Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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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
90654600 110064 None 0 Mouse Functional pEC50 = 9 9.0 8 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 577 8 2 6 5.3 N#Cc1ccc(CCNC(=O)[C@@H]2CCN2c2cc(-c3ccc([C@H]4CC[C@H](C(=O)O)CC4)cc3)nc(C(F)(F)F)n2)cc1 10.1021/jm401731q
CHEMBL3234871 110064 None 0 Mouse Functional pEC50 = 9 9.0 8 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 577 8 2 6 5.3 N#Cc1ccc(CCNC(=O)[C@@H]2CCN2c2cc(-c3ccc([C@H]4CC[C@H](C(=O)O)CC4)cc3)nc(C(F)(F)F)n2)cc1 10.1021/jm401731q
162645557 179780 None 0 Human Functional pEC50 = 9.0 9.0 - 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 323 4 0 3 3.9 C[C@H](c1ccccc1)n1cncc1C(=O)N(C)c1ccc(F)cc1 10.1016/j.bmc.2020.115972
CHEMBL4743463 179780 None 0 Human Functional pEC50 = 9.0 9.0 - 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 323 4 0 3 3.9 C[C@H](c1ccccc1)n1cncc1C(=O)N(C)c1ccc(F)cc1 10.1016/j.bmc.2020.115972
162669860 182851 None 0 Human Functional pEC50 = 9.0 9.0 - 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 378 4 0 4 3.6 C[C@H](c1ccccc1)n1cncc1C(=O)N1CCN(c2ccccc2F)CC1 10.1016/j.bmc.2020.115972
CHEMBL4790044 182851 None 0 Human Functional pEC50 = 9.0 9.0 - 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 378 4 0 4 3.6 C[C@H](c1ccccc1)n1cncc1C(=O)N1CCN(c2ccccc2F)CC1 10.1016/j.bmc.2020.115972
71561753 87677 None 0 Human Functional pEC50 = 8.9 8.9 - 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 418 6 0 5 4.9 CCN(Cc1cccnc1)C(=O)c1c(C)nn(C)c1Oc1cccc(Cl)c1Cl 10.1016/j.bmcl.2012.12.076
CHEMBL2336231 87677 None 0 Human Functional pEC50 = 8.9 8.9 - 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 418 6 0 5 4.9 CCN(Cc1cccnc1)C(=O)c1c(C)nn(C)c1Oc1cccc(Cl)c1Cl 10.1016/j.bmcl.2012.12.076
71561756 87679 None 0 Human Functional pEC50 = 8.9 8.9 - 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 446 6 0 5 5.6 Cc1ccc(CN(C(=O)c2c(C)nn(C)c2Oc2cccc(Cl)c2Cl)C(C)C)cn1 10.1016/j.bmcl.2012.12.076
CHEMBL2336233 87679 None 0 Human Functional pEC50 = 8.9 8.9 - 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 446 6 0 5 5.6 Cc1ccc(CN(C(=O)c2c(C)nn(C)c2Oc2cccc(Cl)c2Cl)C(C)C)cn1 10.1016/j.bmcl.2012.12.076
71599441 163648 None 0 Mouse Functional pEC50 = 8.9 8.9 109 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 760 14 6 11 2.6 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(COc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)cc1 10.1021/acs.jmedchem.8b00308
CHEMBL4202981 163648 None 0 Mouse Functional pEC50 = 8.9 8.9 109 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 760 14 6 11 2.6 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(COc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)cc1 10.1021/acs.jmedchem.8b00308
71599441 163648 None 0 Mouse Functional pEC50 = 8.9 8.9 109 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 760 14 6 11 2.6 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(COc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)cc1 10.1021/acs.jmedchem.8b00308
CHEMBL4202981 163648 None 0 Mouse Functional pEC50 = 8.9 8.9 109 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 760 14 6 11 2.6 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(COc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)cc1 10.1021/acs.jmedchem.8b00308
71626700 112272 None 0 Human Functional pEC50 = 8.9 8.9 7 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 445 4 0 5 5.9 O=C(c1cnccc1Oc1cc2ccoc2cc1Cl)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
CHEMBL3290715 112272 None 0 Human Functional pEC50 = 8.9 8.9 7 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 445 4 0 5 5.9 O=C(c1cnccc1Oc1cc2ccoc2cc1Cl)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
71626488 112270 None 0 Human Functional pEC50 = 8.8 8.8 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 426 4 0 6 5.0 Cc1noc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
CHEMBL3290713 112270 None 0 Human Functional pEC50 = 8.8 8.8 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 426 4 0 6 5.0 Cc1noc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
53311869 83037 None 0 Human Functional pEC50 = 8.8 8.8 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 439 4 0 4 5.8 O=C(c1cnccc1Oc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/jm301071h
CHEMBL2181239 83037 None 0 Human Functional pEC50 = 8.8 8.8 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 439 4 0 4 5.8 O=C(c1cnccc1Oc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/jm301071h
118694559 1134 None 3 Human Functional pEC50 = 8.8 8.8 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COC1=C(C=CC=C1)COC(=O)C=2[C@@H](CC(N(C2C)C[C@@H]3OCCC3)=O)C=4C=NC(=CC4)Cl 10.1021/acs.jmedchem.2c01881
12906 1134 None 3 Human Functional pEC50 = 8.8 8.8 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COC1=C(C=CC=C1)COC(=O)C=2[C@@H](CC(N(C2C)C[C@@H]3OCCC3)=O)C=4C=NC(=CC4)Cl 10.1021/acs.jmedchem.2c01881
CHEMBL5434983 1134 None 3 Human Functional pEC50 = 8.8 8.8 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COC1=C(C=CC=C1)COC(=O)C=2[C@@H](CC(N(C2C)C[C@@H]3OCCC3)=O)C=4C=NC(=CC4)Cl 10.1021/acs.jmedchem.2c01881
89501409 161454 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assay
ChEMBL 558 11 0 6 7.5 COc1ccc(C(C)(C)c2cnc(SCCOCc3c(F)cccc3Cl)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2018.04.011
CHEMBL4126062 161454 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assay
ChEMBL 558 11 0 6 7.5 COc1ccc(C(C)(C)c2cnc(SCCOCc3c(F)cccc3Cl)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2018.04.011
71540074 87326 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 453 7 2 6 3.1 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(SC(F)(F)F)cc1)CC2 10.1021/ml300277t
CHEMBL2331649 87326 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 453 7 2 6 3.1 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(SC(F)(F)F)cc1)CC2 10.1021/ml300277t
77845059 112277 None 0 Human Functional pEC50 = 8.8 8.8 22 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 517 6 0 7 6.1 CCOC(=O)c1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
CHEMBL3290720 112277 None 0 Human Functional pEC50 = 8.8 8.8 22 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 517 6 0 7 6.1 CCOC(=O)c1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
71561755 87317 None 0 Human Functional pEC50 = 8.7 8.7 - 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 438 6 0 6 5.3 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N(Cc1cncs1)C(C)C 10.1016/j.bmcl.2012.12.076
CHEMBL2331604 87317 None 0 Human Functional pEC50 = 8.7 8.7 - 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 438 6 0 6 5.3 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N(Cc1cncs1)C(C)C 10.1016/j.bmcl.2012.12.076
76314787 106078 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 382 5 0 5 4.1 COc1cccc(-n2nnc(C3CC3)c2C(=O)N(C)c2ccc(Cl)cc2)c1 10.1039/C2MD20174G
CHEMBL3132966 106078 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 382 5 0 5 4.1 COc1cccc(-n2nnc(C3CC3)c2C(=O)N(C)c2ccc(Cl)cc2)c1 10.1039/C2MD20174G
118103698 163767 None 0 Mouse Functional pEC50 = 8.7 8.7 12 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 724 15 5 10 2.5 CN(C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)C(=O)CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4204655 163767 None 0 Mouse Functional pEC50 = 8.7 8.7 12 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 724 15 5 10 2.5 CN(C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)C(=O)CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
118093476 164198 None 0 Mouse Functional pEC50 = 8.7 8.7 39 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 780 14 6 13 2.1 Cn1c(C(=O)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)cnc1SCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4209669 164198 None 0 Mouse Functional pEC50 = 8.7 8.7 39 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 780 14 6 13 2.1 Cn1c(C(=O)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)cnc1SCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
118104387 164207 None 0 Mouse Functional pEC50 = 8.7 8.7 - 1
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 718 15 4 8 3.0 O=C(O)CNC(=O)CNC(=O)CNC(=O)CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4209799 164207 None 0 Mouse Functional pEC50 = 8.7 8.7 - 1
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 718 15 4 8 3.0 O=C(O)CNC(=O)CNC(=O)CNC(=O)CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
145974037 164849 None 0 Mouse Functional pEC50 = 8.7 8.7 15 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 725 15 7 10 1.9 O=C(NCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4217797 164849 None 0 Mouse Functional pEC50 = 8.7 8.7 15 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 725 15 7 10 1.9 O=C(NCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4212707 215732 None 0 Mouse Functional pEC50 = 8.7 8.7 - 1
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 None None None O=C(O)CNC(=O)[C@H](CSSC[C@H](NC(=O)CCC(NC(=O)CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)C(=O)O)C(=O)NCC(=O)O)NC(=O)CCC(NC(=O)CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)C(=O)O 10.1021/acs.jmedchem.8b00308
91972025 156049 None 0 Mouse Functional pEC50 = 8 8.0 43 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 540 7 0 5 7.8 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4061329 156049 None 0 Mouse Functional pEC50 = 8 8.0 43 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 540 7 0 5 7.8 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
46195848 83043 None 0 Human Functional pEC50 = 8 8.0 257 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 398 3 0 3 5.8 O=C(c1cccnc1Oc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 10.1021/jm301071h
CHEMBL2181246 83043 None 0 Human Functional pEC50 = 8 8.0 257 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 398 3 0 3 5.8 O=C(c1cccnc1Oc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 10.1021/jm301071h
46232694 203370 None 0 Human Functional pEC50 = 8 8.0 - 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 388 5 0 3 5.9 CCCc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL601637 203370 None 0 Human Functional pEC50 = 8 8.0 - 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 388 5 0 3 5.9 CCCc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
46232696 203997 None 0 Human Functional pEC50 = 8 8.0 - 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 388 5 0 3 5.9 CCc1onc(-c2ccccc2Cl)c1C(=O)N(CC)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL605367 203997 None 0 Human Functional pEC50 = 8 8.0 - 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 388 5 0 3 5.9 CCc1onc(-c2ccccc2Cl)c1C(=O)N(CC)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
76318386 106081 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 391 4 0 5 4.3 COc1cccc(-c2noc(C)c2C(=O)N(C)c2ccc(C(F)(F)F)nc2)c1 10.1039/C2MD20174G
CHEMBL3132969 106081 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 391 4 0 5 4.3 COc1cccc(-c2noc(C)c2C(=O)N(C)c2ccc(C(F)(F)F)nc2)c1 10.1039/C2MD20174G
118093484 163618 None 0 Mouse Functional pEC50 = 8 8.0 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 617 8 1 8 5.6 Cn1c(C(=O)O)cnc1SCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4202656 163618 None 0 Mouse Functional pEC50 = 8 8.0 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 617 8 1 8 5.6 Cn1c(C(=O)O)cnc1SCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
118093390 163965 None 0 Mouse Functional pEC50 = 8 8.0 19 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 760 14 6 11 2.6 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(OCc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)cc1 10.1021/acs.jmedchem.8b00308
CHEMBL4206832 163965 None 0 Mouse Functional pEC50 = 8 8.0 19 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 760 14 6 11 2.6 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(OCc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)cc1 10.1021/acs.jmedchem.8b00308
118093562 163982 None 0 Mouse Functional pEC50 = 8 8.0 5 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 547 9 1 5 5.7 O=C(O)CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4207005 163982 None 0 Mouse Functional pEC50 = 8 8.0 5 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 547 9 1 5 5.7 O=C(O)CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
118103738 163983 None 0 Mouse Functional pEC50 = 8 8.0 - 1
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 669 12 4 6 5.0 O=C(NCCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NCP(=O)(O)O 10.1021/acs.jmedchem.8b00308
CHEMBL4207008 163983 None 0 Mouse Functional pEC50 = 8 8.0 - 1
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 669 12 4 6 5.0 O=C(NCCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NCP(=O)(O)O 10.1021/acs.jmedchem.8b00308
118103697 164052 None 0 Mouse Functional pEC50 = 8 8.0 7 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 696 13 5 10 1.7 CN(C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)C(=O)CCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4207801 164052 None 0 Mouse Functional pEC50 = 8 8.0 7 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 696 13 5 10 1.7 CN(C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)C(=O)CCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
118103728 164098 None 0 Mouse Functional pEC50 = 8 8.0 - 1
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 853 20 7 12 1.8 CN(C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)C(=O)CC[C@H](NC(=O)CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)C(=O)O 10.1021/acs.jmedchem.8b00308
CHEMBL4208317 164098 None 0 Mouse Functional pEC50 = 8 8.0 - 1
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 853 20 7 12 1.8 CN(C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)C(=O)CC[C@H](NC(=O)CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)C(=O)O 10.1021/acs.jmedchem.8b00308
71661092 164147 None 0 Mouse Functional pEC50 = 8 8.0 10 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 665 13 5 8 3.2 O=C(NCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC(CO)(CO)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4208999 164147 None 0 Mouse Functional pEC50 = 8 8.0 10 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 665 13 5 8 3.2 O=C(NCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC(CO)(CO)CO 10.1021/acs.jmedchem.8b00308
118103732 164181 None 0 Mouse Functional pEC50 = 8 8.0 - 1
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 648 14 2 7 5.1 O=C(O)CN(CCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)CC(=O)O 10.1021/acs.jmedchem.8b00308
CHEMBL4209515 164181 None 0 Mouse Functional pEC50 = 8 8.0 - 1
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 648 14 2 7 5.1 O=C(O)CN(CCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)CC(=O)O 10.1021/acs.jmedchem.8b00308
71626700 112272 None 0 Mouse Functional pEC50 = 8 8.0 -7 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 445 4 0 5 5.9 O=C(c1cnccc1Oc1cc2ccoc2cc1Cl)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
CHEMBL3290715 112272 None 0 Mouse Functional pEC50 = 8 8.0 -7 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 445 4 0 5 5.9 O=C(c1cnccc1Oc1cc2ccoc2cc1Cl)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
90654593 110024 None 0 Mouse Functional pEC50 = 8 8.0 2 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 530 7 2 7 3.2 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3cc(N4CCC(C(=O)O)CC4)nc(C(F)(F)F)n3)C2)cc1 10.1021/jm401731q
CHEMBL3234580 110024 None 0 Mouse Functional pEC50 = 8 8.0 2 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 530 7 2 7 3.2 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3cc(N4CCC(C(=O)O)CC4)nc(C(F)(F)F)n3)C2)cc1 10.1021/jm401731q
164613236 184612 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 541 4 2 3 8.1 CC(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
CHEMBL4847424 184612 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 541 4 2 3 8.1 CC(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
77846018 195248 None 0 Mouse Functional pEC50 = 8.0 8.0 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 516 7 1 5 6.5 O=C(O)CCc1cc(Cl)c(Oc2ccsc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1016/j.ejmech.2022.114697
CHEMBL5399395 195248 None 0 Mouse Functional pEC50 = 8.0 8.0 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 516 7 1 5 6.5 O=C(O)CCc1cc(Cl)c(Oc2ccsc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1016/j.ejmech.2022.114697
155339362 173191 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 459 5 1 3 5.7 CO[C@@H]1C[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)N3CCCC3)[C@@H]21 10.1021/acs.jmedchem.9b00770
CHEMBL4519993 173191 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 459 5 1 3 5.7 CO[C@@H]1C[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)N3CCCC3)[C@@H]21 10.1021/acs.jmedchem.9b00770
71626492 112263 None 0 Human Functional pEC50 = 8.0 8.0 2 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 411 4 0 5 5.2 O=C(c1cnccc1Oc1ccc2occc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
CHEMBL3290706 112263 None 0 Human Functional pEC50 = 8.0 8.0 2 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 411 4 0 5 5.2 O=C(c1cnccc1Oc1ccc2occc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
168288290 191463 None 0 Human Functional pEC50 = 7 7.0 95 2
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 307 6 0 3 5.0 CCC(C)Oc1cccc(OCc2ccc3ccccc3n2)c1 10.1021/acs.jmedchem.1c01078
CHEMBL5192002 191463 None 0 Human Functional pEC50 = 7 7.0 95 2
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 307 6 0 3 5.0 CCC(C)Oc1cccc(OCc2ccc3ccccc3n2)c1 10.1021/acs.jmedchem.1c01078
156016578 177811 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 399 4 2 3 5.5 C=CC[C@@]1(O)C[C@H]2[C@@H]3CC[C@H]([C@H](C)CC#N)[C@@]3(C)CC[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1021/acsmedchemlett.9b00636
CHEMBL4642126 177811 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 399 4 2 3 5.5 C=CC[C@@]1(O)C[C@H]2[C@@H]3CC[C@H]([C@H](C)CC#N)[C@@]3(C)CC[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1021/acsmedchemlett.9b00636
118093575 163723 None 1 Human Functional pEC50 = 7 7.0 -6 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 463 4 1 5 4.6 O=C([C@@H]1CSCN1Cc1cc(Cl)c(O)cc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4203848 163723 None 1 Human Functional pEC50 = 7 7.0 -6 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 463 4 1 5 4.6 O=C([C@@H]1CSCN1Cc1cc(Cl)c(O)cc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118103679 164043 None 0 Human Functional pEC50 = 7 7.0 -39 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 761 14 6 12 2.0 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(COc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)nc1 10.1021/acs.jmedchem.8b00308
CHEMBL4207707 164043 None 0 Human Functional pEC50 = 7 7.0 -39 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 761 14 6 12 2.0 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(COc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)nc1 10.1021/acs.jmedchem.8b00308
118103700 164078 None 0 Human Functional pEC50 = 7 7.0 -3 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 764 14 6 13 1.4 Cn1nc(C(=O)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)cc1OCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4208057 164078 None 0 Human Functional pEC50 = 7 7.0 -3 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 764 14 6 13 1.4 Cn1nc(C(=O)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)cc1OCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
71661092 164147 None 0 Human Functional pEC50 = 7 7.0 -10 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 665 13 5 8 3.2 O=C(NCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC(CO)(CO)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4208999 164147 None 0 Human Functional pEC50 = 7 7.0 -10 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 665 13 5 8 3.2 O=C(NCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC(CO)(CO)CO 10.1021/acs.jmedchem.8b00308
118103668 164502 None 0 Human Functional pEC50 = 7 7.0 -7 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 741 16 7 11 1.8 O=C(NCCCCOc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4213391 164502 None 0 Human Functional pEC50 = 7 7.0 -7 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 741 16 7 11 1.8 O=C(NCCCCOc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
145972818 164737 None 0 Human Functional pEC50 = 7 7.0 -3 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 734 13 6 12 1.3 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccn(Cc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)n1 10.1021/acs.jmedchem.8b00308
CHEMBL4216361 164737 None 0 Human Functional pEC50 = 7 7.0 -3 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 734 13 6 12 1.3 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccn(Cc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)n1 10.1021/acs.jmedchem.8b00308
118103734 164745 None 0 Human Functional pEC50 = 7 7.0 -25 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 761 14 6 12 2.0 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(OCc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)nc1 10.1021/acs.jmedchem.8b00308
CHEMBL4216584 164745 None 0 Human Functional pEC50 = 7 7.0 -25 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 761 14 6 12 2.0 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(OCc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)nc1 10.1021/acs.jmedchem.8b00308
118694538 196021 None 0 Human Functional pEC50 = 7 7.0 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 6 0 5 3.8 COC(=O)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5415202 196021 None 0 Human Functional pEC50 = 7 7.0 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 6 0 5 3.8 COC(=O)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
46233056 201836 None 0 Human Functional pEC50 = 7 7.0 - 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 394 3 0 3 5.9 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.01.003
CHEMBL590982 201836 None 0 Human Functional pEC50 = 7 7.0 - 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 394 3 0 3 5.9 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.01.003
73357024 92766 None 0 Mouse Functional pEC50 = 7 7.0 -1 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 471 5 1 3 6.4 N#CC(NCc1cnccc1-c1c(F)cccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435926 92766 None 0 Mouse Functional pEC50 = 7 7.0 -1 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 471 5 1 3 6.4 N#CC(NCc1cnccc1-c1c(F)cccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
71660979 163638 None 0 Mouse Functional pEC50 = 7 7.0 -1 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 447 4 0 3 4.9 O=C([C@@H]1C[C@@H](F)CN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4202908 163638 None 0 Mouse Functional pEC50 = 7 7.0 -1 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 447 4 0 3 4.9 O=C([C@@H]1C[C@@H](F)CN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
71660960 163685 None 0 Mouse Functional pEC50 = 7 7.0 1 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 459 5 0 4 4.6 CO[C@@H]1C[C@@H](C(=O)N2CCN(C3CC3)c3ccccc32)N(Cc2cc(Cl)ccc2Cl)C1 10.1021/acs.jmedchem.8b00308
CHEMBL4203445 163685 None 0 Mouse Functional pEC50 = 7 7.0 1 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 459 5 0 4 4.6 CO[C@@H]1C[C@@H](C(=O)N2CCN(C3CC3)c3ccccc32)N(Cc2cc(Cl)ccc2Cl)C1 10.1021/acs.jmedchem.8b00308
71661220 163716 None 0 Mouse Functional pEC50 = 7 7.0 1 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 429 4 0 3 5.0 O=C([C@@H]1CCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4203777 163716 None 0 Mouse Functional pEC50 = 7 7.0 1 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 429 4 0 3 5.0 O=C([C@@H]1CCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
168280068 191298 None 0 Human Functional pEC50 = 6 6.0 5 2
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 293 6 0 3 4.6 CCCOc1cccc(OCc2ccc3ccccc3n2)c1 10.1021/acs.jmedchem.1c01078
CHEMBL5189181 191298 None 0 Human Functional pEC50 = 6 6.0 5 2
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 293 6 0 3 4.6 CCCOc1cccc(OCc2ccc3ccccc3n2)c1 10.1021/acs.jmedchem.1c01078
44457490 158021 None 1 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 458 5 4 5 3.3 C[C@H](CCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](C[C@H](O)[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
CHEMBL408445 158021 None 1 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 458 5 4 5 3.3 C[C@H](CCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](C[C@H](O)[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
118093441 163867 None 0 Human Functional pEC50 = 6 6.0 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 443 4 0 3 5.4 C[C@@]1(C(=O)N2CCN(C3CC3)c3ccccc32)CCCN1Cc1cc(Cl)ccc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4205745 163867 None 0 Human Functional pEC50 = 6 6.0 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 443 4 0 3 5.4 C[C@@]1(C(=O)N2CCN(C3CC3)c3ccccc32)CCCN1Cc1cc(Cl)ccc1Cl 10.1021/acs.jmedchem.8b00308
71661224 164235 None 0 Human Functional pEC50 = 6 6.0 -1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 415 4 0 3 4.6 O=C([C@@H]1CCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4210112 164235 None 0 Human Functional pEC50 = 6 6.0 -1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 415 4 0 3 4.6 O=C([C@@H]1CCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
71660910 164352 None 0 Human Functional pEC50 = 6 6.0 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 418 6 0 3 5.2 CN(C(=O)[C@@H]1CCCN1Cc1cc(Cl)ccc1Cl)c1ccccc1OC1CC1 10.1021/acs.jmedchem.8b00308
CHEMBL4211549 164352 None 0 Human Functional pEC50 = 6 6.0 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 418 6 0 3 5.2 CN(C(=O)[C@@H]1CCCN1Cc1cc(Cl)ccc1Cl)c1ccccc1OC1CC1 10.1021/acs.jmedchem.8b00308
118700253 195316 None 0 Human Functional pEC50 = 6 6.0 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 414 7 0 5 3.7 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccncc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5400773 195316 None 0 Human Functional pEC50 = 6 6.0 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 414 7 0 5 3.7 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccncc2)=C1C 10.1021/acs.jmedchem.2c01881
46232410 203031 None 0 Human Functional pEC50 = 6 6.0 - 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 354 4 0 3 5.1 CCc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL599126 203031 None 0 Human Functional pEC50 = 6 6.0 - 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 354 4 0 3 5.1 CCc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2010.01.003
46232569 203579 None 0 Human Functional pEC50 = 6 6.0 - 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 340 3 0 3 4.9 Cc1ccc(-c2noc(C)c2C(=O)N(C)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL603096 203579 None 0 Human Functional pEC50 = 6 6.0 - 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 340 3 0 3 4.9 Cc1ccc(-c2noc(C)c2C(=O)N(C)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2010.01.003
71660910 164352 None 0 Mouse Functional pEC50 = 6 6.0 -1 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 418 6 0 3 5.2 CN(C(=O)[C@@H]1CCCN1Cc1cc(Cl)ccc1Cl)c1ccccc1OC1CC1 10.1021/acs.jmedchem.8b00308
CHEMBL4211549 164352 None 0 Mouse Functional pEC50 = 6 6.0 -1 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 418 6 0 3 5.2 CN(C(=O)[C@@H]1CCCN1Cc1cc(Cl)ccc1Cl)c1ccccc1OC1CC1 10.1021/acs.jmedchem.8b00308
89651284 164741 None 0 Mouse Functional pEC50 = 6 6.0 -1 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 432 6 0 3 5.6 CN(C(=O)[C@@H]1CCCN1Cc1cc(Cl)ccc1Cl)c1ccccc1OC1CCC1 10.1021/acs.jmedchem.8b00308
CHEMBL4216520 164741 None 0 Mouse Functional pEC50 = 6 6.0 -1 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 432 6 0 3 5.6 CN(C(=O)[C@@H]1CCCN1Cc1cc(Cl)ccc1Cl)c1ccccc1OC1CCC1 10.1021/acs.jmedchem.8b00308
