.3 3 2
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 60848 None 0 Mouse Functional pEC50 = 7.3 7.3 3 2
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 60862 None 0 Mouse Functional pEC50 = 5.3 5.3 1 2
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 60862 None 0 Mouse Functional pEC50 = 5.3 5.3 1 2
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 6352 None 0 Human Functional pEC50 = 5.3 5.3 -5 2
Agonistic activity 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 6352 None 0 Human Functional pEC50 = 5.3 5.3 -5 2
Agonistic activity 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 9077 None 0 Mouse Functional pEC50 = 8.2 8.2 15 2
Agonistic activity 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 9077 None 0 Mouse Functional pEC50 = 8.2 8.2 15 2
Agonistic activity 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 7442 None 0 Mouse Functional pEC50 = 8.2 8.2 2 2
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 7442 None 0 Mouse Functional pEC50 = 8.2 8.2 2 2
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 82808 None 0 Human Functional pEC50 = 7.3 7.3 3 2
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 82808 None 0 Human Functional pEC50 = 7.3 7.3 3 2
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 82813 None 0 Human Functional pEC50 = 7.3 7.3 18 2
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 82813 None 0 Human Functional pEC50 = 7.3 7.3 18 2
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 82808 None 0 Mouse Functional pEC50 = 7.3 7.3 -3 2
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 82808 None 0 Mouse Functional pEC50 = 7.3 7.3 -3 2
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 7335 None 0 Mouse Functional pEC50 = 7.3 7.3 31 2
Agonistic activity 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 7335 None 0 Mouse Functional pEC50 = 7.3 7.3 31 2
Agonistic activity 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 60850 None 0 Human Functional pEC50 = 7.3 7.3 -4 2
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 60850 None 0 Human Functional pEC50 = 7.3 7.3 -4 2
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 60872 None 0 Mouse Functional pEC50 = 7.3 7.3 3 2
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 60872 None 0 Mouse Functional pEC50 = 7.3 7.3 3 2
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 178933 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 178933 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 6176 None 0 Mouse Functional pEC50 = 6.3 6.3 10 2
Agonistic activity 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 6176 None 0 Mouse Functional pEC50 = 6.3 6.3 10 2
Agonistic activity 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 81819 None 0 Human Functional pEC50 = 7.3 7.3 12 2
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 81819 None 0 Human Functional pEC50 = 7.3 7.3 12 2
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 81908 None 0 Human Functional pEC50 = 7.3 7.3 11 2
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 81908 None 0 Human Functional pEC50 = 7.3 7.3 11 2
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
132427031 195960 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 430 8 2 8 4.5 C=CC(C)(C)C(OC(=O)CC(C)C)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5414271 195960 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 430 8 2 8 4.5 C=CC(C)(C)C(OC(=O)CC(C)C)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
141325733 196323 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 416 9 2 7 5.1 COc1cc(C(CC=C(C)C)OCCC(C)C)c(OC)c2c1/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5421389 196323 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 416 9 2 7 5.1 COc1cc(C(CC=C(C)C)OCCC(C)C)c(OC)c2c1/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
46885313 8104 None 0 Human Functional pEC50 = 5.3 5.3 -3 2
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 8104 None 0 Human Functional pEC50 = 5.3 5.3 -3 2
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 5894 None 0 Mouse Functional pEC50 = 6.3 6.3 5 2
Agonistic activity 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 5894 None 0 Mouse Functional pEC50 = 6.3 6.3 5 2
Agonistic activity 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 6176 None 0 Human Functional pEC50 = 5.3 5.3 -10 2
Agonistic activity 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 6176 None 0 Human Functional pEC50 = 5.3 5.3 -10 2
Agonistic activity 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 7819 None 0 Human Functional pEC50 = 6.3 6.3 -3 2
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 7819 None 0 Human Functional pEC50 = 6.3 6.3 -3 2
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 7687 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 7687 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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
132427043 195579 None 3 Mouse Functional pEC50 = 7.3 7.3 -1 3
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5406411 195579 None 3 Mouse Functional pEC50 = 7.3 7.3 -1 3
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
59618778 82692 None 0 Human Functional pEC50 = 6.3 6.3 2 2
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 82692 None 0 Human Functional pEC50 = 6.3 6.3 2 2
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 9098 None 0 Human Functional pEC50 = 6.3 6.3 -2 2
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 9098 None 0 Human Functional pEC50 = 6.3 6.3 -2 2
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 6860 None 0 Human Functional pEC50 = 5.3 5.3 -8 2
Agonistic activity 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 6860 None 0 Human Functional pEC50 = 5.3 5.3 -8 2
Agonistic activity 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 60847 None 0 Human Functional pEC50 = 7.3 7.3 -3 2
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 60847 None 0 Human Functional pEC50 = 7.3 7.3 -3 2
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 9027 None 0 Human Functional pEC50 = 5.3 5.3 -16 2
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 9027 None 0 Human Functional pEC50 = 5.3 5.3 -16 2
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 5954 None 0 Human Functional pEC50 = 5.3 5.3 -14 2
Agonistic activity 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 5954 None 0 Human Functional pEC50 = 5.3 5.3 -14 2
Agonistic activity 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 81907 None 0 Human Functional pEC50 = 7.3 7.3 14 2
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 81907 None 0 Human Functional pEC50 = 7.3 7.3 14 2
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 7515 None 0 Human Functional pEC50 = 7.3 7.3 -1 2
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 7515 None 0 Human Functional pEC50 = 7.3 7.3 -1 2
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 9078 None 0 Human Functional pEC50 = 7.3 7.3 -1 2
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 9078 None 0 Human Functional pEC50 = 7.3 7.3 -1 2
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 82692 None 0 Mouse Functional pEC50 = 6.3 6.3 -2 2
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 82692 None 0 Mouse Functional pEC50 = 6.3 6.3 -2 2
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 7825 None 0 Mouse Functional pEC50 = 7.2 7.2 3 2
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 7825 None 0 Mouse Functional pEC50 = 7.2 7.2 3 2
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 81906 None 0 Mouse Functional pEC50 = 7.2 7.2 -8 2
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 81906 None 0 Mouse Functional pEC50 = 7.2 7.2 -8 2
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 106843 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 106843 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 7824 None 0 Human Functional pEC50 = 6.2 6.2 -6 2
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 7824 None 0 Human Functional pEC50 = 6.2 6.2 -6 2
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 179110 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 179110 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 81902 None 0 Mouse Functional pEC50 = 7.2 7.2 -6 2
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 81902 None 0 Mouse Functional pEC50 = 7.2 7.2 -6 2
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 6995 None 0 Human Functional pEC50 = 6.2 6.2 -83 2
Agonistic activity 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 6995 None 0 Human Functional pEC50 = 6.2 6.2 -83 2
Agonistic activity 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 6177 None 0 Human Functional pEC50 = 5.2 5.2 -8 2
Agonistic activity 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 6177 None 0 Human Functional pEC50 = 5.2 5.2 -8 2
Agonistic activity 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
172457037 196351 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 469 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1cncc(F)c1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5422040 196351 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 469 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1cncc(F)c1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
54584421 60863 None 0 Mouse Functional pEC50 = 6.2 6.2 13 2
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 60863 None 0 Mouse Functional pEC50 = 6.2 6.2 13 2
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 199378 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 199378 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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
132427043 195579 None 3 Rat Functional pEC50 = 8.2 8.2 1 3
Agonist activity at rat BB3 transiently expressed in human HEK293T cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at rat BB3 transiently expressed in human HEK293T cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5406411 195579 None 3 Rat Functional pEC50 = 8.2 8.2 1 3
Agonist activity at rat BB3 transiently expressed in human HEK293T cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at rat BB3 transiently expressed in human HEK293T cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
46881643 7783 None 0 Mouse Functional pEC50 = 8.2 8.2 6 2
Agonistic activity 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 7783 None 0 Mouse Functional pEC50 = 8.2 8.2 6 2
Agonistic activity 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 7784 None 0 Mouse Functional pEC50 = 8.2 8.2 16 2
Agonistic activity 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 7784 None 0 Mouse Functional pEC50 = 8.2 8.2 16 2
Agonistic activity 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 6444 None 0 Mouse Functional pEC50 = 8.2 8.2 1 2
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 6444 None 0 Mouse Functional pEC50 = 8.2 8.2 1 2
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 82695 None 0 Human Functional pEC50 = 7.2 7.2 4 2
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 82695 None 0 Human Functional pEC50 = 7.2 7.2 4 2
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 8677 None 0 Rat Functional pEC50 = 5.2 5.2 1 2
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 8677 None 0 Rat Functional pEC50 = 5.2 5.2 1 2
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
123695309 196718 None 0 Mouse Functional pEC50 = 6.2 6.2 4 2
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 346 5 3 7 3.0 COc1cc(C(O)CC=C(C)C)c(OC)c2c1/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5430646 196718 None 0 Mouse Functional pEC50 = 6.2 6.2 4 2
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 346 5 3 7 3.0 COc1cc(C(O)CC=C(C)C)c(OC)c2c1/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
46885311 8317 None 0 Human Functional pEC50 = 7.2 7.2 -2 2
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 8317 None 0 Human Functional pEC50 = 7.2 7.2 -2 2
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 8422 None 0 Human Functional pEC50 = 7.2 7.2 -2 2
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 8422 None 0 Human Functional pEC50 = 7.2 7.2 -2 2
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 81903 None 0 Human Functional pEC50 = 7.2 7.2 14 2
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 81903 None 0 Human Functional pEC50 = 7.2 7.2 14 2
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 82814 None 0 Human Functional pEC50 = 7.2 7.2 10 2
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 82814 None 0 Human Functional pEC50 = 7.2 7.2 10 2
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 9063 None 0 Rat Functional pEC50 = 7.2 7.2 24 2
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 9063 None 0 Rat Functional pEC50 = 7.2 7.2 24 2
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 74216 None 0 Human Functional pEC50 = 7.2 7.2 7 2
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 74216 None 0 Human Functional pEC50 = 7.2 7.2 7 2
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 60864 None 0 Human Functional pEC50 = 6.2 6.2 -3 2
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 60864 None 0 Human Functional pEC50 = 6.2 6.2 -3 2
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 60861 None 0 Human Functional pEC50 = 5.2 5.2 -18 2
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 60861 None 0 Human Functional pEC50 = 5.2 5.2 -18 2
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 106838 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 106838 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 216272 None 15 Human Functional pEC50 = 5.2 5.2 -190 3
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 7825 None 0 Human Functional pEC50 = 6.2 6.2 -3 2
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 7825 None 0 Human Functional pEC50 = 6.2 6.2 -3 2
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 9134 None 0 Human Functional pEC50 = 6.2 6.2 -19 2
Agonistic activity 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 9134 None 0 Human Functional pEC50 = 6.2 6.2 -19 2
Agonistic activity 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 6860 None 0 Mouse Functional pEC50 = 6.2 6.2 8 2
Agonistic activity 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 6860 None 0 Mouse Functional pEC50 = 6.2 6.2 8 2
Agonistic activity 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 60866 None 0 Mouse Functional pEC50 = 5.2 5.2 1 2
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 60866 None 0 Mouse Functional pEC50 = 5.2 5.2 1 2
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 8382 None 0 Human Functional pEC50 = 7.2 7.2 1 2
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 8382 None 0 Human Functional pEC50 = 7.2 7.2 1 2
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 8382 None 0 Human Functional pEC50 = 7.2 7.2 1 2
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 8382 None 0 Human Functional pEC50 = 7.2 7.2 1 2
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
132427043 195579 None 3 Mouse Functional pEC50 = 7.2 7.2 -1 3
