Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| 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 | ||
Showing 1 to 50 of 1,156 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| 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 | ||
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