118694374 194957 None 0 Mouse Functional pEC50 = 6 6.0 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 413 7 0 4 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5394113 194957 None 0 Mouse Functional pEC50 = 6 6.0 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 413 7 0 4 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694581 194966 None 0 Mouse Functional pEC50 = 6 6.0 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 393 5 0 3 4.3 C#CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5394245 194966 None 0 Mouse Functional pEC50 = 6 6.0 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 393 5 0 3 4.3 C#CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694430 195107 None 0 Mouse Functional pEC50 = 6 6.0 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 383 5 0 3 4.7 CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5396796 195107 None 0 Mouse Functional pEC50 = 6 6.0 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 383 5 0 3 4.7 CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694576 195995 None 0 Mouse Functional pEC50 = 6 6.0 -3 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2Cl)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5414847 195995 None 0 Mouse Functional pEC50 = 6 6.0 -3 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2Cl)=C1C 10.1021/acs.jmedchem.2c01881
118694569 196448 None 0 Mouse Functional pEC50 = 6 6.0 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 441 9 0 4 4.8 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCCCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5424150 196448 None 0 Mouse Functional pEC50 = 6 6.0 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 441 9 0 4 4.8 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCCCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694370 197118 None 0 Mouse Functional pEC50 = 6 6.0 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 411 7 0 3 5.5 CCCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5439183 197118 None 0 Mouse Functional pEC50 = 6 6.0 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 411 7 0 3 5.5 CCCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694489 195118 None 0 Mouse Functional pEC50 = 5 5.0 -8 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 497 8 0 5 5.2 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC(F)(F)F)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5396998 195118 None 0 Mouse Functional pEC50 = 5 5.0 -8 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 497 8 0 5 5.2 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC(F)(F)F)=C1C 10.1021/acs.jmedchem.2c01881
45483949 3582 None 33 Human Functional pEC50 = 6 6.0 -2 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 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2020.112619
7048 3582 None 33 Human Functional pEC50 = 6 6.0 -2 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 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2020.112619
CHEMBL567640 3582 None 33 Human Functional pEC50 = 6 6.0 -2 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 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2020.112619
439763 158218 None 15 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 483 7 3 4 4.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1039/d0md00425a
CHEMBL408701 158218 None 15 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 483 7 3 4 4.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1039/d0md00425a
90644448 112293 None 0 Mouse Functional pEC50 = 7 7.0 -2 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 531 7 1 6 6.2 Cc1c(CCC(=O)O)oc2ccc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c12 10.1016/j.ejmech.2014.05.031
CHEMBL3290736 112293 None 0 Mouse Functional pEC50 = 7 7.0 -2 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 531 7 1 6 6.2 Cc1c(CCC(=O)O)oc2ccc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c12 10.1016/j.ejmech.2014.05.031
76314788 106079 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 383 5 0 6 3.5 COc1cccc(-n2nnc(C3CC3)c2C(=O)N(C)c2ccc(Cl)cn2)c1 10.1039/C2MD20174G
CHEMBL3132967 106079 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 383 5 0 6 3.5 COc1cccc(-n2nnc(C3CC3)c2C(=O)N(C)c2ccc(Cl)cn2)c1 10.1039/C2MD20174G
71561884 87682 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 430 6 0 5 5.0 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N(Cc1cccnc1)C1CC1 10.1016/j.bmcl.2012.12.076
CHEMBL2336236 87682 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 430 6 0 5 5.0 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N(Cc1cccnc1)C1CC1 10.1016/j.bmcl.2012.12.076
101886302 114974 None 36 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at GP-BAR1 (unknown origin) in human HEK293 cells assessed as receptor transactivation at 100 nM to 50 uM incubated for 16 hrs by CRE-driven luciferase reporter gene assayAgonist activity at GP-BAR1 (unknown origin) in human HEK293 cells assessed as receptor transactivation at 100 nM to 50 uM incubated for 16 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 406 5 3 3 5.0 CC[C@@H]1[C@H](O)[C@@H]2[C@H](CC[C@@]3(C)[C@H]2CC[C@@H]3[C@H](C)CCCO)[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1021/jm501273r
CHEMBL3342082 114974 None 36 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at GP-BAR1 (unknown origin) in human HEK293 cells assessed as receptor transactivation at 100 nM to 50 uM incubated for 16 hrs by CRE-driven luciferase reporter gene assayAgonist activity at GP-BAR1 (unknown origin) in human HEK293 cells assessed as receptor transactivation at 100 nM to 50 uM incubated for 16 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 406 5 3 3 5.0 CC[C@@H]1[C@H](O)[C@@H]2[C@H](CC[C@@]3(C)[C@H]2CC[C@@H]3[C@H](C)CCCO)[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1021/jm501273r
136166966 91645 None 0 Human Functional pEC50 = 6.0 6.0 4 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
ChEMBL 359 6 1 4 4.9 Cc1ccccc1C(C/C(=N\O)c1ccncc1)c1ccc(N(C)C)cc1 10.1016/j.bmcl.2013.06.017
CHEMBL2407944 91645 None 0 Human Functional pEC50 = 6.0 6.0 4 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
ChEMBL 359 6 1 4 4.9 Cc1ccccc1C(C/C(=N\O)c1ccncc1)c1ccc(N(C)C)cc1 10.1016/j.bmcl.2013.06.017
3945 625 None 56 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 456 2 2 2 7.1 CC(=C)[C@@H]1CC[C@]2([C@H]1[C@H]1CC[C@H]3[C@@]([C@]1(C)CC2)(C)CC[C@@H]1[C@]3(C)CC[C@@H](C1(C)C)O)C(=O)O 10.1021/jm900872z
64971 625 None 56 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 456 2 2 2 7.1 CC(=C)[C@@H]1CC[C@]2([C@H]1[C@H]1CC[C@H]3[C@@]([C@]1(C)CC2)(C)CC[C@@H]1[C@]3(C)CC[C@@H](C1(C)C)O)C(=O)O 10.1021/jm900872z
CHEMBL269277 625 None 56 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 456 2 2 2 7.1 CC(=C)[C@@H]1CC[C@]2([C@H]1[C@H]1CC[C@H]3[C@@]([C@]1(C)CC2)(C)CC[C@@H]1[C@]3(C)CC[C@@H](C1(C)C)O)C(=O)O 10.1021/jm900872z
DB12480 625 None 56 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 456 2 2 2 7.1 CC(=C)[C@@H]1CC[C@]2([C@H]1[C@H]1CC[C@H]3[C@@]([C@]1(C)CC2)(C)CC[C@@H]1[C@]3(C)CC[C@@H](C1(C)C)O)C(=O)O 10.1021/jm900872z
9929677 157777 None 4 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 378 3 3 3 4.1 C[C@H](CC(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
CHEMBL408175 157777 None 4 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 378 3 3 3 4.1 C[C@H](CC(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
71561753 87677 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 418 6 0 5 4.9 CCN(Cc1cccnc1)C(=O)c1c(C)nn(C)c1Oc1cccc(Cl)c1Cl 10.1016/j.bmcl.2012.12.076
CHEMBL2336231 87677 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 418 6 0 5 4.9 CCN(Cc1cccnc1)C(=O)c1c(C)nn(C)c1Oc1cccc(Cl)c1Cl 10.1016/j.bmcl.2012.12.076
67922813 117739 None 1 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 406 4 3 3 4.7 C[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C)C(=O)O 10.1016/j.bmc.2015.01.048
CHEMBL3401352 117739 None 1 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 406 4 3 3 4.7 C[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C)C(=O)O 10.1016/j.bmc.2015.01.048
71561885 87683 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 460 6 0 6 4.7 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N(Cc1cccnc1)C1CCOC1 10.1016/j.bmcl.2012.12.076
CHEMBL2336237 87683 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 460 6 0 6 4.7 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N(Cc1cccnc1)C1CCOC1 10.1016/j.bmcl.2012.12.076
118464662 159232 None 0 Mouse Functional pEC50 = 6.0 6.0 22 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 687 16 0 8 7.3 COc1cc(C2(C)CCCc3nc(SCc4c(F)cc(OCCOCCOCCN(C)C)cc4F)n(-c4ccc(F)cc4)c32)ccc1F 10.1021/acsmedchemlett.7b00116
CHEMBL4097990 159232 None 0 Mouse Functional pEC50 = 6.0 6.0 22 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 687 16 0 8 7.3 COc1cc(C2(C)CCCc3nc(SCc4c(F)cc(OCCOCCOCCN(C)C)cc4F)n(-c4ccc(F)cc4)c32)ccc1F 10.1021/acsmedchemlett.7b00116
73353937 92758 None 0 Mouse Functional pEC50 = 6.0 6.0 -20 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 588 6 0 5 7.0 O=C(c1ccsc1)N(Cc1cnccc1-c1ccccc1F)S(=O)(=O)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435914 92758 None 0 Mouse Functional pEC50 = 6.0 6.0 -20 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 588 6 0 5 7.0 O=C(c1ccsc1)N(Cc1cnccc1-c1ccccc1F)S(=O)(=O)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
94192 17029 None 13 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 388 4 1 3 4.9 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@@H]3C(=O)C[C@@H]4CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/j.bmc.2015.01.048
CHEMBL1254261 17029 None 13 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 388 4 1 3 4.9 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@@H]3C(=O)C[C@@H]4CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/j.bmc.2015.01.048
90654598 110062 None 0 Human Functional pEC50 = 8.0 8.0 -21 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 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 Human Functional pEC50 = 8.0 8.0 -21 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 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
76336516 106083 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 405 5 0 5 4.6 CCc1onc(-c2cccc(OC)c2)c1C(=O)N(C)c1ccc(C(F)(F)F)nc1 10.1039/C2MD20174G
CHEMBL3132970 106083 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 405 5 0 5 4.6 CCc1onc(-c2cccc(OC)c2)c1C(=O)N(C)c1ccc(C(F)(F)F)nc1 10.1039/C2MD20174G
90654585 110009 None 0 Mouse Functional pEC50 = 8.0 8.0 -2 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 465 6 1 7 2.1 Cc1nc(N2CCC[C@@H](C(=O)NCCc3ccc(C#N)cc3)C2)nc(N2CCN(C)CC2)c1F 10.1021/jm401731q
CHEMBL3234566 110009 None 0 Mouse Functional pEC50 = 8.0 8.0 -2 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 465 6 1 7 2.1 Cc1nc(N2CCC[C@@H](C(=O)NCCc3ccc(C#N)cc3)C2)nc(N2CCN(C)CC2)c1F 10.1021/jm401731q
77846018 195248 None 0 Human Functional pEC50 = 8.0 8.0 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 516 7 1 5 6.5 O=C(O)CCc1cc(Cl)c(Oc2ccsc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1016/j.ejmech.2022.114697
CHEMBL5399395 195248 None 0 Human Functional pEC50 = 8.0 8.0 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 516 7 1 5 6.5 O=C(O)CCc1cc(Cl)c(Oc2ccsc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1016/j.ejmech.2022.114697
71540073 87325 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human TGR5 in human PBMC cells assessed as increase in intracellular cAMP measured after 1 hr by human whole blood assayAgonist activity at human TGR5 in human PBMC cells assessed as increase in intracellular cAMP measured after 1 hr by human whole blood assay
ChEMBL 437 7 2 6 2.4 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1021/ml300277t
CHEMBL2331648 87325 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human TGR5 in human PBMC cells assessed as increase in intracellular cAMP measured after 1 hr by human whole blood assayAgonist activity at human TGR5 in human PBMC cells assessed as increase in intracellular cAMP measured after 1 hr by human whole blood assay
ChEMBL 437 7 2 6 2.4 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1021/ml300277t
118700249 196340 None 0 Human Functional pEC50 = 7.0 7.0 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5421793 196340 None 0 Human Functional pEC50 = 7.0 7.0 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
101886309 114975 None 29 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assayAgonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assay
ChEMBL 392 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)CCO)[C@@H]2[C@@H]1O 10.1016/j.ejmech.2022.114652
CHEMBL3342086 114975 None 29 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assayAgonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assay
ChEMBL 392 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)CCO)[C@@H]2[C@@H]1O 10.1016/j.ejmech.2022.114652
118694376 197153 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 355 4 0 3 3.9 CN1C=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC1=O 10.1021/acs.jmedchem.2c01881
CHEMBL5439939 197153 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 355 4 0 3 3.9 CN1C=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC1=O 10.1021/acs.jmedchem.2c01881
118694453 196864 None 0 Mouse Functional pEC50 = 6.0 6.0 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 409 6 0 3 5.2 C=C(C)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5433643 196864 None 0 Mouse Functional pEC50 = 6.0 6.0 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 409 6 0 3 5.2 C=C(C)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
71626765 118888 None 0 Mouse Functional pEC50 = 5.0 5.0 -2 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 539 8 0 6 6.3 CCOC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421893 118888 None 0 Mouse Functional pEC50 = 5.0 5.0 -2 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 539 8 0 6 6.3 CCOC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
118586281 158655 None 0 Human Functional pEC50 = 6.0 6.0 -7 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 455 7 0 5 6.4 COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.6b01873
CHEMBL4091702 158655 None 0 Human Functional pEC50 = 6.0 6.0 -7 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 455 7 0 5 6.4 COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.6b01873
126673489 156763 None 0 Human Functional pEC50 = 6.0 6.0 -13 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 571 11 0 8 6.5 COC(=O)CCc1nc(SCc2c(F)cccc2F)n(-c2ccc(F)cc2)c1N(C)c1ccc(OC)c(OC)c1 10.1021/acs.jmedchem.6b01873
CHEMBL4069569 156763 None 0 Human Functional pEC50 = 6.0 6.0 -13 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 571 11 0 8 6.5 COC(=O)CCc1nc(SCc2c(F)cccc2F)n(-c2ccc(F)cc2)c1N(C)c1ccc(OC)c(OC)c1 10.1021/acs.jmedchem.6b01873
71540174 87331 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 438 7 1 6 2.4 CCOc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1021/ml300277t
CHEMBL2331654 87331 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 438 7 1 6 2.4 CCOc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1021/ml300277t
71561370 87664 None 0 Human Functional pEC50 = 7.0 7.0 - 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 424 4 0 5 5.2 Cc1ccc(Oc2c(C(=O)N3CCCCC3c3cccnc3)c(C)nn2C)c(Cl)c1 10.1016/j.bmcl.2012.12.076
CHEMBL2336215 87664 None 0 Human Functional pEC50 = 7.0 7.0 - 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 424 4 0 5 5.2 Cc1ccc(Oc2c(C(=O)N3CCCCC3c3cccnc3)c(C)nn2C)c(Cl)c1 10.1016/j.bmcl.2012.12.076
156705090 181813 None 0 Mouse Functional pEC50 = 6.9 6.9 -54 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 497 7 0 7 5.8 CCCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4776876 181813 None 0 Mouse Functional pEC50 = 6.9 6.9 -54 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 497 7 0 7 5.8 CCCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
164621408 185857 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 436 5 4 4 3.9 CC[C@H]1[C@@H](O)[C@@H]2[C@H](C[C@H](O)[C@H]3[C@H]2CC[C@@H]3[C@H](C)C[C@H](C)C(=O)O)[C@@]2(C)CC[C@@H](O)C[C@H]12 10.1021/acs.jmedchem.1c00851
CHEMBL4866257 185857 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 436 5 4 4 3.9 CC[C@H]1[C@@H](O)[C@@H]2[C@H](C[C@H](O)[C@H]3[C@H]2CC[C@@H]3[C@H](C)C[C@H](C)C(=O)O)[C@@]2(C)CC[C@@H](O)C[C@H]12 10.1021/acs.jmedchem.1c00851
137629931 161110 None 0 Mouse Functional pEC50 = 4.9 4.9 1 2
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 739 18 1 9 6.4 COc1ccc(SCc2cnc(SCc3c(F)cc(S(=O)(=O)N(CCCO)CCC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4064764 161110 None 0 Mouse Functional pEC50 = 4.9 4.9 1 2
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 739 18 1 9 6.4 COc1ccc(SCc2cnc(SCc3c(F)cc(S(=O)(=O)N(CCCO)CCC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4116312 161110 None 0 Mouse Functional pEC50 = 4.9 4.9 1 2
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 739 18 1 9 6.4 COc1ccc(SCc2cnc(SCc3c(F)cc(S(=O)(=O)N(CCCO)CCC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
155669593 183328 None 0 Human Functional pEC50 = 6.9 6.9 31 2
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 392 4 0 4 4.2 O=C(c1cncn1Cc1ccccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
CHEMBL4796107 183328 None 0 Human Functional pEC50 = 6.9 6.9 31 2
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 392 4 0 4 4.2 O=C(c1cncn1Cc1ccccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
3035026 95837 None 27 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 449 6 4 4 3.6 C[C@H](CCC(=O)NCC(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@@]21C 10.1021/jm7015864
CHEMBL258605 95837 None 27 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 449 6 4 4 3.6 C[C@H](CCC(=O)NCC(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@@]21C 10.1021/jm7015864
73353943 92784 None 0 Mouse Functional pEC50 = 5.9 5.9 -3 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 518 6 0 3 7.8 CC(c1cc(C(F)(F)F)cc(C(F)(F)F)c1)N(Cc1cnccc1-c1ccccc1)C(=O)c1ccco1 10.1016/j.ejmech.2013.07.050
CHEMBL2435945 92784 None 0 Mouse Functional pEC50 = 5.9 5.9 -3 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 518 6 0 3 7.8 CC(c1cc(C(F)(F)F)cc(C(F)(F)F)c1)N(Cc1cnccc1-c1ccccc1)C(=O)c1ccco1 10.1016/j.ejmech.2013.07.050
90327533 112287 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 602 10 1 8 5.5 CCOC(=O)CNC(=O)CCc1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
CHEMBL3290730 112287 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 602 10 1 8 5.5 CCOC(=O)CNC(=O)CCc1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
126673464 159257 None 0 Mouse Functional pEC50 = 6.9 6.9 - 1
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 556 12 1 7 6.6 COc1ccc(N(C)c2c(CCCCN)nc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4098315 159257 None 0 Mouse Functional pEC50 = 6.9 6.9 - 1
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 556 12 1 7 6.6 COc1ccc(N(C)c2c(CCCCN)nc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
71561368 87662 None 0 Human Functional pEC50 = 7.9 7.9 - 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 444 4 0 5 5.6 Cc1nn(C)c(Oc2ccc(Cl)cc2Cl)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336213 87662 None 0 Human Functional pEC50 = 7.9 7.9 - 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 444 4 0 5 5.6 Cc1nn(C)c(Oc2ccc(Cl)cc2Cl)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
118709772 113624 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 460 4 0 6 5.4 CSc1ncc(C(=O)N2CCN(C)c3ccccc32)c(Oc2cc(Cl)ccc2Cl)n1 10.1016/j.bmcl.2014.07.026
CHEMBL3321843 113624 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 460 4 0 6 5.4 CSc1ncc(C(=O)N2CCN(C)c3ccccc32)c(Oc2cc(Cl)ccc2Cl)n1 10.1016/j.bmcl.2014.07.026
71455632 83020 None 0 Human Functional pEC50 = 7.9 7.9 2 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 401 5 0 5 4.5 COc1cccc(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)c1 10.1021/jm301071h
CHEMBL2181223 83020 None 0 Human Functional pEC50 = 7.9 7.9 2 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 401 5 0 5 4.5 COc1cccc(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)c1 10.1021/jm301071h
71455633 83021 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 431 6 0 6 4.5 COc1ccc(OC)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)c1 10.1021/jm301071h
CHEMBL2181224 83021 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 431 6 0 6 4.5 COc1ccc(OC)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)c1 10.1021/jm301071h
71457418 83022 None 0 Human Functional pEC50 = 7.9 7.9 1 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 385 4 0 4 4.8 Cc1ccc(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1 10.1021/jm301071h
CHEMBL2181225 83022 None 0 Human Functional pEC50 = 7.9 7.9 1 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 385 4 0 4 4.8 Cc1ccc(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1 10.1021/jm301071h
90654594 110025 None 0 Human Functional pEC50 = 7.9 7.9 -3 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 544 7 2 7 3.6 CC1(C(=O)O)CCN(c2cc(N3CCC[C@@H](C(=O)NCCc4ccc(C#N)cc4)C3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
CHEMBL3234581 110025 None 0 Human Functional pEC50 = 7.9 7.9 -3 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 544 7 2 7 3.6 CC1(C(=O)O)CCN(c2cc(N3CCC[C@@H](C(=O)NCCc4ccc(C#N)cc4)C3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
118576974 157279 None 0 Mouse Functional pEC50 = 7.9 7.9 10 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 467 8 0 6 6.2 COc1ccc(N(C)c2cnc(SCc3ccccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4075688 157279 None 0 Mouse Functional pEC50 = 7.9 7.9 10 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 467 8 0 6 6.2 COc1ccc(N(C)c2cnc(SCc3ccccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
46232360 201771 None 0 Human Functional pEC50 = 7.9 7.9 - 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 496 3 0 3 6.4 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1cc(Br)c(C)c(Br)c1 10.1016/j.bmcl.2010.01.003
CHEMBL590495 201771 None 0 Human Functional pEC50 = 7.9 7.9 - 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 496 3 0 3 6.4 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1cc(Br)c(C)c(Br)c1 10.1016/j.bmcl.2010.01.003
46232566 203268 None 0 Human Functional pEC50 = 7.9 7.9 - 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 360 3 0 3 5.2 Cc1onc(-c2ccc(Cl)cc2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL600821 203268 None 0 Human Functional pEC50 = 7.9 7.9 - 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 360 3 0 3 5.2 Cc1onc(-c2ccc(Cl)cc2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
46232532 203343 None 0 Human Functional pEC50 = 7.9 7.9 - 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 360 3 0 3 5.2 Cc1onc(-c2cccc(Cl)c2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL601441 203343 None 0 Human Functional pEC50 = 7.9 7.9 - 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 360 3 0 3 5.2 Cc1onc(-c2cccc(Cl)c2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
46232736 203765 None 0 Human Functional pEC50 = 7.9 7.9 - 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 340 4 0 4 3.8 CCc1nnn(-c2ccccc2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL604131 203765 None 0 Human Functional pEC50 = 7.9 7.9 - 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 340 4 0 4 3.8 CCc1nnn(-c2ccccc2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
46232567 203838 None 0 Human Functional pEC50 = 7.9 7.9 - 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 340 3 0 3 4.9 Cc1ccccc1-c1noc(C)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL604537 203838 None 0 Human Functional pEC50 = 7.9 7.9 - 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 340 3 0 3 4.9 Cc1ccccc1-c1noc(C)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
118103692 164491 None 0 Mouse Functional pEC50 = 7.9 7.9 - 1
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 768 17 6 11 1.9 O=C(O)CN(C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)C(=O)CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4213249 164491 None 0 Mouse Functional pEC50 = 7.9 7.9 - 1
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 768 17 6 11 1.9 O=C(O)CN(C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)C(=O)CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
118103668 164502 None 0 Mouse Functional pEC50 = 7.9 7.9 7 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 741 16 7 11 1.8 O=C(NCCCCOc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4213391 164502 None 0 Mouse Functional pEC50 = 7.9 7.9 7 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 741 16 7 11 1.8 O=C(NCCCCOc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
44627312 201446 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 496 4 2 2 8.0 C=CC[C@]1(O)CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(=C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/jm900872z
CHEMBL585494 201446 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 496 4 2 2 8.0 C=CC[C@]1(O)CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(=C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/jm900872z
74766512 157539 None 0 Mouse Functional pEC50 = 6.9 6.9 3 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 699 17 0 9 7.2 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cc(OCCOCCOCCN(C)C)cc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4079040 157539 None 0 Mouse Functional pEC50 = 6.9 6.9 3 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 699 17 0 9 7.2 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cc(OCCOCCOCCN(C)C)cc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
118464638 159629 None 0 Mouse Functional pEC50 = 6.9 6.9 15 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 494 6 0 6 6.4 COc1cc(C2(C)CCCc3nc(SCc4ncccn4)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4102357 159629 None 0 Mouse Functional pEC50 = 6.9 6.9 15 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 494 6 0 6 6.4 COc1cc(C2(C)CCCc3nc(SCc4ncccn4)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
71720725 87685 None 0 Human Functional pEC50 = 6.9 6.9 - 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 428 4 0 5 5.1 Cc1nn(C)c(Oc2cccc(Cl)c2F)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336239 87685 None 0 Human Functional pEC50 = 6.9 6.9 - 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 428 4 0 5 5.1 Cc1nn(C)c(Oc2cccc(Cl)c2F)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
5284060 97547 None 8 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 378 4 3 3 4.4 C[C@H](CCCO)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
CHEMBL270287 97547 None 8 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 378 4 3 3 4.4 C[C@H](CCCO)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
73350995 92782 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 520 6 0 3 7.7 O=C(c1ccsc1)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
CHEMBL2435943 92782 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 520 6 0 3 7.7 O=C(c1ccsc1)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
118694344 195706 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5409356 195706 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
90654577 110001 None 0 Mouse Functional pEC50 = 6.9 6.9 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 358 5 1 4 3.0 Cc1nccc(N2CCC[C@@H](C(=O)NCCc3ccc(Cl)cc3)C2)n1 10.1021/jm401731q
CHEMBL3234558 110001 None 0 Mouse Functional pEC50 = 6.9 6.9 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 358 5 1 4 3.0 Cc1nccc(N2CCC[C@@H](C(=O)NCCc3ccc(Cl)cc3)C2)n1 10.1021/jm401731q
118694344 195706 None 0 Mouse Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5409356 195706 None 0 Mouse Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
156020210 178251 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 401 4 2 3 5.7 CCC[C@]1(O)C[C@H]2[C@@H]3CC[C@H]([C@H](C)CC#N)[C@@]3(C)CC[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1021/acsmedchemlett.9b00636
CHEMBL4648823 178251 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 401 4 2 3 5.7 CCC[C@]1(O)C[C@H]2[C@@H]3CC[C@H]([C@H](C)CC#N)[C@@]3(C)CC[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1021/acsmedchemlett.9b00636
118700209 196039 None 0 Human Functional pEC50 = 5.9 5.9 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2C(F)(F)F)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5415630 196039 None 0 Human Functional pEC50 = 5.9 5.9 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2C(F)(F)F)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL4574407 216489 None 7 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL None None None CC1=C(C(=O)OCc2ccccc2)C(c2ccc(C(F)(F)F)cc2)CC(=O)N1 10.1021/acs.jmedchem.2c01881