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5406411 195579 None 3 Mouse Functional pEC50 = 7.2 7.2 -1 3
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
25026445 57962 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 57962 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 74216 None 0 Mouse Functional pEC50 = 7.2 7.2 -7 2
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 74216 None 0 Mouse Functional pEC50 = 7.2 7.2 -7 2
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 8974 None 0 Human Functional pEC50 = 5.2 5.2 -19 2
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 8974 None 0 Human Functional pEC50 = 5.2 5.2 -19 2
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 8675 None 0 Rat Functional pEC50 = 6.2 6.2 6 2
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 8675 None 0 Rat Functional pEC50 = 6.2 6.2 6 2
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 60858 None 0 Human Functional pEC50 = 5.2 5.2 -3 2
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 60858 None 0 Human Functional pEC50 = 5.2 5.2 -3 2
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 81818 None 0 Human Functional pEC50 = 7.2 7.2 11 2
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 81818 None 0 Human Functional pEC50 = 7.2 7.2 11 2
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 82694 None 0 Human Functional pEC50 = 7.2 7.2 10 2
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 82694 None 0 Human Functional pEC50 = 7.2 7.2 10 2
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 60856 None 0 Mouse Functional pEC50 = 5.2 5.2 1 2
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 60856 None 0 Mouse Functional pEC50 = 5.2 5.2 1 2
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 6995 None 0 Mouse Functional pEC50 = 8.2 8.2 83 2
Agonistic activity 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 6995 None 0 Mouse Functional pEC50 = 8.2 8.2 83 2
Agonistic activity 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 9076 None 0 Mouse Functional pEC50 = 8.1 8.1 5 2
Agonistic activity 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 9076 None 0 Mouse Functional pEC50 = 8.1 8.1 5 2
Agonistic activity 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 106837 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 106837 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
ChEMBL 540 11 4 5 3.0 C[C@H](NC(=O)Cc1ccc2c(c1)OCO2)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 10.1021/jm0210921
25025654 570 None 12 Mouse Functional pEC50 = 8.1 8.1 1 3
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 10.1016/j.bmcl.2010.01.154
6189 570 None 12 Mouse Functional pEC50 = 8.1 8.1 1 3
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 10.1016/j.bmcl.2010.01.154
8506 570 None 12 Mouse Functional pEC50 = 8.1 8.1 1 3
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 10.1016/j.bmcl.2010.01.154
CHEMBL1084942 570 None 12 Mouse Functional pEC50 = 8.1 8.1 1 3
Agonistic activity 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 7678 None 0 Mouse Functional pEC50 = 8.1 8.1 19 2
Agonistic activity 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 7678 None 0 Mouse Functional pEC50 = 8.1 8.1 19 2
Agonistic activity 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 100954 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 100954 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 60865 None 0 Mouse Functional pEC50 = 5.2 5.2 1 2
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 60865 None 0 Mouse Functional pEC50 = 5.2 5.2 1 2
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 9065 None 0 Human Functional pEC50 = 6.2 6.2 -1 2
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 9065 None 0 Human Functional pEC50 = 6.2 6.2 -1 2
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 106841 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 106841 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 6994 None 0 Mouse Functional pEC50 = 7.1 7.1 13 2
Agonistic activity 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 6994 None 0 Mouse Functional pEC50 = 7.1 7.1 13 2
Agonistic activity 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 60849 None 0 Human Functional pEC50 = 6.1 6.1 -6 2
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 60849 None 0 Human Functional pEC50 = 6.1 6.1 -6 2
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 6177 None 0 Mouse Functional pEC50 = 6.1 6.1 8 2
Agonistic activity 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 6177 None 0 Mouse Functional pEC50 = 6.1 6.1 8 2
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 407 7 2 3 5.0 N#Cc1ccc(Cc2cnc(CCc3ccc(-c4ccccc4C(=O)O)cc3)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46200989 2562 None 14 Human Functional pEC50 = 7.1 7.1 9 2
Agonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2012.03.029
8502 2562 None 14 Human Functional pEC50 = 7.1 7.1 9 2
Agonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assayAgonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2012.03.029
CHEMBL2023109 2562 None 14 Human Functional pEC50 = 7.1 7.1 9 2
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 7664 None 0 Mouse Functional pEC50 = 7.1 7.1 56 2
Agonistic activity 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 7664 None 0 Mouse Functional pEC50 = 7.1 7.1 56 2
Agonistic activity 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 60856 None 0 Human Functional pEC50 = 5.1 5.1 -1 2
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 60856 None 0 Human Functional pEC50 = 5.1 5.1 -1 2
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 8885 None 0 Rat Functional pEC50 = 6.1 6.1 13 2
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 8885 None 0 Rat Functional pEC50 = 6.1 6.1 13 2
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 81905 None 0 Mouse Functional pEC50 = 7.1 7.1 -1 2
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 81905 None 0 Mouse Functional pEC50 = 7.1 7.1 -1 2
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 74217 None 0 Mouse Functional pEC50 = 7.1 7.1 -10 2
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 74217 None 0 Mouse Functional pEC50 = 7.1 7.1 -10 2
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 8364 None 0 Human Functional pEC50 = 7.1 7.1 -2 2
Agonistic activity 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 8364 None 0 Human Functional pEC50 = 7.1 7.1 -2 2
Agonistic activity 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 8905 None 0 Rat Functional pEC50 = 5.1 5.1 1 2
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 8905 None 0 Rat Functional pEC50 = 5.1 5.1 1 2
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 81905 None 0 Human Functional pEC50 = 7.1 7.1 1 2
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 81905 None 0 Human Functional pEC50 = 7.1 7.1 1 2
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 82817 None 0 Human Functional pEC50 = 7.1 7.1 6 2
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 82817 None 0 Human Functional pEC50 = 7.1 7.1 6 2
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
135398415 195415 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 432 11 3 8 4.1 C=CC(C)(C)C(OCCCCCO)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5403261 195415 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 432 11 3 8 4.1 C=CC(C)(C)C(OCCCCCO)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
123695309 196718 None 0 Mouse Functional pEC50 = 6.1 6.1 4 2
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assay
ChEMBL 346 5 3 7 3.0 COc1cc(C(O)CC=C(C)C)c(OC)c2c1/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5430646 196718 None 0 Mouse Functional pEC50 = 6.1 6.1 4 2
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assay
ChEMBL 346 5 3 7 3.0 COc1cc(C(O)CC=C(C)C)c(OC)c2c1/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
46889176 7444 None 0 Human Functional pEC50 = 7.1 7.1 -10 2
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 7444 None 0 Human Functional pEC50 = 7.1 7.1 -10 2
Agonist activity at human BRS3Agonist activity at human BRS3
ChEMBL 444 10 3 5 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(N)n[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
25025860 569 None 23 Mouse Functional pEC50 = 7.1 7.1 -4 5
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
6188 569 None 23 Mouse Functional pEC50 = 7.1 7.1 -4 5
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1091720 569 None 23 Mouse Functional pEC50 = 7.1 7.1 -4 5
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 82691 None 0 Mouse Functional pEC50 = 7.1 7.1 -2 2
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 82691 None 0 Mouse Functional pEC50 = 7.1 7.1 -2 2
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 82695 None 0 Mouse Functional pEC50 = 7.1 7.1 -4 2
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 82695 None 0 Mouse Functional pEC50 = 7.1 7.1 -4 2
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 6175 None 0 Mouse Functional pEC50 = 7.1 7.1 52 2
Agonistic activity 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 6175 None 0 Mouse Functional pEC50 = 7.1 7.1 52 2
Agonistic activity 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 106834 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 106834 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 201147 None 0 Human Functional pEC50 = 5.1 5.1 - 1
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 201147 None 0 Human Functional pEC50 = 5.1 5.1 - 1
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 9031 None 0 Rat Functional pEC50 = 5.1 5.1 1 2
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 9031 None 0 Rat Functional pEC50 = 5.1 5.1 1 2
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 6993 None 0 Mouse Functional pEC50 = 8.1 8.1 10 2
Agonistic activity 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 6993 None 0 Mouse Functional pEC50 = 8.1 8.1 10 2
Agonistic activity 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 82693 None 0 Mouse Functional pEC50 = 7.1 7.1 -6 2
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 82693 None 0 Mouse Functional pEC50 = 7.1 7.1 -6 2
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 60847 None 0 Human Functional pEC50 = 7.1 7.1 -3 2
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 60847 None 0 Human Functional pEC50 = 7.1 7.1 -3 2
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
132427037 196736 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 464 7 2 8 5.0 C=CC(C)(C)C(OC(=O)c1ccc(C)cc1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5431181 196736 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 464 7 2 8 5.0 C=CC(C)(C)C(OC(=O)c1ccc(C)cc1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
54580465 60857 None 0 Human Functional pEC50 = 5.1 5.1 -1 2
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 60857 None 0 Human Functional pEC50 = 5.1 5.1 -1 2
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 6462 None 0 Human Functional pEC50 = 6.1 6.1 -40 2
Agonistic activity 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 6462 None 0 Human Functional pEC50 = 6.1 6.1 -40 2
Agonistic activity 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 74217 None 0 Human Functional pEC50 = 7.1 7.1 10 2
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 74217 None 0 Human Functional pEC50 = 7.1 7.1 10 2
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 60863 None 0 Human Functional pEC50 = 5.1 5.1 -13 2
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 60863 None 0 Human Functional pEC50 = 5.1 5.1 -13 2
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
118539074 196794 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 430 8 2 8 4.6 COc1cc(C(CC=C(C)C)OC(=O)CC(C)C)c(OC)c2c1/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5432370 196794 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay
ChEMBL 430 8 2 8 4.6 COc1cc(C(CC=C(C)C)OC(=O)CC(C)C)c(OC)c2c1/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
46881508 7468 None 0 Human Functional pEC50 = 6.1 6.1 -26 2
Agonistic activity 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 7468 None 0 Human Functional pEC50 = 6.1 6.1 -26 2
Agonistic activity 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 81819 None 0 Mouse Functional pEC50 = 7.1 7.1 -12 2
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 81819 None 0 Mouse Functional pEC50 = 7.1 7.1 -12 2
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 60862 None 0 Human Functional pEC50 = 5.1 5.1 -1 2
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 60862 None 0 Human Functional pEC50 = 5.1 5.1 -1 2
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 60866 None 0 Human Functional pEC50 = 5.1 5.1 -1 2
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 60866 None 0 Human Functional pEC50 = 5.1 5.1 -1 2
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 82690 None 0 Mouse Functional pEC50 = 7.1 7.1 -9 2
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 82690 None 0 Mouse Functional pEC50 = 7.1 7.1 -9 2
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 8588 None 0 Rat Functional pEC50 = 6.1 6.1 11 2
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 8588 None 0 Rat Functional pEC50 = 6.1 6.1 11 2
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 60845 None 0 Mouse Functional pEC50 = 7.1 7.1 5 2
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 60845 None 0 Mouse Functional pEC50 = 7.1 7.1 5 2
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 6993 None 0 Human Functional pEC50 = 7.1 7.1 -10 2
Agonistic activity 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 6993 None 0 Human Functional pEC50 = 7.1 7.1 -10 2
Agonistic activity 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 6352 None 0 Mouse Functional pEC50 = 6.1 6.1 5 2
Agonistic activity 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 6352 None 0 Mouse Functional pEC50 = 6.1 6.1 5 2
Agonistic activity 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 82818 None 0 Human Functional pEC50 = 7.1 7.1 15 2
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 82818 None 0 Human Functional pEC50 = 7.1 7.1 15 2
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 9077 None 0 Human Functional pEC50 = 7.1 7.1 -15 2
Agonistic activity 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 9077 None 0 Human Functional pEC50 = 7.1 7.1 -15 2
Agonistic activity 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 7824 None 0 Human Functional pEC50 = 7.1 7.1 -6 2
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 7824 None 0 Human Functional pEC50 = 7.1 7.1 -6 2
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 8174 None 0 Human Functional pEC50 = 7.1 7.1 -3 2
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 8174 None 0 Human Functional pEC50 = 7.1 7.1 -3 2
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 81908 None 0 Mouse Functional pEC50 = 7.1 7.1 -11 2
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 81908 None 0 Mouse Functional pEC50 = 7.1 7.1 -11 2
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 8583 None 0 Rat Functional pEC50 = 5.1 5.1 1 2
