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
| |
| 11656002 | 83044 | None | 22 | Human | Functional | pEC50 | = | 9.6 | 9.6 | 61 | 8 | Agonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay |
ChEMBL | 484 | 3 | 0 | 3 | 5.8 | O=C1COc2nccc(-c3ccccc3F)c2CN1Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1 | 10.1021/jm301071h | ||
| CHEMBL2181247 | 83044 | None | 22 | Human | Functional | pEC50 | = | 9.6 | 9.6 | 61 | 8 | Agonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay |
ChEMBL | 484 | 3 | 0 | 3 | 5.8 | O=C1COc2nccc(-c3ccccc3F)c2CN1Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1 | 10.1021/jm301071h | ||
| 90644451 | 112274 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | 3 | 2 | Agonist activity at human TGR5 expressed in HEK293 cells co-expressing CRE after 5.5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells co-expressing CRE after 5.5 hrs by luciferase reporter gene assay |
ChEMBL | 459 | 4 | 0 | 5 | 6.2 | Cc1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 | 10.1016/j.ejmech.2014.05.031 | ||
| CHEMBL3290717 | 112274 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | 3 | 2 | Agonist activity at human TGR5 expressed in HEK293 cells co-expressing CRE after 5.5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells co-expressing CRE after 5.5 hrs by luciferase reporter gene assay |
ChEMBL | 459 | 4 | 0 | 5 | 6.2 | Cc1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 | 10.1016/j.ejmech.2014.05.031 | ||
| 71561754 | 87678 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Agonist activity at doxycycline-promoter regulated overexpressed human TGR5 receptor in CHO cells assessed as elevation of cAMP level by induced-cAMP assayAgonist activity at doxycycline-promoter regulated overexpressed human TGR5 receptor in CHO cells assessed as elevation of cAMP level by induced-cAMP assay |
ChEMBL | 432 | 6 | 0 | 5 | 5.3 | Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N(Cc1cccnc1)C(C)C | 10.1016/j.bmcl.2012.12.076 | ||
| CHEMBL2336232 | 87678 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Agonist activity at doxycycline-promoter regulated overexpressed human TGR5 receptor in CHO cells assessed as elevation of cAMP level by induced-cAMP assayAgonist activity at doxycycline-promoter regulated overexpressed human TGR5 receptor in CHO cells assessed as elevation of cAMP level by induced-cAMP assay |
ChEMBL | 432 | 6 | 0 | 5 | 5.3 | Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N(Cc1cccnc1)C(C)C | 10.1016/j.bmcl.2012.12.076 | ||
| 126673452 | 161247 | None | 0 | Mouse | Functional | pEC50 | = | 9.5 | 9.5 | 257 | 2 | Agonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay |
ChEMBL | 774 | 19 | 2 | 12 | 5.2 | COc1ccc(N(C)c2cnc(SCc3c(F)cc(OCCCN(CCS(=O)(=O)O)CCS(=O)(=O)O)cc3F)n2-c2ccc(F)cc2)cc1OC | 10.1021/acs.jmedchem.6b01873 | ||
| CHEMBL4087611 | 161247 | None | 0 | Mouse | Functional | pEC50 | = | 9.5 | 9.5 | 257 | 2 | Agonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay |
ChEMBL | 774 | 19 | 2 | 12 | 5.2 | COc1ccc(N(C)c2cnc(SCc3c(F)cc(OCCCN(CCS(=O)(=O)O)CCS(=O)(=O)O)cc3F)n2-c2ccc(F)cc2)cc1OC | 10.1021/acs.jmedchem.6b01873 | ||
| CHEMBL4117342 | 161247 | None | 0 | Mouse | Functional | pEC50 | = | 9.5 | 9.5 | 257 | 2 | Agonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay |
ChEMBL | 774 | 19 | 2 | 12 | 5.2 | COc1ccc(N(C)c2cnc(SCc3c(F)cc(OCCCN(CCS(=O)(=O)O)CCS(=O)(=O)O)cc3F)n2-c2ccc(F)cc2)cc1OC | 10.1021/acs.jmedchem.6b01873 | ||
| 71462787 | 83026 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | 3 | 2 | Agonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay |
ChEMBL | 453 | 4 | 0 | 4 | 6.1 | Cc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl | 10.1021/jm301071h | ||
| CHEMBL2181229 | 83026 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | 3 | 2 | Agonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay |
ChEMBL | 453 | 4 | 0 | 4 | 6.1 | Cc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl | 10.1021/jm301071h | ||
| 155669602 | 182046 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Agonist activity at human TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assayAgonist activity at human TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay |
ChEMBL | 372 | 4 | 0 | 4 | 4.1 | C[C@H](c1ccccc1)n1cncc1C(=O)N1CCN(C2CC2)c2ccccc21 | 10.1016/j.bmc.2020.115972 | ||