118694489 195118 None 0 Mouse Functional pEC50 = 5.9 5.9 -8 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 497 8 0 5 5.2 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC(F)(F)F)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5396998 195118 None 0 Mouse Functional pEC50 = 5.9 5.9 -8 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 497 8 0 5 5.2 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC(F)(F)F)=C1C 10.1021/acs.jmedchem.2c01881
118694423 197114 None 0 Mouse Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 419 7 0 4 4.7 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCC2CCCCC2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5439109 197114 None 0 Mouse Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 419 7 0 4 4.7 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCC2CCCCC2)=C1C 10.1021/acs.jmedchem.2c01881
71626833 118891 None 0 Human Functional pEC50 = 4.9 4.9 1 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 610 11 1 7 5.8 CCOC(=O)CCNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421897 118891 None 0 Human Functional pEC50 = 4.9 4.9 1 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 610 11 1 7 5.8 CCOC(=O)CCNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
118735268 118898 None 0 Mouse Functional pEC50 = 4.9 4.9 2 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 1398 41 2 18 10.9 O=C(CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421904 118898 None 0 Mouse Functional pEC50 = 4.9 4.9 2 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 1398 41 2 18 10.9 O=C(CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
172463152 196656 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 462 6 1 5 5.2 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC(=O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)OC(C)C)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
CHEMBL5429083 196656 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 462 6 1 5 5.2 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC(=O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)OC(C)C)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
71626559 112265 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 410 4 1 4 5.0 O=C(c1cnccc1Oc1ccc2[nH]ccc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
CHEMBL3290708 112265 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 410 4 1 4 5.0 O=C(c1cnccc1Oc1ccc2[nH]ccc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
118721858 116152 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 389 3 1 3 3.3 CN1CCN(C(=O)C2(C(=O)Nc3cc(F)c(F)cc3F)CC2)c2ccccc21 10.1016/j.bmcl.2014.07.026
CHEMBL3356914 116152 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 389 3 1 3 3.3 CN1CCN(C(=O)C2(C(=O)Nc3cc(F)c(F)cc3F)CC2)c2ccccc21 10.1016/j.bmcl.2014.07.026
164609554 184519 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 543 4 2 3 8.3 CC(C)NC(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
CHEMBL4846090 184519 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 543 4 2 3 8.3 CC(C)NC(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
45483949 3582 None 33 Human Functional pEC50 = 5.9 5.9 -2 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2013.07.050
7048 3582 None 33 Human Functional pEC50 = 5.9 5.9 -2 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2013.07.050
CHEMBL567640 3582 None 33 Human Functional pEC50 = 5.9 5.9 -2 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2013.07.050
73353944 92785 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 532 7 0 3 8.2 CCC(c1cc(C(F)(F)F)cc(C(F)(F)F)c1)N(Cc1cnccc1-c1ccccc1)C(=O)c1ccco1 10.1016/j.ejmech.2013.07.050
CHEMBL2435946 92785 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 532 7 0 3 8.2 CCC(c1cc(C(F)(F)F)cc(C(F)(F)F)c1)N(Cc1cnccc1-c1ccccc1)C(=O)c1ccco1 10.1016/j.ejmech.2013.07.050
118700249 196340 None 0 Mouse Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5421793 196340 None 0 Mouse Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
118455158 157671 None 0 Mouse Functional pEC50 = 6.9 6.9 100 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 526 7 0 5 7.6 COc1ccc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4080612 157671 None 0 Mouse Functional pEC50 = 6.9 6.9 100 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 526 7 0 5 7.6 COc1ccc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
71599441 163648 None 0 Human Functional pEC50 = 6.9 6.9 -109 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 760 14 6 11 2.6 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(COc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)cc1 10.1021/acs.jmedchem.8b00308
CHEMBL4202981 163648 None 0 Human Functional pEC50 = 6.9 6.9 -109 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 760 14 6 11 2.6 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(COc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)cc1 10.1021/acs.jmedchem.8b00308
118093493 163667 None 0 Human Functional pEC50 = 6.9 6.9 3 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 664 13 6 9 1.5 O=C(CCc1cc(Cl)c(CN2CCC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4203191 163667 None 0 Human Functional pEC50 = 6.9 6.9 3 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 664 13 6 9 1.5 O=C(CCc1cc(Cl)c(CN2CCC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
71660960 163685 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 459 5 0 4 4.6 CO[C@@H]1C[C@@H](C(=O)N2CCN(C3CC3)c3ccccc32)N(Cc2cc(Cl)ccc2Cl)C1 10.1021/acs.jmedchem.8b00308
CHEMBL4203445 163685 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 459 5 0 4 4.6 CO[C@@H]1C[C@@H](C(=O)N2CCN(C3CC3)c3ccccc32)N(Cc2cc(Cl)ccc2Cl)C1 10.1021/acs.jmedchem.8b00308
145978106 163920 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 539 4 0 4 4.8 O=C([C@@H]1CSCN1Cc1cc(I)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4206320 163920 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 539 4 0 4 4.8 O=C([C@@H]1CSCN1Cc1cc(I)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118093410 164879 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 465 4 0 3 5.2 O=C([C@@H]1CC(F)(F)CN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4218210 164879 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 465 4 0 3 5.2 O=C([C@@H]1CC(F)(F)CN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118694344 195706 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5409356 195706 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
118700249 196340 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5421793 196340 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
46233022 203220 None 0 Human Functional pEC50 = 6.9 6.9 - 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 452 3 0 3 5.2 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(I)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL600421 203220 None 0 Human Functional pEC50 = 6.9 6.9 - 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 452 3 0 3 5.2 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(I)cc1 10.1016/j.bmcl.2010.01.003
46233052 203247 None 0 Human Functional pEC50 = 6.9 6.9 - 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 340 3 0 3 4.9 Cc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL600629 203247 None 0 Human Functional pEC50 = 6.9 6.9 - 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 340 3 0 3 4.9 Cc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2010.01.003
145978106 163920 None 0 Mouse Functional pEC50 = 6.9 6.9 -1 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 539 4 0 4 4.8 O=C([C@@H]1CSCN1Cc1cc(I)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4206320 163920 None 0 Mouse Functional pEC50 = 6.9 6.9 -1 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 539 4 0 4 4.8 O=C([C@@H]1CSCN1Cc1cc(I)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118093410 164879 None 0 Mouse Functional pEC50 = 6.9 6.9 -1 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 465 4 0 3 5.2 O=C([C@@H]1CC(F)(F)CN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4218210 164879 None 0 Mouse Functional pEC50 = 6.9 6.9 -1 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 465 4 0 3 5.2 O=C([C@@H]1CC(F)(F)CN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118700249 196340 None 0 Mouse Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5421793 196340 None 0 Mouse Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
222528 1368 None 55 Human Functional pEC50 = 5.9 5.9 144 2
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 392 4 3 3 4.5 O[C@@H]1CC[C@]2([C@@H](C1)CC[C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)C 10.1021/jm7015864
4988 1368 None 55 Human Functional pEC50 = 5.9 5.9 144 2
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 392 4 3 3 4.5 O[C@@H]1CC[C@]2([C@@H](C1)CC[C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)C 10.1021/jm7015864
610 1368 None 55 Human Functional pEC50 = 5.9 5.9 144 2
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 392 4 3 3 4.5 O[C@@H]1CC[C@]2([C@@H](C1)CC[C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)C 10.1021/jm7015864
CHEMBL406393 1368 None 55 Human Functional pEC50 = 5.9 5.9 144 2
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 392 4 3 3 4.5 O[C@@H]1CC[C@]2([C@@H](C1)CC[C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)C 10.1021/jm7015864
DB03619 1368 None 55 Human Functional pEC50 = 5.9 5.9 144 2
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 392 4 3 3 4.5 O[C@@H]1CC[C@]2([C@@H](C1)CC[C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)C 10.1021/jm7015864
44372853 119959 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 376 4 2 2 5.5 CC(CCC(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
CHEMBL349105 119959 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 376 4 2 2 5.5 CC(CCC(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
118455158 157671 None 0 Human Functional pEC50 = 4.9 4.9 -100 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 526 7 0 5 7.6 COc1ccc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4080612 157671 None 0 Human Functional pEC50 = 4.9 4.9 -100 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 526 7 0 5 7.6 COc1ccc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
118455116 156283 None 0 Mouse Functional pEC50 = 4.9 4.9 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 560 7 1 5 7.4 COc1cc(C2(CO)CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4064131 156283 None 0 Mouse Functional pEC50 = 4.9 4.9 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 560 7 1 5 7.4 COc1cc(C2(CO)CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
118700209 196039 None 0 Human Functional pEC50 = 5.9 5.9 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2C(F)(F)F)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5415630 196039 None 0 Human Functional pEC50 = 5.9 5.9 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2C(F)(F)F)=C1C 10.1021/acs.jmedchem.2c01881
118694376 197153 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 355 4 0 3 3.9 CN1C=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC1=O 10.1021/acs.jmedchem.2c01881
CHEMBL5439939 197153 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 355 4 0 3 3.9 CN1C=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC1=O 10.1021/acs.jmedchem.2c01881
CHEMBL4574407 216489 None 7 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL None None None CC1=C(C(=O)OCc2ccccc2)C(c2ccc(C(F)(F)F)cc2)CC(=O)N1 10.1021/acs.jmedchem.2c01881
46232658 201984 None 0 Human Functional pEC50 = 5.9 5.9 - 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 346 3 0 3 4.9 CN(C(=O)c1conc1-c1ccccc1Cl)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL592158 201984 None 0 Human Functional pEC50 = 5.9 5.9 - 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 346 3 0 3 4.9 CN(C(=O)c1conc1-c1ccccc1Cl)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
46232412 203032 None 0 Human Functional pEC50 = 5.9 5.9 - 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 368 4 0 3 5.7 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(C(C)C)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL599127 203032 None 0 Human Functional pEC50 = 5.9 5.9 - 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 368 4 0 3 5.7 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(C(C)C)cc1 10.1016/j.bmcl.2010.01.003
46232875 203219 None 0 Human Functional pEC50 = 5.9 5.9 - 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(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)c1 10.1016/j.bmcl.2010.01.003
CHEMBL600410 203219 None 0 Human Functional pEC50 = 5.9 5.9 - 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(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)c1 10.1016/j.bmcl.2010.01.003
46233024 203221 None 0 Human Functional pEC50 = 5.9 5.9 - 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 340 3 0 3 4.9 Cc1cccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)c1 10.1016/j.bmcl.2010.01.003
CHEMBL600422 203221 None 0 Human Functional pEC50 = 5.9 5.9 - 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 340 3 0 3 4.9 Cc1cccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)c1 10.1016/j.bmcl.2010.01.003
46232597 203690 None 0 Human Functional pEC50 = 5.9 5.9 - 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 394 3 0 3 5.6 Cc1onc(-c2ccc(C(F)(F)F)cc2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL603706 203690 None 0 Human Functional pEC50 = 5.9 5.9 - 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 394 3 0 3 5.6 Cc1onc(-c2ccc(C(F)(F)F)cc2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
118093441 163867 None 0 Mouse Functional pEC50 = 5.9 5.9 -1 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 443 4 0 3 5.4 C[C@@]1(C(=O)N2CCN(C3CC3)c3ccccc32)CCCN1Cc1cc(Cl)ccc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4205745 163867 None 0 Mouse Functional pEC50 = 5.9 5.9 -1 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 443 4 0 3 5.4 C[C@@]1(C(=O)N2CCN(C3CC3)c3ccccc32)CCCN1Cc1cc(Cl)ccc1Cl 10.1021/acs.jmedchem.8b00308
71661223 164528 None 0 Mouse Functional pEC50 = 5.9 5.9 1 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 429 4 0 3 5.0 O=C([C@H]1CCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4213705 164528 None 0 Mouse Functional pEC50 = 5.9 5.9 1 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 429 4 0 3 5.0 O=C([C@H]1CCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118700209 196039 None 0 Mouse Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2C(F)(F)F)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5415630 196039 None 0 Mouse Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2C(F)(F)F)=C1C 10.1021/acs.jmedchem.2c01881
118694453 196864 None 0 Mouse Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 409 6 0 3 5.2 C=C(C)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5433643 196864 None 0 Mouse Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 409 6 0 3 5.2 C=C(C)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694423 197114 None 0 Mouse Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 419 7 0 4 4.7 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCC2CCCCC2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5439109 197114 None 0 Mouse Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 419 7 0 4 4.7 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCC2CCCCC2)=C1C 10.1021/acs.jmedchem.2c01881
118694398 196465 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 412 7 1 3 3.9 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)NCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5424539 196465 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 412 7 1 3 3.9 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)NCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
46232488 204034 None 0 Human Functional pEC50 = 4.9 4.9 - 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 368 4 0 4 4.8 CC(=O)c1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL605554 204034 None 0 Human Functional pEC50 = 4.9 4.9 - 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 368 4 0 4 4.8 CC(=O)c1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2010.01.003
71452077 83032 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 400 3 0 4 5.2 O=C(c1cnccc1Oc1cc(Cl)ccc1Cl)N1CCOc2ccccc21 10.1021/jm301071h
CHEMBL2181234 83032 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 400 3 0 4 5.2 O=C(c1cnccc1Oc1cc(Cl)ccc1Cl)N1CCOc2ccccc21 10.1021/jm301071h
73347898 92775 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 466 6 0 2 6.7 CCC(=O)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
CHEMBL2435935 92775 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 466 6 0 2 6.7 CCC(=O)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
118576974 157279 None 0 Human Functional pEC50 = 6.9 6.9 -10 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 467 8 0 6 6.2 COc1ccc(N(C)c2cnc(SCc3ccccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4075688 157279 None 0 Human Functional pEC50 = 6.9 6.9 -10 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 467 8 0 6 6.2 COc1ccc(N(C)c2cnc(SCc3ccccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
156705100 182355 None 0 Human Functional pEC50 = 5.9 5.9 4 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 567 7 0 10 5.5 Cc1oc(=O)oc1COC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4783601 182355 None 0 Human Functional pEC50 = 5.9 5.9 4 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 567 7 0 10 5.5 Cc1oc(=O)oc1COC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
3223370 109990 None 0 Mouse Functional pEC50 = 5.9 5.9 -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 344 5 1 4 2.7 O=C(NCCc1ccc(Cl)cc1)C1CCCN(c2ncccn2)C1 10.1021/jm401731q
CHEMBL3234546 109990 None 0 Mouse Functional pEC50 = 5.9 5.9 -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 344 5 1 4 2.7 O=C(NCCc1ccc(Cl)cc1)C1CCCN(c2ncccn2)C1 10.1021/jm401731q
90654580 110004 None 0 Human Functional pEC50 = 7.9 7.9 4 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 367 5 1 5 2.4 Cc1nc(N2CCC[C@@H](C(=O)NCCc3ccc(C#N)cc3)C2)ncc1F 10.1021/jm401731q
CHEMBL3234561 110004 None 0 Human Functional pEC50 = 7.9 7.9 4 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 367 5 1 5 2.4 Cc1nc(N2CCC[C@@H](C(=O)NCCc3ccc(C#N)cc3)C2)ncc1F 10.1021/jm401731q
90644457 112291 None 0 Mouse Functional pEC50 = 7.9 7.9 2 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 614 8 2 8 4.9 Cc1c(/C=C/C(=O)NCC(=O)O)oc2ccc(Cl)c(C(=O)Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c12 10.1016/j.ejmech.2014.05.031
CHEMBL3290734 112291 None 0 Mouse Functional pEC50 = 7.9 7.9 2 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 614 8 2 8 4.9 Cc1c(/C=C/C(=O)NCC(=O)O)oc2ccc(Cl)c(C(=O)Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c12 10.1016/j.ejmech.2014.05.031
90654588 110012 None 0 Mouse Functional pEC50 = 7.9 7.9 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 487 6 2 7 2.4 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3cc(N4CCNCC4)nc(C(F)(F)F)n3)C2)cc1 10.1021/jm401731q
CHEMBL3234569 110012 None 0 Mouse Functional pEC50 = 7.9 7.9 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 487 6 2 7 2.4 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3cc(N4CCNCC4)nc(C(F)(F)F)n3)C2)cc1 10.1021/jm401731q
164611903 185246 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 529 4 2 3 7.9 CCNC(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
CHEMBL4856750 185246 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 529 4 2 3 7.9 CCNC(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
164621055 186043 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 541 4 2 4 7.0 CC(=O)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
CHEMBL4869294 186043 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 541 4 2 4 7.0 CC(=O)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
11656002 83044 None 22 Mouse Functional pEC50 = 6.9 6.9 -61 8
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 484 3 0 3 5.8 O=C1COc2nccc(-c3ccccc3F)c2CN1Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2181247 83044 None 22 Mouse Functional pEC50 = 6.9 6.9 -61 8
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 484 3 0 3 5.8 O=C1COc2nccc(-c3ccccc3F)c2CN1Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
90654581 110005 None 0 Mouse Functional pEC50 = 6.9 6.9 -7 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 403 5 1 5 2.9 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3nccc(C(F)(F)F)n3)C2)cc1 10.1021/jm401731q
CHEMBL3234562 110005 None 0 Mouse Functional pEC50 = 6.9 6.9 -7 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 403 5 1 5 2.9 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3nccc(C(F)(F)F)n3)C2)cc1 10.1021/jm401731q
118700209 196039 None 0 Mouse Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2C(F)(F)F)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5415630 196039 None 0 Mouse Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2C(F)(F)F)=C1C 10.1021/acs.jmedchem.2c01881
45483949 3582 None 33 Human Functional pEC50 = 4.9 4.9 -2 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.bmcl.2013.06.017
7048 3582 None 33 Human Functional pEC50 = 4.9 4.9 -2 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.bmcl.2013.06.017
CHEMBL567640 3582 None 33 Human Functional pEC50 = 4.9 4.9 -2 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.bmcl.2013.06.017
118694398 196465 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 412 7 1 3 3.9 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)NCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5424539 196465 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 412 7 1 3 3.9 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)NCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118735267 118897 None 0 Mouse Functional pEC50 = 4.9 4.9 1 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 1310 35 2 16 10.8 O=C(CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NCCOCCOCCOCCOCCOCCOCCNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421903 118897 None 0 Mouse Functional pEC50 = 4.9 4.9 1 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 1310 35 2 16 10.8 O=C(CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NCCOCCOCCOCCOCCOCCOCCNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
164609009 184530 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 570 5 2 5 7.4 CO/N=C(/C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
CHEMBL4846185 184530 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 570 5 2 5 7.4 CO/N=C(/C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
1434463 157837 None 2 Human Functional pEC50 = 5.9 5.9 1 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 404 4 0 6 4.4 CCn1c(=O)c2ccccc2n2c(SCc3ccc(C(F)(F)F)cc3)nnc12 10.1021/acs.jmedchem.6b01873
CHEMBL4082345 157837 None 2 Human Functional pEC50 = 5.9 5.9 1 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 404 4 0 6 4.4 CCn1c(=O)c2ccccc2n2c(SCc3ccc(C(F)(F)F)cc3)nnc12 10.1021/acs.jmedchem.6b01873
45483949 3582 None 33 Mouse Functional pEC50 = 6.9 6.9 2 2
Agonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assayAgonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.bmc.2020.115972
7048 3582 None 33 Mouse Functional pEC50 = 6.9 6.9 2 2
Agonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assayAgonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.bmc.2020.115972
CHEMBL567640 3582 None 33 Mouse Functional pEC50 = 6.9 6.9 2 2
Agonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assayAgonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.bmc.2020.115972
11165617 158969 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 404 3 3 3 4.3 C[C@H]([C@@H]1C[C@@H]1C(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
CHEMBL409511 158969 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 404 3 3 3 4.3 C[C@H]([C@@H]1C[C@@H]1C(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
118464622 158963 None 0 Mouse Functional pEC50 = 5.9 5.9 26 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 548 6 0 4 8.4 COc1cc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4F)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4095058 158963 None 0 Mouse Functional pEC50 = 5.9 5.9 26 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 548 6 0 4 8.4 COc1cc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4F)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
118464720 157196 None 0 Mouse Functional pEC50 = 4.9 4.9 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 598 6 0 4 9.2 COc1cc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)c(C(F)(F)F)c4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4074596 157196 None 0 Mouse Functional pEC50 = 4.9 4.9 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 598 6 0 4 9.2 COc1cc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)c(C(F)(F)F)c4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
76332905 106085 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 391 4 0 6 3.2 COc1cccc(-c2nnn(C)c2C(=O)N(C)c2ccc(C(F)(F)F)nc2)c1 10.1039/C2MD20174G
CHEMBL3132972 106085 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 391 4 0 6 3.2 COc1cccc(-c2nnn(C)c2C(=O)N(C)c2ccc(C(F)(F)F)nc2)c1 10.1039/C2MD20174G
77845211 112282 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 503 6 1 6 5.5 O=C(O)Cc1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
CHEMBL3290725 112282 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 503 6 1 6 5.5 O=C(O)Cc1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
221493 921 None 58 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1021/ml200256d
3096 921 None 58 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1021/ml200256d
609 921 None 58 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1021/ml200256d
CHEMBL205596 921 None 58 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1021/ml200256d
DB02659 921 None 58 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1021/ml200256d
221493 921 None 58 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1021/jm070633p
3096 921 None 58 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1021/jm070633p
609 921 None 58 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1021/jm070633p
CHEMBL205596 921 None 58 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1021/jm070633p
DB02659 921 None 58 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1021/jm070633p
221493 921 None 58 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1021/jm901390p
3096 921 None 58 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1021/jm901390p
609 921 None 58 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1021/jm901390p
CHEMBL205596 921 None 58 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1021/jm901390p
DB02659 921 None 58 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1021/jm901390p
221493 921 None 58 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1021/jm7015864
3096 921 None 58 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1021/jm7015864
609 921 None 58 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1021/jm7015864
CHEMBL205596 921 None 58 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1021/jm7015864
DB02659 921 None 58 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1021/jm7015864
10140 160431 None 40 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 465 6 5 5 2.6 C[C@H](CCC(=O)NCC(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](C[C@H](O)[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
CHEMBL411070 160431 None 40 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 465 6 5 5 2.6 C[C@H](CCC(=O)NCC(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](C[C@H](O)[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
156705083 183202 None 0 Human Functional pEC50 = 6.9 6.9 10 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 557 8 0 10 5.5 CCOC(=O)OCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4794523 183202 None 0 Human Functional pEC50 = 6.9 6.9 10 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 557 8 0 10 5.5 CCOC(=O)OCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
71541723 87324 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 383 7 2 6 1.5 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC)cc1)CC2 10.1021/ml300277t
CHEMBL2331647 87324 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 383 7 2 6 1.5 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC)cc1)CC2 10.1021/ml300277t