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 8583 None 0 Rat Functional pEC50 = 5.1 5.1 1 2
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 7823 None 0 Mouse Functional pEC50 = 8.1 8.1 2 2
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 7823 None 0 Mouse Functional pEC50 = 8.1 8.1 2 2
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 6463 None 0 Mouse Functional pEC50 = 8.0 8.0 13 2
Agonistic activity 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 6463 None 0 Mouse Functional pEC50 = 8.0 8.0 13 2
Agonistic activity 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 100780 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 100780 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 7616 None 0 Mouse Functional pEC50 = 8.0 8.0 18 2
Agonistic activity 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 7616 None 0 Mouse Functional pEC50 = 8.0 8.0 18 2
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 400 7 2 2 5.3 O=C(O)c1ccccc1-c1ccc(CCc2ncc(Cc3ccccc3F)[nH]2)cc1 10.1016/j.bmcl.2010.01.154
46845425 1032 None 2 Mouse Functional pEC50 = 8.0 8.0 -1 2
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
8504 1032 None 2 Mouse Functional pEC50 = 8.0 8.0 -1 2
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1089721 1032 None 2 Mouse Functional pEC50 = 8.0 8.0 -1 2
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assayAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
46845425 1032 None 2 Mouse Functional pEC50 = 8.0 8.0 -1 2
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.03.028
8504 1032 None 2 Mouse Functional pEC50 = 8.0 8.0 -1 2
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.03.028
CHEMBL1089721 1032 None 2 Mouse Functional pEC50 = 8.0 8.0 -1 2
Agonist activity at mouse BRS3Agonist activity at mouse BRS3
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.03.028
46845425 1032 None 2 Mouse Functional pEC50 = 8.0 8.0 -1 2
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.01.154
8504 1032 None 2 Mouse Functional pEC50 = 8.0 8.0 -1 2
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.01.154
CHEMBL1089721 1032 None 2 Mouse Functional pEC50 = 8.0 8.0 -1 2
Agonistic activity 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 8104 None 0 Mouse Functional pEC50 = 7.1 7.1 3 2
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 8104 None 0 Mouse Functional pEC50 = 7.1 7.1 3 2
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 60854 None 0 Mouse Functional pEC50 = 7.1 7.1 12 2
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 60854 None 0 Mouse Functional pEC50 = 7.1 7.1 12 2
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 8379 None 0 Mouse Functional pEC50 = 7.0 7.0 3 2
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 8379 None 0 Mouse Functional pEC50 = 7.0 7.0 3 2
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 7825 None 0 Human Functional pEC50 = 7.0 7.0 -3 2
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 7825 None 0 Human Functional pEC50 = 7.0 7.0 -3 2
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 81907 None 0 Mouse Functional pEC50 = 7.0 7.0 -14 2
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 81907 None 0 Mouse Functional pEC50 = 7.0 7.0 -14 2
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 5833 None 0 Mouse Functional pEC50 = 7.0 7.0 28 2
Agonistic activity 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 5833 None 0 Mouse Functional pEC50 = 7.0 7.0 28 2
Agonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assayAgonistic activity at mouse BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
ChEMBL 348 8 2 2 4.9 CCCCc1cnc(CCc2ccc(-c3ccccc3C(=O)O)cc2)[nH]1 10.1016/j.bmcl.2010.01.154
46845425 1032 None 2 Mouse Functional pEC50 = 7.0 7.0 -1 2
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
8504 1032 None 2 Mouse Functional pEC50 = 7.0 7.0 -1 2
Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1089721 1032 None 2 Mouse Functional pEC50 = 7.0 7.0 -1 2
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 60846 None 0 Human Functional pEC50 = 6.0 6.0 -8 2
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 60846 None 0 Human Functional pEC50 = 6.0 6.0 -8 2
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 8103 None 0 Human Functional pEC50 = 7.0 7.0 -10 2
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 8103 None 0 Human Functional pEC50 = 7.0 7.0 -10 2
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 8182 None 0 Human Functional pEC50 = 7.0 7.0 -3 2
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 8182 None 0 Human Functional pEC50 = 7.0 7.0 -3 2
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 8381 None 0 Human Functional pEC50 = 7.0 7.0 -2 2
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 8381 None 0 Human Functional pEC50 = 7.0 7.0 -2 2
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 81821 None 0 Mouse Functional pEC50 = 7.0 7.0 -11 2
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 81821 None 0 Mouse Functional pEC50 = 7.0 7.0 -11 2
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 8317 None 0 Mouse Functional pEC50 = 7.0 7.0 2 2
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 8317 None 0 Mouse Functional pEC50 = 7.0 7.0 2 2
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 82698 None 0 Mouse Functional pEC50 = 7.0 7.0 -2 2
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 82698 None 0 Mouse Functional pEC50 = 7.0 7.0 -2 2
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 8659 None 0 Rat Functional pEC50 = 6.0 6.0 10 2
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 8659 None 0 Rat Functional pEC50 = 6.0 6.0 10 2
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 8255 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
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 8255 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
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 8382 None 0 Human Functional pEC50 = 7.0 7.0 1 2
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 8382 None 0 Human Functional pEC50 = 7.0 7.0 1 2
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 351 7 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccc(F)cn3)cc2)n1 10.1016/j.bmcl.2010.02.076
56840673 1141 None 0 Human Functional pEC50 = 7.0 7.0 2 2
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
8503 1141 None 0 Human Functional pEC50 = 7.0 7.0 2 2
Agonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at human BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
CHEMBL2164575 1141 None 0 Human Functional pEC50 = 7.0 7.0 2 2
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 8103 None 0 Mouse Functional pEC50 = 7.0 7.0 10 2
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 8103 None 0 Mouse Functional pEC50 = 7.0 7.0 10 2
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 8114 None 0 Mouse Functional pEC50 = 7.0 7.0 2 2
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 8114 None 0 Mouse Functional pEC50 = 7.0 7.0 2 2
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 8113 None 0 Human Functional pEC50 = 7.0 7.0 -4 2
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 8113 None 0 Human Functional pEC50 = 7.0 7.0 -4 2
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 8114 None 0 Human Functional pEC50 = 7.0 7.0 -2 2
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 8114 None 0 Human Functional pEC50 = 7.0 7.0 -2 2
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 60846 None 0 Mouse Functional pEC50 = 7.0 7.0 8 2
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 60846 None 0 Mouse Functional pEC50 = 7.0 7.0 8 2
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 82809 None 0 Mouse Functional pEC50 = 7.0 7.0 -14 2
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 82809 None 0 Mouse Functional pEC50 = 7.0 7.0 -14 2
Agonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assayAgonist activity at mouse BRS3 expressed in HEK293 cells expressing aequorin measured for 30 secs by bioluminescence assay
ChEMBL 455 2 1 4 6.1 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(Cl)nc1N2 10.1021/ml200207w
25025860 569 None 23 Human Functional pEC50 = 7 7.0 -14 5
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
6188 569 None 23 Human Functional pEC50 = 7 7.0 -14 5
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesinAgonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1091720 569 None 23 Human Functional pEC50 = 7 7.0 -14 5
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 8174 None 0 Mouse Functional pEC50 = 7 7.0 3 2
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 8174 None 0 Mouse Functional pEC50 = 7 7.0 3 2
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 81822 None 0 Mouse Functional pEC50 = 7 7.0 -5 2
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 81822 None 0 Mouse Functional pEC50 = 7 7.0 -5 2
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 8746 None 0 Rat Functional pEC50 = 7 7.0 47 2
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 8746 None 0 Rat Functional pEC50 = 7 7.0 47 2
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
132427043 195579 None 3 Mouse Functional pIC50 = 8.8 8.8 -1 3
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5406411 195579 None 3 Mouse Functional pIC50 = 8.8 8.8 -1 3
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
49871766 2557 None 36 Human Functional pIC50 = 7.0 7.0 -6 5
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by 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 10.1021/acs.jmedchem.3c00323
6170 2557 None 36 Human Functional pIC50 = 7.0 7.0 -6 5
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by 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 10.1021/acs.jmedchem.3c00323
CHEMBL1672354 2557 None 36 Human Functional pIC50 = 7.0 7.0 -6 5
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by 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 10.1021/acs.jmedchem.3c00323
123695309 196718 None 0 Human Functional pIC50 = 7.9 7.9 -4 2
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assay
ChEMBL 346 5 3 7 3.0 COc1cc(C(O)CC=C(C)C)c(OC)c2c1/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5430646 196718 None 0 Human Functional pIC50 = 7.9 7.9 -4 2
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assay
ChEMBL 346 5 3 7 3.0 COc1cc(C(O)CC=C(C)C)c(OC)c2c1/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
49871766 2557 None 36 Mouse Functional pIC50 = 7.7 7.7 -3 5
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by 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 10.1021/acs.jmedchem.3c00323
6170 2557 None 36 Mouse Functional pIC50 = 7.7 7.7 -3 5
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by 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 10.1021/acs.jmedchem.3c00323
CHEMBL1672354 2557 None 36 Mouse Functional pIC50 = 7.7 7.7 -3 5
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by 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 10.1021/acs.jmedchem.3c00323
132427043 195579 None 3 Human Functional pIC50 = 8.6 8.6 -2 3
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5406411 195579 None 3 Human Functional pIC50 = 8.6 8.6 -2 3
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
49871766 2557 None 36 Human Functional pIC50 = 7.6 7.6 -6 5
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 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/acs.jmedchem.3c00323
6170 2557 None 36 Human Functional pIC50 = 7.6 7.6 -6 5
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 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/acs.jmedchem.3c00323
CHEMBL1672354 2557 None 36 Human Functional pIC50 = 7.6 7.6 -6 5
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 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/acs.jmedchem.3c00323
123695309 196718 None 0 Mouse Functional pIC50 = 8.4 8.4 4 2
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assay
ChEMBL 346 5 3 7 3.0 COc1cc(C(O)CC=C(C)C)c(OC)c2c1/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5430646 196718 None 0 Mouse Functional pIC50 = 8.4 8.4 4 2
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assay
ChEMBL 346 5 3 7 3.0 COc1cc(C(O)CC=C(C)C)c(OC)c2c1/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
132427043 195579 None 3 Mouse Functional pIC50 = 7.5 7.5 -1 3
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5406411 195579 None 3 Mouse Functional pIC50 = 7.5 7.5 -1 3
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
49871766 2557 None 36 Mouse Functional pIC50 = 8.4 8.4 -3 5
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 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/acs.jmedchem.3c00323
6170 2557 None 36 Mouse Functional pIC50 = 8.4 8.4 -3 5
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 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/acs.jmedchem.3c00323
CHEMBL1672354 2557 None 36 Mouse Functional pIC50 = 8.4 8.4 -3 5
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 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/acs.jmedchem.3c00323
123695309 196718 None 0 Mouse Functional pIC50 = 8.2 8.2 4 2
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assay
ChEMBL 346 5 3 7 3.0 COc1cc(C(O)CC=C(C)C)c(OC)c2c1/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5430646 196718 None 0 Mouse Functional pIC50 = 8.2 8.2 4 2
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assayAgonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assay
ChEMBL 346 5 3 7 3.0 COc1cc(C(O)CC=C(C)C)c(OC)c2c1/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
123695309 196718 None 0 Human Functional pIC50 = 7.2 7.2 -4 2
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assay
ChEMBL 346 5 3 7 3.0 COc1cc(C(O)CC=C(C)C)c(OC)c2c1/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5430646 196718 None 0 Human Functional pIC50 = 7.2 7.2 -4 2
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assay
ChEMBL 346 5 3 7 3.0 COc1cc(C(O)CC=C(C)C)c(OC)c2c1/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
132427043 195579 None 3 Human Functional pIC50 = 7.1 7.1 -2 3
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
CHEMBL5406411 195579 None 3 Human Functional pIC50 = 7.1 7.1 -2 3
Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assayAgonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assay
ChEMBL 440 7 2 9 4.3 C=CC(C)(C)C(OC(=O)c1ccco1)c1cc(OC)c2c(c1OC)/C(=N/O)C=C/C2=N\O 10.1021/acs.jmedchem.3c00323
11261 1155 None 0 Human Functional pEC50 = 6.6 6.6 -2 2
In a Ca aequorin assay.In a Ca aequorin assay.
Guide to Pharmacology 428 4 1 3 5.0 COc1ccc2c(c1)C(=O)N(Cc1ccccc1)C(c1c2cccc1)C(=O)NC(C)(C)C 28324017
154733031 1155 None 0 Human Functional pEC50 = 6.6 6.6 -2 2
In a Ca aequorin assay.In a Ca aequorin assay.
Guide to Pharmacology 428 4 1 3 5.0 COc1ccc2c(c1)C(=O)N(Cc1ccccc1)C(c1c2cccc1)C(=O)NC(C)(C)C 28324017
11261 1155 None 0 Rat Functional pEC50 = 7 7.0 2 2
In a Ca aequorin assay.In a Ca aequorin assay.
Guide to Pharmacology 428 4 1 3 5.0 COc1ccc2c(c1)C(=O)N(Cc1ccccc1)C(c1c2cccc1)C(=O)NC(C)(C)C 28324017
154733031 1155 None 0 Rat Functional pEC50 = 7 7.0 2 2
In a Ca aequorin assay.In a Ca aequorin assay.