| CHEMBL4779837 | 182046 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Agonist activity at human TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assayAgonist activity at human TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay |
ChEMBL | 372 | 4 | 0 | 4 | 4.1 | C[C@H](c1ccccc1)n1cncc1C(=O)N1CCN(C2CC2)c2ccccc21 | 10.1016/j.bmc.2020.115972 | ||
| 118577239 | 161077 | None | 0 | Mouse | Functional | pEC50 | = | 9.4 | 9.4 | 60 | 2 | Agonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay |
ChEMBL | 623 | 13 | 1 | 9 | 6.0 | COc1ccc(N(C)c2cnc(SCc3c(F)cc(OCCCS(=O)(=O)O)cc3F)n2-c2ccc(F)cc2)cc1OC | 10.1021/acs.jmedchem.6b01873 | ||
| CHEMBL4060410 | 161077 | None | 0 | Mouse | Functional | pEC50 | = | 9.4 | 9.4 | 60 | 2 | Agonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay |
ChEMBL | 623 | 13 | 1 | 9 | 6.0 | COc1ccc(N(C)c2cnc(SCc3c(F)cc(OCCCS(=O)(=O)O)cc3F)n2-c2ccc(F)cc2)cc1OC | 10.1021/acs.jmedchem.6b01873 | ||
| CHEMBL4116055 | 161077 | None | 0 | Mouse | Functional | pEC50 | = | 9.4 | 9.4 | 60 | 2 | Agonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay |
ChEMBL | 623 | 13 | 1 | 9 | 6.0 | COc1ccc(N(C)c2cnc(SCc3c(F)cc(OCCCS(=O)(=O)O)cc3F)n2-c2ccc(F)cc2)cc1OC | 10.1021/acs.jmedchem.6b01873 | ||
| 71626699 | 112273 | None | 0 | Human | Functional | pEC50 | = | 9.4 | 9.4 | 5 | 2 | Agonist activity at human TGR5 expressed in HEK293 cells co-expressing CRE after 5.5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells co-expressing CRE after 5.5 hrs by luciferase reporter gene assay |
ChEMBL | 425 | 4 | 0 | 5 | 5.6 | Cc1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 | 10.1016/j.ejmech.2014.05.031 | ||
| CHEMBL3290716 | 112273 | None | 0 | Human | Functional | pEC50 | = | 9.4 | 9.4 | 5 | 2 | Agonist activity at human TGR5 expressed in HEK293 cells co-expressing CRE after 5.5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells co-expressing CRE after 5.5 hrs by luciferase reporter gene assay |
ChEMBL | 425 | 4 | 0 | 5 | 5.6 | Cc1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 | 10.1016/j.ejmech.2014.05.031 | ||
| 71455634 | 83024 | None | 0 | Human | Functional | pEC50 | = | 9.3 | 9.3 | 4 | 2 | Agonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay |
ChEMBL | 473 | 4 | 0 | 4 | 6.5 | O=C(c1cnccc1Oc1cc(Cl)c(Cl)cc1Cl)N1CCN(C2CC2)c2ccccc21 | 10.1021/jm301071h | ||
| CHEMBL2181227 | 83024 | None | 0 | Human | Functional | pEC50 | = | 9.3 | 9.3 | 4 | 2 | Agonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay |
ChEMBL | 473 | 4 | 0 | 4 | 6.5 | O=C(c1cnccc1Oc1cc(Cl)c(Cl)cc1Cl)N1CCN(C2CC2)c2ccccc21 | 10.1021/jm301071h | ||
| 90654589 | 110014 | None | 0 | Mouse | Functional | pEC50 | = | 9.3 | 9.3 | 1 | 2 | Agonist activity at mouse TGR5 expressed in Jurkat cells assessed as intracellular cAMP level after 1 hr by HTRF assayAgonist activity at mouse TGR5 expressed in Jurkat cells assessed as intracellular cAMP level after 1 hr by HTRF assay |
ChEMBL | 543 | 7 | 1 | 8 | 2.5 | N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3cc(N4CCN(C5COC5)CC4)nc(C(F)(F)F)n3)C2)cc1 | 10.1021/jm401731q | ||
| CHEMBL3234570 | 110014 | None | 0 | Mouse | Functional | pEC50 | = | 9.3 | 9.3 | 1 | 2 | Agonist activity at mouse TGR5 expressed in Jurkat cells assessed as intracellular cAMP level after 1 hr by HTRF assayAgonist activity at mouse TGR5 expressed in Jurkat cells assessed as intracellular cAMP level after 1 hr by HTRF assay |
ChEMBL | 543 | 7 | 1 | 8 | 2.5 | N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3cc(N4CCN(C5COC5)CC4)nc(C(F)(F)F)n3)C2)cc1 | 10.1021/jm401731q | ||
| 90654598 | 110062 | None | 0 | Mouse | Functional | pEC50 | = | 9.3 | 9.3 | 21 | 2 | Agonist activity at mouse TGR5 expressed in Jurkat cells assessed as intracellular cAMP level after 1 hr by HTRF assayAgonist activity at mouse TGR5 expressed in Jurkat cells assessed as intracellular cAMP level after 1 hr by HTRF assay |
ChEMBL | 608 | 9 | 2 | 8 | 4.4 | COc1cc(C2CCN(c3cc(N4CC[C@H]4C(=O)NCCc4ccc(C#N)cc4)nc(C(F)(F)F)n3)CC2)ccc1C(=O)O | 10.1021/jm401731q | ||
| CHEMBL3234869 | 110062 | None | 0 | Mouse | Functional | pEC50 | = | 9.3 | 9.3 | 21 | 2 | Agonist activity at mouse TGR5 expressed in Jurkat cells assessed as intracellular cAMP level after 1 hr by HTRF assayAgonist activity at mouse TGR5 expressed in Jurkat cells assessed as intracellular cAMP level after 1 hr by HTRF assay |
ChEMBL | 608 | 9 | 2 | 8 | 4.4 | COc1cc(C2CCN(c3cc(N4CC[C@H]4C(=O)NCCc4ccc(C#N)cc4)nc(C(F)(F)F)n3)CC2)ccc1C(=O)O | 10.1021/jm401731q | ||