156705119 183220 None 0 Mouse Functional pEC50 = 6.9 6.9 -29 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 499 7 0 8 5.0 COCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4794753 183220 None 0 Mouse Functional pEC50 = 6.9 6.9 -29 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 499 7 0 8 5.0 COCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
90654576 110000 None 0 Human Functional pEC50 = 4.9 4.9 -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 344 5 1 4 2.7 O=C(NCCc1ccc(Cl)cc1)[C@@H]1CCCN(c2ccncn2)C1 10.1021/jm401731q
CHEMBL3234557 110000 None 0 Human Functional pEC50 = 4.9 4.9 -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 344 5 1 4 2.7 O=C(NCCc1ccc(Cl)cc1)[C@@H]1CCCN(c2ccncn2)C1 10.1021/jm401731q
156705083 183202 None 0 Mouse Functional pEC50 = 5.9 5.9 -10 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 557 8 0 10 5.5 CCOC(=O)OCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4794523 183202 None 0 Mouse Functional pEC50 = 5.9 5.9 -10 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 557 8 0 10 5.5 CCOC(=O)OCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
130361963 171250 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 387 4 1 3 5.6 CO[C@@H]1CC[C@]2(C)[C@H]3CC[C@@]4(C)[C@@H](CC[C@@H]4[C@H](C)CCC#N)[C@@H]3[C@H](O)C[C@@H]2C1 10.1021/acs.jmedchem.9b00770
CHEMBL4458539 171250 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 387 4 1 3 5.6 CO[C@@H]1CC[C@]2(C)[C@H]3CC[C@@]4(C)[C@@H](CC[C@@H]4[C@H](C)CCC#N)[C@@H]3[C@H](O)C[C@@H]2C1 10.1021/acs.jmedchem.9b00770
71561883 87681 None 0 Human Functional pEC50 = 7.9 7.9 - 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 404 5 0 5 4.5 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N(C)Cc1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336235 87681 None 0 Human Functional pEC50 = 7.9 7.9 - 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 404 5 0 5 4.5 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N(C)Cc1cccnc1 10.1016/j.bmcl.2012.12.076
90654588 110012 None 0 Human Functional pEC50 = 7.9 7.9 -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 487 6 2 7 2.4 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3cc(N4CCNCC4)nc(C(F)(F)F)n3)C2)cc1 10.1021/jm401731q
CHEMBL3234569 110012 None 0 Human Functional pEC50 = 7.9 7.9 -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 487 6 2 7 2.4 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3cc(N4CCNCC4)nc(C(F)(F)F)n3)C2)cc1 10.1021/jm401731q
90654595 110026 None 0 Human Functional pEC50 = 7.9 7.9 -7 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 636 10 2 8 4.6 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3cc(N4CCC(Oc5ccc(CC(=O)O)cc5)CC4)nc(C(F)(F)F)n3)C2)cc1 10.1021/jm401731q
CHEMBL3234582 110026 None 0 Human Functional pEC50 = 7.9 7.9 -7 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 636 10 2 8 4.6 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3cc(N4CCC(Oc5ccc(CC(=O)O)cc5)CC4)nc(C(F)(F)F)n3)C2)cc1 10.1021/jm401731q
118694573 196130 None 0 Human Functional pEC50 = 7.9 7.9 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5417359 196130 None 0 Human Functional pEC50 = 7.9 7.9 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
89501434 161491 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assay
ChEMBL 542 11 0 6 6.9 COc1ccc(C(C)(C)c2cnc(SCCOCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2018.04.011
CHEMBL4126485 161491 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assay
ChEMBL 542 11 0 6 6.9 COc1ccc(C(C)(C)c2cnc(SCCOCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2018.04.011
172433366 197250 None 0 Human Functional pEC50 = 7.8 7.8 -2 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 955 16 2 9 6.8 CC1C(=O)N(CC(=O)NCCN(C)C(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5483060 197250 None 0 Human Functional pEC50 = 7.8 7.8 -2 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 955 16 2 9 6.8 CC1C(=O)N(CC(=O)NCCN(C)C(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
44427761 93280 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 420 4 3 3 5.0 C[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)CC1[C@@H](C)[C@H]3O)C(=O)O 10.1021/jm070633p
CHEMBL244784 93280 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 420 4 3 3 5.0 C[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)CC1[C@@H](C)[C@H]3O)C(=O)O 10.1021/jm070633p
90654582 110006 None 0 Human Functional pEC50 = 6.9 6.9 -6 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 403 5 1 5 2.9 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3ccnc(C(F)(F)F)n3)C2)cc1 10.1021/jm401731q
CHEMBL3234563 110006 None 0 Human Functional pEC50 = 6.9 6.9 -6 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 403 5 1 5 2.9 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3ccnc(C(F)(F)F)n3)C2)cc1 10.1021/jm401731q
90654569 109992 None 0 Mouse Functional pEC50 = 6.9 6.9 -2 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 358 5 1 4 3.0 Cc1ccnc(N2CCC[C@@H](C(=O)NCCc3ccc(Cl)cc3)C2)n1 10.1021/jm401731q
CHEMBL3234549 109992 None 0 Mouse Functional pEC50 = 6.9 6.9 -2 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 358 5 1 4 3.0 Cc1ccnc(N2CCC[C@@H](C(=O)NCCc3ccc(Cl)cc3)C2)n1 10.1021/jm401731q
58043589 91642 None 0 Human Functional pEC50 = 5.9 5.9 8 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
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
CHEMBL2407935 91642 None 0 Human Functional pEC50 = 5.9 5.9 8 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
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
118464804 156634 None 0 Human Functional pEC50 = 5.9 5.9 -4 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 568 9 1 6 6.8 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cc(CCO)cc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4068168 156634 None 0 Human Functional pEC50 = 5.9 5.9 -4 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 568 9 1 6 6.8 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cc(CCO)cc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
71561618 87673 None 0 Human Functional pEC50 = 5.9 5.9 - 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 457 4 0 4 6.5 Cc1ccccc1C1CCCCN1C(=O)c1c(C)nn(C)c1Oc1cccc(Cl)c1Cl 10.1016/j.bmcl.2012.12.076
CHEMBL2336226 87673 None 0 Human Functional pEC50 = 5.9 5.9 - 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 457 4 0 4 6.5 Cc1ccccc1C1CCCCN1C(=O)c1c(C)nn(C)c1Oc1cccc(Cl)c1Cl 10.1016/j.bmcl.2012.12.076
90654575 109999 None 0 Mouse Functional pEC50 = 5.9 5.9 -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 343 5 1 3 3.3 O=C(NCCc1ccc(Cl)cc1)[C@@H]1CCCN(c2ccccn2)C1 10.1021/jm401731q
CHEMBL3234556 109999 None 0 Mouse Functional pEC50 = 5.9 5.9 -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 343 5 1 3 3.3 O=C(NCCc1ccc(Cl)cc1)[C@@H]1CCCN(c2ccccn2)C1 10.1021/jm401731q
118694537 197046 None 0 Mouse Functional pEC50 = 5.9 5.9 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 369 4 0 3 4.3 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1C 10.1021/acs.jmedchem.2c01881
CHEMBL5437459 197046 None 0 Mouse Functional pEC50 = 5.9 5.9 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 369 4 0 3 4.3 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1C 10.1021/acs.jmedchem.2c01881
447715 199383 None 50 Human Functional pEC50 = 4.9 4.9 6 7
Agonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assayAgonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assay
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 10.1016/j.ejmech.2022.114652
CHEMBL566315 199383 None 50 Human Functional pEC50 = 4.9 4.9 6 7
Agonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assayAgonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assay
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 10.1016/j.ejmech.2022.114652
118735266 118896 None 0 Mouse Functional pEC50 = 4.9 4.9 2 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 1178 26 2 13 10.8 O=C(CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NCCOCCOCCOCCNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421902 118896 None 0 Mouse Functional pEC50 = 4.9 4.9 2 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 1178 26 2 13 10.8 O=C(CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NCCOCCOCCOCCNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
90644460 112285 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 602 8 1 9 4.6 CCOC(=O)CNC(=O)c1coc2cc(Cl)c(C(=O)Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
CHEMBL3290728 112285 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 602 8 1 9 4.6 CCOC(=O)CNC(=O)c1coc2cc(Cl)c(C(=O)Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
118586281 158655 None 0 Mouse Functional pEC50 = 6.9 6.9 7 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 455 7 0 5 6.4 COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.6b01873
CHEMBL4091702 158655 None 0 Mouse Functional pEC50 = 6.9 6.9 7 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 455 7 0 5 6.4 COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.6b01873
172464611 196711 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 476 7 2 5 5.0 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)OCC4CC4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
CHEMBL5430487 196711 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 476 7 2 5 5.0 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)OCC4CC4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
46232736 203765 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 340 4 0 4 3.8 CCc1nnn(-c2ccccc2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1021/ml300277t
CHEMBL604131 203765 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 340 4 0 4 3.8 CCc1nnn(-c2ccccc2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1021/ml300277t
46232736 203765 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human recombinant TGR5 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 340 4 0 4 3.8 CCc1nnn(-c2ccccc2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1039/C2MD20174G
CHEMBL604131 203765 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human recombinant TGR5 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 340 4 0 4 3.8 CCc1nnn(-c2ccccc2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1039/C2MD20174G
71599441 163648 None 0 Human Functional pEC50 = 6.8 6.8 -109 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 760 14 6 11 2.6 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(COc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)cc1 10.1021/acs.jmedchem.8b00308
CHEMBL4202981 163648 None 0 Human Functional pEC50 = 6.8 6.8 -109 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 760 14 6 11 2.6 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(COc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)cc1 10.1021/acs.jmedchem.8b00308
156705091 182313 None 0 Mouse Functional pEC50 = 6.8 6.8 -20 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 515 7 0 8 5.7 CSCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4783037 182313 None 0 Mouse Functional pEC50 = 6.8 6.8 -20 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 515 7 0 8 5.7 CSCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
64945 59008 None 44 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 456 1 2 2 7.1 C[C@@H]1[C@H]2C3=CC[C@@H]4[C@@]5(C)CC[C@H](O)C(C)(C)[C@@H]5CC[C@@]4(C)[C@]3(C)CC[C@@]2(C(=O)O)CC[C@H]1C 10.1021/jm900872z
CHEMBL169 59008 None 44 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 456 1 2 2 7.1 C[C@@H]1[C@H]2C3=CC[C@@H]4[C@@]5(C)CC[C@H](O)C(C)(C)[C@@H]5CC[C@@]4(C)[C@]3(C)CC[C@@]2(C(=O)O)CC[C@H]1C 10.1021/jm900872z
156705115 182225 None 0 Human Functional pEC50 = 6.8 6.8 3 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 527 7 0 9 4.9 CC(=O)OCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4782069 182225 None 0 Human Functional pEC50 = 6.8 6.8 3 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 527 7 0 9 4.9 CC(=O)OCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
447718 97550 None 8 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 376 4 2 2 5.5 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CCCC[C@H]1C[C@H]3O 10.1021/jm7015864
CHEMBL270311 97550 None 8 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 376 4 2 2 5.5 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CCCC[C@H]1C[C@H]3O 10.1021/jm7015864
71540076 87328 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 417 7 2 5 2.6 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(C(C)(F)F)cc1)CC2 10.1021/ml300277t
CHEMBL2331651 87328 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 417 7 2 5 2.6 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(C(C)(F)F)cc1)CC2 10.1021/ml300277t
71561365 87659 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 410 4 0 5 4.9 Cc1nn(C)c(Oc2ccccc2Cl)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336210 87659 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 410 4 0 5 4.9 Cc1nn(C)c(Oc2ccccc2Cl)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
71540073 87325 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human recombinant TGR5 expressed in NCI-H716 cells assessed as increase in intracellular cAMP measured after 1 hrAgonist activity at human recombinant TGR5 expressed in NCI-H716 cells assessed as increase in intracellular cAMP measured after 1 hr
ChEMBL 437 7 2 6 2.4 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1021/ml300277t
CHEMBL2331648 87325 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human recombinant TGR5 expressed in NCI-H716 cells assessed as increase in intracellular cAMP measured after 1 hrAgonist activity at human recombinant TGR5 expressed in NCI-H716 cells assessed as increase in intracellular cAMP measured after 1 hr
ChEMBL 437 7 2 6 2.4 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1021/ml300277t
71626558 112266 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 410 4 1 4 5.0 O=C(c1cnccc1Oc1cccc2[nH]ccc12)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
CHEMBL3290709 112266 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 410 4 1 4 5.0 O=C(c1cnccc1Oc1cccc2[nH]ccc12)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
71561369 87663 None 0 Human Functional pEC50 = 5.8 5.8 - 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 444 4 0 5 5.6 Cc1nn(C)c(Oc2cc(Cl)ccc2Cl)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336214 87663 None 0 Human Functional pEC50 = 5.8 5.8 - 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 444 4 0 5 5.6 Cc1nn(C)c(Oc2cc(Cl)ccc2Cl)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
11281589 117742 None 12 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 420 5 3 3 5.1 CC[C@H]1[C@H](O)[C@@H]2[C@H](CC[C@@]3(C)[C@H]2CC[C@@H]3[C@H](C)CCC(=O)O)[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1016/j.bmc.2015.01.048
CHEMBL3401355 117742 None 12 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 420 5 3 3 5.1 CC[C@H]1[C@H](O)[C@@H]2[C@H](CC[C@@]3(C)[C@H]2CC[C@@H]3[C@H](C)CCC(=O)O)[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1016/j.bmc.2015.01.048
71561365 87659 None 0 Human Functional pEC50 = 7.8 7.8 - 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 410 4 0 5 4.9 Cc1nn(C)c(Oc2ccccc2Cl)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336210 87659 None 0 Human Functional pEC50 = 7.8 7.8 - 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 410 4 0 5 4.9 Cc1nn(C)c(Oc2ccccc2Cl)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
71561614 87665 None 0 Human Functional pEC50 = 7.8 7.8 - 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 444 4 0 5 5.3 Cc1nn(C)c(Oc2ccccc2C(F)(F)F)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336216 87665 None 0 Human Functional pEC50 = 7.8 7.8 - 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 444 4 0 5 5.3 Cc1nn(C)c(Oc2ccccc2C(F)(F)F)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
71626560 112269 None 0 Human Functional pEC50 = 7.8 7.8 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 428 4 0 6 5.1 O=C(c1cnccc1Oc1ccc2ncsc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
CHEMBL3290712 112269 None 0 Human Functional pEC50 = 7.8 7.8 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 428 4 0 6 5.1 O=C(c1cnccc1Oc1ccc2ncsc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
90654600 110064 None 0 Human Functional pEC50 = 7.8 7.8 -8 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 577 8 2 6 5.3 N#Cc1ccc(CCNC(=O)[C@@H]2CCN2c2cc(-c3ccc([C@H]4CC[C@H](C(=O)O)CC4)cc3)nc(C(F)(F)F)n2)cc1 10.1021/jm401731q
CHEMBL3234871 110064 None 0 Human Functional pEC50 = 7.8 7.8 -8 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 577 8 2 6 5.3 N#Cc1ccc(CCNC(=O)[C@@H]2CCN2c2cc(-c3ccc([C@H]4CC[C@H](C(=O)O)CC4)cc3)nc(C(F)(F)F)n2)cc1 10.1021/jm401731q
71457418 83022 None 0 Mouse Functional pEC50 = 7.8 7.8 -1 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 385 4 0 4 4.8 Cc1ccc(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1 10.1021/jm301071h
CHEMBL2181225 83022 None 0 Mouse Functional pEC50 = 7.8 7.8 -1 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 385 4 0 4 4.8 Cc1ccc(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1 10.1021/jm301071h
118694573 196130 None 0 Human Functional pEC50 = 7.8 7.8 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5417359 196130 None 0 Human Functional pEC50 = 7.8 7.8 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
46233021 203270 None 0 Human Functional pEC50 = 7.8 7.8 - 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 404 3 0 3 5.3 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(Br)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL600827 203270 None 0 Human Functional pEC50 = 7.8 7.8 - 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 404 3 0 3 5.3 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(Br)cc1 10.1016/j.bmcl.2010.01.003
118093575 163723 None 1 Mouse Functional pEC50 = 7.8 7.8 6 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 463 4 1 5 4.6 O=C([C@@H]1CSCN1Cc1cc(Cl)c(O)cc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4203848 163723 None 1 Mouse Functional pEC50 = 7.8 7.8 6 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 463 4 1 5 4.6 O=C([C@@H]1CSCN1Cc1cc(Cl)c(O)cc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118104397 164268 None 0 Mouse Functional pEC50 = 7.8 7.8 15 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 750 14 6 12 2.2 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(COc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)o1 10.1021/acs.jmedchem.8b00308
CHEMBL4210547 164268 None 0 Mouse Functional pEC50 = 7.8 7.8 15 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 750 14 6 12 2.2 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(COc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)o1 10.1021/acs.jmedchem.8b00308
118694573 196130 None 0 Mouse Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5417359 196130 None 0 Mouse Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
73352466 92764 None 0 Mouse Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 453 5 1 3 6.3 N#CC(NCc1cnccc1-c1ccccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435924 92764 None 0 Mouse Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 453 5 1 3 6.3 N#CC(NCc1cnccc1-c1ccccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
118694349 196959 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 355 4 1 3 4.0 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1 10.1021/acs.jmedchem.2c01881
CHEMBL5435593 196959 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 355 4 1 3 4.0 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1 10.1021/acs.jmedchem.2c01881
42854551 196992 None 0 Mouse Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 395 6 0 3 4.9 C=CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5436242 196992 None 0 Mouse Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 395 6 0 3 4.9 C=CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
447715 199383 None 50 Human Functional pEC50 = 4.8 4.8 6 7
Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay
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/acs.jmedchem.6b01126
CHEMBL566315 199383 None 50 Human Functional pEC50 = 4.8 4.8 6 7
Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay
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/acs.jmedchem.6b01126
71626229 118895 None 0 Human Functional pEC50 = 4.8 4.8 -2 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 582 9 1 6 5.3 CN(CC(=O)O)C(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421901 118895 None 0 Human Functional pEC50 = 4.8 4.8 -2 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 582 9 1 6 5.3 CN(CC(=O)O)C(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
5306292 196577 None 8 Mouse Functional pEC50 = 4.8 4.8 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 293 2 0 3 2.7 COC(=O)C1=C(C)N(C)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5427123 196577 None 8 Mouse Functional pEC50 = 4.8 4.8 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 293 2 0 3 2.7 COC(=O)C1=C(C)N(C)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
164628742 186676 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 595 4 2 3 9.6 CC(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)Nc6ccc(F)cc6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
CHEMBL4878269 186676 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 595 4 2 3 9.6 CC(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)Nc6ccc(F)cc6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
118464786 156721 None 0 Mouse Functional pEC50 = 5.8 5.8 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 530 6 0 4 8.2 COc1ccc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)cc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4069164 156721 None 0 Mouse Functional pEC50 = 5.8 5.8 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 530 6 0 4 8.2 COc1ccc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)cc1Cl 10.1021/acsmedchemlett.7b00116
24969872 17676 None 0 Human Functional pEC50 = 6.8 6.8 10 2
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 452 7 1 4 6.1 COc1ccc2cc(CNCCc3ccc(Br)cc3)c(-c3ccsc3)nc2c1 10.1021/ml300277t
CHEMBL1258423 17676 None 0 Human Functional pEC50 = 6.8 6.8 10 2
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 452 7 1 4 6.1 COc1ccc2cc(CNCCc3ccc(Br)cc3)c(-c3ccsc3)nc2c1 10.1021/ml300277t
71540075 87327 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 435 7 2 5 2.6 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(CC(F)(F)F)cc1)CC2 10.1021/ml300277t
CHEMBL2331650 87327 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 435 7 2 5 2.6 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(CC(F)(F)F)cc1)CC2 10.1021/ml300277t
53311618 83047 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 3 0 4 5.2 O=C(c1cncnc1Oc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 10.1021/jm301071h
CHEMBL2181251 83047 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 3 0 4 5.2 O=C(c1cncnc1Oc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 10.1021/jm301071h
118586298 158118 None 0 Human Functional pEC50 = 6.8 6.8 -2 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 449 8 0 6 6.1 COc1ccc(N(C)c2cnc(SCc3ccccc3)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4085664 158118 None 0 Human Functional pEC50 = 6.8 6.8 -2 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 449 8 0 6 6.1 COc1ccc(N(C)c2cnc(SCc3ccccc3)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
10133 910 None 49 Human Functional pEC50 = 4.8 4.8 -1 4
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
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/acs.jmedchem.9b00770
145714624 910 None 49 Human Functional pEC50 = 4.8 4.8 -1 4
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
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/acs.jmedchem.9b00770
4361 910 None 49 Human Functional pEC50 = 4.8 4.8 -1 4
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
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/acs.jmedchem.9b00770
608 910 None 49 Human Functional pEC50 = 4.8 4.8 -1 4
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
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/acs.jmedchem.9b00770
CHEMBL240597 910 None 49 Human Functional pEC50 = 4.8 4.8 -1 4
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
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/acs.jmedchem.9b00770
DB06777 910 None 49 Human Functional pEC50 = 4.8 4.8 -1 4
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
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/acs.jmedchem.9b00770
71541719 87323 None 1 Human Functional pEC50 = 6.8 6.8 194 3
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 395 7 2 5 2.6 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(C(C)C)cc1)CC2 10.1021/ml300277t
CHEMBL2331646 87323 None 1 Human Functional pEC50 = 6.8 6.8 194 3
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 395 7 2 5 2.6 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(C(C)C)cc1)CC2 10.1021/ml300277t
44605616 200751 None 49 Human Functional pEC50 = 6.8 6.8 28 2
Agonist activity at TGR5 expressed in human U2-OS cells assessed as increase in MRE/CRE-driven gene expression by luciferase reporter gene assayAgonist activity at TGR5 expressed in human U2-OS cells assessed as increase in MRE/CRE-driven gene expression by luciferase reporter gene assay
ChEMBL 360 3 0 3 5.2 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(Cl)cc1 10.1021/jm901434t
CHEMBL575966 200751 None 49 Human Functional pEC50 = 6.8 6.8 28 2
Agonist activity at TGR5 expressed in human U2-OS cells assessed as increase in MRE/CRE-driven gene expression by luciferase reporter gene assayAgonist activity at TGR5 expressed in human U2-OS cells assessed as increase in MRE/CRE-driven gene expression by luciferase reporter gene assay
ChEMBL 360 3 0 3 5.2 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(Cl)cc1 10.1021/jm901434t
118093402 164315 None 0 Human Functional pEC50 = 6.8 6.8 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 445 4 1 4 3.9 O=C([C@@H]1C[C@@H](O)CN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4211041 164315 None 0 Human Functional pEC50 = 6.8 6.8 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 445 4 1 4 3.9 O=C([C@@H]1C[C@@H](O)CN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118694538 196021 None 0 Human Functional pEC50 = 6.8 6.8 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 6 0 5 3.8 COC(=O)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5415202 196021 None 0 Human Functional pEC50 = 6.8 6.8 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 6 0 5 3.8 COC(=O)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
46232529 203310 None 0 Human Functional pEC50 = 6.8 6.8 - 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 344 3 0 3 4.7 Cc1onc(-c2ccccc2F)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL601233 203310 None 0 Human Functional pEC50 = 6.8 6.8 - 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 344 3 0 3 4.7 Cc1onc(-c2ccccc2F)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
118104385 163678 None 0 Mouse Functional pEC50 = 6.8 6.8 5 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 648 13 6 10 0.7 O=C(CCc1ccc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)c1)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4203321 163678 None 0 Mouse Functional pEC50 = 6.8 6.8 5 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 648 13 6 10 0.7 O=C(CCc1ccc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)c1)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
118700251 194992 None 0 Mouse Functional pEC50 = 6.8 6.8 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 465 7 0 5 5.5 COc1ccccc1COC(=O)C1=C(C)N(Cc2ccco2)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5394522 194992 None 0 Mouse Functional pEC50 = 6.8 6.8 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 465 7 0 5 5.5 COc1ccccc1COC(=O)C1=C(C)N(Cc2ccco2)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
118464806 159150 None 0 Human Functional pEC50 = 4.8 4.8 -34 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 703 16 0 8 7.9 COc1cc(C2(C)CCCc3nc(SCc4c(F)cc(OCCOCCOCCN(C)C)cc4F)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4097059 159150 None 0 Human Functional pEC50 = 4.8 4.8 -34 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 703 16 0 8 7.9 COc1cc(C2(C)CCCc3nc(SCc4c(F)cc(OCCOCCOCCN(C)C)cc4F)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