Guide to Pharmacology 428 4 1 3 5.0 COc1ccc2c(c1)C(=O)N(Cc1ccccc1)C(c1c2cccc1)C(=O)NC(C)(C)C 28324017
10569 2837 None 0 Human Functional pEC50 = 5.7 5.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 31675498
145996512 2837 None 0 Human Functional pEC50 = 5.7 5.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 31675498
6192 3097 None 0 Rat Functional pEC50 = 7.0 7.0 -3 3
UnclassifiedUnclassified
Guide to Pharmacology 482 10 4 3 3.4 CC(C(=O)NC(C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NC(=O)c1ccccc1 19580790
73755184 3097 None 0 Rat Functional pEC50 = 7.0 7.0 -3 3
UnclassifiedUnclassified
Guide to Pharmacology 482 10 4 3 3.4 CC(C(=O)NC(C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NC(=O)c1ccccc1 19580790
6191 264 None 0 Human Functional pEC50 = 7.3 7.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15635635
6191 264 None 0 Human Functional pEC50 = 7.3 7.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18006692
6191 264 None 0 Human Functional pEC50 = 7.3 7.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20438784
6192 3097 None 0 Mouse Functional pEC50 = 7.5 7.5 3 3
UnclassifiedUnclassified
Guide to Pharmacology 482 10 4 3 3.4 CC(C(=O)NC(C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NC(=O)c1ccccc1 19580790
73755184 3097 None 0 Mouse Functional pEC50 = 7.5 7.5 3 3
UnclassifiedUnclassified
Guide to Pharmacology 482 10 4 3 3.4 CC(C(=O)NC(C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NC(=O)c1ccccc1 19580790
49871766 2557 None 36 Human Functional pEC50 = 7.6 7.6 -6 5
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 24900253
6170 2557 None 36 Human Functional pEC50 = 7.6 7.6 -6 5
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 24900253
CHEMBL1672354 2557 None 36 Human Functional pEC50 = 7.6 7.6 -6 5
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 24900253
8508 1150 None 0 Human Functional pEC50 = 7.8 7.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 479 8 2 5 4.5 CC(CCOc1cccc(c1)CC(=O)N1CCNc2c([C@H]1CC(=O)O)ccc(n2)C(F)(F)F)C 24412111
91827365 1150 None 0 Human Functional pEC50 = 7.8 7.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 479 8 2 5 4.5 CC(CCOc1cccc(c1)CC(=O)N1CCNc2c([C@H]1CC(=O)O)ccc(n2)C(F)(F)F)C 24412111
8507 1002 None 0 Human Functional pEC50 = 7.9 7.9 3 2
UnclassifiedUnclassified
Guide to Pharmacology 493 7 2 6 4.1 CC(CC(=O)Oc1cccc(c1)CC(=O)N1CCNc2c([C@H]1CC(=O)O)ccc(n2)C(F)(F)F)C 25497965
91827364 1002 None 0 Human Functional pEC50 = 7.9 7.9 3 2
UnclassifiedUnclassified
Guide to Pharmacology 493 7 2 6 4.1 CC(CC(=O)Oc1cccc(c1)CC(=O)N1CCNc2c([C@H]1CC(=O)O)ccc(n2)C(F)(F)F)C 25497965
CHEMBL3356404 1002 None 0 Human Functional pEC50 = 7.9 7.9 3 2
UnclassifiedUnclassified
Guide to Pharmacology 493 7 2 6 4.1 CC(CC(=O)Oc1cccc(c1)CC(=O)N1CCNc2c([C@H]1CC(=O)O)ccc(n2)C(F)(F)F)C 25497965
6192 3097 None 0 Human Functional pEC50 = 8.4 8.4 -4 3
UnclassifiedUnclassified
Guide to Pharmacology 482 10 4 3 3.4 CC(C(=O)NC(C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NC(=O)c1ccccc1 12212809
6192 3097 None 0 Human Functional pEC50 = 8.4 8.4 -4 3
UnclassifiedUnclassified
Guide to Pharmacology 482 10 4 3 3.4 CC(C(=O)NC(C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NC(=O)c1ccccc1 19580790
73755184 3097 None 0 Human Functional pEC50 = 8.4 8.4 -4 3
UnclassifiedUnclassified
Guide to Pharmacology 482 10 4 3 3.4 CC(C(=O)NC(C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NC(=O)c1ccccc1 12212809
73755184 3097 None 0 Human Functional pEC50 = 8.4 8.4 -4 3
UnclassifiedUnclassified
Guide to Pharmacology 482 10 4 3 3.4 CC(C(=O)NC(C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NC(=O)c1ccccc1 19580790
72944991 1151 None 0 Human Functional pEC50 = 8.8 8.8 2 2
UnclassifiedUnclassified
Guide to Pharmacology 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 24412111
72944991 1151 None 0 Human Functional pEC50 = 8.8 8.8 2 2
UnclassifiedUnclassified
Guide to Pharmacology 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 26524625
72944991 1151 None 0 Human Functional pEC50 = 8.8 8.8 2 2
UnclassifiedUnclassified
Guide to Pharmacology 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 35644465
8509 1151 None 0 Human Functional pEC50 = 8.8 8.8 2 2
UnclassifiedUnclassified
Guide to Pharmacology 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 24412111
8509 1151 None 0 Human Functional pEC50 = 8.8 8.8 2 2
UnclassifiedUnclassified
Guide to Pharmacology 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 26524625
8509 1151 None 0 Human Functional pEC50 = 8.8 8.8 2 2
UnclassifiedUnclassified
Guide to Pharmacology 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 35644465
CHEMBL3115390 1151 None 0 Human Functional pEC50 = 8.8 8.8 2 2
UnclassifiedUnclassified
Guide to Pharmacology 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 24412111
CHEMBL3115390 1151 None 0 Human Functional pEC50 = 8.8 8.8 2 2
UnclassifiedUnclassified
Guide to Pharmacology 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 26524625
CHEMBL3115390 1151 None 0 Human Functional pEC50 = 8.8 8.8 2 2
UnclassifiedUnclassified
Guide to Pharmacology 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 35644465
10254379 1026 None 0 Human Functional pEC50 None 9.7 9.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 475 9 5 3 4.4 O=C(N[C@@H](C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NNc1ccc(cc1)Cl 12723954
630 1026 None 0 Human Functional pEC50 None 9.7 9.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 475 9 5 3 4.4 O=C(N[C@@H](C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NNc1ccc(cc1)Cl 12723954
6192 3097 None 0 Human Functional pIC50 = 5.3 5.3 -4 3
UnclassifiedUnclassified
Guide to Pharmacology 482 10 4 3 3.4 CC(C(=O)NC(C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NC(=O)c1ccccc1 20438784
73755184 3097 None 0 Human Functional pIC50 = 5.3 5.3 -4 3
UnclassifiedUnclassified
Guide to Pharmacology 482 10 4 3 3.4 CC(C(=O)NC(C(=O)NCCc1ccccc1)Cc1c[nH]c2c1cccc2)NC(=O)c1ccccc1 20438784
8505 2567 None 0 Human Functional pIC50 = 5.3 5.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 569 10 4 5 5.8 COc1ccc(cc1)C1(CCCCC1)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)Nc1ccc(cc1)[N+](=O)[O-] 25554218
91827363 2567 None 0 Human Functional pIC50 = 5.3 5.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 569 10 4 5 5.8 COc1ccc(cc1)C1(CCCCC1)CNC(=O)[C@H](Cc1c[nH]c2c1cccc2)NC(=O)Nc1ccc(cc1)[N+](=O)[O-] 25554218
6191 264 None 0 Human Functional pIC50 = 6.8 6.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18006692
6191 264 None 0 Human Functional pIC50 = 6.8 6.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20438784
25025654 570 None 12 Human Functional pIC50 = 7.0 7.0 -15 3
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
6189 570 None 12 Human Functional pIC50 = 7.0 7.0 -15 3
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
8506 570 None 12 Human Functional pIC50 = 7.0 7.0 -15 3
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
CHEMBL1084942 570 None 12 Human Functional pIC50 = 7.0 7.0 -15 3
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
49871766 2557 None 36 Human Functional pIC50 = 7.2 7.2 -6 5
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 23892571
49871766 2557 None 36 Human Functional pIC50 = 7.2 7.2 -6 5
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 24900253
6170 2557 None 36 Human Functional pIC50 = 7.2 7.2 -6 5
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 23892571
6170 2557 None 36 Human Functional pIC50 = 7.2 7.2 -6 5
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 24900253
CHEMBL1672354 2557 None 36 Human Functional pIC50 = 7.2 7.2 -6 5
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 23892571
CHEMBL1672354 2557 None 36 Human Functional pIC50 = 7.2 7.2 -6 5
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 24900253
46845425 1032 None 2 Human Functional pIC50 = 7.6 7.6 1 2
UnclassifiedUnclassified
Guide to Pharmacology 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 20167483
8504 1032 None 2 Human Functional pIC50 = 7.6 7.6 1 2
UnclassifiedUnclassified
Guide to Pharmacology 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 20167483
CHEMBL1089721 1032 None 2 Human Functional pIC50 = 7.6 7.6 1 2
UnclassifiedUnclassified
Guide to Pharmacology 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 20167483
25025860 569 None 23 Human Functional pIC50 = 7.7 7.7 -14 5
UnclassifiedUnclassified
Guide to Pharmacology 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 20096642
6188 569 None 23 Human Functional pIC50 = 7.7 7.7 -14 5
UnclassifiedUnclassified
Guide to Pharmacology 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 20096642
CHEMBL1091720 569 None 23 Human Functional pIC50 = 7.7 7.7 -14 5
UnclassifiedUnclassified
Guide to Pharmacology 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 20096642
633 1505 None 0 Human Functional pIC50 = 8.0 8.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18006692
633 1505 None 0 Human Functional pIC50 = 8.0 8.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20438784
25025654 570 None 12 Rat Functional pIC50 = 8.0 8.0 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
6189 570 None 12 Rat Functional pIC50 = 8.0 8.0 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
8506 570 None 12 Rat Functional pIC50 = 8.0 8.0 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
CHEMBL1084942 570 None 12 Rat Functional pIC50 = 8.0 8.0 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
6176 573 None 0 Mouse Functional pIC50 = 8.1 8.1 -4 5
UnclassifiedUnclassified
Guide to Pharmacology 895 23 7 8 4.8 CC(C[C@@H](C(=O)NCC1=CCCC(=C1)C[N+](C)(C)C)NC(=O)C[C@@H]([C@@H](NC([C@@H](N(C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C)Cc1c[nH]c[nH+]1)O)CC1CCCCC1)O)C 20096642
73755180 573 None 0 Mouse Functional pIC50 = 8.1 8.1 -4 5
UnclassifiedUnclassified
Guide to Pharmacology 895 23 7 8 4.8 CC(C[C@@H](C(=O)NCC1=CCCC(=C1)C[N+](C)(C)C)NC(=O)C[C@@H]([C@@H](NC([C@@H](N(C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C)Cc1c[nH]c[nH+]1)O)CC1CCCCC1)O)C 20096642
3946 1503 None 0 Human Functional pIC50 = 8.1 8.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18006692
3946 1503 None 0 Human Functional pIC50 = 8.1 8.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20438784
25025860 569 None 23 Mouse Functional pIC50 = 8.2 8.2 -4 5
UnclassifiedUnclassified
Guide to Pharmacology 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 20096642
6188 569 None 23 Mouse Functional pIC50 = 8.2 8.2 -4 5
UnclassifiedUnclassified
Guide to Pharmacology 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 20096642
CHEMBL1091720 569 None 23 Mouse Functional pIC50 = 8.2 8.2 -4 5
UnclassifiedUnclassified
Guide to Pharmacology 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 20096642
25025654 570 None 12 Mouse Functional pIC50 = 8.2 8.2 1 3
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
6189 570 None 12 Mouse Functional pIC50 = 8.2 8.2 1 3
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
8506 570 None 12 Mouse Functional pIC50 = 8.2 8.2 1 3
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
CHEMBL1084942 570 None 12 Mouse Functional pIC50 = 8.2 8.2 1 3
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
46200989 2562 None 14 Human Functional pIC50 = 8.5 8.5 9 2
UnclassifiedUnclassified
Guide to Pharmacology 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 24900461
8502 2562 None 14 Human Functional pIC50 = 8.5 8.5 9 2
UnclassifiedUnclassified
Guide to Pharmacology 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 24900461
CHEMBL2023109 2562 None 14 Human Functional pIC50 = 8.5 8.5 9 2
UnclassifiedUnclassified
Guide to Pharmacology 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 24900461
25025860 569 None 23 Rat Functional pIC50 = 8.6 8.6 4 5
UnclassifiedUnclassified
Guide to Pharmacology 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 20096642
6188 569 None 23 Rat Functional pIC50 = 8.6 8.6 4 5
UnclassifiedUnclassified
Guide to Pharmacology 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 20096642
CHEMBL1091720 569 None 23 Rat Functional pIC50 = 8.6 8.6 4 5
UnclassifiedUnclassified
Guide to Pharmacology 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 20096642
6176 573 None 0 Human Functional pIC50 = 8.7 8.7 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 895 23 7 8 4.8 CC(C[C@@H](C(=O)NCC1=CCCC(=C1)C[N+](C)(C)C)NC(=O)C[C@@H]([C@@H](NC([C@@H](N(C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C)Cc1c[nH]c[nH+]1)O)CC1CCCCC1)O)C 20096642
6176 573 None 0 Human Functional pIC50 = 8.7 8.7 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 895 23 7 8 4.8 CC(C[C@@H](C(=O)NCC1=CCCC(=C1)C[N+](C)(C)C)NC(=O)C[C@@H]([C@@H](NC([C@@H](N(C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C)Cc1c[nH]c[nH+]1)O)CC1CCCCC1)O)C 23892571
6176 573 None 0 Human Functional pIC50 = 8.7 8.7 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 895 23 7 8 4.8 CC(C[C@@H](C(=O)NCC1=CCCC(=C1)C[N+](C)(C)C)NC(=O)C[C@@H]([C@@H](NC([C@@H](N(C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C)Cc1c[nH]c[nH+]1)O)CC1CCCCC1)O)C 30971479
73755180 573 None 0 Human Functional pIC50 = 8.7 8.7 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 895 23 7 8 4.8 CC(C[C@@H](C(=O)NCC1=CCCC(=C1)C[N+](C)(C)C)NC(=O)C[C@@H]([C@@H](NC([C@@H](N(C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C)Cc1c[nH]c[nH+]1)O)CC1CCCCC1)O)C 20096642
73755180 573 None 0 Human Functional pIC50 = 8.7 8.7 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 895 23 7 8 4.8 CC(C[C@@H](C(=O)NCC1=CCCC(=C1)C[N+](C)(C)C)NC(=O)C[C@@H]([C@@H](NC([C@@H](N(C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C)Cc1c[nH]c[nH+]1)O)CC1CCCCC1)O)C 23892571
73755180 573 None 0 Human Functional pIC50 = 8.7 8.7 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 895 23 7 8 4.8 CC(C[C@@H](C(=O)NCC1=CCCC(=C1)C[N+](C)(C)C)NC(=O)C[C@@H]([C@@H](NC([C@@H](N(C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C)Cc1c[nH]c[nH+]1)O)CC1CCCCC1)O)C 30971479
6176 573 None 0 Rat Functional pIC50 = 8.8 8.8 1 5
UnclassifiedUnclassified
Guide to Pharmacology 895 23 7 8 4.8 CC(C[C@@H](C(=O)NCC1=CCCC(=C1)C[N+](C)(C)C)NC(=O)C[C@@H]([C@@H](NC([C@@H](N(C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C)Cc1c[nH]c[nH+]1)O)CC1CCCCC1)O)C 20096642
73755180 573 None 0 Rat Functional pIC50 = 8.8 8.8 1 5
UnclassifiedUnclassified
Guide to Pharmacology 895 23 7 8 4.8 CC(C[C@@H](C(=O)NCC1=CCCC(=C1)C[N+](C)(C)C)NC(=O)C[C@@H]([C@@H](NC([C@@H](N(C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C)Cc1c[nH]c[nH+]1)O)CC1CCCCC1)O)C 20096642
56840673 1141 None 0 Human Functional pIC50 = 8.9 8.9 2 2
UnclassifiedUnclassified
Guide to Pharmacology 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 24900283
8503 1141 None 0 Human Functional pIC50 = 8.9 8.9 2 2
UnclassifiedUnclassified
Guide to Pharmacology 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 24900283
CHEMBL2164575 1141 None 0 Human Functional pIC50 = 8.9 8.9 2 2
UnclassifiedUnclassified
Guide to Pharmacology 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 24900283
635 1450 None 0 Human Functional pIC50 None 5.6 5.6 -6 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9325344
635 1450 None 0 Human Functional pIC50 None 5.6 5.6 -6 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9593699
635 1450 None 0 Human Functional pIC50 None 5.6 5.6 -6 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9765358




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

155511392 169651 None 0 Mouse Binding pEC50 = 9.1 9.1 - 0
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 169651 None 0 Mouse Binding pEC50 = 9.1 9.1 - 0
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 169651 None 0 Human Binding pEC50 = 9.1 9.1 - 0
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 169651 None 0 Human Binding pEC50 = 9.1 9.1 - 0
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 171430 None 0 Human Binding pEC50 = 9 9.0 - 0
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 171430 None 0 Human Binding pEC50 = 9 9.0 - 0
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 105349 None 0 Mouse Binding pEC50 = 9 9.0 - 0
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 105349 None 0 Mouse Binding pEC50 = 9 9.0 - 0
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 105349 None 0 Mouse Binding pEC50 = 9 9.0 - 0
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 105349 None 0 Mouse Binding pEC50 = 9 9.0 - 0