| 71462786 | 83025 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | 3 | 2 | Agonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay |
ChEMBL | 413 | 4 | 0 | 4 | 5.4 | Cc1cc(C)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1C | 10.1021/jm301071h | ||
| CHEMBL2181228 | 83025 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | 3 | 2 | Agonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay |
ChEMBL | 413 | 4 | 0 | 4 | 5.4 | Cc1cc(C)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1C | 10.1021/jm301071h | ||
| 71450251 | 83023 | None | 29 | Human | Functional | pEC50 | = | 9.1 | 9.1 | 8 | 3 | Agonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay |
ChEMBL | 399 | 4 | 0 | 4 | 5.1 | Cc1ccc(C)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)c1 | 10.1021/jm301071h | ||
| CHEMBL2181226 | 83023 | None | 29 | Human | Functional | pEC50 | = | 9.1 | 9.1 | 8 | 3 | Agonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay |
ChEMBL | 399 | 4 | 0 | 4 | 5.1 | Cc1ccc(C)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)c1 | 10.1021/jm301071h | ||
| 71461054 | 83028 | None | 0 | Human | Functional | pEC50 | = | 9.1 | 9.1 | 3 | 2 | Agonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay |
ChEMBL | 467 | 5 | 0 | 4 | 6.4 | CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl | 10.1021/jm301071h | ||
| CHEMBL2181230 | 83028 | None | 0 | Human | Functional | pEC50 | = | 9.1 | 9.1 | 3 | 2 | Agonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay |
ChEMBL | 467 | 5 | 0 | 4 | 6.4 | CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl | 10.1021/jm301071h | ||
| 118576935 | 158042 | None | 0 | Mouse | Functional | pEC50 | = | 9.1 | 9.1 | 43 | 2 | Agonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay |
ChEMBL | 485 | 8 | 0 | 6 | 6.4 | COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC | 10.1021/acs.jmedchem.6b01873 | ||
| CHEMBL4084668 | 158042 | None | 0 | Mouse | Functional | pEC50 | = | 9.1 | 9.1 | 43 | 2 | Agonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay |
ChEMBL | 485 | 8 | 0 | 6 | 6.4 | COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC | 10.1021/acs.jmedchem.6b01873 | ||
| 118576930 | 158907 | None | 0 | Mouse | Functional | pEC50 | = | 9.1 | 9.1 | 25 | 2 | Agonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay |
ChEMBL | 515 | 9 | 0 | 7 | 6.4 | COc1cc(-n2c(N(C)c3ccc(OC)c(OC)c3)cnc2SCc2c(F)cccc2F)ccc1F | 10.1021/acs.jmedchem.6b01873 | ||
| CHEMBL4094487 | 158907 | None | 0 | Mouse | Functional | pEC50 | = | 9.1 | 9.1 | 25 | 2 | Agonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at mouse TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay |
ChEMBL | 515 | 9 | 0 | 7 | 6.4 | COc1cc(-n2c(N(C)c3ccc(OC)c(OC)c3)cnc2SCc2c(F)cccc2F)ccc1F | 10.1021/acs.jmedchem.6b01873 | ||
| 156705093 | 181996 | None | 0 | Human | Functional | pEC50 | = | 9.1 | 9.1 | 25 | 2 | Agonist activity at human TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter gene activity incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter gene activity incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay |
ChEMBL | 469 | 5 | 0 | 7 | 5.0 | COC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 | 10.1016/j.ejmech.2020.112619 | ||
| CHEMBL4779084 | 181996 | None | 0 | Human | Functional | pEC50 | = | 9.1 | 9.1 | 25 | 2 | Agonist activity at human TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter gene activity incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter gene activity incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay |
ChEMBL | 469 | 5 | 0 | 7 | 5.0 | COC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 | 10.1016/j.ejmech.2020.112619 | ||
| 90644451 | 112274 | None | 0 | Mouse | Functional | pEC50 | = | 9.0 | 9.0 | -3 | 2 | Agonist activity at mouse TGR5 expressed in HEK293 cells co-expressing CRE after 5.5 hrs by luciferase reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells co-expressing CRE after 5.5 hrs by luciferase reporter gene assay |
ChEMBL | 459 | 4 | 0 | 5 | 6.2 | Cc1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 | 10.1016/j.ejmech.2014.05.031 | ||
| CHEMBL3290717 | 112274 | None | 0 | Mouse | Functional | pEC50 | = | 9.0 | 9.0 | -3 | 2 | Agonist activity at mouse TGR5 expressed in HEK293 cells co-expressing CRE after 5.5 hrs by luciferase reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells co-expressing CRE after 5.5 hrs by luciferase reporter gene assay |