71661222 164592 None 0 Human Functional pEC50 = 5.8 5.8 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 443 4 0 3 5.4 O=C([C@@H]1CCCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4214506 164592 None 0 Human Functional pEC50 = 5.8 5.8 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 443 4 0 3 5.4 O=C([C@@H]1CCCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118694349 196959 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 355 4 1 3 4.0 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1 10.1021/acs.jmedchem.2c01881
CHEMBL5435593 196959 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 355 4 1 3 4.0 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1 10.1021/acs.jmedchem.2c01881
71660822 164860 None 0 Mouse Functional pEC50 = 5.8 5.8 -5 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 461 4 0 4 4.9 O=C([C@@H]1CSCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4217961 164860 None 0 Mouse Functional pEC50 = 5.8 5.8 -5 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 461 4 0 4 4.9 O=C([C@@H]1CSCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
42854551 196992 None 0 Mouse Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 395 6 0 3 4.9 C=CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5436242 196992 None 0 Mouse Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 395 6 0 3 4.9 C=CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694537 197046 None 0 Mouse Functional pEC50 = 5.8 5.8 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 369 4 0 3 4.3 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1C 10.1021/acs.jmedchem.2c01881
CHEMBL5437459 197046 None 0 Mouse Functional pEC50 = 5.8 5.8 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 369 4 0 3 4.3 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1C 10.1021/acs.jmedchem.2c01881
5306292 196577 None 8 Mouse Functional pEC50 = 4.8 4.8 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 293 2 0 3 2.7 COC(=O)C1=C(C)N(C)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5427123 196577 None 8 Mouse Functional pEC50 = 4.8 4.8 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 293 2 0 3 2.7 COC(=O)C1=C(C)N(C)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
71561504 87669 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 444 4 0 5 5.6 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N1CCCC[C@@H]1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336222 87669 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 444 4 0 5 5.6 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N1CCCC[C@@H]1c1cccnc1 10.1016/j.bmcl.2012.12.076
71626697 112268 None 0 Human Functional pEC50 = 7.8 7.8 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 427 4 0 5 5.7 O=C(c1cnccc1Oc1ccc2sccc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
CHEMBL3290711 112268 None 0 Human Functional pEC50 = 7.8 7.8 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 427 4 0 5 5.7 O=C(c1cnccc1Oc1ccc2sccc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
90644456 112288 None 0 Mouse Functional pEC50 = 7.8 7.8 -1 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 557 7 0 7 6.8 CCOC(=O)/C=C/c1oc2ccc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c2c1C 10.1016/j.ejmech.2014.05.031
CHEMBL3290731 112288 None 0 Mouse Functional pEC50 = 7.8 7.8 -1 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 557 7 0 7 6.8 CCOC(=O)/C=C/c1oc2ccc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c2c1C 10.1016/j.ejmech.2014.05.031
156705098 183500 None 2 Human Functional pEC50 = 7.8 7.8 12 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 513 8 0 8 5.4 CCOCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4798091 183500 None 2 Human Functional pEC50 = 7.8 7.8 12 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 513 8 0 8 5.4 CCOCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
137634612 156206 None 0 Mouse Functional pEC50 = 6.8 6.8 35 2
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 518 9 0 6 7.4 COc1ccc(SCc2cnc(SCc3c(F)cccc3Cl)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4063237 156206 None 0 Mouse Functional pEC50 = 6.8 6.8 35 2
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 518 9 0 6 7.4 COc1ccc(SCc2cnc(SCc3c(F)cccc3Cl)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
145955827 162777 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay
ChEMBL 504 5 4 4 4.4 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)CCNC(=O)N3CC[C@H](O)C3)[C@@H]2[C@@H]1O 10.1021/acsmedchemlett.7b00318
CHEMBL4170310 162777 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay
ChEMBL 504 5 4 4 4.4 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)CCNC(=O)N3CC[C@H](O)C3)[C@@H]2[C@@H]1O 10.1021/acsmedchemlett.7b00318
71461057 83042 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 403 5 0 5 4.9 COc1ccccc1N(C)C(=O)c1cncnc1Oc1cc(Cl)ccc1Cl 10.1021/jm301071h
CHEMBL2181244 83042 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 403 5 0 5 4.9 COc1ccccc1N(C)C(=O)c1cncnc1Oc1cc(Cl)ccc1Cl 10.1021/jm301071h
76322065 106080 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 417 5 0 6 3.8 COc1cccc(-n2nnc(C3CC3)c2C(=O)N(C)c2ccc(C(F)(F)F)nc2)c1 10.1039/C2MD20174G
CHEMBL3132968 106080 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 417 5 0 6 3.8 COc1cccc(-n2nnc(C3CC3)c2C(=O)N(C)c2ccc(C(F)(F)F)nc2)c1 10.1039/C2MD20174G
90654573 109997 None 0 Mouse Functional pEC50 = 6.8 6.8 -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 362 5 1 4 2.8 O=C(NCCc1ccc(Cl)cc1)[C@@H]1CCCN(c2ncc(F)cn2)C1 10.1021/jm401731q
CHEMBL3234554 109997 None 0 Mouse Functional pEC50 = 6.8 6.8 -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 362 5 1 4 2.8 O=C(NCCc1ccc(Cl)cc1)[C@@H]1CCCN(c2ncc(F)cn2)C1 10.1021/jm401731q
90654565 110020 None 0 Mouse Functional pEC50 = 6.8 6.8 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 487 6 1 7 2.4 CN1CCN(c2cc(N3CCC[C@@H]3C(=O)NCCc3ccc(C#N)cc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
CHEMBL3234576 110020 None 0 Mouse Functional pEC50 = 6.8 6.8 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 487 6 1 7 2.4 CN1CCN(c2cc(N3CCC[C@@H]3C(=O)NCCc3ccc(C#N)cc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
118700251 194992 None 0 Mouse Functional pEC50 = 6.8 6.8 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 465 7 0 5 5.5 COc1ccccc1COC(=O)C1=C(C)N(Cc2ccco2)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5394522 194992 None 0 Mouse Functional pEC50 = 6.8 6.8 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 465 7 0 5 5.5 COc1ccccc1COC(=O)C1=C(C)N(Cc2ccco2)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
136166950 91636 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
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
CHEMBL2407929 91636 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
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
130361811 156482 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 445 4 2 3 5.0 C[C@H](CCC(=O)N1CCCC1)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/acs.jmedchem.9b00770
CHEMBL4066443 156482 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 445 4 2 3 5.0 C[C@H](CCC(=O)N1CCCC1)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/acs.jmedchem.9b00770
172465697 196936 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 436 5 4 4 4.2 CC[C@@]1(O)C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)O)CC[C@H]3[C@@H]21 10.1016/j.ejmech.2023.115851
CHEMBL5435161 196936 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 436 5 4 4 4.2 CC[C@@]1(O)C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)O)CC[C@H]3[C@@H]21 10.1016/j.ejmech.2023.115851
71626491 112267 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 410 4 1 4 5.0 O=C(c1cnccc1Oc1ccc2cc[nH]c2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
CHEMBL3290710 112267 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 410 4 1 4 5.0 O=C(c1cnccc1Oc1ccc2cc[nH]c2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
71462788 83030 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 417 3 0 5 5.3 O=C(c1cncnc1Oc1cc(Cl)ccc1Cl)N1CCSc2ccccc21 10.1021/jm301071h
CHEMBL2181232 83030 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 417 3 0 5 5.3 O=C(c1cncnc1Oc1cc(Cl)ccc1Cl)N1CCSc2ccccc21 10.1021/jm301071h
9838552 192201 None 40 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 279 4 1 3 3.5 O=C(O)c1ccc(OCc2ccc3ccccc3n2)cc1 10.1021/acs.jmedchem.1c01078
CHEMBL5202995 192201 None 40 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 279 4 1 3 3.5 O=C(O)c1ccc(OCc2ccc3ccccc3n2)cc1 10.1021/acs.jmedchem.1c01078
45483949 3582 None 33 Human Functional pEC50 = 6.8 6.8 -2 2
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1021/ml300277t
7048 3582 None 33 Human Functional pEC50 = 6.8 6.8 -2 2
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1021/ml300277t
CHEMBL567640 3582 None 33 Human Functional pEC50 = 6.8 6.8 -2 2
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1021/ml300277t
137641119 157101 None 0 Human Functional pEC50 = 4.8 4.8 -28 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 636 12 0 8 6.2 COc1ccc(SCc2cnc(SCc3c(F)cc(S(=O)(=O)/N=C/N(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4073356 157101 None 0 Human Functional pEC50 = 4.8 4.8 -28 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 636 12 0 8 6.2 COc1ccc(SCc2cnc(SCc3c(F)cc(S(=O)(=O)/N=C/N(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
77845060 112281 None 0 Human Functional pEC50 = 5.8 5.8 -7 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 489 5 1 6 5.6 O=C(O)c1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL3290724 112281 None 0 Human Functional pEC50 = 5.8 5.8 -7 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 489 5 1 6 5.6 O=C(O)c1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
1434463 157837 None 2 Mouse Functional pEC50 = 5.8 5.8 -1 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 404 4 0 6 4.4 CCn1c(=O)c2ccccc2n2c(SCc3ccc(C(F)(F)F)cc3)nnc12 10.1021/acs.jmedchem.6b01873
CHEMBL4082345 157837 None 2 Mouse Functional pEC50 = 5.8 5.8 -1 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 404 4 0 6 4.4 CCn1c(=O)c2ccccc2n2c(SCc3ccc(C(F)(F)F)cc3)nnc12 10.1021/acs.jmedchem.6b01873
71626489 112257 None 0 Human Functional pEC50 = 7.8 7.8 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 421 4 0 4 5.7 O=C(c1cnccc1Oc1cccc2ccccc12)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
CHEMBL3290700 112257 None 0 Human Functional pEC50 = 7.8 7.8 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 421 4 0 4 5.7 O=C(c1cnccc1Oc1cccc2ccccc12)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
90654581 110005 None 0 Human Functional pEC50 = 7.8 7.8 7 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 403 5 1 5 2.9 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3nccc(C(F)(F)F)n3)C2)cc1 10.1021/jm401731q
CHEMBL3234562 110005 None 0 Human Functional pEC50 = 7.8 7.8 7 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 403 5 1 5 2.9 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3nccc(C(F)(F)F)n3)C2)cc1 10.1021/jm401731q
90654592 110017 None 0 Mouse Functional pEC50 = 7.8 7.8 2 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 517 7 1 9 1.9 CCN1CCN(c2cc(N3CCC[C@@H](C(=O)NCCc4cnc(C#N)nc4)C3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
CHEMBL3234573 110017 None 0 Mouse Functional pEC50 = 7.8 7.8 2 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 517 7 1 9 1.9 CCN1CCN(c2cc(N3CCC[C@@H](C(=O)NCCc4cnc(C#N)nc4)C3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
118577298 161080 None 0 Mouse Functional pEC50 = 7.8 7.8 18 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 581 9 0 6 6.4 COc1ccc(N(C)c2cnc(SCc3c(F)cc(C#CC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4086463 161080 None 0 Mouse Functional pEC50 = 7.8 7.8 18 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 581 9 0 6 6.4 COc1ccc(N(C)c2cnc(SCc3c(F)cc(C#CC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4096633 161080 None 0 Mouse Functional pEC50 = 7.8 7.8 18 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 581 9 0 6 6.4 COc1ccc(N(C)c2cnc(SCc3c(F)cc(C#CC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4116110 161080 None 0 Mouse Functional pEC50 = 7.8 7.8 18 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 581 9 0 6 6.4 COc1ccc(N(C)c2cnc(SCc3c(F)cc(C#CC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
66739980 139552 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assay
ChEMBL 514 8 0 5 7.4 COc1ccc(C(C)(C)c2cnc(SCc3c(F)cccc3Cl)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2018.04.011
CHEMBL3794175 139552 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assay
ChEMBL 514 8 0 5 7.4 COc1ccc(C(C)(C)c2cnc(SCc3c(F)cccc3Cl)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2018.04.011
89501851 161638 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assay
ChEMBL 540 11 0 6 7.3 COc1ccc(C(C)(C)c2cnc(SCCOCc3cccc(Cl)c3)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2018.04.011
CHEMBL4128655 161638 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assay
ChEMBL 540 11 0 6 7.3 COc1ccc(C(C)(C)c2cnc(SCCOCc3cccc(Cl)c3)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2018.04.011
164611905 185247 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 515 3 2 3 7.5 CNC(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
CHEMBL4856752 185247 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 515 3 2 3 7.5 CNC(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
168277662 190281 None 1 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 321 7 0 3 5.2 CCC(C)COc1cccc(OCc2ccc3ccccc3n2)c1 10.1021/acs.jmedchem.1c01078
CHEMBL5173976 190281 None 1 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 321 7 0 3 5.2 CCC(C)COc1cccc(OCc2ccc3ccccc3n2)c1 10.1021/acs.jmedchem.1c01078
58043414 91651 None 0 Human Functional pEC50 = 6.8 6.8 38 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
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
CHEMBL2407951 91651 None 0 Human Functional pEC50 = 6.8 6.8 38 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
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
90654586 110010 None 0 Mouse Functional pEC50 = 6.8 6.8 2 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 447 6 1 7 2.0 Cc1nc(N2CCN(C)CC2)cc(N2CCC[C@@H](C(=O)NCCc3ccc(C#N)cc3)C2)n1 10.1021/jm401731q
CHEMBL3234567 110010 None 0 Mouse Functional pEC50 = 6.8 6.8 2 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 447 6 1 7 2.0 Cc1nc(N2CCN(C)CC2)cc(N2CCC[C@@H](C(=O)NCCc3ccc(C#N)cc3)C2)n1 10.1021/jm401731q
71626833 118891 None 0 Mouse Functional pEC50 = 4.8 4.8 -1 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 610 11 1 7 5.8 CCOC(=O)CCNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421897 118891 None 0 Mouse Functional pEC50 = 4.8 4.8 -1 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 610 11 1 7 5.8 CCOC(=O)CCNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
101882379 114311 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human GPBAR1 expressed in HEK293T cells assessed as stimulation of cAMP response element-mediated receptor transactivation by luciferase reporter gene assayAgonist activity at human GPBAR1 expressed in HEK293T cells assessed as stimulation of cAMP response element-mediated receptor transactivation by luciferase reporter gene assay
ChEMBL 420 6 3 3 5.3 C[C@H](CCCCC(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm500889f
CHEMBL3330019 114311 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human GPBAR1 expressed in HEK293T cells assessed as stimulation of cAMP response element-mediated receptor transactivation by luciferase reporter gene assayAgonist activity at human GPBAR1 expressed in HEK293T cells assessed as stimulation of cAMP response element-mediated receptor transactivation by luciferase reporter gene assay
ChEMBL 420 6 3 3 5.3 C[C@H](CCCCC(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm500889f
52905075 158851 None 5 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 445 4 2 3 5.0 C[C@H](CCC(=O)N1CCCC1)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/acs.jmedchem.9b00770
CHEMBL4093987 158851 None 5 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 445 4 2 3 5.0 C[C@H](CCC(=O)N1CCCC1)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/acs.jmedchem.9b00770
164617191 184618 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 613 6 4 4 7.1 CC(C)[C@@H]1CC[C@]2(NC(=O)NCC(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
CHEMBL4847526 184618 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 613 6 4 4 7.1 CC(C)[C@@H]1CC[C@]2(NC(=O)NCC(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
164608751 184559 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 567 4 3 4 8.1 CC(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)Nc6cc[nH]n6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
CHEMBL4846632 184559 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 567 4 3 4 8.1 CC(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)Nc6cc[nH]n6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
10790510 101326 None 1 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 469 2 2 3 7.6 C=C(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC/C(=N\O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/jm900872z
CHEMBL296302 101326 None 1 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 469 2 2 3 7.6 C=C(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC/C(=N\O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/jm900872z
172450202 195901 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 448 6 4 4 4.4 C=CC[C@@]1(O)C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)O)CC[C@H]3[C@@H]21 10.1016/j.ejmech.2023.115851
CHEMBL5412957 195901 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 448 6 4 4 4.4 C=CC[C@@]1(O)C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)O)CC[C@H]3[C@@H]21 10.1016/j.ejmech.2023.115851
155669596 180775 None 0 Human Functional pEC50 = 5.8 5.8 1 2
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 358 4 0 4 3.6 O=C(c1cncn1Cc1ccccc1)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
CHEMBL4755237 180775 None 0 Human Functional pEC50 = 5.8 5.8 1 2
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 358 4 0 4 3.6 O=C(c1cncn1Cc1ccccc1)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
118577298 161080 None 0 Human Functional pEC50 = 6.8 6.8 -18 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 581 9 0 6 6.4 COc1ccc(N(C)c2cnc(SCc3c(F)cc(C#CC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4086463 161080 None 0 Human Functional pEC50 = 6.8 6.8 -18 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 581 9 0 6 6.4 COc1ccc(N(C)c2cnc(SCc3c(F)cc(C#CC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4096633 161080 None 0 Human Functional pEC50 = 6.8 6.8 -18 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 581 9 0 6 6.4 COc1ccc(N(C)c2cnc(SCc3c(F)cc(C#CC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4116110 161080 None 0 Human Functional pEC50 = 6.8 6.8 -18 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 581 9 0 6 6.4 COc1ccc(N(C)c2cnc(SCc3c(F)cc(C#CC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
121355127 162906 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay
ChEMBL 444 5 3 5 4.4 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)CCc3nn[nH]n3)[C@@H]2[C@@H]1O 10.1021/acsmedchemlett.7b00318
CHEMBL4172477 162906 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay
ChEMBL 444 5 3 5 4.4 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)CCc3nn[nH]n3)[C@@H]2[C@@H]1O 10.1021/acsmedchemlett.7b00318
118709776 113628 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 389 3 2 3 4.2 O=C(Nc1cc(Cl)ccc1Cl)C1(C(=O)N2CCNc3ccccc32)CC1 10.1016/j.bmcl.2014.07.026
CHEMBL3321849 113628 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 389 3 2 3 4.2 O=C(Nc1cc(Cl)ccc1Cl)C1(C(=O)N2CCNc3ccccc32)CC1 10.1016/j.bmcl.2014.07.026
90644449 112262 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 422 4 0 5 5.1 O=C(c1cnccc1Oc1cccc2cccnc12)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
CHEMBL3290705 112262 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 422 4 0 5 5.1 O=C(c1cnccc1Oc1cccc2cccnc12)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
137646061 157907 None 0 Human Functional pEC50 = 4.8 4.8 -3 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 502 9 0 6 6.7 COc1ccc(OCc2cnc(SCc3c(F)cccc3Cl)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4083324 157907 None 0 Human Functional pEC50 = 4.8 4.8 -3 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 502 9 0 6 6.7 COc1ccc(OCc2cnc(SCc3c(F)cccc3Cl)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
71561885 87683 None 0 Human Functional pEC50 = 7.8 7.8 - 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 460 6 0 6 4.7 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N(Cc1cccnc1)C1CCOC1 10.1016/j.bmcl.2012.12.076
CHEMBL2336237 87683 None 0 Human Functional pEC50 = 7.8 7.8 - 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 460 6 0 6 4.7 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N(Cc1cccnc1)C1CCOC1 10.1016/j.bmcl.2012.12.076
90644444 112292 None 0 Human Functional pEC50 = 7.8 7.8 4 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 587 8 0 8 6.1 CCOC(=O)CCc1oc2ccc(Cl)c(C(=O)Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c2c1C 10.1016/j.ejmech.2014.05.031
CHEMBL3290735 112292 None 0 Human Functional pEC50 = 7.8 7.8 4 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 587 8 0 8 6.1 CCOC(=O)CCc1oc2ccc(Cl)c(C(=O)Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c2c1C 10.1016/j.ejmech.2014.05.031
90654597 110061 None 0 Human Functional pEC50 = 7.8 7.8 -17 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 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 Human Functional pEC50 = 7.8 7.8 -17 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 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
90644458 112289 None 0 Mouse Functional pEC50 = 7.8 7.8 1 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 529 6 1 6 6.3 Cc1c(/C=C/C(=O)O)oc2ccc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c12 10.1016/j.ejmech.2014.05.031
CHEMBL3290732 112289 None 0 Mouse Functional pEC50 = 7.8 7.8 1 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 529 6 1 6 6.3 Cc1c(/C=C/C(=O)O)oc2ccc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c12 10.1016/j.ejmech.2014.05.031
53311869 83037 None 0 Mouse Functional pEC50 = 7.8 7.8 -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 439 4 0 4 5.8 O=C(c1cnccc1Oc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/jm301071h
CHEMBL2181239 83037 None 0 Mouse Functional pEC50 = 7.8 7.8 -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 439 4 0 4 5.8 O=C(c1cnccc1Oc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/jm301071h
118694573 196130 None 0 Mouse Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5417359 196130 None 0 Mouse Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
164628005 186592 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 555 4 2 4 7.2 CC1(C)[C@H](OC(=O)NC2CC2)CC[C@@]2(C)[C@H]1CC[C@]1(C)[C@@H]2CC[C@@H]2[C@H]3[C@H]([C@@]4(C)CO4)CC[C@]3(C(=O)O)CC[C@]21C 10.1021/acs.jmedchem.1c00851
CHEMBL4877060 186592 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 555 4 2 4 7.2 CC1(C)[C@H](OC(=O)NC2CC2)CC[C@@]2(C)[C@H]1CC[C@]1(C)[C@@H]2CC[C@@H]2[C@H]3[C@H]([C@@]4(C)CO4)CC[C@]3(C(=O)O)CC[C@]21C 10.1021/acs.jmedchem.1c00851
118586282 159649 None 0 Mouse Functional pEC50 = 6.8 6.8 23 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 486 8 0 7 5.8 COc1ccc(N(C)c2nnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4102610 159649 None 0 Mouse Functional pEC50 = 6.8 6.8 23 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 486 8 0 7 5.8 COc1ccc(N(C)c2nnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
168270223 190174 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 321 8 0 3 5.4 CCCCCOc1cccc(OCc2ccc3ccccc3n2)c1 10.1021/acs.jmedchem.1c01078
CHEMBL5172427 190174 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 321 8 0 3 5.4 CCCCCOc1cccc(OCc2ccc3ccccc3n2)c1 10.1021/acs.jmedchem.1c01078
118694337 196734 None 0 Human Functional pEC50 = 5.8 5.8 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 426 7 0 4 4.2 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CCN(C)C 10.1021/acs.jmedchem.2c01881
CHEMBL5431170 196734 None 0 Human Functional pEC50 = 5.8 5.8 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 426 7 0 4 4.2 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CCN(C)C 10.1021/acs.jmedchem.2c01881
118694407 196885 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 399 4 1 3 4.1 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Br)cc2)CC(=O)N1 10.1021/acs.jmedchem.2c01881
CHEMBL5434173 196885 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 399 4 1 3 4.1 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Br)cc2)CC(=O)N1 10.1021/acs.jmedchem.2c01881
6013 141957 None 24 Human Functional pEC50 = 4.7 4.7 -575 2
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 288 0 1 2 3.9 C[C@]12CC[C@H]3[C@@H](CCC4=CC(=O)CC[C@@]43C)[C@@H]1CC[C@@H]2O 10.1021/jm7015864
CHEMBL386630 141957 None 24 Human Functional pEC50 = 4.7 4.7 -575 2
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 288 0 1 2 3.9 C[C@]12CC[C@H]3[C@@H](CCC4=CC(=O)CC[C@@]43C)[C@@H]1CC[C@@H]2O 10.1021/jm7015864
172460837 196263 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 498 6 2 5 5.6 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)Oc4ccccc4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
CHEMBL5419988 196263 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 498 6 2 5 5.6 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)Oc4ccccc4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
137651596 157220 None 0 Mouse Functional pEC50 = 4.7 4.7 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 546 6 0 4 8.7 COc1cc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(Cl)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4075062 157220 None 0 Mouse Functional pEC50 = 4.7 4.7 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 546 6 0 4 8.7 COc1cc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(Cl)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
118464638 159629 None 0 Human Functional pEC50 = 5.7 5.7 -15 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 494 6 0 6 6.4 COc1cc(C2(C)CCCc3nc(SCc4ncccn4)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4102357 159629 None 0 Human Functional pEC50 = 5.7 5.7 -15 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 494 6 0 6 6.4 COc1cc(C2(C)CCCc3nc(SCc4ncccn4)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
11656002 83044 None 22 Human Functional pEC50 = 7.7 7.7 61 8
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 484 3 0 3 5.8 O=C1COc2nccc(-c3ccccc3F)c2CN1Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2181247 83044 None 22 Human Functional pEC50 = 7.7 7.7 61 8
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 484 3 0 3 5.8 O=C1COc2nccc(-c3ccccc3F)c2CN1Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
90654568 110023 None 0 Human Functional pEC50 = 7.7 7.7 -4 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 488 7 1 8 1.8 CCN1CCN(c2cc(N3CC[C@H]3C(=O)NCCc3ccc(C#N)nc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
CHEMBL3234579 110023 None 0 Human Functional pEC50 = 7.7 7.7 -4 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 488 7 1 8 1.8 CCN1CCN(c2cc(N3CC[C@H]3C(=O)NCCc3ccc(C#N)nc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
46232361 202962 None 0 Human Functional pEC50 = 7.7 7.7 - 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 354 3 0 3 5.2 Cc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1C 10.1016/j.bmcl.2010.01.003
CHEMBL598743 202962 None 0 Human Functional pEC50 = 7.7 7.7 - 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 354 3 0 3 5.2 Cc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1C 10.1016/j.bmcl.2010.01.003
46232414 203068 None 0 Human Functional pEC50 = 7.7 7.7 - 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 394 3 0 3 5.6 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL599328 203068 None 0 Human Functional pEC50 = 7.7 7.7 - 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 394 3 0 3 5.6 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.01.003
46232598 203415 None 0 Human Functional pEC50 = 7.7 7.7 - 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 326 3 0 3 4.6 Cc1onc(-c2ccccc2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL601882 203415 None 0 Human Functional pEC50 = 7.7 7.7 - 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 326 3 0 3 4.6 Cc1onc(-c2ccccc2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