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 105349 None 0 Human Binding pEC50 = 8.9 8.9 - 0
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 105349 None 0 Human Binding pEC50 = 8.9 8.9 - 0
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 105349 None 0 Human Binding pEC50 = 8.9 8.9 - 0
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 105349 None 0 Human Binding pEC50 = 8.9 8.9 - 0
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 441 4 1 4 5.2 Cc1ccc(Oc2cccc(CC(=O)N3CCNc4nc(C(F)(F)F)ccc4C3)c2)cc1 10.1016/j.bmc.2014.11.018
46200989 2562 None 14 Human Binding pEC50 = 8.9 8.9 - 0
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmcl.2013.12.106
8502 2562 None 14 Human Binding pEC50 = 8.9 8.9 - 0
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmcl.2013.12.106
CHEMBL2023109 2562 None 14 Human Binding pEC50 = 8.9 8.9 - 0
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 105335 None 0 Human Binding pEC50 = 8.8 8.8 - 0
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 105335 None 0 Human Binding pEC50 = 8.8 8.8 - 0
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 105335 None 0 Human Binding pEC50 = 8.8 8.8 - 0
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 105335 None 0 Human Binding pEC50 = 8.8 8.8 - 0
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmc.2014.11.018
72944991 1151 None 0 Human Binding pEC50 = 8.8 8.8 - 0
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 10.1016/j.bmcl.2013.12.106
8509 1151 None 0 Human Binding pEC50 = 8.8 8.8 - 0
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 10.1016/j.bmcl.2013.12.106
CHEMBL3115390 1151 None 0 Human Binding pEC50 = 8.8 8.8 - 0
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 105337 None 0 Human Binding pEC50 = 8.8 8.8 - 0
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 105337 None 0 Human Binding pEC50 = 8.8 8.8 - 0
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 503 6 2 5 5.0 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccc(F)cc2)c1 10.1016/j.bmcl.2013.12.106
72944991 1151 None 0 Human Binding pEC50 = 8.8 8.8 - 0
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 10.1016/j.bmc.2014.11.018
8509 1151 None 0 Human Binding pEC50 = 8.8 8.8 - 0
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 10.1016/j.bmc.2014.11.018
CHEMBL3115390 1151 None 0 Human Binding pEC50 = 8.8 8.8 - 0
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 105337 None 0 Human Binding pEC50 = 8.8 8.8 - 0
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 105337 None 0 Human Binding pEC50 = 8.8 8.8 - 0
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 105329 None 0 Mouse Binding pEC50 = 7 7.0 - 0
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 105329 None 0 Mouse Binding pEC50 = 7 7.0 - 0
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 105320 None 0 Mouse Binding pEC50 = 7.0 7.0 - 0
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 105320 None 0 Mouse Binding pEC50 = 7.0 7.0 - 0
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 105333 None 0 Human Binding pEC50 = 8.0 8.0 - 0
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 105333 None 0 Human Binding pEC50 = 8.0 8.0 - 0
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 170753 None 0 Human Binding pEC50 = 8.0 8.0 - 0
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 170753 None 0 Human Binding pEC50 = 8.0 8.0 - 0
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 171637 None 0 Human Binding pEC50 = 8.0 8.0 - 0
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 171637 None 0 Human Binding pEC50 = 8.0 8.0 - 0
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 105333 None 0 Mouse Binding pEC50 = 8.0 8.0 - 0
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 105333 None 0 Mouse Binding pEC50 = 8.0 8.0 - 0
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 105331 None 0 Human Binding pEC50 = 7.9 7.9 - 0
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 105331 None 0 Human Binding pEC50 = 7.9 7.9 - 0
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 457 5 2 5 4.4 O=C(Cc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1CO 10.1016/j.bmcl.2013.12.106
8507 1002 None 0 Human Binding pEC50 = 7.9 7.9 - 0
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 7 2 6 4.1 CC(CC(=O)Oc1cccc(c1)CC(=O)N1CCNc2c([C@H]1CC(=O)O)ccc(n2)C(F)(F)F)C 10.1016/j.bmc.2014.11.018
91827364 1002 None 0 Human Binding pEC50 = 7.9 7.9 - 0
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 7 2 6 4.1 CC(CC(=O)Oc1cccc(c1)CC(=O)N1CCNc2c([C@H]1CC(=O)O)ccc(n2)C(F)(F)F)C 10.1016/j.bmc.2014.11.018
CHEMBL3356404 1002 None 0 Human Binding pEC50 = 7.9 7.9 - 0
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 173306 None 0 Human Binding pEC50 = 7.9 7.9 - 0
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 173306 None 0 Human Binding pEC50 = 7.9 7.9 - 0
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 105343 None 0 Mouse Binding pEC50 = 7.9 7.9 - 0
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 105343 None 0 Mouse Binding pEC50 = 7.9 7.9 - 0
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 105343 None 0 Mouse Binding pEC50 = 7.9 7.9 - 0
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 105343 None 0 Mouse Binding pEC50 = 7.9 7.9 - 0
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 105324 None 0 Mouse Binding pEC50 = 5.9 5.9 - 0
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 105324 None 0 Mouse Binding pEC50 = 5.9 5.9 - 0
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 105328 None 0 Mouse Binding pEC50 = 6.9 6.9 - 0
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 105328 None 0 Mouse Binding pEC50 = 6.9 6.9 - 0
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 105328 None 0 Mouse Binding pEC50 = 6.9 6.9 - 0
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 105328 None 0 Mouse Binding pEC50 = 6.9 6.9 - 0
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 176147 None 0 Mouse Binding pEC50 = 5.9 5.9 - 0
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 176147 None 0 Mouse Binding pEC50 = 5.9 5.9 - 0
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 105334 None 0 Human Binding pEC50 = 7.9 7.9 - 0
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 105334 None 0 Human Binding pEC50 = 7.9 7.9 - 0
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 105334 None 0 Human Binding pEC50 = 7.9 7.9 - 0
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 105334 None 0 Human Binding pEC50 = 7.9 7.9 - 0
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 174727 None 0 Human Binding pEC50 = 7.9 7.9 - 0
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 174727 None 0 Human Binding pEC50 = 7.9 7.9 - 0
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 173306 None 0 Mouse Binding pEC50 = 7.9 7.9 - 0
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 173306 None 0 Mouse Binding pEC50 = 7.9 7.9 - 0
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 514 9 2 4 6.5 CC(C)(C)Cc1cnc(CCc2ccc(-c3cccc(F)c3C(=O)O)cc2)n1Cc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2016.07.056
46200989 2562 None 14 Mouse Binding pEC50 = 6.9 6.9 - 0
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2014.11.018
8502 2562 None 14 Mouse Binding pEC50 = 6.9 6.9 - 0
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2014.11.018
CHEMBL2023109 2562 None 14 Mouse Binding pEC50 = 6.9 6.9 - 0
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 105318 None 0 Human Binding pEC50 = 6.9 6.9 - 0
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 105318 None 0 Human Binding pEC50 = 6.9 6.9 - 0
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 105318 None 0 Human Binding pEC50 = 6.9 6.9 - 0
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 105318 None 0 Human Binding pEC50 = 6.9 6.9 - 0
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 105344 None 0 Mouse Binding pEC50 = 5.9 5.9 - 0
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 105344 None 0 Mouse Binding pEC50 = 5.9 5.9 - 0
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 428 3 2 4 5.4 O=C(Nc1cccc(Oc2ccccc2)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
49871766 2557 None 36 Human Binding pEC50 = 7.9 7.9 -9 3
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1016/j.bmc.2014.11.018
6170 2557 None 36 Human Binding pEC50 = 7.9 7.9 -9 3
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1016/j.bmc.2014.11.018
CHEMBL1672354 2557 None 36 Human Binding pEC50 = 7.9 7.9 -9 3
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 172469 None 0 Mouse Binding pEC50 = 6.9 6.9 - 0
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 172469 None 0 Mouse Binding pEC50 = 6.9 6.9 - 0
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 105334 None 0 Mouse Binding pEC50 = 7.8 7.8 - 0
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 105334 None 0 Mouse Binding pEC50 = 7.8 7.8 - 0
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 105334 None 0 Mouse Binding pEC50 = 7.8 7.8 - 0
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 105334 None 0 Mouse Binding pEC50 = 7.8 7.8 - 0
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 105320 None 0 Human Binding pEC50 = 6.8 6.8 - 0
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 105320 None 0 Human Binding pEC50 = 6.8 6.8 - 0
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 105332 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 105332 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 105338 None 0 Human Binding pEC50 = 7.8 7.8 - 0
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 105338 None 0 Human Binding pEC50 = 7.8 7.8 - 0
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 105338 None 0 Human Binding pEC50 = 7.8 7.8 - 0
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 105338 None 0 Human Binding pEC50 = 7.8 7.8 - 0
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 105323 None 0 Mouse Binding pEC50 = 5.8 5.8 - 0
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 105323 None 0 Mouse Binding pEC50 = 5.8 5.8 - 0
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 116136 None 0 Human Binding pEC50 = 7.7 7.7 - 0
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 116136 None 0 Human Binding pEC50 = 7.7 7.7 - 0
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 105331 None 0 Mouse Binding pEC50 = 7.7 7.7 - 0
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 105331 None 0 Mouse Binding pEC50 = 7.7 7.7 - 0
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 173103 None 0 Mouse Binding pEC50 = 5.7 5.7 - 0
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 173103 None 0 Mouse Binding pEC50 = 5.7 5.7 - 0
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 105328 None 0 Human Binding pEC50 = 6.7 6.7 - 0
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 105328 None 0 Human Binding pEC50 = 6.7 6.7 - 0
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 105328 None 0 Human Binding pEC50 = 6.7 6.7 - 0
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 105328 None 0 Human Binding pEC50 = 6.7 6.7 - 0
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 170542 None 0 Human Binding pEC50 = 8.7 8.7 - 0
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 170542 None 0 Human Binding pEC50 = 8.7 8.7 - 0
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 175734 None 0 Mouse Binding pEC50 = 8.7 8.7 - 0
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 175734 None 0 Mouse Binding pEC50 = 8.7 8.7 - 0
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 105337 None 0 Mouse Binding pEC50 = 8.6 8.6 - 0
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 105337 None 0 Mouse Binding pEC50 = 8.6 8.6 - 0
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 105347 None 0 Mouse Binding pEC50 = 8.6 8.6 - 0
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 105347 None 0 Mouse Binding pEC50 = 8.6 8.6 - 0
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 105337 None 0 Mouse Binding pEC50 = 8.6 8.6 - 0
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 105337 None 0 Mouse Binding pEC50 = 8.6 8.6 - 0
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 105347 None 0 Mouse Binding pEC50 = 8.6 8.6 - 0
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 105347 None 0 Mouse Binding pEC50 = 8.6 8.6 - 0
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 105322 None 0 Mouse Binding pEC50 = 8.6 8.6 - 0
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 105322 None 0 Mouse Binding pEC50 = 8.6 8.6 - 0
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 105322 None 0 Mouse Binding pEC50 = 8.6 8.6 - 0
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 105322 None 0 Mouse Binding pEC50 = 8.6 8.6 - 0
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 116138 None 0 Mouse Binding pEC50 = 7.7 7.7 - 0
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 116138 None 0 Mouse Binding pEC50 = 7.7 7.7 - 0
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 105323 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 105323 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 105324 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 105324 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 105336 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 105336 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 105336 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 105336 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 172585 None 0 Human Binding pEC50 = 7.7 7.7 - 0
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 172585 None 0 Human Binding pEC50 = 7.7 7.7 - 0
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 438 8 1 5 4.8 COC(=O)c1c(F)cccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CCO)cc1 10.1016/j.bmcl.2016.07.056
49871766 2557 None 36 Mouse Binding pEC50 = 7.7 7.7 -2 3
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1016/j.bmc.2014.11.018
6170 2557 None 36 Mouse Binding pEC50 = 7.7 7.7 -2 3
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1016/j.bmc.2014.11.018
CHEMBL1672354 2557 None 36 Mouse Binding pEC50 = 7.7 7.7 -2 3
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1016/j.bmc.2014.11.018
46200989 2562 None 14 Mouse Binding pEC50 = 7.7 7.7 - 0
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmcl.2013.12.106
8502 2562 None 14 Mouse Binding pEC50 = 7.7 7.7 - 0
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmcl.2013.12.106
CHEMBL2023109 2562 None 14 Mouse Binding pEC50 = 7.7 7.7 - 0
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 170545 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 170545 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 105332 None 0 Mouse Binding pEC50 = 5.7 5.7 - 0
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 105332 None 0 Mouse Binding pEC50 = 5.7 5.7 - 0
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 105340 None 0 Mouse Binding pEC50 = 6.6 6.6 - 0
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 105340 None 0 Mouse Binding pEC50 = 6.6 6.6 - 0
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 105340 None 0 Mouse Binding pEC50 = 6.6 6.6 - 0
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 105340 None 0 Mouse Binding pEC50 = 6.6 6.6 - 0
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 172585 None 0 Mouse Binding pEC50 = 7.6 7.6 - 0
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 172585 None 0 Mouse Binding pEC50 = 7.6 7.6 - 0
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 105350 None 0 Mouse Binding pEC50 = 6.6 6.6 - 0
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 105350 None 0 Mouse Binding pEC50 = 6.6 6.6 - 0
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 105342 None 0 Human Binding pEC50 = 7.6 7.6 - 0
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 105342 None 0 Human Binding pEC50 = 7.6 7.6 - 0
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 105342 None 0 Human Binding pEC50 = 7.6 7.6 - 0
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 105342 None 0 Human Binding pEC50 = 7.6 7.6 - 0
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 174727 None 0 Mouse Binding pEC50 = 7.6 7.6 - 0
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 174727 None 0 Mouse Binding pEC50 = 7.6 7.6 - 0
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 105350 None 0 Human Binding pEC50 = 6.6 6.6 - 0
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 105350 None 0 Human Binding pEC50 = 6.6 6.6 - 0
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 105319 None 0 Mouse Binding pEC50 = 6.6 6.6 - 0
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 105319 None 0 Mouse Binding pEC50 = 6.6 6.6 - 0