ChEMBL | 459 | 4 | 0 | 5 | 6.2 | Cc1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 | 10.1016/j.ejmech.2014.05.031 | ||
| 71462787 | 83026 | None | 0 | Mouse | Functional | pEC50 | = | 9.0 | 9.0 | -3 | 2 | Agonist activity at mouse TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay |
ChEMBL | 453 | 4 | 0 | 4 | 6.1 | Cc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl | 10.1021/jm301071h | ||
| CHEMBL2181229 | 83026 | None | 0 | Mouse | Functional | pEC50 | = | 9.0 | 9.0 | -3 | 2 | Agonist activity at mouse TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay |
ChEMBL | 453 | 4 | 0 | 4 | 6.1 | Cc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl | 10.1021/jm301071h | ||
| 90654589 | 110014 | None | 0 | Human | Functional | pEC50 | = | 9 | 9.0 | -1 | 2 | Agonist activity at human TGR5 expressed in Jurkat cells assessed as intracellular cAMP level after 1 hr by HTRF assayAgonist activity at human TGR5 expressed in Jurkat cells assessed as intracellular cAMP level after 1 hr by HTRF assay |
ChEMBL | 543 | 7 | 1 | 8 | 2.5 | N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3cc(N4CCN(C5COC5)CC4)nc(C(F)(F)F)n3)C2)cc1 | 10.1021/jm401731q | ||
| CHEMBL3234570 | 110014 | None | 0 | Human | Functional | pEC50 | = | 9 | 9.0 | -1 | 2 | Agonist activity at human TGR5 expressed in Jurkat cells assessed as intracellular cAMP level after 1 hr by HTRF assayAgonist activity at human TGR5 expressed in Jurkat cells assessed as intracellular cAMP level after 1 hr by HTRF assay |
ChEMBL | 543 | 7 | 1 | 8 | 2.5 | N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3cc(N4CCN(C5COC5)CC4)nc(C(F)(F)F)n3)C2)cc1 | 10.1021/jm401731q | ||
| 46232571 | 205071 | None | 0 | Human | Functional | pEC50 | = | 9 | 9.0 | - | 1 | Agonist activity at human TGR5 receptor expressed in human U2-OS cells assessed as changes in response to cAMP level by MRE/CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in human U2-OS cells assessed as changes in response to cAMP level by MRE/CRE-driven luciferase reporter gene assay |
ChEMBL | 356 | 4 | 0 | 4 | 4.6 | COc1cccc(-c2noc(C)c2C(=O)N(C)c2ccc(Cl)cc2)c1 | 10.1016/j.bmcl.2010.01.003 | ||
| CHEMBL612138 | 205071 | None | 0 | Human | Functional | pEC50 | = | 9 | 9.0 | - | 1 | Agonist activity at human TGR5 receptor expressed in human U2-OS cells assessed as changes in response to cAMP level by MRE/CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in human U2-OS cells assessed as changes in response to cAMP level by MRE/CRE-driven luciferase reporter gene assay |
ChEMBL | 356 | 4 | 0 | 4 | 4.6 | COc1cccc(-c2noc(C)c2C(=O)N(C)c2ccc(Cl)cc2)c1 | 10.1016/j.bmcl.2010.01.003 | ||
| 118103672 | 164545 | None | 0 | Mouse | Functional | pEC50 | = | 9 | 9.0 | 31 | 2 | Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay |
ChEMBL | 679 | 14 | 5 | 8 | 3.6 | O=C(NCCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC(CO)(CO)CO | 10.1021/acs.jmedchem.8b00308 | ||
| CHEMBL4213913 | 164545 | None | 0 | Mouse | Functional | pEC50 | = | 9 | 9.0 | 31 | 2 | Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay |
ChEMBL | 679 | 14 | 5 | 8 | 3.6 | O=C(NCCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC(CO)(CO)CO | 10.1021/acs.jmedchem.8b00308 | ||
| 90654587 | 110011 | None | 0 | Mouse | Functional | pEC50 | = | 9 | 9.0 | -1 | 2 | Agonist activity at mouse TGR5 expressed in Jurkat cells assessed as intracellular cAMP level after 1 hr by HTRF assayAgonist activity at mouse TGR5 expressed in Jurkat cells assessed as intracellular cAMP level after 1 hr by HTRF assay |
ChEMBL | 501 | 6 | 1 | 7 | 2.7 | CN1CCN(c2cc(N3CCC[C@@H](C(=O)NCCc4ccc(C#N)cc4)C3)nc(C(F)(F)F)n2)CC1 | 10.1021/jm401731q | ||
| CHEMBL3234568 | 110011 | None | 0 | Mouse | Functional | pEC50 | = | 9 | 9.0 | -1 | 2 | Agonist activity at mouse TGR5 expressed in Jurkat cells assessed as intracellular cAMP level after 1 hr by HTRF assayAgonist activity at mouse TGR5 expressed in Jurkat cells assessed as intracellular cAMP level after 1 hr by HTRF assay |
ChEMBL | 501 | 6 | 1 | 7 | 2.7 | CN1CCN(c2cc(N3CCC[C@@H](C(=O)NCCc4ccc(C#N)cc4)C3)nc(C(F)(F)F)n2)CC1 | 10.1021/jm401731q | ||
| 90654597 | 110061 | None | 0 | Mouse | Functional | pEC50 | = | 9 | 9.0 | 17 | 2 | Agonist activity at mouse TGR5 expressed in Jurkat cells assessed as intracellular cAMP level after 1 hr by HTRF assayAgonist activity at mouse TGR5 expressed in Jurkat cells assessed as intracellular cAMP level after 1 hr by HTRF assay |