46232660 203721 None 0 Human Functional pEC50 = 7.7 7.7 - 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 388 4 0 3 6.0 CC(C)c1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL603921 203721 None 0 Human Functional pEC50 = 7.7 7.7 - 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 388 4 0 3 6.0 CC(C)c1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
118694352 195534 None 0 Human Functional pEC50 = 6.7 6.7 3 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 457 9 0 5 4.7 COCCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5405469 195534 None 0 Human Functional pEC50 = 6.7 6.7 3 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 457 9 0 5 4.7 COCCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
90654583 110007 None 0 Mouse Functional pEC50 = 6.7 6.7 -2 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 447 6 1 7 2.0 Cc1cc(N2CCN(C)CC2)nc(N2CCC[C@@H](C(=O)NCCc3ccc(C#N)cc3)C2)n1 10.1021/jm401731q
CHEMBL3234564 110007 None 0 Mouse Functional pEC50 = 6.7 6.7 -2 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 447 6 1 7 2.0 Cc1cc(N2CCN(C)CC2)nc(N2CCC[C@@H](C(=O)NCCc3ccc(C#N)cc3)C2)n1 10.1021/jm401731q
66737485 195258 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human TGR5 transfected in HEK293T cells by CRE-driven luciferase reporter assayAgonist activity at human TGR5 transfected in HEK293T cells by CRE-driven luciferase reporter assay
ChEMBL 422 4 4 4 3.8 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](C[C@H](O)[C@]12C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@]3(C)O 10.1016/j.ejmech.2023.115851
CHEMBL5399551 195258 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human TGR5 transfected in HEK293T cells by CRE-driven luciferase reporter assayAgonist activity at human TGR5 transfected in HEK293T cells by CRE-driven luciferase reporter assay
ChEMBL 422 4 4 4 3.8 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](C[C@H](O)[C@]12C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@]3(C)O 10.1016/j.ejmech.2023.115851
130361919 157200 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 459 5 1 3 5.7 CO[C@@H]1CC[C@]2(C)[C@H]3CC[C@@]4(C)[C@@H](CC[C@@H]4[C@H](C)CCC(=O)N4CCCC4)[C@@H]3[C@H](O)C[C@@H]2C1 10.1021/acs.jmedchem.9b00770
CHEMBL4074652 157200 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 459 5 1 3 5.7 CO[C@@H]1CC[C@]2(C)[C@H]3CC[C@@]4(C)[C@@H](CC[C@@H]4[C@H](C)CCC(=O)N4CCCC4)[C@@H]3[C@H](O)C[C@@H]2C1 10.1021/acs.jmedchem.9b00770
172459385 196473 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 436 5 4 4 4.1 CC[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@]12C)C(=O)O 10.1016/j.ejmech.2023.115851
CHEMBL5424633 196473 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 436 5 4 4 4.1 CC[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@]12C)C(=O)O 10.1016/j.ejmech.2023.115851
387316 66790 None 37 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 499 7 4 5 3.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
CHEMBL185878 66790 None 37 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 499 7 4 5 3.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
126700763 158545 None 0 Mouse Functional pEC50 = 5.7 5.7 - 1
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 557 11 1 7 6.4 COc1ccc(N(C)c2c(CCC(=O)O)nc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4090586 158545 None 0 Mouse Functional pEC50 = 5.7 5.7 - 1
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 557 11 1 7 6.4 COc1ccc(N(C)c2c(CCC(=O)O)nc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
172456467 196438 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 450 6 2 5 4.6 CCOC(=O)CC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](OC)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@]12C 10.1016/j.bmc.2023.117418
CHEMBL5423954 196438 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 450 6 2 5 4.6 CCOC(=O)CC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](OC)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@]12C 10.1016/j.bmc.2023.117418
118103740 163649 None 0 Human Functional pEC50 = 6.7 6.7 -25 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 761 14 6 12 2.0 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(OCc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)cn1 10.1021/acs.jmedchem.8b00308
CHEMBL4202994 163649 None 0 Human Functional pEC50 = 6.7 6.7 -25 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 761 14 6 12 2.0 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(OCc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)cn1 10.1021/acs.jmedchem.8b00308
71661220 163716 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 429 4 0 3 5.0 O=C([C@@H]1CCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4203777 163716 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 429 4 0 3 5.0 O=C([C@@H]1CCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118093390 163965 None 0 Human Functional pEC50 = 6.7 6.7 -19 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 760 14 6 11 2.6 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(OCc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)cc1 10.1021/acs.jmedchem.8b00308
CHEMBL4206832 163965 None 0 Human Functional pEC50 = 6.7 6.7 -19 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 760 14 6 11 2.6 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(OCc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)cc1 10.1021/acs.jmedchem.8b00308
71661186 164377 None 0 Human Functional pEC50 = 6.7 6.7 -3 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 532 9 1 5 5.6 NCCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4211892 164377 None 0 Human Functional pEC50 = 6.7 6.7 -3 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 532 9 1 5 5.6 NCCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
118093420 164640 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 459 5 0 4 4.6 CO[C@H]1C[C@@H](C(=O)N2CCN(C3CC3)c3ccccc32)N(Cc2cc(Cl)ccc2Cl)C1 10.1021/acs.jmedchem.8b00308
CHEMBL4215113 164640 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 459 5 0 4 4.6 CO[C@H]1C[C@@H](C(=O)N2CCN(C3CC3)c3ccccc32)N(Cc2cc(Cl)ccc2Cl)C1 10.1021/acs.jmedchem.8b00308
118694469 194962 None 0 Human Functional pEC50 = 6.7 6.7 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
CHEMBL5394197 194962 None 0 Human Functional pEC50 = 6.7 6.7 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
118694360 195298 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5400262 195298 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694352 195534 None 0 Human Functional pEC50 = 6.7 6.7 3 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 457 9 0 5 4.7 COCCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5405469 195534 None 0 Human Functional pEC50 = 6.7 6.7 3 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 457 9 0 5 4.7 COCCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
118694528 195681 None 0 Human Functional pEC50 = 6.7 6.7 3 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(Cl)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5408901 195681 None 0 Human Functional pEC50 = 6.7 6.7 3 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(Cl)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694566 195890 None 0 Human Functional pEC50 = 6.7 6.7 3 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(F)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5412722 195890 None 0 Human Functional pEC50 = 6.7 6.7 3 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(F)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694348 196364 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(OC)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5422305 196364 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(OC)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694371 197143 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 455 7 0 4 5.2 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2c(C)cc(C)cc2C)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5439826 197143 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 455 7 0 4 5.2 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2c(C)cc(C)cc2C)=C1C 10.1021/acs.jmedchem.2c01881
118694344 195706 None 0 Mouse Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5409356 195706 None 0 Mouse Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
118694538 196021 None 0 Mouse Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 6 0 5 3.8 COC(=O)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5415202 196021 None 0 Mouse Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 6 0 5 3.8 COC(=O)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
155528730 171482 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 469 5 3 5 3.5 C[C@H](CCC(=O)NS(C)(=O)=O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/acs.jmedchem.9b00770
CHEMBL4461961 171482 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 469 5 3 5 3.5 C[C@H](CCC(=O)NS(C)(=O)=O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/acs.jmedchem.9b00770
118093418 164190 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 443 4 0 3 5.4 O=C([C@H]1CCCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4209597 164190 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 443 4 0 3 5.4 O=C([C@H]1CCCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118694337 196734 None 0 Human Functional pEC50 = 5.7 5.7 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 426 7 0 4 4.2 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CCN(C)C 10.1021/acs.jmedchem.2c01881
CHEMBL5431170 196734 None 0 Human Functional pEC50 = 5.7 5.7 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 426 7 0 4 4.2 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CCN(C)C 10.1021/acs.jmedchem.2c01881
118694407 196885 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 399 4 1 3 4.1 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Br)cc2)CC(=O)N1 10.1021/acs.jmedchem.2c01881
CHEMBL5434173 196885 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 399 4 1 3 4.1 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Br)cc2)CC(=O)N1 10.1021/acs.jmedchem.2c01881
118694325 197155 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 373 4 1 3 4.1 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2F)CC(=O)N1 10.1021/acs.jmedchem.2c01881
CHEMBL5439948 197155 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 373 4 1 3 4.1 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2F)CC(=O)N1 10.1021/acs.jmedchem.2c01881
46232986 203246 None 0 Human Functional pEC50 = 5.7 5.7 - 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 360 3 0 3 5.2 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccccc1Cl 10.1016/j.bmcl.2010.01.003
CHEMBL600624 203246 None 0 Human Functional pEC50 = 5.7 5.7 - 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 360 3 0 3 5.2 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccccc1Cl 10.1016/j.bmcl.2010.01.003
71661222 164592 None 0 Mouse Functional pEC50 = 5.7 5.7 -1 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 443 4 0 3 5.4 O=C([C@@H]1CCCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4214506 164592 None 0 Mouse Functional pEC50 = 5.7 5.7 -1 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 443 4 0 3 5.4 O=C([C@@H]1CCCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
44605616 200751 None 49 Rat Functional pEC50 = 5.7 5.7 -28 2
Agonist activity at rat TGR5 expressed in melanophores assessed as melanosome dispersion by melanophore assayAgonist activity at rat TGR5 expressed in melanophores assessed as melanosome dispersion by melanophore assay
ChEMBL 360 3 0 3 5.2 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(Cl)cc1 10.1021/jm901434t
CHEMBL575966 200751 None 49 Rat Functional pEC50 = 5.7 5.7 -28 2
Agonist activity at rat TGR5 expressed in melanophores assessed as melanosome dispersion by melanophore assayAgonist activity at rat TGR5 expressed in melanophores assessed as melanosome dispersion by melanophore assay
ChEMBL 360 3 0 3 5.2 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(Cl)cc1 10.1021/jm901434t
90654584 110008 None 0 Human Functional pEC50 = 8.7 8.7 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 501 6 1 7 2.7 CN1CCN(c2cc(C(F)(F)F)nc(N3CCC[C@@H](C(=O)NCCc4ccc(C#N)cc4)C3)n2)CC1 10.1021/jm401731q
CHEMBL3234565 110008 None 0 Human Functional pEC50 = 8.7 8.7 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 501 6 1 7 2.7 CN1CCN(c2cc(C(F)(F)F)nc(N3CCC[C@@H](C(=O)NCCc4ccc(C#N)cc4)C3)n2)CC1 10.1021/jm401731q
71540078 87330 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 422 6 1 5 2.6 CCc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1021/ml300277t
CHEMBL2331653 87330 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 422 6 1 5 2.6 CCc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1021/ml300277t
118694559 1134 None 3 Human Functional pEC50 = 8.7 8.7 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COC1=C(C=CC=C1)COC(=O)C=2[C@@H](CC(N(C2C)C[C@@H]3OCCC3)=O)C=4C=NC(=CC4)Cl 10.1021/acs.jmedchem.2c01881
12906 1134 None 3 Human Functional pEC50 = 8.7 8.7 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COC1=C(C=CC=C1)COC(=O)C=2[C@@H](CC(N(C2C)C[C@@H]3OCCC3)=O)C=4C=NC(=CC4)Cl 10.1021/acs.jmedchem.2c01881
CHEMBL5434983 1134 None 3 Human Functional pEC50 = 8.7 8.7 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COC1=C(C=CC=C1)COC(=O)C=2[C@@H](CC(N(C2C)C[C@@H]3OCCC3)=O)C=4C=NC(=CC4)Cl 10.1021/acs.jmedchem.2c01881
145007569 195011 None 0 Human Functional pEC50 = 8.7 8.7 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(CC2CCCO2)C(=O)CC1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
CHEMBL5394911 195011 None 0 Human Functional pEC50 = 8.7 8.7 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(CC2CCCO2)C(=O)CC1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
71455634 83024 None 0 Mouse Functional pEC50 = 8.7 8.7 -4 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 473 4 0 4 6.5 O=C(c1cnccc1Oc1cc(Cl)c(Cl)cc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/jm301071h
CHEMBL2181227 83024 None 0 Mouse Functional pEC50 = 8.7 8.7 -4 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 473 4 0 4 6.5 O=C(c1cnccc1Oc1cc(Cl)c(Cl)cc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/jm301071h
90654566 110021 None 0 Mouse Functional pEC50 = 8.7 8.7 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 473 6 1 7 2.1 CN1CCN(c2cc(N3CC[C@H]3C(=O)NCCc3ccc(C#N)cc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
CHEMBL3234577 110021 None 0 Mouse Functional pEC50 = 8.7 8.7 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 473 6 1 7 2.1 CN1CCN(c2cc(N3CC[C@H]3C(=O)NCCc3ccc(C#N)cc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
90654595 110026 None 0 Mouse Functional pEC50 = 8.7 8.7 7 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 636 10 2 8 4.6 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3cc(N4CCC(Oc5ccc(CC(=O)O)cc5)CC4)nc(C(F)(F)F)n3)C2)cc1 10.1021/jm401731q
CHEMBL3234582 110026 None 0 Mouse Functional pEC50 = 8.7 8.7 7 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 636 10 2 8 4.6 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3cc(N4CCC(Oc5ccc(CC(=O)O)cc5)CC4)nc(C(F)(F)F)n3)C2)cc1 10.1021/jm401731q
90654596 110027 None 0 Mouse Functional pEC50 = 8.7 8.7 15 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 10 2 8 4.0 N#Cc1ccc(CCNC(=O)[C@@H]2CCN2c2cc(N3CCC(Oc4ccc(CC(=O)O)cc4)CC3)nc(C(F)(F)F)n2)cc1 10.1021/jm401731q
CHEMBL3234583 110027 None 0 Mouse Functional pEC50 = 8.7 8.7 15 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 10 2 8 4.0 N#Cc1ccc(CCNC(=O)[C@@H]2CCN2c2cc(N3CCC(Oc4ccc(CC(=O)O)cc4)CC3)nc(C(F)(F)F)n2)cc1 10.1021/jm401731q
90654599 110063 None 0 Mouse Functional pEC50 = 8.7 8.7 12 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 571 8 2 6 5.3 N#Cc1ccc(CCNC(=O)[C@@H]2CCN2c2cc(-c3ccc(-c4ccc(C(=O)O)cc4)cc3)nc(C(F)(F)F)n2)cc1 10.1021/jm401731q
CHEMBL3234870 110063 None 0 Mouse Functional pEC50 = 8.7 8.7 12 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 571 8 2 6 5.3 N#Cc1ccc(CCNC(=O)[C@@H]2CCN2c2cc(-c3ccc(-c4ccc(C(=O)O)cc4)cc3)nc(C(F)(F)F)n2)cc1 10.1021/jm401731q
118576958 158497 None 0 Mouse Functional pEC50 = 8.7 8.7 17 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 519 8 0 6 7.0 COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)c(Cl)c2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4090147 158497 None 0 Mouse Functional pEC50 = 8.7 8.7 17 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 519 8 0 6 7.0 COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)c(Cl)c2)cc1OC 10.1021/acs.jmedchem.6b01873
156705090 181813 None 0 Human Functional pEC50 = 8.7 8.7 54 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 497 7 0 7 5.8 CCCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4776876 181813 None 0 Human Functional pEC50 = 8.7 8.7 54 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 497 7 0 7 5.8 CCCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
76322064 106077 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 370 5 0 5 3.8 CCc1nnn(-c2cccc(OC)c2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1039/C2MD20174G
CHEMBL3132965 106077 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 370 5 0 5 3.8 CCc1nnn(-c2cccc(OC)c2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1039/C2MD20174G
71462786 83025 None 0 Mouse Functional pEC50 = 8.7 8.7 -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 413 4 0 4 5.4 Cc1cc(C)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1C 10.1021/jm301071h
CHEMBL2181228 83025 None 0 Mouse Functional pEC50 = 8.7 8.7 -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 413 4 0 4 5.4 Cc1cc(C)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1C 10.1021/jm301071h
172442531 194984 None 0 Mouse Functional pEC50 = 8.7 8.7 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1325 39 3 16 7.8 N[C@@H](CC(=O)N1CCCN(CC(=O)NCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)C(=O)C1Cc1ccccc1)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5394421 194984 None 0 Mouse Functional pEC50 = 8.7 8.7 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1325 39 3 16 7.8 N[C@@H](CC(=O)N1CCCN(CC(=O)NCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)C(=O)C1Cc1ccccc1)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
172470380 197057 None 0 Mouse Functional pEC50 = 8.7 8.7 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1249 37 3 16 6.6 CC1C(=O)N(CC(=O)NCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5437749 197057 None 0 Mouse Functional pEC50 = 8.7 8.7 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1249 37 3 16 6.6 CC1C(=O)N(CC(=O)NCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
71540073 87325 None 0 Human Functional pEC50 = 8.6 8.6 - 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 437 7 2 6 2.4 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1016/j.bmcl.2012.12.076
CHEMBL2331648 87325 None 0 Human Functional pEC50 = 8.6 8.6 - 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 437 7 2 6 2.4 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1016/j.bmcl.2012.12.076
145962358 161535 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assay
ChEMBL 531 11 0 7 6.5 COc1ccc(C(C)(C)c2cnc(SCCOCc3ccc(C#N)cc3)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2018.04.011
CHEMBL4127302 161535 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assay
ChEMBL 531 11 0 7 6.5 COc1ccc(C(C)(C)c2cnc(SCCOCc3ccc(C#N)cc3)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2018.04.011
71540073 87325 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 437 7 2 6 2.4 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1021/ml300277t
CHEMBL2331648 87325 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 437 7 2 6 2.4 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1021/ml300277t
71461054 83028 None 0 Mouse Functional pEC50 = 8.6 8.6 -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 467 5 0 4 6.4 CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm301071h
CHEMBL2181230 83028 None 0 Mouse Functional pEC50 = 8.6 8.6 -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 467 5 0 4 6.4 CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm301071h
172454739 196023 None 0 Mouse Functional pEC50 = 8.6 8.6 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1281 36 3 15 7.8 N[C@@H](CC(=O)N1CCCN(CC(=O)NCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)C(=O)C1Cc1ccccc1)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5415272 196023 None 0 Mouse Functional pEC50 = 8.6 8.6 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1281 36 3 15 7.8 N[C@@H](CC(=O)N1CCCN(CC(=O)NCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)C(=O)C1Cc1ccccc1)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
172455948 196396 None 0 Mouse Functional pEC50 = 8.6 8.6 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1386 42 3 17 8.5 C.N[C@@H](CC(=O)N1CCCN(CC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)C(=O)C1Cc1ccccc1)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5422904 196396 None 0 Mouse Functional pEC50 = 8.6 8.6 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1386 42 3 17 8.5 C.N[C@@H](CC(=O)N1CCCN(CC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)C(=O)C1Cc1ccccc1)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
172464926 196610 None 0 Mouse Functional pEC50 = 8.6 8.6 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1161 31 3 14 6.6 CC1C(=O)N(CC(=O)NCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5427760 196610 None 0 Mouse Functional pEC50 = 8.6 8.6 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1161 31 3 14 6.6 CC1C(=O)N(CC(=O)NCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
172449851 197423 None 0 Mouse Functional pEC50 = 8.6 8.6 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1205 34 3 15 6.6 CC1C(=O)N(CC(=O)NCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5414305 197423 None 0 Mouse Functional pEC50 = 8.6 8.6 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1205 34 3 15 6.6 CC1C(=O)N(CC(=O)NCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5499101 197423 None 0 Mouse Functional pEC50 = 8.6 8.6 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1205 34 3 15 6.6 CC1C(=O)N(CC(=O)NCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
71561882 87680 None 0 Human Functional pEC50 = 8.6 8.6 - 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 446 7 0 5 5.7 CCC(C)N(Cc1cccnc1)C(=O)c1c(C)nn(C)c1Oc1cccc(Cl)c1Cl 10.1016/j.bmcl.2012.12.076
CHEMBL2336234 87680 None 0 Human Functional pEC50 = 8.6 8.6 - 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 446 7 0 5 5.7 CCC(C)N(Cc1cccnc1)C(=O)c1c(C)nn(C)c1Oc1cccc(Cl)c1Cl 10.1016/j.bmcl.2012.12.076
71626699 112273 None 0 Mouse Functional pEC50 = 8.6 8.6 -5 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 425 4 0 5 5.6 Cc1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
CHEMBL3290716 112273 None 0 Mouse Functional pEC50 = 8.6 8.6 -5 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 425 4 0 5 5.6 Cc1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
172439348 195035 None 0 Mouse Functional pEC50 = 8.6 8.6 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1293 40 3 17 6.6 CC1C(=O)N(CC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5395284 195035 None 0 Mouse Functional pEC50 = 8.6 8.6 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1293 40 3 17 6.6 CC1C(=O)N(CC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
71541719 87323 None 1 Human Functional pEC50 = 8.6 8.6 194 3
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 395 7 2 5 2.6 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(C(C)C)cc1)CC2 10.1021/ml300277t
CHEMBL2331646 87323 None 1 Human Functional pEC50 = 8.6 8.6 194 3
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 395 7 2 5 2.6 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(C(C)C)cc1)CC2 10.1021/ml300277t
172464926 196610 None 0 Human Functional pEC50 = 8.6 8.6 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1161 31 3 14 6.6 CC1C(=O)N(CC(=O)NCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5427760 196610 None 0 Human Functional pEC50 = 8.6 8.6 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1161 31 3 14 6.6 CC1C(=O)N(CC(=O)NCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
118103679 164043 None 0 Mouse Functional pEC50 = 8.6 8.6 39 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 761 14 6 12 2.0 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(COc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)nc1 10.1021/acs.jmedchem.8b00308
CHEMBL4207707 164043 None 0 Mouse Functional pEC50 = 8.6 8.6 39 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 761 14 6 12 2.0 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(COc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)nc1 10.1021/acs.jmedchem.8b00308
118103737 164926 None 0 Mouse Functional pEC50 = 8.6 8.6 - 1
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 738 12 3 7 5.1 O=C(NCCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)N1CCN(CP(=O)(O)O)CC1 10.1021/acs.jmedchem.8b00308
CHEMBL4218746 164926 None 0 Mouse Functional pEC50 = 8.6 8.6 - 1
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 738 12 3 7 5.1 O=C(NCCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)N1CCN(CP(=O)(O)O)CC1 10.1021/acs.jmedchem.8b00308
118694559 1134 None 3 Mouse Functional pEC50 = 8.6 8.6 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COC1=C(C=CC=C1)COC(=O)C=2[C@@H](CC(N(C2C)C[C@@H]3OCCC3)=O)C=4C=NC(=CC4)Cl 10.1021/acs.jmedchem.2c01881
12906 1134 None 3 Mouse Functional pEC50 = 8.6 8.6 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COC1=C(C=CC=C1)COC(=O)C=2[C@@H](CC(N(C2C)C[C@@H]3OCCC3)=O)C=4C=NC(=CC4)Cl 10.1021/acs.jmedchem.2c01881
CHEMBL5434983 1134 None 3 Mouse Functional pEC50 = 8.6 8.6 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COC1=C(C=CC=C1)COC(=O)C=2[C@@H](CC(N(C2C)C[C@@H]3OCCC3)=O)C=4C=NC(=CC4)Cl 10.1021/acs.jmedchem.2c01881
71540076 87328 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 417 7 2 5 2.6 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(C(C)(F)F)cc1)CC2 10.1021/ml300277t
CHEMBL2331651 87328 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 417 7 2 5 2.6 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(C(C)(F)F)cc1)CC2 10.1021/ml300277t
172470699 197151 None 0 Mouse Functional pEC50 = 8.6 8.6 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1237 33 3 14 7.8 N[C@@H](CC(=O)N1CCCN(CC(=O)NCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)C(=O)C1Cc1ccccc1)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5439914 197151 None 0 Mouse Functional pEC50 = 8.6 8.6 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1237 33 3 14 7.8 N[C@@H](CC(=O)N1CCCN(CC(=O)NCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)C(=O)C1Cc1ccccc1)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
156705112 182970 None 0 Human Functional pEC50 = 8.6 8.6 15 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 483 6 0 7 5.4 CCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4791709 182970 None 0 Human Functional pEC50 = 8.6 8.6 15 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 483 6 0 7 5.4 CCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
71450252 83038 None 0 Human Functional pEC50 = 8.6 8.6 10 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 6.2 O=C(c1cnccc1Oc1cc(Cl)ccc1Cl)N1CCN(C2CCC2)c2ccccc21 10.1021/jm301071h
CHEMBL2181240 83038 None 0 Human Functional pEC50 = 8.6 8.6 10 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 6.2 O=C(c1cnccc1Oc1cc(Cl)ccc1Cl)N1CCN(C2CCC2)c2ccccc21 10.1021/jm301071h
71540175 87332 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 434 6 1 5 2.9 NC(=O)c1nc(C2CC2)nc2c1CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1021/ml300277t
CHEMBL2331655 87332 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 434 6 1 5 2.9 NC(=O)c1nc(C2CC2)nc2c1CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1021/ml300277t
172470380 197057 None 0 Human Functional pEC50 = 8.6 8.6 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1249 37 3 16 6.6 CC1C(=O)N(CC(=O)NCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5437749 197057 None 0 Human Functional pEC50 = 8.6 8.6 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1249 37 3 16 6.6 CC1C(=O)N(CC(=O)NCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