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 105319 None 0 Mouse Binding pEC50 = 6.6 6.6 - 0
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 105319 None 0 Mouse Binding pEC50 = 6.6 6.6 - 0
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 170599 None 0 Mouse Binding pEC50 = 7.6 7.6 - 0
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 170599 None 0 Mouse Binding pEC50 = 7.6 7.6 - 0
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 116135 None 0 Mouse Binding pEC50 = 6.6 6.6 - 0
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 116135 None 0 Mouse Binding pEC50 = 6.6 6.6 - 0
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 175734 None 0 Human Binding pEC50 = 8.5 8.5 - 0
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 175734 None 0 Human Binding pEC50 = 8.5 8.5 - 0
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 176286 None 0 Human Binding pEC50 = 8.5 8.5 - 0
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 176286 None 0 Human Binding pEC50 = 8.5 8.5 - 0
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 171430 None 0 Mouse Binding pEC50 = 8.5 8.5 - 0
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 171430 None 0 Mouse Binding pEC50 = 8.5 8.5 - 0
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 116142 None 0 Human Binding pEC50 = 8.5 8.5 - 0
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 116142 None 0 Human Binding pEC50 = 8.5 8.5 - 0
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 105335 None 0 Mouse Binding pEC50 = 8.5 8.5 - 0
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 105335 None 0 Mouse Binding pEC50 = 8.5 8.5 - 0
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 105335 None 0 Mouse Binding pEC50 = 8.5 8.5 - 0
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 105335 None 0 Mouse Binding pEC50 = 8.5 8.5 - 0
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)C[C@@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmc.2014.11.018
72944991 1151 None 0 Mouse Binding pEC50 = 8.5 8.5 - 0
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 10.1016/j.bmcl.2013.12.106
8509 1151 None 0 Mouse Binding pEC50 = 8.5 8.5 - 0
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 10.1016/j.bmcl.2013.12.106
CHEMBL3115390 1151 None 0 Mouse Binding pEC50 = 8.5 8.5 - 0
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 105345 None 0 Mouse Binding pEC50 = 8.5 8.5 - 0
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 105345 None 0 Mouse Binding pEC50 = 8.5 8.5 - 0
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 445 4 1 4 5.0 O=C(Cc1cccc(Oc2ccccc2F)c1)N1CCNc2nc(C(F)(F)F)ccc2C1 10.1016/j.bmcl.2013.12.106
72944991 1151 None 0 Mouse Binding pEC50 = 8.5 8.5 - 0
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 10.1016/j.bmc.2014.11.018
8509 1151 None 0 Mouse Binding pEC50 = 8.5 8.5 - 0
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 500 6 2 6 4.6 OC(=O)C[C@H]1N(CCNc2c1ccc(n2)C(F)(F)F)C(=O)Cc1cccc(c1)Oc1ccc(nc1)C 10.1016/j.bmc.2014.11.018
CHEMBL3115390 1151 None 0 Mouse Binding pEC50 = 8.5 8.5 - 0
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 105347 None 0 Human Binding pEC50 = 8.4 8.4 - 0
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 105347 None 0 Human Binding pEC50 = 8.4 8.4 - 0
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 105347 None 0 Human Binding pEC50 = 8.4 8.4 - 0
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 105347 None 0 Human Binding pEC50 = 8.4 8.4 - 0
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 116142 None 0 Mouse Binding pEC50 = 8.4 8.4 - 0
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 116142 None 0 Mouse Binding pEC50 = 8.4 8.4 - 0
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 105336 None 0 Mouse Binding pEC50 = 5.5 5.5 - 0
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 105336 None 0 Mouse Binding pEC50 = 5.5 5.5 - 0
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 105336 None 0 Mouse Binding pEC50 = 5.5 5.5 - 0
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 105336 None 0 Mouse Binding pEC50 = 5.5 5.5 - 0
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 485 6 2 5 4.9 O=C(O)C[C@H]1c2ccc(C(F)(F)F)nc2NCCN1C(=O)Cc1cccc(Oc2ccccc2)c1 10.1016/j.bmc.2014.11.018
56840673 1141 None 0 Mouse Binding pEC50 = 7.5 7.5 - 0
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2013.12.106
8503 1141 None 0 Mouse Binding pEC50 = 7.5 7.5 - 0
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2013.12.106
CHEMBL2164575 1141 None 0 Mouse Binding pEC50 = 7.5 7.5 - 0
Agonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at mouse BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2013.12.106
56840673 1141 None 0 Mouse Binding pEC50 = 7.5 7.5 - 0
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmc.2014.11.018
8503 1141 None 0 Mouse Binding pEC50 = 7.5 7.5 - 0
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmc.2014.11.018
CHEMBL2164575 1141 None 0 Mouse Binding pEC50 = 7.5 7.5 - 0
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 105318 None 0 Mouse Binding pEC50 = 7.5 7.5 - 0
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 105318 None 0 Mouse Binding pEC50 = 7.5 7.5 - 0
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 105318 None 0 Mouse Binding pEC50 = 7.5 7.5 - 0
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 105318 None 0 Mouse Binding pEC50 = 7.5 7.5 - 0
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 116136 None 0 Mouse Binding pEC50 = 7.5 7.5 - 0
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 116136 None 0 Mouse Binding pEC50 = 7.5 7.5 - 0
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 105341 None 0 Human Binding pEC50 = 6.4 6.4 - 0
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 105341 None 0 Human Binding pEC50 = 6.4 6.4 - 0
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 105341 None 0 Human Binding pEC50 = 6.4 6.4 - 0
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 105341 None 0 Human Binding pEC50 = 6.4 6.4 - 0
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 105325 None 0 Human Binding pEC50 = 6.4 6.4 - 0
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 105325 None 0 Human Binding pEC50 = 6.4 6.4 - 0
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 105325 None 0 Human Binding pEC50 = 6.4 6.4 - 0
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 105325 None 0 Human Binding pEC50 = 6.4 6.4 - 0
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 172933 None 0 Human Binding pEC50 = 7.4 7.4 - 0
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 172933 None 0 Human Binding pEC50 = 7.4 7.4 - 0
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 116141 None 0 Human Binding pEC50 = 8.4 8.4 - 0
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 116141 None 0 Human Binding pEC50 = 8.4 8.4 - 0
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 170542 None 0 Mouse Binding pEC50 = 8.4 8.4 - 0
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 170542 None 0 Mouse Binding pEC50 = 8.4 8.4 - 0
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 116140 None 0 Human Binding pEC50 = 8.4 8.4 - 0
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 116140 None 0 Human Binding pEC50 = 8.4 8.4 - 0
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 116139 None 0 Human Binding pEC50 = 7.4 7.4 - 0
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 116139 None 0 Human Binding pEC50 = 7.4 7.4 - 0
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 173103 None 0 Human Binding pEC50 = 5.4 5.4 - 0
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 173103 None 0 Human Binding pEC50 = 5.4 5.4 - 0
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 105329 None 0 Human Binding pEC50 = 7.4 7.4 - 0
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 105329 None 0 Human Binding pEC50 = 7.4 7.4 - 0
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 116137 None 0 Human Binding pEC50 = 7.4 7.4 - 0
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 116137 None 0 Human Binding pEC50 = 7.4 7.4 - 0
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 170599 None 0 Human Binding pEC50 = 7.4 7.4 - 0
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 170599 None 0 Human Binding pEC50 = 7.4 7.4 - 0
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 391 9 1 4 4.8 CCC(C)(C)Cc1cnc(CCc2ccc(-c3ccccn3)cc2)n1CC(=O)O 10.1016/j.bmcl.2016.07.056
8507 1002 None 0 Mouse Binding pEC50 = 7.4 7.4 - 0
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 7 2 6 4.1 CC(CC(=O)Oc1cccc(c1)CC(=O)N1CCNc2c([C@H]1CC(=O)O)ccc(n2)C(F)(F)F)C 10.1016/j.bmc.2014.11.018
91827364 1002 None 0 Mouse Binding pEC50 = 7.4 7.4 - 0
Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 493 7 2 6 4.1 CC(CC(=O)Oc1cccc(c1)CC(=O)N1CCNc2c([C@H]1CC(=O)O)ccc(n2)C(F)(F)F)C 10.1016/j.bmc.2014.11.018
CHEMBL3356404 1002 None 0 Mouse Binding pEC50 = 7.4 7.4 - 0
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 105344 None 0 Human Binding pEC50 = 5.4 5.4 - 0
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 105344 None 0 Human Binding pEC50 = 5.4 5.4 - 0
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 172933 None 0 Mouse Binding pEC50 = 7.4 7.4 - 0
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 172933 None 0 Mouse Binding pEC50 = 7.4 7.4 - 0
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 116139 None 0 Mouse Binding pEC50 = 7.4 7.4 - 0
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 116139 None 0 Mouse Binding pEC50 = 7.4 7.4 - 0
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 105342 None 0 Mouse Binding pEC50 = 7.3 7.3 - 0
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 105342 None 0 Mouse Binding pEC50 = 7.3 7.3 - 0
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 105342 None 0 Mouse Binding pEC50 = 7.3 7.3 - 0
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 105342 None 0 Mouse Binding pEC50 = 7.3 7.3 - 0
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 105340 None 0 Human Binding pEC50 = 7.3 7.3 - 0
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 105340 None 0 Human Binding pEC50 = 7.3 7.3 - 0
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 105340 None 0 Human Binding pEC50 = 7.3 7.3 - 0
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 105340 None 0 Human Binding pEC50 = 7.3 7.3 - 0
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 174185 None 0 Mouse Binding pEC50 = 6.3 6.3 - 0
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 174185 None 0 Mouse Binding pEC50 = 6.3 6.3 - 0
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 176286 None 0 Mouse Binding pEC50 = 8.3 8.3 - 0
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 176286 None 0 Mouse Binding pEC50 = 8.3 8.3 - 0
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 116140 None 0 Mouse Binding pEC50 = 8.3 8.3 - 0
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 116140 None 0 Mouse Binding pEC50 = 8.3 8.3 - 0
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 116143 None 0 Human Binding pEC50 = 8.3 8.3 - 0
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 116143 None 0 Human Binding pEC50 = 8.3 8.3 - 0
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 116141 None 0 Mouse Binding pEC50 = 8.3 8.3 - 0
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 116141 None 0 Mouse Binding pEC50 = 8.3 8.3 - 0
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 105326 None 0 Mouse Binding pEC50 = 7.3 7.3 - 0
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 105326 None 0 Mouse Binding pEC50 = 7.3 7.3 - 0
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 105326 None 0 Mouse Binding pEC50 = 7.3 7.3 - 0
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 105326 None 0 Mouse Binding pEC50 = 7.3 7.3 - 0
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 105325 None 0 Mouse Binding pEC50 = 6.3 6.3 - 0
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 105325 None 0 Mouse Binding pEC50 = 6.3 6.3 - 0
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 105325 None 0 Mouse Binding pEC50 = 6.3 6.3 - 0
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 105325 None 0 Mouse Binding pEC50 = 6.3 6.3 - 0
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 105326 None 0 Human Binding pEC50 = 7.2 7.2 - 0
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 105326 None 0 Human Binding pEC50 = 7.2 7.2 - 0
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 105326 None 0 Human Binding pEC50 = 7.2 7.2 - 0
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 105326 None 0 Human Binding pEC50 = 7.2 7.2 - 0
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 105346 None 0 Human Binding pEC50 = 8.2 8.2 - 0
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 105346 None 0 Human Binding pEC50 = 8.2 8.2 - 0
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 105345 None 0 Human Binding pEC50 = 8.2 8.2 - 0
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 105345 None 0 Human Binding pEC50 = 8.2 8.2 - 0
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 170753 None 0 Mouse Binding pEC50 = 7.2 7.2 - 0
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 170753 None 0 Mouse Binding pEC50 = 7.2 7.2 - 0
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 105327 None 0 Mouse Binding pEC50 = 7.2 7.2 - 0
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 105327 None 0 Mouse Binding pEC50 = 7.2 7.2 - 0
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 105338 None 0 Mouse Binding pEC50 = 7.2 7.2 - 0
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 105338 None 0 Mouse Binding pEC50 = 7.2 7.2 - 0
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 105327 None 0 Mouse Binding pEC50 = 7.2 7.2 - 0
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 105327 None 0 Mouse Binding pEC50 = 7.2 7.2 - 0
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 105338 None 0 Mouse Binding pEC50 = 7.2 7.2 - 0
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 105338 None 0 Mouse Binding pEC50 = 7.2 7.2 - 0
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 105321 None 0 Mouse Binding pEC50 = 6.2 6.2 - 0
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 105321 None 0 Mouse Binding pEC50 = 6.2 6.2 - 0
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 170103 None 0 Mouse Binding pEC50 = 6.2 6.2 - 0
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 170103 None 0 Mouse Binding pEC50 = 6.2 6.2 - 0
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 174185 None 0 Human Binding pEC50 = 6.2 6.2 - 0
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 174185 None 0 Human Binding pEC50 = 6.2 6.2 - 0
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 116135 None 0 Human Binding pEC50 = 7.2 7.2 - 0
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 116135 None 0 Human Binding pEC50 = 7.2 7.2 - 0
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 172469 None 0 Human Binding pEC50 = 7.2 7.2 - 0
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 172469 None 0 Human Binding pEC50 = 7.2 7.2 - 0
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 173318 None 0 Mouse Binding pEC50 = 6.2 6.2 - 0
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 173318 None 0 Mouse Binding pEC50 = 6.2 6.2 - 0
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 171637 None 0 Mouse Binding pEC50 = 8.2 8.2 - 0
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 171637 None 0 Mouse Binding pEC50 = 8.2 8.2 - 0
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 105327 None 0 Human Binding pEC50 = 7.2 7.2 - 0
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 105327 None 0 Human Binding pEC50 = 7.2 7.2 - 0
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 105327 None 0 Human Binding pEC50 = 7.2 7.2 - 0
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 105327 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 407 5 1 4 4.1 CC(C)COc1cccc(CC(=O)N2CCNc3nc(C(F)(F)F)ccc3C2)c1 10.1016/j.bmc.2014.11.018
46200989 2562 None 14 Human Binding pEC50 = 7.1 7.1 - 0
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2014.11.018
8502 2562 None 14 Human Binding pEC50 = 7.1 7.1 - 0
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2014.11.018
CHEMBL2023109 2562 None 14 Human Binding pEC50 = 7.1 7.1 - 0
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 105330 None 0 Human Binding pEC50 = 8.1 8.1 - 0
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 105330 None 0 Human Binding pEC50 = 8.1 8.1 - 0
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 116143 None 0 Mouse Binding pEC50 = 8.1 8.1 - 0