ChEMBL | 594 | 9 | 2 | 8 | 4.1 | N#Cc1ccc(CCNC(=O)[C@@H]2CCN2c2cc(N3CCC(Oc4ccc(C(=O)O)cc4)CC3)nc(C(F)(F)F)n2)cc1 | 10.1021/jm401731q | ||
| CHEMBL3234868 | 110061 | None | 0 | Mouse | Functional | pEC50 | = | 9 | 9.0 | 17 | 2 | Agonist activity at mouse TGR5 expressed in Jurkat cells assessed as intracellular cAMP level after 1 hr by HTRF assayAgonist activity at mouse TGR5 expressed in Jurkat cells assessed as intracellular cAMP level after 1 hr by HTRF assay |
ChEMBL | 594 | 9 | 2 | 8 | 4.1 | N#Cc1ccc(CCNC(=O)[C@@H]2CCN2c2cc(N3CCC(Oc4ccc(C(=O)O)cc4)CC3)nc(C(F)(F)F)n2)cc1 | 10.1021/jm401731q | ||
Showing 1 to 50 of 2,896 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
| |
| 89501446 | 139489 | None | 2 | Human | Binding | pEC50 | = | 10.2 | 10.2 | - | 0 | Agonist activity at human TGR5 expressed in CHO-K1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO-K1 cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 558 | 11 | 0 | 8 | 6.7 | COc1ccc(C(C)(C)c2cnc(SCCOc3ccc(-n4ccnc4)cc3)n2-c2ccc(F)cc2)cc1OC | 10.1021/acsmedchemlett.5b00323 | ||
| CHEMBL3793436 | 139489 | None | 2 | Human | Binding | pEC50 | = | 10.2 | 10.2 | - | 0 | Agonist activity at human TGR5 expressed in CHO-K1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO-K1 cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 558 | 11 | 0 | 8 | 6.7 | COc1ccc(C(C)(C)c2cnc(SCCOc3ccc(-n4ccnc4)cc3)n2-c2ccc(F)cc2)cc1OC | 10.1021/acsmedchemlett.5b00323 | ||
| 89501446 | 139489 | None | 2 | Mouse | Binding | pEC50 | = | 10.2 | 10.2 | - | 0 | Agonist activity at mouse TGR5 expressed in CHO-K1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at mouse TGR5 expressed in CHO-K1 cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 558 | 11 | 0 | 8 | 6.7 | COc1ccc(C(C)(C)c2cnc(SCCOc3ccc(-n4ccnc4)cc3)n2-c2ccc(F)cc2)cc1OC | 10.1021/acsmedchemlett.5b00323 | ||
| CHEMBL3793436 | 139489 | None | 2 | Mouse | Binding | pEC50 | = | 10.2 | 10.2 | - | 0 | Agonist activity at mouse TGR5 expressed in CHO-K1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at mouse TGR5 expressed in CHO-K1 cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 558 | 11 | 0 | 8 | 6.7 | COc1ccc(C(C)(C)c2cnc(SCCOc3ccc(-n4ccnc4)cc3)n2-c2ccc(F)cc2)cc1OC | 10.1021/acsmedchemlett.5b00323 | ||
| 71626633 | 193761 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at TGR5 in human HEK293 cells assessed as increase in cAMP productionAgonist activity at TGR5 in human HEK293 cells assessed as increase in cAMP production |
ChEMBL | 460 | 4 | 0 | 6 | 5.6 | Cc1noc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 | 10.1021/acs.jmedchem.5b00342 | ||
| CHEMBL5270816 | 193761 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at TGR5 in human HEK293 cells assessed as increase in cAMP productionAgonist activity at TGR5 in human HEK293 cells assessed as increase in cAMP production |
ChEMBL | 460 | 4 | 0 | 6 | 5.6 | Cc1noc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 | 10.1021/acs.jmedchem.5b00342 | ||
| 90327592 | 194734 | None | 0 | Mouse | Binding | pEC50 | = | 9.2 | 9.2 | - | 0 | Inhibition of mouse TGR5Inhibition of mouse TGR5 |
ChEMBL | 615 | 10 | 0 | 5 | 6.6 | CN(CC[N+](C)(C)C)C(=O)CCc1cc(Cl)c(Oc2ccsc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl | 10.1021/acsmedchemlett.3c00001 | ||
| CHEMBL5286836 | 194734 | None | 0 | Mouse | Binding | pEC50 | = | 9.2 | 9.2 | - | 0 | Inhibition of mouse TGR5Inhibition of mouse TGR5 |
ChEMBL | 615 | 10 | 0 | 5 | 6.6 | CN(CC[N+](C)(C)C)C(=O)CCc1cc(Cl)c(Oc2ccsc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl | 10.1021/acsmedchemlett.3c00001 | ||
| CHEMBL5315434 | 194734 | None | 0 | Mouse | Binding | pEC50 | = | 9.2 | 9.2 | - | 0 | Inhibition of mouse TGR5Inhibition of mouse TGR5 |
ChEMBL | 615 | 10 | 0 | 5 | 6.6 | CN(CC[N+](C)(C)C)C(=O)CCc1cc(Cl)c(Oc2ccsc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl | 10.1021/acsmedchemlett.3c00001 | ||
| 171358457 | 194624 | None | 0 | Human | Binding | pEC50 | = | 9 | 9.0 | - | 0 | Agonist activity at human TGR5 transfected in CHO cells assessed as increase in cAMP productionAgonist activity at human TGR5 transfected in CHO cells assessed as increase in cAMP production |
ChEMBL | 476 | 7 | 2 | 4 | 5.9 | Cc1cc(/C(C[C@H](c2ccc(C3C[C@@H]4C(C(=O)O)[C@@H]4C3)cc2)c2ccc(F)cc2F)=N\O)ccn1 | 10.1021/acs.jmedchem.5b00342 | ||