172449851 197423 None 0 Human Functional pEC50 = 8.6 8.6 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1205 34 3 15 6.6 CC1C(=O)N(CC(=O)NCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5414305 197423 None 0 Human Functional pEC50 = 8.6 8.6 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1205 34 3 15 6.6 CC1C(=O)N(CC(=O)NCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5499101 197423 None 0 Human Functional pEC50 = 8.6 8.6 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1205 34 3 15 6.6 CC1C(=O)N(CC(=O)NCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
53311869 83037 None 0 Human Functional pEC50 = 8.6 8.6 3 2
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 439 4 0 4 5.8 O=C(c1cnccc1Oc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
CHEMBL2181239 83037 None 0 Human Functional pEC50 = 8.6 8.6 3 2
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 439 4 0 4 5.8 O=C(c1cnccc1Oc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
71452080 83052 None 0 Human Functional pEC50 = 8.5 8.5 10 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 440 4 0 5 5.2 O=C(c1cncnc1Oc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/jm301071h
CHEMBL2181256 83052 None 0 Human Functional pEC50 = 8.5 8.5 10 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 440 4 0 5 5.2 O=C(c1cncnc1Oc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/jm301071h
118709771 113592 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 429 3 2 6 4.3 CN1CCN(C(=O)c2cnc(O)nc2Nc2cc(Cl)ccc2Cl)c2ccccc21 10.1016/j.bmcl.2014.07.026
CHEMBL3321758 113592 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 429 3 2 6 4.3 CN1CCN(C(=O)c2cnc(O)nc2Nc2cc(Cl)ccc2Cl)c2ccccc21 10.1016/j.bmcl.2014.07.026
71452078 83048 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 428 4 0 5 5.1 CCN1CCN(C(=O)c2cncnc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
CHEMBL2181252 83048 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 428 4 0 5 5.1 CCN1CCN(C(=O)c2cncnc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
90654563 110018 None 0 Human Functional pEC50 = 7.7 7.7 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 501 6 1 7 2.8 CN1CCN(c2cc(N3CCCC[C@H]3C(=O)NCCc3ccc(C#N)cc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
CHEMBL3234574 110018 None 0 Human Functional pEC50 = 7.7 7.7 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 501 6 1 7 2.8 CN1CCN(c2cc(N3CCCC[C@H]3C(=O)NCCc3ccc(C#N)cc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
118576930 158907 None 0 Human Functional pEC50 = 7.7 7.7 -25 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human 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 Human Functional pEC50 = 7.7 7.7 -25 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human 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
118694360 195298 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5400262 195298 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694528 195681 None 0 Human Functional pEC50 = 6.7 6.7 3 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(Cl)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5408901 195681 None 0 Human Functional pEC50 = 6.7 6.7 3 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(Cl)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694566 195890 None 0 Human Functional pEC50 = 6.7 6.7 3 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(F)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5412722 195890 None 0 Human Functional pEC50 = 6.7 6.7 3 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(F)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694348 196364 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(OC)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5422305 196364 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(OC)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694371 197143 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 455 7 0 4 5.2 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2c(C)cc(C)cc2C)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5439826 197143 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 455 7 0 4 5.2 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2c(C)cc(C)cc2C)=C1C 10.1021/acs.jmedchem.2c01881
118694344 195706 None 0 Mouse Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5409356 195706 None 0 Mouse Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
118694538 196021 None 0 Mouse Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 6 0 5 3.8 COC(=O)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5415202 196021 None 0 Mouse Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 6 0 5 3.8 COC(=O)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694477 196545 None 0 Mouse Functional pEC50 = 6.7 6.7 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 463 7 0 4 5.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc3ccccc3c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5426387 196545 None 0 Mouse Functional pEC50 = 6.7 6.7 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 463 7 0 4 5.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc3ccccc3c2)=C1C 10.1021/acs.jmedchem.2c01881
90655904 112869 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Transactivation of human GP-BAR1 transfected in HEK293T cells assessed as induction of intracellular cAMP production after 18 hrs by cAMP responsive element containing luciferase reporter gene assayTransactivation of human GP-BAR1 transfected in HEK293T cells assessed as induction of intracellular cAMP production after 18 hrs by cAMP responsive element containing luciferase reporter gene assay
ChEMBL 486 7 3 5 4.8 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)CCCOS(=O)(=O)O)[C@@H]2[C@@H]1O 10.1021/jm401873d
CHEMBL3260994 112869 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Transactivation of human GP-BAR1 transfected in HEK293T cells assessed as induction of intracellular cAMP production after 18 hrs by cAMP responsive element containing luciferase reporter gene assayTransactivation of human GP-BAR1 transfected in HEK293T cells assessed as induction of intracellular cAMP production after 18 hrs by cAMP responsive element containing luciferase reporter gene assay
ChEMBL 486 7 3 5 4.8 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)CCCOS(=O)(=O)O)[C@@H]2[C@@H]1O 10.1021/jm401873d
CHEMBL3306811 112869 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Transactivation of human GP-BAR1 transfected in HEK293T cells assessed as induction of intracellular cAMP production after 18 hrs by cAMP responsive element containing luciferase reporter gene assayTransactivation of human GP-BAR1 transfected in HEK293T cells assessed as induction of intracellular cAMP production after 18 hrs by cAMP responsive element containing luciferase reporter gene assay
ChEMBL 486 7 3 5 4.8 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)CCCOS(=O)(=O)O)[C@@H]2[C@@H]1O 10.1021/jm401873d
56601732 91639 None 0 Human Functional pEC50 = 5.7 5.7 1 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
ChEMBL 466 7 2 5 5.5 Cc1ccccc1[C@H](C/C(=N\O)c1ccc(=O)n(C)c1)c1ccc(-c2ccc(C(=O)O)cc2)cc1 10.1016/j.bmcl.2013.06.017
CHEMBL2407932 91639 None 0 Human Functional pEC50 = 5.7 5.7 1 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
ChEMBL 466 7 2 5 5.5 Cc1ccccc1[C@H](C/C(=N\O)c1ccc(=O)n(C)c1)c1ccc(-c2ccc(C(=O)O)cc2)cc1 10.1016/j.bmcl.2013.06.017
172462321 196737 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 498 6 4 4 4.9 C[C@H](C[C@H](Cc1ccccc1)C(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@]12C 10.1016/j.ejmech.2023.115851
CHEMBL5431182 196737 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 498 6 4 4 4.9 C[C@H](C[C@H](Cc1ccccc1)C(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@]12C 10.1016/j.ejmech.2023.115851
118694325 197155 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 373 4 1 3 4.1 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2F)CC(=O)N1 10.1021/acs.jmedchem.2c01881
CHEMBL5439948 197155 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 373 4 1 3 4.1 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2F)CC(=O)N1 10.1021/acs.jmedchem.2c01881
168276623 190520 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 295 4 2 4 3.2 O=C(O)c1cc(O)cc(OCc2ccc3ccccc3n2)c1 10.1021/acs.jmedchem.1c01078
CHEMBL5177797 190520 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 295 4 2 4 3.2 O=C(O)c1cc(O)cc(OCc2ccc3ccccc3n2)c1 10.1021/acs.jmedchem.1c01078
13799246 196702 None 4 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 422 4 4 4 3.8 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](C[C@H](O)[C@]12C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@@]3(C)O 10.1016/j.ejmech.2023.115851
CHEMBL5430282 196702 None 4 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 422 4 4 4 3.8 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](C[C@H](O)[C@]12C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@@]3(C)O 10.1016/j.ejmech.2023.115851
118735267 118897 None 0 Human Functional pEC50 = 4.7 4.7 -1 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 1310 35 2 16 10.8 O=C(CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NCCOCCOCCOCCOCCOCCOCCNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421903 118897 None 0 Human Functional pEC50 = 4.7 4.7 -1 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 1310 35 2 16 10.8 O=C(CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NCCOCCOCCOCCOCCOCCOCCNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
447715 199383 None 50 Human Functional pEC50 = 4.7 4.7 6 7
Agonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assayAgonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assay
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 10.1016/j.bmc.2011.03.004
CHEMBL566315 199383 None 50 Human Functional pEC50 = 4.7 4.7 6 7
Agonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assayAgonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assay
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 10.1016/j.bmc.2011.03.004
73350992 92762 None 0 Human Functional pEC50 = 6.7 6.7 10 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 442 5 1 2 6.8 CC(NCc1cnccc1-c1ccccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435921 92762 None 0 Human Functional pEC50 = 6.7 6.7 10 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 442 5 1 2 6.8 CC(NCc1cnccc1-c1ccccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
73350992 92762 None 0 Mouse Functional pEC50 = 5.7 5.7 -10 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 442 5 1 2 6.8 CC(NCc1cnccc1-c1ccccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435921 92762 None 0 Mouse Functional pEC50 = 5.7 5.7 -10 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 442 5 1 2 6.8 CC(NCc1cnccc1-c1ccccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
118464724 159559 None 0 Human Functional pEC50 = 4.7 4.7 -61 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 528 7 0 6 6.8 COc1ccc(C2OCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4101442 159559 None 0 Human Functional pEC50 = 4.7 4.7 -61 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 528 7 0 6 6.8 COc1ccc(C2OCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
137651232 157460 None 0 Mouse Functional pEC50 = 5.7 5.7 20 2
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 570 10 1 9 6.1 COc1ccc(SCc2cnc(SCc3c(F)cc(-c4nn[nH]n4)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4077972 157460 None 0 Mouse Functional pEC50 = 5.7 5.7 20 2
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 570 10 1 9 6.1 COc1ccc(SCc2cnc(SCc3c(F)cc(-c4nn[nH]n4)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
137629931 161110 None 0 Human Functional pEC50 = 4.7 4.7 -1 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 739 18 1 9 6.4 COc1ccc(SCc2cnc(SCc3c(F)cc(S(=O)(=O)N(CCCO)CCC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4064764 161110 None 0 Human Functional pEC50 = 4.7 4.7 -1 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 739 18 1 9 6.4 COc1ccc(SCc2cnc(SCc3c(F)cc(S(=O)(=O)N(CCCO)CCC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4116312 161110 None 0 Human Functional pEC50 = 4.7 4.7 -1 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 739 18 1 9 6.4 COc1ccc(SCc2cnc(SCc3c(F)cc(S(=O)(=O)N(CCCO)CCC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
44627311 199738 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 496 4 2 2 8.0 C=CC[C@@]1(O)CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(=C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/jm900872z
CHEMBL568584 199738 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 496 4 2 2 8.0 C=CC[C@@]1(O)CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(=C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/jm900872z
156705098 183500 None 2 Mouse Functional pEC50 = 6.7 6.7 -12 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 513 8 0 8 5.4 CCOCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4798091 183500 None 2 Mouse Functional pEC50 = 6.7 6.7 -12 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 513 8 0 8 5.4 CCOCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
66740913 158747 None 0 Mouse Functional pEC50 = 7.7 7.7 22 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 471 8 0 6 5.6 COc1ccc(Cc2nnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4092629 158747 None 0 Mouse Functional pEC50 = 7.7 7.7 22 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 471 8 0 6 5.6 COc1ccc(Cc2nnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
89501422 161725 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assay
ChEMBL 531 11 0 7 6.5 COc1ccc(C(C)(C)c2cnc(SCCOCc3cccc(C#N)c3)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2018.04.011
CHEMBL4130025 161725 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assay
ChEMBL 531 11 0 7 6.5 COc1ccc(C(C)(C)c2cnc(SCCOCc3cccc(C#N)c3)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2018.04.011
118464747 158426 None 0 Mouse Functional pEC50 = 6.7 6.7 4 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 743 19 2 10 6.0 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cc(C(=O)NCCOCCOCCOCCO)cc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4089352 158426 None 0 Mouse Functional pEC50 = 6.7 6.7 4 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 743 19 2 10 6.0 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cc(C(=O)NCCOCCOCCOCCO)cc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
73357025 92771 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 568 7 0 3 7.3 O=S(=O)(c1cc(C(F)(F)F)cc(C(F)(F)F)c1)N(Cc1ccccc1)Cc1cnccc1-c1ccccc1F 10.1016/j.ejmech.2013.07.050
CHEMBL2435931 92771 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 568 7 0 3 7.3 O=S(=O)(c1cc(C(F)(F)F)cc(C(F)(F)F)c1)N(Cc1ccccc1)Cc1cnccc1-c1ccccc1F 10.1016/j.ejmech.2013.07.050
90654577 110001 None 0 Human Functional pEC50 = 5.7 5.7 -17 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 358 5 1 4 3.0 Cc1nccc(N2CCC[C@@H](C(=O)NCCc3ccc(Cl)cc3)C2)n1 10.1021/jm401731q
CHEMBL3234558 110001 None 0 Human Functional pEC50 = 5.7 5.7 -17 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 358 5 1 4 3.0 Cc1nccc(N2CCC[C@@H](C(=O)NCCc3ccc(Cl)cc3)C2)n1 10.1021/jm401731q
156705085 183093 None 0 Mouse Functional pEC50 = 6.7 6.7 -2 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 543 10 0 9 5.0 COCCOCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4793377 183093 None 0 Mouse Functional pEC50 = 6.7 6.7 -2 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 543 10 0 9 5.0 COCCOCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
164628559 186652 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 543 4 1 3 8.3 CCN(C)C(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
CHEMBL4877942 186652 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 543 4 1 3 8.3 CCN(C)C(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
71718878 87684 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 373 5 0 6 3.3 COc1cccc(-n2nnc(C3CC3)c2C(=O)N(C)c2ccc(C#N)cc2)c1 10.1016/j.bmcl.2012.12.076
CHEMBL2336238 87684 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 373 5 0 6 3.3 COc1cccc(-n2nnc(C3CC3)c2C(=O)N(C)c2ccc(C#N)cc2)c1 10.1016/j.bmcl.2012.12.076
71718878 87684 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human recombinant TGR5 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 373 5 0 6 3.3 COc1cccc(-n2nnc(C3CC3)c2C(=O)N(C)c2ccc(C#N)cc2)c1 10.1039/C2MD20174G
CHEMBL2336238 87684 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human recombinant TGR5 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 373 5 0 6 3.3 COc1cccc(-n2nnc(C3CC3)c2C(=O)N(C)c2ccc(C#N)cc2)c1 10.1039/C2MD20174G
118464713 159391 None 0 Mouse Functional pEC50 = 6.7 6.7 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 516 6 0 5 6.9 COc1cc(C2OCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)ccc1F 10.1021/acsmedchemlett.7b00116
CHEMBL4099616 159391 None 0 Mouse Functional pEC50 = 6.7 6.7 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 516 6 0 5 6.9 COc1cc(C2OCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)ccc1F 10.1021/acsmedchemlett.7b00116
71541722 87322 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 381 7 2 5 2.1 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(CC)cc1)CC2 10.1021/ml300277t
CHEMBL2331645 87322 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 381 7 2 5 2.1 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(CC)cc1)CC2 10.1021/ml300277t
77845060 112281 None 0 Mouse Functional pEC50 = 6.7 6.7 7 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 489 5 1 6 5.6 O=C(O)c1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL3290724 112281 None 0 Mouse Functional pEC50 = 6.7 6.7 7 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 489 5 1 6 5.6 O=C(O)c1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
44337790 7089 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 458 2 2 2 7.2 CC(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)C(CCC4[C@@]5(C)CC[C@H](O)C(C)(C)C5CC[C@]43C)C12 10.1021/jm900872z
CHEMBL108505 7089 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 458 2 2 2 7.2 CC(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)C(CCC4[C@@]5(C)CC[C@H](O)C(C)(C)C5CC[C@]43C)C12 10.1021/jm900872z
90654572 109996 None 0 Mouse Functional pEC50 = 5.7 5.7 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 324 5 1 4 2.4 Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3ncccn3)C2)cc1 10.1021/jm401731q
CHEMBL3234553 109996 None 0 Mouse Functional pEC50 = 5.7 5.7 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 324 5 1 4 2.4 Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3ncccn3)C2)cc1 10.1021/jm401731q
137634963 155971 None 0 Human Functional pEC50 = 4.7 4.7 -21 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 529 10 0 6 6.3 COc1ccc(N(C=O)Cc2cnc(SCc3c(F)cccc3Cl)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4060463 155971 None 0 Human Functional pEC50 = 4.7 4.7 -21 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 529 10 0 6 6.3 COc1ccc(N(C=O)Cc2cnc(SCc3c(F)cccc3Cl)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
5284061 16983 None 15 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 378 4 3 3 4.4 C[C@H](CCCO)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
CHEMBL1253814 16983 None 15 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 378 4 3 3 4.4 C[C@H](CCCO)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
172471283 197163 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 490 6 2 5 5.5 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)OC4CCCC4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
CHEMBL5440151 197163 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 490 6 2 5 5.5 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)OC4CCCC4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
66737876 117738 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 390 4 2 2 5.8 C[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C)C(=O)O 10.1016/j.bmc.2015.01.048
CHEMBL3401351 117738 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 390 4 2 2 5.8 C[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C)C(=O)O 10.1016/j.bmc.2015.01.048
90654578 110002 None 0 Human Functional pEC50 = 6.7 6.7 3 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 357 5 1 3 3.6 Cc1cccc(N2CCC[C@@H](C(=O)NCCc3ccc(Cl)cc3)C2)n1 10.1021/jm401731q
CHEMBL3234559 110002 None 0 Human Functional pEC50 = 6.7 6.7 3 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 357 5 1 3 3.6 Cc1cccc(N2CCC[C@@H](C(=O)NCCc3ccc(Cl)cc3)C2)n1 10.1021/jm401731q
118694469 194962 None 0 Human Functional pEC50 = 6.7 6.7 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
CHEMBL5394197 194962 None 0 Human Functional pEC50 = 6.7 6.7 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
155534242 172026 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 430 4 2 5 4.9 Cc1nnc(CC[C@@H](C)[C@H]2CC[C@H]3[C@H]4[C@H](CC[C@@]32C)[C@@]2(C)CC[C@@H](O)C[C@H]2C[C@H]4O)o1 10.1021/acs.jmedchem.9b00770
CHEMBL4470072 172026 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 430 4 2 5 4.9 Cc1nnc(CC[C@@H](C)[C@H]2CC[C@H]3[C@H]4[C@H](CC[C@@]32C)[C@@]2(C)CC[C@@H](O)C[C@H]2C[C@H]4O)o1 10.1021/acs.jmedchem.9b00770
10494 2916 None 51 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 456 1 2 2 7.2 O[C@H]1CC[C@]2([C@H](C1(C)C)CC[C@@]1([C@@H]2CC=C2[C@@]1(C)CC[C@@]1([C@H]2CC(C)(C)CC1)C(=O)O)C)C 10.1021/jm900872z
3306 2916 None 51 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 456 1 2 2 7.2 O[C@H]1CC[C@]2([C@H](C1(C)C)CC[C@@]1([C@@H]2CC=C2[C@@]1(C)CC[C@@]1([C@H]2CC(C)(C)CC1)C(=O)O)C)C 10.1021/jm900872z
CHEMBL168 2916 None 51 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 456 1 2 2 7.2 O[C@H]1CC[C@]2([C@H](C1(C)C)CC[C@@]1([C@@H]2CC=C2[C@@]1(C)CC[C@@]1([C@H]2CC(C)(C)CC1)C(=O)O)C)C 10.1021/jm900872z
156019954 178100 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 385 3 2 3 5.1 C=C[C@]1(O)C[C@H]2[C@@H]3CC[C@H]([C@H](C)CC#N)[C@@]3(C)CC[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1021/acsmedchemlett.9b00636
CHEMBL4646264 178100 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 385 3 2 3 5.1 C=C[C@]1(O)C[C@H]2[C@@H]3CC[C@H]([C@H](C)CC#N)[C@@]3(C)CC[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1021/acsmedchemlett.9b00636
164613461 185096 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 607 5 2 4 9.4 COc1ccc(NC(=O)O[C@@H]2CC[C@@]3(C)[C@@H](CC[C@]4(C)[C@@H]3CC[C@@H]3[C@H]5[C@H](C(C)C)CC[C@]5(C(=O)O)CC[C@]34C)C2(C)C)cc1 10.1021/acs.jmedchem.1c00851
CHEMBL4854339 185096 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 607 5 2 4 9.4 COc1ccc(NC(=O)O[C@@H]2CC[C@@]3(C)[C@@H](CC[C@]4(C)[C@@H]3CC[C@@H]3[C@H]5[C@H](C(C)C)CC[C@]5(C(=O)O)CC[C@]34C)C2(C)C)cc1 10.1021/acs.jmedchem.1c00851
44457460 96168 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 394 4 2 2 5.5 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@@H](F)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
CHEMBL260314 96168 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 394 4 2 2 5.5 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@@H](F)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
44605617 200775 None 1 Human Functional pEC50 = 7.6 7.6 5 2
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 374 3 0 3 5.5 Cc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1Cl 10.1016/j.bmcl.2012.12.076
CHEMBL576138 200775 None 1 Human Functional pEC50 = 7.6 7.6 5 2
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 374 3 0 3 5.5 Cc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1Cl 10.1016/j.bmcl.2012.12.076
71452076 83029 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 454 4 0 5 5.6 O=C(c1cncnc1Oc1cc(Cl)ccc1Cl)N1CCN(C2CCC2)c2ccccc21 10.1021/jm301071h
CHEMBL2181231 83029 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 454 4 0 5 5.6 O=C(c1cncnc1Oc1cc(Cl)ccc1Cl)N1CCN(C2CCC2)c2ccccc21 10.1021/jm301071h
90654582 110006 None 0 Mouse Functional pEC50 = 7.6 7.6 6 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 403 5 1 5 2.9 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3ccnc(C(F)(F)F)n3)C2)cc1 10.1021/jm401731q
CHEMBL3234563 110006 None 0 Mouse Functional pEC50 = 7.6 7.6 6 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 403 5 1 5 2.9 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3ccnc(C(F)(F)F)n3)C2)cc1 10.1021/jm401731q
156705093 181996 None 0 Mouse Functional pEC50 = 7.6 7.6 -25 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter 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 Mouse Functional pEC50 = 7.6 7.6 -25 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter 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
162665892 182431 None 0 Human Functional pEC50 = 7.6 7.6 16 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 537 6 0 7 6.0 O=C(OCC(F)(F)F)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4784355 182431 None 0 Human Functional pEC50 = 7.6 7.6 16 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 537 6 0 7 6.0 O=C(OCC(F)(F)F)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
73350995 92782 None 0 Mouse Functional pEC50 = 6.6 6.6 -1 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 520 6 0 3 7.7 O=C(c1ccsc1)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
CHEMBL2435943 92782 None 0 Mouse Functional pEC50 = 6.6 6.6 -1 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 520 6 0 3 7.7 O=C(c1ccsc1)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
137630517 161164 None 0 Mouse Functional pEC50 = 5.6 5.6 - 1
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 631 13 1 7 6.3 COc1ccc(SCc2cnc(SCc3c(F)cc(C(=O)NCC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4083747 161164 None 0 Mouse Functional pEC50 = 5.6 5.6 - 1
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 631 13 1 7 6.3 COc1ccc(SCc2cnc(SCc3c(F)cc(C(=O)NCC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4116717 161164 None 0 Mouse Functional pEC50 = 5.6 5.6 - 1
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 631 13 1 7 6.3 COc1ccc(SCc2cnc(SCc3c(F)cc(C(=O)NCC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4581956 216495 None 7 Mouse Functional pEC50 = 5.6 5.6 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL None None None CC1=C(C(=O)OCc2ccccc2)C(c2ccccc2OC(C)C)CC(=O)N1 10.1021/acs.jmedchem.2c01881
387316 66790 None 37 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at wild type human TGR5 expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assayAgonist activity at wild type human TGR5 expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assay
ChEMBL 499 7 4 5 3.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1016/j.ejmech.2015.09.024
CHEMBL185878 66790 None 37 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at wild type human TGR5 expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assayAgonist activity at wild type human TGR5 expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assay
ChEMBL 499 7 4 5 3.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1016/j.ejmech.2015.09.024
168281036 191065 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 281 4 2 4 3.0 OCc1cc(O)cc(OCc2ccc3ccccc3n2)c1 10.1021/acs.jmedchem.1c01078
CHEMBL5185938 191065 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 281 4 2 4 3.0 OCc1cc(O)cc(OCc2ccc3ccccc3n2)c1 10.1021/acs.jmedchem.1c01078
172452366 195984 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 488 6 1 5 5.7 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC(=O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)OC4CCCC4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
CHEMBL5414606 195984 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 488 6 1 5 5.7 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC(=O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)OC4CCCC4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
71561366 87660 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 444 4 0 5 5.6 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336211 87660 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 444 4 0 5 5.6 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
44457491 96448 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 481 7 2 3 5.7 C[C@H]1C[C@@H]2CCCC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)NCCS(=O)(=O)O)[C@H]12 10.1021/jm7015864
CHEMBL261826 96448 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 481 7 2 3 5.7 C[C@H]1C[C@@H]2CCCC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)NCCS(=O)(=O)O)[C@H]12 10.1021/jm7015864