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 116143 None 0 Mouse Binding pEC50 = 8.1 8.1 - 0
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 105343 None 0 Human Binding pEC50 = 8.1 8.1 - 0
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 105343 None 0 Human Binding pEC50 = 8.1 8.1 - 0
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 105343 None 0 Human Binding pEC50 = 8.1 8.1 - 0
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 105343 None 0 Human Binding pEC50 = 8.1 8.1 - 0
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 116138 None 0 Human Binding pEC50 = 8.1 8.1 - 0
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 116138 None 0 Human Binding pEC50 = 8.1 8.1 - 0
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 105330 None 0 Mouse Binding pEC50 = 8.1 8.1 - 0
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 105330 None 0 Mouse Binding pEC50 = 8.1 8.1 - 0
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 105346 None 0 Mouse Binding pEC50 = 8.1 8.1 - 0
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 105346 None 0 Mouse Binding pEC50 = 8.1 8.1 - 0
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 116137 None 0 Mouse Binding pEC50 = 7.1 7.1 - 0
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 116137 None 0 Mouse Binding pEC50 = 7.1 7.1 - 0
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 176147 None 0 Human Binding pEC50 = 6.1 6.1 - 0
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 176147 None 0 Human Binding pEC50 = 6.1 6.1 - 0
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 105322 None 0 Human Binding pEC50 = 8.0 8.0 - 0
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 105322 None 0 Human Binding pEC50 = 8.0 8.0 - 0
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 105322 None 0 Human Binding pEC50 = 8.0 8.0 - 0
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 105322 None 0 Human Binding pEC50 = 8.0 8.0 - 0
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 105319 None 0 Human Binding pEC50 = 6.0 6.0 - 0
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 105319 None 0 Human Binding pEC50 = 6.0 6.0 - 0
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 105319 None 0 Human Binding pEC50 = 6.0 6.0 - 0
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 105319 None 0 Human Binding pEC50 = 6.0 6.0 - 0
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 173318 None 0 Human Binding pEC50 = 6.0 6.0 - 0
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 173318 None 0 Human Binding pEC50 = 6.0 6.0 - 0
Agonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
ChEMBL 434 8 1 5 4.8 COC(=O)c1ccccc1-c1ccc(CCc2ncc(CC(C)(C)C)n2CC(=O)O)cc1 10.1016/j.bmcl.2016.07.056
56840673 1141 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2013.12.106
8503 1141 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2013.12.106
CHEMBL2164575 1141 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Agonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assayAgonist activity at human BRS-3 expressed in CHOK1 cells after 1 hr by HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2013.12.106
56840673 1141 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmc.2014.11.018
8503 1141 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assayAgonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1016/j.bmc.2014.11.018
CHEMBL2164575 1141 None 0 Human Binding pEC50 = 7.0 7.0 - 0
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 105321 None 0 Human Binding pEC50 = 6.0 6.0 - 0
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 105321 None 0 Human Binding pEC50 = 6.0 6.0 - 0
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 170545 None 0 Mouse Binding pEC50 = 5 5.0 - 0
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 170545 None 0 Mouse Binding pEC50 = 5 5.0 - 0
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 74218 None 0 Human Binding pIC50 = 9.3 9.3 - 0
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 74218 None 0 Human Binding pIC50 = 9.3 9.3 - 0
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 74219 None 0 Human Binding pIC50 = 9.3 9.3 - 0
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 74219 None 0 Human Binding pIC50 = 9.3 9.3 - 0
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 74217 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 74217 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 82820 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 82820 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 81907 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 81907 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 81903 None 0 Human Binding pIC50 = 9.1 9.1 - 0
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 81903 None 0 Human Binding pIC50 = 9.1 9.1 - 0
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 82813 None 0 Human Binding pIC50 = 9.1 9.1 - 0
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 82813 None 0 Human Binding pIC50 = 9.1 9.1 - 0
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 81819 None 0 Human Binding pIC50 = 9.1 9.1 - 0
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 81819 None 0 Human Binding pIC50 = 9.1 9.1 - 0
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 81906 None 0 Human Binding pIC50 = 9.0 9.0 - 0
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 81906 None 0 Human Binding pIC50 = 9.0 9.0 - 0
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 215559 None 0 Human Binding pIC50 = 9.0 9.0 - 0
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 82809 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 82809 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 81908 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 81908 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 573 4 2 8 6.0 C[C@H](O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(C(C)(C)C)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
49871766 2557 None 36 Rat Binding pIC50 = 8.9 8.9 2 3
Displacement of [3H]Bag-3 from rat BRS-3Displacement of [3H]Bag-3 from rat BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
6170 2557 None 36 Rat Binding pIC50 = 8.9 8.9 2 3
Displacement of [3H]Bag-3 from rat BRS-3Displacement of [3H]Bag-3 from rat BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
CHEMBL1672354 2557 None 36 Rat Binding pIC50 = 8.9 8.9 2 3
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 74216 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 74216 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingDisplacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
ChEMBL 657 6 2 9 6.4 CC(C)(O)c1nc(C(C)(C)c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1016/j.bmc.2012.03.029
56840673 1141 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
8503 1141 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
CHEMBL2164575 1141 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 81904 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 81904 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 82690 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 82690 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 81820 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 81820 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 81902 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 81902 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 81818 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 81818 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 7534 None 0 Human Binding pIC50 = 8 8.0 - 0
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 7534 None 0 Human Binding pIC50 = 8 8.0 - 0
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 82697 None 0 Human Binding pIC50 = 8 8.0 - 0
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 82697 None 0 Human Binding pIC50 = 8 8.0 - 0
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 82700 None 0 Human Binding pIC50 = 8 8.0 - 0
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 82700 None 0 Human Binding pIC50 = 8 8.0 - 0
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 6444 None 0 Human Binding pIC50 = 8 8.0 - 0
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 6444 None 0 Human Binding pIC50 = 8 8.0 - 0
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 60847 None 0 Human Binding pIC50 = 7 7.0 - 0
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 60847 None 0 Human Binding pIC50 = 7 7.0 - 0
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 8182 None 0 Human Binding pIC50 = 7 7.0 - 0
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 8182 None 0 Human Binding pIC50 = 7 7.0 - 0
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 7687 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 7687 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 406 10 2 3 5.3 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCC(=O)O)cc2)n1 10.1016/j.bmcl.2010.03.028
46845425 1032 None 2 Human Binding pIC50 = 8.0 8.0 - 0
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.03.028
8504 1032 None 2 Human Binding pIC50 = 8.0 8.0 - 0
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.03.028
CHEMBL1089721 1032 None 2 Human Binding pIC50 = 8.0 8.0 - 0
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 57859 None 1 Human Binding pIC50 = 8.0 8.0 - 0
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 57859 None 1 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 390 6 2 4 3.9 CC(O)(Cc1nc(CC2(C(F)(F)F)CC2)c[nH]1)c1ccc(-n2cccn2)cc1 10.1021/ml100196d
46845425 1032 None 2 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
8504 1032 None 2 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 376 8 2 2 5.5 CCC(Cc1c[nH]c(n1)CCc1ccc(cc1)c1ccccc1C(=O)O)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1089721 1032 None 2 Human Binding pIC50 = 8.0 8.0 - 0
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 8422 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 8422 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 7486 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 7486 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 82698 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 82698 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 8381 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 8381 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 9078 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 9078 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 8382 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 8382 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 351 7 1 2 5.4 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccc(F)cn3)cc2)n1 10.1021/ml100196d
56840673 1141 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
8503 1141 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 489 2 1 4 6.5 Cc1c(C)ccc2c1N(Cc1c(N2)nc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/ml200207w
CHEMBL2164575 1141 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 57962 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 57962 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 8113 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 8113 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 7671 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 7671 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 81822 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 81822 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 597 6 2 9 5.4 CC(C)(O)c1nc(-c2cccc3c2N(S(=O)(=O)c2ccc(OC(F)F)cc2)Cc2ccc(C(F)(F)F)nc2N3)no1 10.1021/ml200304j
25025860 569 None 23 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
6188 569 None 23 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1091720 569 None 23 Human Binding pIC50 = 7.8 7.8 - 0
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 8382 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 8382 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 74220 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 74220 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 82818 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 82818 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 477 2 2 5 5.6 CC(C)(C)c1ccc(S(=O)(=O)N2Cc3ccc(C(F)(F)F)nc3Nc3cccc(O)c32)cc1 10.1021/ml200207w
25025860 569 None 23 Rat Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from rat BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from rat BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
6188 569 None 23 Rat Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from rat BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from rat BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1091720 569 None 23 Rat Binding pIC50 = 8.6 8.6 - 0
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 7515 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 7515 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 82696 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 82696 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 8174 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 8174 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 7443 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 7443 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 60848 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 60848 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 60869 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 60869 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 60868 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 60868 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 7661 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 7661 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 7444 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 7444 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity to human BRS3Binding affinity to human BRS3
ChEMBL 444 10 3 5 5.1 CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(N)n[nH]3)cc2)n1 10.1016/j.bmcl.2010.03.028
49871766 2557 None 36 Human Binding pIC50 = 7.6 7.6 -9 3
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
6170 2557 None 36 Human Binding pIC50 = 7.6 7.6 -9 3
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
CHEMBL1672354 2557 None 36 Human Binding pIC50 = 7.6 7.6 -9 3
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 8175 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 8175 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 8104 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 8104 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 7686 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 7686 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 81905 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 81905 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 60871 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 60871 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 82814 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 82814 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 82693 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 82693 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 517 3 1 5 6.1 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(OC(F)(F)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
46200989 2562 None 14 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingDisplacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2012.03.029
8502 2562 None 14 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingDisplacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2012.03.029
CHEMBL2023109 2562 None 14 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation countingDisplacement of 125I-dY-peptide from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1016/j.bmc.2012.03.029
46200989 2562 None 14 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1021/ml200304j
8502 2562 None 14 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation countingDisplacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
ChEMBL 615 5 2 9 5.7 FC(Oc1ccc(cc1)S(=O)(=O)N1Cc2ccc(nc2Nc2c1c(ccc2)c1noc(n1)C(O)(C)C)C(F)(F)F)(F)F 10.1021/ml200304j
CHEMBL2023109 2562 None 14 Human Binding pIC50 = 8.4 8.4 - 0