| CHEMBL5290871 | 194624 | None | 0 | Human | Binding | pEC50 | = | 9 | 9.0 | - | 0 | Agonist activity at human TGR5 transfected in CHO cells assessed as increase in cAMP productionAgonist activity at human TGR5 transfected in CHO cells assessed as increase in cAMP production |
ChEMBL | 476 | 7 | 2 | 4 | 5.9 | Cc1cc(/C(C[C@H](c2ccc(C3C[C@@H]4C(C(=O)O)[C@@H]4C3)cc2)c2ccc(F)cc2F)=N\O)ccn1 | 10.1021/acs.jmedchem.5b00342 | ||
| 71732478 | 194363 | None | 0 | Human | Binding | pEC50 | = | 8.9 | 8.9 | - | 0 | Agonist activity at human TGR5 expressed in human HEK293 cells measured after 5.5 hrs by steady-glo luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells measured after 5.5 hrs by steady-glo luciferase assay |
ChEMBL | 587 | 5 | 0 | 5 | 8.2 | Fc1cccc(F)c1-c1ccncc1CN1C(c2ccco2)=NO[C@@H]1c1cc(C(F)(F)F)cc(C(F)(F)F)c1Cl | 10.1021/acs.jmedchem.5b00342 | ||
| CHEMBL5284434 | 194363 | None | 0 | Human | Binding | pEC50 | = | 8.9 | 8.9 | - | 0 | Agonist activity at human TGR5 expressed in human HEK293 cells measured after 5.5 hrs by steady-glo luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells measured after 5.5 hrs by steady-glo luciferase assay |
ChEMBL | 587 | 5 | 0 | 5 | 8.2 | Fc1cccc(F)c1-c1ccncc1CN1C(c2ccco2)=NO[C@@H]1c1cc(C(F)(F)F)cc(C(F)(F)F)c1Cl | 10.1021/acs.jmedchem.5b00342 | ||
| 89501666 | 139573 | None | 0 | Human | Binding | pEC50 | = | 8.8 | 8.8 | - | 0 | Agonist activity at human TGR5 expressed in CHO-K1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO-K1 cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 572 | 11 | 0 | 8 | 7.0 | COc1ccc(C(C)(C)c2cnc(SCCOc3ccc(-n4ccnc4C)cc3)n2-c2ccc(F)cc2)cc1OC | 10.1021/acsmedchemlett.5b00323 | ||
| CHEMBL3794442 | 139573 | None | 0 | Human | Binding | pEC50 | = | 8.8 | 8.8 | - | 0 | Agonist activity at human TGR5 expressed in CHO-K1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO-K1 cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 572 | 11 | 0 | 8 | 7.0 | COc1ccc(C(C)(C)c2cnc(SCCOc3ccc(-n4ccnc4C)cc3)n2-c2ccc(F)cc2)cc1OC | 10.1021/acsmedchemlett.5b00323 | ||
| 46195848 | 83043 | None | 0 | Human | Binding | pEC50 | = | 8 | 8.0 | - | 0 | Agonist activity at GPBAR1 in human NCI-H716 cellsAgonist activity at GPBAR1 in human NCI-H716 cells |
ChEMBL | 398 | 3 | 0 | 3 | 5.8 | O=C(c1cccnc1Oc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 | 10.1021/acs.jmedchem.5b01875 | ||
| CHEMBL2181246 | 83043 | None | 0 | Human | Binding | pEC50 | = | 8 | 8.0 | - | 0 | Agonist activity at GPBAR1 in human NCI-H716 cellsAgonist activity at GPBAR1 in human NCI-H716 cells |
ChEMBL | 398 | 3 | 0 | 3 | 5.8 | O=C(c1cccnc1Oc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 | 10.1021/acs.jmedchem.5b01875 | ||
| 46195848 | 83043 | None | 0 | Human | Binding | pEC50 | = | 8 | 8.0 | - | 0 | Agonist activity at TGR5 (unknown origin)Agonist activity at TGR5 (unknown origin) |
ChEMBL | 398 | 3 | 0 | 3 | 5.8 | O=C(c1cccnc1Oc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 | 10.1016/j.ejmech.2013.07.050 | ||
| CHEMBL2181246 | 83043 | None | 0 | Human | Binding | pEC50 | = | 8 | 8.0 | - | 0 | Agonist activity at TGR5 (unknown origin)Agonist activity at TGR5 (unknown origin) |
ChEMBL | 398 | 3 | 0 | 3 | 5.8 | O=C(c1cccnc1Oc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 | 10.1016/j.ejmech.2013.07.050 | ||
| 46195848 | 83043 | None | 0 | Human | Binding | pEC50 | = | 8 | 8.0 | - | 0 | Agonist activity at human TGR5Agonist activity at human TGR5 |
ChEMBL | 398 | 3 | 0 | 3 | 5.8 | O=C(c1cccnc1Oc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 | 10.1021/acs.jmedchem.5b00342 | ||
| CHEMBL2181246 | 83043 | None | 0 | Human | Binding | pEC50 | = | 8 | 8.0 | - | 0 | Agonist activity at human TGR5Agonist activity at human TGR5 |
ChEMBL | 398 | 3 | 0 | 3 | 5.8 | O=C(c1cccnc1Oc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 | 10.1021/acs.jmedchem.5b00342 | ||
| 136239453 | 91647 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | Agonist activity at recombinant human GPBAR1 expressed in CHO cellsAgonist activity at recombinant human GPBAR1 expressed in CHO cells |
ChEMBL | 359 | 6 | 1 | 4 | 4.9 | Cc1ccc(C(C/C(=N\O)c2ccncc2)c2ccc(N(C)C)cc2)cc1 | 10.1016/j.bmcl.2013.06.017 | ||
| CHEMBL2407946 | 91647 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | Agonist activity at recombinant human GPBAR1 expressed in CHO cellsAgonist activity at recombinant human GPBAR1 expressed in CHO cells |
ChEMBL | 359 | 6 | 1 | 4 | 4.9 | Cc1ccc(C(C/C(=N\O)c2ccncc2)c2ccc(N(C)C)cc2)cc1 | 10.1016/j.bmcl.2013.06.017 | ||
| 447715 | 199383 | None | 50 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | Agonist activity at wild type TGR5 (unknown origin)Agonist activity at wild type TGR5 (unknown origin) |
ChEMBL | 420 | 5 | 3 | 3 | 5.1 | CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)O)[C@@H]2[C@@H]1O | 10.1021/ml400247k | ||
| CHEMBL566315 | 199383 | None | 50 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | Agonist activity at wild type TGR5 (unknown origin)Agonist activity at wild type TGR5 (unknown origin) |
ChEMBL | 420 | 5 | 3 | 3 | 5.1 | CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)O)[C@@H]2[C@@H]1O | 10.1021/ml400247k | ||
| 1520267 | 167865 | None | 44 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Agonist activity at human TGR5Agonist activity at human TGR5 |
ChEMBL | 500 | 8 | 0 | 8 | 1.8 | COc1ccc(S(=O)(=O)N2CCCN(S(=O)(=O)c3ccc(OC)c(OC)c3)CC2)cc1OC | 10.1021/acs.jmedchem.5b00342 | ||
| CHEMBL4303545 | 167865 | None | 44 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Agonist activity at human TGR5Agonist activity at human TGR5 |
ChEMBL | 500 | 8 | 0 | 8 | 1.8 | COc1ccc(S(=O)(=O)N2CCCN(S(=O)(=O)c3ccc(OC)c(OC)c3)CC2)cc1OC | 10.1021/acs.jmedchem.5b00342 | ||
| 10133 | 910 | None | 49 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at wild type TGR5 (unknown origin)Agonist activity at wild type TGR5 (unknown origin) |
ChEMBL | 392 | 4 | 3 | 3 | 4.5 | O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C | 10.1021/ml400247k | ||
| 145714624 | 910 | None | 49 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at wild type TGR5 (unknown origin)Agonist activity at wild type TGR5 (unknown origin) |
ChEMBL | 392 | 4 | 3 | 3 | 4.5 | O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C | 10.1021/ml400247k | ||
| 4361 | 910 | None | 49 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at wild type TGR5 (unknown origin)Agonist activity at wild type TGR5 (unknown origin) |
ChEMBL | 392 | 4 | 3 | 3 | 4.5 | O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C | 10.1021/ml400247k | ||
| 608 | 910 | None | 49 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at wild type TGR5 (unknown origin)Agonist activity at wild type TGR5 (unknown origin) |
ChEMBL | 392 | 4 | 3 | 3 | 4.5 | O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C | 10.1021/ml400247k | ||
| CHEMBL240597 | 910 | None | 49 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at wild type TGR5 (unknown origin)Agonist activity at wild type TGR5 (unknown origin) |
ChEMBL | 392 | 4 | 3 | 3 | 4.5 | O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C | 10.1021/ml400247k | ||
| DB06777 | 910 | None | 49 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at wild type TGR5 (unknown origin)Agonist activity at wild type TGR5 (unknown origin) |
ChEMBL | 392 | 4 | 3 | 3 | 4.5 | O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C | 10.1021/ml400247k | ||
| 136166852 | 91668 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | Agonist activity at recombinant human GPBAR1 expressed in CHO cellsAgonist activity at recombinant human GPBAR1 expressed in CHO cells |
ChEMBL | 450 | 7 | 2 | 4 | 6.5 | Cc1cc(/C(C[C@H](c2ccc(-c3ccc(C(=O)O)cc3)cc2)c2ccccc2C)=N/O)ccn1 | 10.1016/j.bmcl.2013.06.017 | ||
| CHEMBL2408107 | 91668 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | Agonist activity at recombinant human GPBAR1 expressed in CHO cellsAgonist activity at recombinant human GPBAR1 expressed in CHO cells |
ChEMBL | 450 | 7 | 2 | 4 | 6.5 | Cc1cc(/C(C[C@H](c2ccc(-c3ccc(C(=O)O)cc3)cc2)c2ccccc2C)=N/O)ccn1 | 10.1016/j.bmcl.2013.06.017 | ||
| 136239453 | 91647 | None | 0 | Mouse | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Agonist activity at recombinant mouse GPBAR1 expressed in CHO cellsAgonist activity at recombinant mouse GPBAR1 expressed in CHO cells |
ChEMBL | 359 | 6 | 1 | 4 | 4.9 | Cc1ccc(C(C/C(=N\O)c2ccncc2)c2ccc(N(C)C)cc2)cc1 | 10.1016/j.bmcl.2013.06.017 | ||
| CHEMBL2407946 | 91647 | None | 0 | Mouse | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Agonist activity at recombinant mouse GPBAR1 expressed in CHO cellsAgonist activity at recombinant mouse GPBAR1 expressed in CHO cells |
ChEMBL | 359 | 6 | 1 | 4 | 4.9 | Cc1ccc(C(C/C(=N\O)c2ccncc2)c2ccc(N(C)C)cc2)cc1 | 10.1016/j.bmcl.2013.06.017 | ||