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 60855 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 60855 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 60857 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 60857 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 7445 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 7445 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 7685 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 7685 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 60852 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 60852 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 60872 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 60872 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 7823 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 7823 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 7824 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 7824 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 8317 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 8317 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 5893 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 5893 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 161899 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 161899 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 60858 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 60858 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 7825 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 7825 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 82808 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 82808 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 82699 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 82699 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 60853 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 60853 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 82810 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 82810 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 7819 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 7819 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 57963 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 57963 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 82817 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 82817 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 7659 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 7659 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 8501 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 8501 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 82819 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 82819 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 476 2 1 5 5.6 Cc1ccc2c(n1)N(S(=O)(=O)c1ccc(C(C)(C)C)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
49871766 2557 None 36 Mouse Binding pIC50 = 8.3 8.3 -2 3
Displacement of [3H]Bag-3 from mouse BRS-3Displacement of [3H]Bag-3 from mouse BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
6170 2557 None 36 Mouse Binding pIC50 = 8.3 8.3 -2 3
Displacement of [3H]Bag-3 from mouse BRS-3Displacement of [3H]Bag-3 from mouse BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
CHEMBL1672354 2557 None 36 Mouse Binding pIC50 = 8.3 8.3 -2 3
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 82816 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 82816 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 82694 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 82694 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 82695 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 82695 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 82815 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 82815 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 7820 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 7820 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 8379 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 8379 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 60845 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 60845 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 60867 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 60867 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 60851 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 60851 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 8103 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 8103 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 7442 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 7442 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 7660 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 7660 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 8183 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 8183 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 82691 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 82691 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation countingDisplacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
ChEMBL 501 2 1 4 6.2 Cc1ccc2c(c1C)N(S(=O)(=O)c1ccc(C(F)(F)F)cc1)Cc1ccc(C(F)(F)F)nc1N2 10.1021/ml200207w
25025860 569 None 23 Mouse Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from mouse BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from mouse BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
6188 569 None 23 Mouse Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from mouse BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation countingDisplacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from mouse BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
ChEMBL 333 7 1 2 5.2 CCC(Cc1cnc([nH]1)CCc1ccc(cc1)c1ccccn1)(C)C 10.1016/j.bmcl.2010.02.076
CHEMBL1091720 569 None 23 Mouse Binding pIC50 = 8.2 8.2 - 0
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 25237 None 9 Human Binding pIC50 = 6.2 6.2 - 0
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 25237 None 9 Human Binding pIC50 = 6.2 6.2 - 0
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 60861 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 60861 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 60849 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 60849 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 60864 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 60864 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 60854 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 60854 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 60866 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 60866 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 60847 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 60847 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 60872 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 60872 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 8255 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 8255 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 8114 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 8114 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 82692 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 82692 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 60850 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 60850 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 60870 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 60870 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 81821 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 81821 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 82812 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 82812 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 57961 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 57961 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 60846 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 60846 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 7533 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 7533 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 60860 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 60860 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 60865 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 60865 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 60859 None 0 Human Binding pIC50 = 6 6.0 - 0
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 60859 None 0 Human Binding pIC50 = 6 6.0 - 0
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 218143 None 0 Human Binding pKi = 9.4 9.4 2 3
Binding affinity to BRS-3 receptorBinding affinity to BRS-3 receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](N)Cc1ccccc1)C(C)C)C(N)=O 10.1016/j.bmcl.2008.09.033
49871766 2557 None 36 Rat Binding pKi = 9.2 9.2 2 3
Displacement of [3H]Bag-3 from rat BRS-3Displacement of [3H]Bag-3 from rat BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
6170 2557 None 36 Rat Binding pKi = 9.2 9.2 2 3
Displacement of [3H]Bag-3 from rat BRS-3Displacement of [3H]Bag-3 from rat BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
CHEMBL1672354 2557 None 36 Rat Binding pKi = 9.2 9.2 2 3
Displacement of [3H]Bag-3 from rat BRS-3Displacement of [3H]Bag-3 from rat BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
49871766 2557 None 36 Mouse Binding pKi = 8.8 8.8 -2 3
Displacement of [3H]Bag-3 from mouse BRS-3Displacement of [3H]Bag-3 from mouse BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
6170 2557 None 36 Mouse Binding pKi = 8.8 8.8 -2 3
Displacement of [3H]Bag-3 from mouse BRS-3Displacement of [3H]Bag-3 from mouse BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
CHEMBL1672354 2557 None 36 Mouse Binding pKi = 8.8 8.8 -2 3
Displacement of [3H]Bag-3 from mouse BRS-3Displacement of [3H]Bag-3 from mouse BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
49871766 2557 None 36 Human Binding pKi = 8.4 8.4 -9 3
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
6170 2557 None 36 Human Binding pKi = 8.4 8.4 -9 3
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
CHEMBL1672354 2557 None 36 Human Binding pKi = 8.4 8.4 -9 3
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
ChEMBL 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 10.1021/ml100196d
71300326 118565 None 32 Human Binding pKi = 5.1 5.1 -6 3
Selectivity interaction (Enzyme panel (ion channels, GPCRs, other targets)) EUB0000196bCl BRS3Selectivity interaction (Enzyme panel (ion channels, GPCRs, other targets)) EUB0000196bCl BRS3
ChEMBL 499 6 2 4 3.0 O=C([C@@H](Cc1cccc(C(F)(F)F)c1)NS(=O)(=O)c1cc(F)c2c(c1)CCNC2)N1CCCC1 10.6019/CHEMBL5212743
CHEMBL3414622 118565 None 32 Human Binding pKi = 5.1 5.1 -6 3
Selectivity interaction (Enzyme panel (ion channels, GPCRs, other targets)) EUB0000196bCl BRS3Selectivity interaction (Enzyme panel (ion channels, GPCRs, other targets)) EUB0000196bCl BRS3
ChEMBL 499 6 2 4 3.0 O=C([C@@H](Cc1cccc(C(F)(F)F)c1)NS(=O)(=O)c1cc(F)c2c(c1)CCNC2)N1CCCC1 10.6019/CHEMBL5212743
CHEMBL4789678 118565 None 32 Human Binding pKi = 5.1 5.1 -6 3
Selectivity interaction (Enzyme panel (ion channels, GPCRs, other targets)) EUB0000196bCl BRS3Selectivity interaction (Enzyme panel (ion channels, GPCRs, other targets)) EUB0000196bCl BRS3
ChEMBL 499 6 2 4 3.0 O=C([C@@H](Cc1cccc(C(F)(F)F)c1)NS(=O)(=O)c1cc(F)c2c(c1)CCNC2)N1CCCC1 10.6019/CHEMBL5212743
25025654 570 None 12 Mouse Binding pKd = 8.6 8.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
6189 570 None 12 Mouse Binding pKd = 8.6 8.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
8506 570 None 12 Mouse Binding pKd = 8.6 8.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
CHEMBL1084942 570 None 12 Mouse Binding pKd = 8.6 8.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 374 7 2 2 5.3 OC(=O)c1ccccc1c1ccc(cc1)CCc1ncc([nH]1)CC1CCCC1 20096642
164512405 218439 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5 5.0 -316 12
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
5355 218439 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5 5.0 -316 12
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
5355.0 218439 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5 5.0 -316 12
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
CHEMBL26 218439 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5 5.0 -316 12
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
DB00391 218439 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5 5.0 -316 12
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
None 218575 125I-[D-Tyr6,Beta-Ala11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5 5.0 - 1
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 218575 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5 5.0 - 1
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 218576 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5 5.0 - 1
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 218581 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5 5.0 - 1
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 218579 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5.7 5.7 - 1
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 218580 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5.5 5.5 - 1
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 218578 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5.4 5.4 - 1
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 218577 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5.4 5.4 - 1
NoneNone
PDSP KiDatabase 1084 30 13 13 -2.1 CC(C)C(C(=O)NCC(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCSC)C(=O)N)NC(=O)C(C)NC(=O)C(CC3=CNC4=CC=CC=C43)NC(=O)C(CCC(=O)N)NC(=O)C5CCC(=O)N5 None
164512405 218439 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5.3 5.3 -316 12
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
5355 218439 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5.3 5.3 -316 12
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
5355.0 218439 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5.3 5.3 -316 12
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
CHEMBL26 218439 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5.3 5.3 -316 12
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
DB00391 218439 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5.3 5.3 -316 12
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
164512399 218583 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5.2 5.2 - 1
NoneNone
PDSP KiDatabase 304 7 4 9 -10.5 C(C(C(C(C(=O)COP(=O)([O-])[O-])O)O)O)O.[Na+].[Na+] None
22146595 3290 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5.2 5.2 -3467 3
NoneNone
PDSP KiDatabase None None None None None
618 3290 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5.2 5.2 -3467 3
NoneNone
PDSP KiDatabase None None None None None
None 218582 125I-[DTyr6,BetaAla11,Phe13,Nle14]Bn(6-14) 0 Human Binding pKi = 5.2 5.2 - 1
NoneNone
PDSP KiDatabase None None None None None
49871766 2557 None 36 Human Binding pKi = 8.1 8.1 -9 3
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 23892571
49871766 2557 None 36 Human Binding pKi = 8.1 8.1 -9 3
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 24900253
6170 2557 None 36 Human Binding pKi = 8.1 8.1 -9 3
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 23892571
6170 2557 None 36 Human Binding pKi = 8.1 8.1 -9 3
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 24900253
CHEMBL1672354 2557 None 36 Human Binding pKi = 8.1 8.1 -9 3
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 23892571
CHEMBL1672354 2557 None 36 Human Binding pKi = 8.1 8.1 -9 3
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 24900253
3946 1503 None 0 Human Binding pKi = 8.1 8.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15102928
632 1478 None 0 Human Binding pKi = 8.2 8.2 -6 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9325344
633 1505 None 0 Human Binding pKi = 8.4 8.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11112777
49871766 2557 None 36 Mouse Binding pKi = 8.8 8.8 -2 3
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 21036912
6170 2557 None 36 Mouse Binding pKi = 8.8 8.8 -2 3
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 21036912
CHEMBL1672354 2557 None 36 Mouse Binding pKi = 8.8 8.8 -2 3
UnclassifiedUnclassified
Guide to Pharmacology 444 6 2 4 4.5 FC([C@@](c1ccc(cc1)n1cccn1)(Cc1ncc([nH]1)CC1(CC1)C(F)(F)F)O)(F)F 21036912
632 1478 None 0 Mouse Binding pKi = 8.8 8.8 -1 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10454496
632 1478 None 0 Rat Binding pKi = 9 9.0 1 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10454496