| 136166933 | 91649 | None | 0 | Human | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | Agonist activity at recombinant human GPBAR1 expressed in CHO cellsAgonist activity at recombinant human GPBAR1 expressed in CHO cells |
ChEMBL | 394 | 5 | 1 | 3 | 5.6 | Cc1ccccc1C(C/C(=N\O)c1ccncc1)c1ccc(Br)cc1 | 10.1016/j.bmcl.2013.06.017 | ||
| CHEMBL2407949 | 91649 | None | 0 | Human | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | Agonist activity at recombinant human GPBAR1 expressed in CHO cellsAgonist activity at recombinant human GPBAR1 expressed in CHO cells |
ChEMBL | 394 | 5 | 1 | 3 | 5.6 | Cc1ccccc1C(C/C(=N\O)c1ccncc1)c1ccc(Br)cc1 | 10.1016/j.bmcl.2013.06.017 | ||
| 136166936 | 91638 | None | 0 | Mouse | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Agonist activity at recombinant mouse GPBAR1 expressed in CHO cellsAgonist activity at recombinant mouse GPBAR1 expressed in CHO cells |
ChEMBL | 457 | 7 | 2 | 5 | 5.4 | Cc1cc(/C(C[C@@H](c2ccc(N3CCC(C(=O)O)CC3)cc2)c2ccccc2C)=N/O)ccn1 | 10.1016/j.bmcl.2013.06.017 | ||
| CHEMBL2407931 | 91638 | None | 0 | Mouse | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Agonist activity at recombinant mouse GPBAR1 expressed in CHO cellsAgonist activity at recombinant mouse GPBAR1 expressed in CHO cells |
ChEMBL | 457 | 7 | 2 | 5 | 5.4 | Cc1cc(/C(C[C@@H](c2ccc(N3CCC(C(=O)O)CC3)cc2)c2ccccc2C)=N/O)ccn1 | 10.1016/j.bmcl.2013.06.017 | ||
| 56602333 | 91641 | None | 0 | Mouse | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at recombinant mouse GPBAR1 expressed in CHO cellsAgonist activity at recombinant mouse GPBAR1 expressed in CHO cells |
ChEMBL | 424 | 6 | 1 | 6 | 3.5 | Cc1ccccc1[C@H](C/C(=N\O)c1ccc(=O)n(C)c1)c1ccc(S(C)(=O)=O)cc1 | 10.1016/j.bmcl.2013.06.017 | ||
| CHEMBL2407934 | 91641 | None | 0 | Mouse | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at recombinant mouse GPBAR1 expressed in CHO cellsAgonist activity at recombinant mouse GPBAR1 expressed in CHO cells |
ChEMBL | 424 | 6 | 1 | 6 | 3.5 | Cc1ccccc1[C@H](C/C(=N\O)c1ccc(=O)n(C)c1)c1ccc(S(C)(=O)=O)cc1 | 10.1016/j.bmcl.2013.06.017 | ||
| 76328184 | 104273 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at wild type TGR5 (unknown origin)Agonist activity at wild type TGR5 (unknown origin) |
ChEMBL | 391 | 4 | 3 | 3 | 4.6 | CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCN)[C@@H]2[C@@H]1O | 10.1021/ml400247k | ||
| CHEMBL3098607 | 104273 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at wild type TGR5 (unknown origin)Agonist activity at wild type TGR5 (unknown origin) |
ChEMBL | 391 | 4 | 3 | 3 | 4.6 | CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCN)[C@@H]2[C@@H]1O | 10.1021/ml400247k | ||
| 46195563 | 194473 | None | 0 | Human | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | Agonist activity at human TGR5Agonist activity at human TGR5 |
ChEMBL | 455 | 4 | 0 | 5 | 5.0 | O=C(c1cccnc1Oc1cc(Cl)ccc1Cl)N1CCN(C2COC2)c2ccccc21 | 10.1021/acs.jmedchem.5b00342 | ||
| CHEMBL5286949 | 194473 | None | 0 | Human | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | Agonist activity at human TGR5Agonist activity at human TGR5 |
ChEMBL | 455 | 4 | 0 | 5 | 5.0 | O=C(c1cccnc1Oc1cc(Cl)ccc1Cl)N1CCN(C2COC2)c2ccccc21 | 10.1021/acs.jmedchem.5b00342 | ||
| 136166852 | 91668 | None | 0 | Mouse | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Agonist activity at recombinant mouse GPBAR1 expressed in CHO cellsAgonist activity at recombinant mouse GPBAR1 expressed in CHO cells |
ChEMBL | 450 | 7 | 2 | 4 | 6.5 | Cc1cc(/C(C[C@H](c2ccc(-c3ccc(C(=O)O)cc3)cc2)c2ccccc2C)=N/O)ccn1 | 10.1016/j.bmcl.2013.06.017 | ||
| CHEMBL2408107 | 91668 | None | 0 | Mouse | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Agonist activity at recombinant mouse GPBAR1 expressed in CHO cellsAgonist activity at recombinant mouse GPBAR1 expressed in CHO cells |
ChEMBL | 450 | 7 | 2 | 4 | 6.5 | Cc1cc(/C(C[C@H](c2ccc(-c3ccc(C(=O)O)cc3)cc2)c2ccccc2C)=N/O)ccn1 | 10.1016/j.bmcl.2013.06.017 | ||
| 58043414 | 91651 | None | 0 | Mouse | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at recombinant mouse GPBAR1 expressed in CHO cellsAgonist activity at recombinant mouse GPBAR1 expressed in CHO cells |
ChEMBL | 424 | 5 | 1 | 4 | 4.9 | Cc1ccccc1C(C/C(=N\O)c1ccc(=O)n(C)c1)c1ccc(Br)cc1 | 10.1016/j.bmcl.2013.06.017 | ||
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