118576918 161225 None 0 Human Functional pEC50 = 6.6 6.6 -24 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 654 13 0 8 6.3 COc1ccc(N(C)c2cnc(SCc3c(F)cc(OCCC[N+]45CCN(CC4)CC5)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4078612 161225 None 0 Human Functional pEC50 = 6.6 6.6 -24 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 654 13 0 8 6.3 COc1ccc(N(C)c2cnc(SCc3c(F)cc(OCCC[N+]45CCN(CC4)CC5)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4117224 161225 None 0 Human Functional pEC50 = 6.6 6.6 -24 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 654 13 0 8 6.3 COc1ccc(N(C)c2cnc(SCc3c(F)cc(OCCC[N+]45CCN(CC4)CC5)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
31401 48123 None 48 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 392 4 3 3 4.5 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/j.bmc.2015.01.048
CHEMBL1551 48123 None 48 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 392 4 3 3 4.5 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/j.bmc.2015.01.048
90644446 112279 None 0 Human Functional pEC50 = 7.6 7.6 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 559 7 0 8 5.4 COC(=O)CCc1coc2cc(Cl)c(C(=O)Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
CHEMBL3290722 112279 None 0 Human Functional pEC50 = 7.6 7.6 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 559 7 0 8 5.4 COC(=O)CCc1coc2cc(Cl)c(C(=O)Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
44605617 200775 None 1 Human Functional pEC50 = 7.6 7.6 5 2
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 374 3 0 3 5.5 Cc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1Cl 10.1021/ml300277t
CHEMBL576138 200775 None 1 Human Functional pEC50 = 7.6 7.6 5 2
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 374 3 0 3 5.5 Cc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1Cl 10.1021/ml300277t
118577239 161077 None 0 Human Functional pEC50 = 7.6 7.6 -60 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human 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 Human Functional pEC50 = 7.6 7.6 -60 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human 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 Human Functional pEC50 = 7.6 7.6 -60 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human 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
71459275 83033 None 0 Mouse Functional pEC50 = 7.6 7.6 -7 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 427 4 0 4 5.7 CCN1CCN(C(=O)c2cnccc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
CHEMBL2181235 83033 None 0 Mouse Functional pEC50 = 7.6 7.6 -7 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 427 4 0 4 5.7 CCN1CCN(C(=O)c2cnccc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
145956445 162179 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay
ChEMBL 505 6 3 5 5.2 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)CCNC(=O)O[C@H]3CCOC3)[C@@H]2[C@@H]1O 10.1021/acsmedchemlett.7b00318
CHEMBL4160849 162179 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay
ChEMBL 505 6 3 5 5.2 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)CCNC(=O)O[C@H]3CCOC3)[C@@H]2[C@@H]1O 10.1021/acsmedchemlett.7b00318
145177795 162419 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay
ChEMBL 463 5 4 4 3.8 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)CCNC(=O)C(=O)O)[C@@H]2[C@@H]1O 10.1021/acsmedchemlett.7b00318
CHEMBL4164682 162419 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay
ChEMBL 463 5 4 4 3.8 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)CCNC(=O)C(=O)O)[C@@H]2[C@@H]1O 10.1021/acsmedchemlett.7b00318
71626422 112271 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 426 4 0 6 5.0 Cc1noc2cc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)ccc12 10.1016/j.ejmech.2014.05.031
CHEMBL3290714 112271 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 426 4 0 6 5.0 Cc1noc2cc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)ccc12 10.1016/j.ejmech.2014.05.031
119046 97590 None 33 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 499 7 4 5 3.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3C[C@H](O)[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
CHEMBL270516 97590 None 33 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 499 7 4 5 3.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3C[C@H](O)[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
45483949 3582 None 33 Human Functional pEC50 = 5.6 5.6 -2 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2022.114697
7048 3582 None 33 Human Functional pEC50 = 5.6 5.6 -2 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2022.114697
CHEMBL567640 3582 None 33 Human Functional pEC50 = 5.6 5.6 -2 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2022.114697
71541723 87324 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 383 7 2 6 1.5 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC)cc1)CC2 10.1021/ml300277t
CHEMBL2331647 87324 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 383 7 2 6 1.5 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC)cc1)CC2 10.1021/ml300277t
134494 159839 None 15 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 292 0 2 2 3.8 C[C@]12CC[C@H]3[C@@H](CC[C@@H]4C[C@H](O)CC[C@]34C)[C@@H]1CC[C@@H]2O 10.1021/jm7015864
CHEMBL410494 159839 None 15 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 292 0 2 2 3.8 C[C@]12CC[C@H]3[C@@H](CC[C@@H]4C[C@H](O)CC[C@]34C)[C@@H]1CC[C@@H]2O 10.1021/jm7015864
5284305 114308 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at human GPBAR1 expressed in HEK293T cells assessed as stimulation of cAMP response element-mediated receptor transactivation by luciferase reporter gene assayAgonist activity at human GPBAR1 expressed in HEK293T cells assessed as stimulation of cAMP response element-mediated receptor transactivation by luciferase reporter gene assay
ChEMBL 364 3 3 3 4.0 C[C@H](CCO)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm500889f
CHEMBL3329940 114308 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at human GPBAR1 expressed in HEK293T cells assessed as stimulation of cAMP response element-mediated receptor transactivation by luciferase reporter gene assayAgonist activity at human GPBAR1 expressed in HEK293T cells assessed as stimulation of cAMP response element-mediated receptor transactivation by luciferase reporter gene assay
ChEMBL 364 3 3 3 4.0 C[C@H](CCO)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm500889f
137636348 155955 None 0 Mouse Functional pEC50 = 7.6 7.6 12 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 524 7 0 5 7.2 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cccc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4060315 155955 None 0 Mouse Functional pEC50 = 7.6 7.6 12 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 524 7 0 5 7.2 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cccc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
71626556 112264 None 0 Human Functional pEC50 = 7.6 7.6 1 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 411 4 0 5 5.2 O=C(c1cnccc1Oc1ccc2ccoc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
CHEMBL3290707 112264 None 0 Human Functional pEC50 = 7.6 7.6 1 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 411 4 0 5 5.2 O=C(c1cnccc1Oc1ccc2ccoc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
90644458 112289 None 0 Human Functional pEC50 = 7.6 7.6 -1 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 529 6 1 6 6.3 Cc1c(/C=C/C(=O)O)oc2ccc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c12 10.1016/j.ejmech.2014.05.031
CHEMBL3290732 112289 None 0 Human Functional pEC50 = 7.6 7.6 -1 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 529 6 1 6 6.3 Cc1c(/C=C/C(=O)O)oc2ccc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c12 10.1016/j.ejmech.2014.05.031
90654599 110063 None 0 Human Functional pEC50 = 7.6 7.6 -12 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 571 8 2 6 5.3 N#Cc1ccc(CCNC(=O)[C@@H]2CCN2c2cc(-c3ccc(-c4ccc(C(=O)O)cc4)cc3)nc(C(F)(F)F)n2)cc1 10.1021/jm401731q
CHEMBL3234870 110063 None 0 Human Functional pEC50 = 7.6 7.6 -12 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 571 8 2 6 5.3 N#Cc1ccc(CCNC(=O)[C@@H]2CCN2c2cc(-c3ccc(-c4ccc(C(=O)O)cc4)cc3)nc(C(F)(F)F)n2)cc1 10.1021/jm401731q
118103698 163767 None 0 Human Functional pEC50 = 7.6 7.6 -12 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 724 15 5 10 2.5 CN(C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)C(=O)CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4204655 163767 None 0 Human Functional pEC50 = 7.6 7.6 -12 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 724 15 5 10 2.5 CN(C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)C(=O)CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
71660821 163823 None 0 Human Functional pEC50 = 7.6 7.6 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 447 4 0 4 4.9 O=C([C@@H]1CSCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4205214 163823 None 0 Human Functional pEC50 = 7.6 7.6 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 447 4 0 4 4.9 O=C([C@@H]1CSCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118093557 164754 None 0 Human Functional pEC50 = 7.6 7.6 -3 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 477 5 1 5 4.4 O=C([C@@H]1CSCN1Cc1cc(Cl)c(CO)cc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4216682 164754 None 0 Human Functional pEC50 = 7.6 7.6 -3 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 477 5 1 5 4.4 O=C([C@@H]1CSCN1Cc1cc(Cl)c(CO)cc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118694573 196130 None 0 Human Functional pEC50 = 7.6 7.6 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5417359 196130 None 0 Human Functional pEC50 = 7.6 7.6 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
71660821 163823 None 0 Mouse Functional pEC50 = 7.6 7.6 -1 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 447 4 0 4 4.9 O=C([C@@H]1CSCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4205214 163823 None 0 Mouse Functional pEC50 = 7.6 7.6 -1 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 447 4 0 4 4.9 O=C([C@@H]1CSCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
145972818 164737 None 0 Mouse Functional pEC50 = 7.6 7.6 3 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 734 13 6 12 1.3 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccn(Cc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)n1 10.1021/acs.jmedchem.8b00308
CHEMBL4216361 164737 None 0 Mouse Functional pEC50 = 7.6 7.6 3 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 734 13 6 12 1.3 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccn(Cc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)n1 10.1021/acs.jmedchem.8b00308
118694466 195057 None 0 Mouse Functional pEC50 = 7.6 7.6 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
CHEMBL5395730 195057 None 0 Mouse Functional pEC50 = 7.6 7.6 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
164617636 185456 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 530 5 1 4 7.4 COCC(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
CHEMBL4860100 185456 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 530 5 1 4 7.4 COCC(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
44457471 98096 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 394 4 2 2 5.5 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3F 10.1021/jm7015864
CHEMBL273087 98096 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 394 4 2 2 5.5 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3F 10.1021/jm7015864
5059 208819 None 32 Human Functional pEC50 = 5.6 5.6 -2 3
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 335 8 1 3 5.4 CCCCCC(O)c1cccc(OCc2ccc3ccccc3n2)c1 10.1021/acs.jmedchem.1c01078
CHEMBL8747 208819 None 32 Human Functional pEC50 = 5.6 5.6 -2 3
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 335 8 1 3 5.4 CCCCCC(O)c1cccc(OCc2ccc3ccccc3n2)c1 10.1021/acs.jmedchem.1c01078
10873253 77224 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
ChEMBL 408 4 4 4 3.4 C[C@H](CCC(=O)O)[C@H]1[C@@H](O)C[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/ml200256d
CHEMBL2062552 77224 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
ChEMBL 408 4 4 4 3.4 C[C@H](CCC(=O)O)[C@H]1[C@@H](O)C[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/ml200256d
CHEMBL2079119 77224 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
ChEMBL 408 4 4 4 3.4 C[C@H](CCC(=O)O)[C@H]1[C@@H](O)C[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/ml200256d
118735268 118898 None 0 Human Functional pEC50 = 4.6 4.6 -2 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 1398 41 2 18 10.9 O=C(CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421904 118898 None 0 Human Functional pEC50 = 4.6 4.6 -2 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 1398 41 2 18 10.9 O=C(CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
45483949 3582 None 33 Mouse Functional pEC50 = 6.6 6.6 2 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2020.112619
7048 3582 None 33 Mouse Functional pEC50 = 6.6 6.6 2 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2020.112619
CHEMBL567640 3582 None 33 Mouse Functional pEC50 = 6.6 6.6 2 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2020.112619
118104397 164268 None 0 Human Functional pEC50 = 6.6 6.6 -15 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 750 14 6 12 2.2 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(COc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)o1 10.1021/acs.jmedchem.8b00308
CHEMBL4210547 164268 None 0 Human Functional pEC50 = 6.6 6.6 -15 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 750 14 6 12 2.2 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(COc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)o1 10.1021/acs.jmedchem.8b00308
118093510 164281 None 0 Human Functional pEC50 = 6.6 6.6 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 475 4 0 4 5.7 CC1(C)SC[C@@H](C(=O)N2CCN(C3CC3)c3ccccc32)N1Cc1cc(Cl)ccc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4210686 164281 None 0 Human Functional pEC50 = 6.6 6.6 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 475 4 0 4 5.7 CC1(C)SC[C@@H](C(=O)N2CCN(C3CC3)c3ccccc32)N1Cc1cc(Cl)ccc1Cl 10.1021/acs.jmedchem.8b00308
71660823 164475 None 0 Human Functional pEC50 = 6.6 6.6 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 445 4 0 4 4.2 O=C([C@@H]1COCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4213036 164475 None 0 Human Functional pEC50 = 6.6 6.6 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 445 4 0 4 4.2 O=C([C@@H]1COCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118104381 164630 None 0 Human Functional pEC50 = 6.6 6.6 -7 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 760 14 6 11 2.6 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1cccc(OCc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)c1 10.1021/acs.jmedchem.8b00308
CHEMBL4215045 164630 None 0 Human Functional pEC50 = 6.6 6.6 -7 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 760 14 6 11 2.6 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1cccc(OCc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)c1 10.1021/acs.jmedchem.8b00308
118700251 194992 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 465 7 0 5 5.5 COc1ccccc1COC(=O)C1=C(C)N(Cc2ccco2)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5394522 194992 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 465 7 0 5 5.5 COc1ccccc1COC(=O)C1=C(C)N(Cc2ccco2)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
118694463 196483 None 0 Human Functional pEC50 = 6.6 6.6 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 471 8 0 6 4.1 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C(=O)OC)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5424851 196483 None 0 Human Functional pEC50 = 6.6 6.6 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 471 8 0 6 4.1 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C(=O)OC)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694465 196755 None 0 Human Functional pEC50 = 6.6 6.6 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2F)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5431493 196755 None 0 Human Functional pEC50 = 6.6 6.6 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2F)=C1C 10.1021/acs.jmedchem.2c01881
118700250 197183 None 0 Human Functional pEC50 = 6.6 6.6 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2C)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5440622 197183 None 0 Human Functional pEC50 = 6.6 6.6 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2C)=C1C 10.1021/acs.jmedchem.2c01881
46233055 203179 None 0 Human Functional pEC50 = 6.6 6.6 - 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 374 3 0 3 5.5 Cc1cc(Cl)ccc1N(C)C(=O)c1c(-c2ccccc2Cl)noc1C 10.1016/j.bmcl.2010.01.003
CHEMBL600021 203179 None 0 Human Functional pEC50 = 6.6 6.6 - 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 374 3 0 3 5.5 Cc1cc(Cl)ccc1N(C)C(=O)c1c(-c2ccccc2Cl)noc1C 10.1016/j.bmcl.2010.01.003
118093402 164315 None 0 Mouse Functional pEC50 = 6.6 6.6 -1 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 445 4 1 4 3.9 O=C([C@@H]1C[C@@H](O)CN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4211041 164315 None 0 Mouse Functional pEC50 = 6.6 6.6 -1 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 445 4 1 4 3.9 O=C([C@@H]1C[C@@H](O)CN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118694361 195650 None 0 Mouse Functional pEC50 = 6.6 6.6 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 409 6 0 3 5.1 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC1CC1 10.1021/acs.jmedchem.2c01881
CHEMBL5408025 195650 None 0 Mouse Functional pEC50 = 6.6 6.6 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 409 6 0 3 5.1 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC1CC1 10.1021/acs.jmedchem.2c01881
118694477 196545 None 0 Mouse Functional pEC50 = 6.6 6.6 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 463 7 0 4 5.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc3ccccc3c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5426387 196545 None 0 Mouse Functional pEC50 = 6.6 6.6 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 463 7 0 4 5.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc3ccccc3c2)=C1C 10.1021/acs.jmedchem.2c01881
118694371 197143 None 0 Mouse Functional pEC50 = 6.6 6.6 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 455 7 0 4 5.2 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2c(C)cc(C)cc2C)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5439826 197143 None 0 Mouse Functional pEC50 = 6.6 6.6 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 455 7 0 4 5.2 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2c(C)cc(C)cc2C)=C1C 10.1021/acs.jmedchem.2c01881
118464662 159232 None 0 Human Functional pEC50 = 4.6 4.6 -22 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 687 16 0 8 7.3 COc1cc(C2(C)CCCc3nc(SCc4c(F)cc(OCCOCCOCCN(C)C)cc4F)n(-c4ccc(F)cc4)c32)ccc1F 10.1021/acsmedchemlett.7b00116
CHEMBL4097990 159232 None 0 Human Functional pEC50 = 4.6 4.6 -22 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 687 16 0 8 7.3 COc1cc(C2(C)CCCc3nc(SCc4c(F)cc(OCCOCCOCCN(C)C)cc4F)n(-c4ccc(F)cc4)c32)ccc1F 10.1021/acsmedchemlett.7b00116
71661223 164528 None 0 Human Functional pEC50 = 5.6 5.6 -1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 429 4 0 3 5.0 O=C([C@H]1CCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4213705 164528 None 0 Human Functional pEC50 = 5.6 5.6 -1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 429 4 0 3 5.0 O=C([C@H]1CCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
46232983 203345 None 0 Human Functional pEC50 = 5.6 5.6 - 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 344 3 0 3 4.7 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccccc1F 10.1016/j.bmcl.2010.01.003
CHEMBL601448 203345 None 0 Human Functional pEC50 = 5.6 5.6 - 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 344 3 0 3 4.7 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccccc1F 10.1016/j.bmcl.2010.01.003
46233053 203582 None 0 Human Functional pEC50 = 5.6 5.6 - 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 COc1ccccc1N(C)C(=O)c1c(-c2ccccc2Cl)noc1C 10.1016/j.bmcl.2010.01.003
CHEMBL603107 203582 None 0 Human Functional pEC50 = 5.6 5.6 - 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 COc1ccccc1N(C)C(=O)c1c(-c2ccccc2Cl)noc1C 10.1016/j.bmcl.2010.01.003
46232359 203833 None 0 Human Functional pEC50 = 5.6 5.6 - 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 394 3 0 3 5.9 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2010.01.003
CHEMBL604520 203833 None 0 Human Functional pEC50 = 5.6 5.6 - 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 394 3 0 3 5.9 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2010.01.003
118093511 164120 None 0 Mouse Functional pEC50 = 5.6 5.6 3 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 388 3 0 2 4.9 O=C([C@@H]1CCCN1Cc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4208655 164120 None 0 Mouse Functional pEC50 = 5.6 5.6 3 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 388 3 0 2 4.9 O=C([C@@H]1CCCN1Cc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4581956 216495 None 7 Mouse Functional pEC50 = 5.6 5.6 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL None None None CC1=C(C(=O)OCc2ccccc2)C(c2ccccc2OC(C)C)CC(=O)N1 10.1021/acs.jmedchem.2c01881
118586278 159828 None 0 Human Functional pEC50 = 6.6 6.6 -50 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 467 8 0 6 6.2 COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccccc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4104779 159828 None 0 Human Functional pEC50 = 6.6 6.6 -50 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 467 8 0 6 6.2 COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccccc2)cc1OC 10.1021/acs.jmedchem.6b01873
137630592 161192 None 0 Mouse Functional pEC50 = 6.6 6.6 - 1
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 599 13 0 6 7.4 COc1ccc(N(C)c2c(CCCC[N+](C)(C)C)nc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4068186 161192 None 0 Mouse Functional pEC50 = 6.6 6.6 - 1
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 599 13 0 6 7.4 COc1ccc(N(C)c2c(CCCC[N+](C)(C)C)nc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4116953 161192 None 0 Mouse Functional pEC50 = 6.6 6.6 - 1
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 599 13 0 6 7.4 COc1ccc(N(C)c2c(CCCC[N+](C)(C)C)nc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
44427764 93330 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 406 4 3 3 4.7 C[C@H](C[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)CC1C[C@H]3O)C(=O)O 10.1021/jm070633p
CHEMBL245001 93330 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 406 4 3 3 4.7 C[C@H](C[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)CC1C[C@H]3O)C(=O)O 10.1021/jm070633p
71541720 87320 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 353 6 2 5 1.5 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccccc1)CC2 10.1021/ml300277t
CHEMBL2331643 87320 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 353 6 2 5 1.5 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccccc1)CC2 10.1021/ml300277t
156705111 183036 None 0 Human Functional pEC50 = 5.6 5.6 2 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 455 5 1 6 4.9 O=C(O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4792593 183036 None 0 Human Functional pEC50 = 5.6 5.6 2 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 455 5 1 6 4.9 O=C(O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
172468431 196929 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 504 7 2 5 5.8 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)OCC4CCCC4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
CHEMBL5435030 196929 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 504 7 2 5 5.8 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)OCC4CCCC4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
90654593 110024 None 0 Human Functional pEC50 = 7.6 7.6 -2 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 530 7 2 7 3.2 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3cc(N4CCC(C(=O)O)CC4)nc(C(F)(F)F)n3)C2)cc1 10.1021/jm401731q
CHEMBL3234580 110024 None 0 Human Functional pEC50 = 7.6 7.6 -2 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 530 7 2 7 3.2 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3cc(N4CCC(C(=O)O)CC4)nc(C(F)(F)F)n3)C2)cc1 10.1021/jm401731q
71455632 83020 None 0 Mouse Functional pEC50 = 7.6 7.6 -2 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 401 5 0 5 4.5 COc1cccc(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)c1 10.1021/jm301071h
CHEMBL2181223 83020 None 0 Mouse Functional pEC50 = 7.6 7.6 -2 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 401 5 0 5 4.5 COc1cccc(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)c1 10.1021/jm301071h
118694466 195057 None 0 Mouse Functional pEC50 = 7.6 7.6 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
CHEMBL5395730 195057 None 0 Mouse Functional pEC50 = 7.6 7.6 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
164620346 186320 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 555 4 2 3 8.5 CC(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CCC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
CHEMBL4873169 186320 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 555 4 2 3 8.5 CC(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CCC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
164626982 186412 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 543 5 2 3 8.3 CCCNC(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
CHEMBL4874555 186412 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 543 5 2 3 8.3 CCCNC(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
164627955 186506 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 516 4 2 4 6.7 CC(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)CO)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
CHEMBL4875868 186506 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 516 4 2 4 6.7 CC(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)CO)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
73350994 92781 None 0 Human Functional pEC50 = 6.6 6.6 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 520 6 0 3 7.7 O=C(c1cccs1)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
CHEMBL2435942 92781 None 0 Human Functional pEC50 = 6.6 6.6 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 520 6 0 3 7.7 O=C(c1cccs1)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
118700251 194992 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 465 7 0 5 5.5 COc1ccccc1COC(=O)C1=C(C)N(Cc2ccco2)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5394522 194992 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 465 7 0 5 5.5 COc1ccccc1COC(=O)C1=C(C)N(Cc2ccco2)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
118577298 161080 None 0 Human Functional pEC50 = 6.6 6.6 -18 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 581 9 0 6 6.4 COc1ccc(N(C)c2cnc(SCc3c(F)cc(C#CC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4086463 161080 None 0 Human Functional pEC50 = 6.6 6.6 -18 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 581 9 0 6 6.4 COc1ccc(N(C)c2cnc(SCc3c(F)cc(C#CC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4096633 161080 None 0 Human Functional pEC50 = 6.6 6.6 -18 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 581 9 0 6 6.4 COc1ccc(N(C)c2cnc(SCc3c(F)cc(C#CC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4116110 161080 None 0 Human Functional pEC50 = 6.6 6.6 -18 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 581 9 0 6 6.4 COc1ccc(N(C)c2cnc(SCc3c(F)cc(C#CC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
137656785 159780 None 0 Mouse Functional pEC50 = 4.6 4.6 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 510 5 0 5 7.3 Fc1ccc(-n2c(SCc3c(F)cccc3Cl)nc3c2C(c2ccc4c(c2)OCO4)CCC3)cc1 10.1021/acsmedchemlett.7b00116
CHEMBL4104148 159780 None 0 Mouse Functional pEC50 = 4.6 4.6 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 510 5 0 5 7.3 Fc1ccc(-n2c(SCc3c(F)cccc3Cl)nc3c2C(c2ccc4c(c2)OCO4)CCC3)cc1 10.1021/acsmedchemlett.7b00116
164623929 186347 None 0 Mouse Functional pEC50 = 5.6 5.6 -31 2
Agonist activity at N-terminal HA-tagged mouse TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged mouse TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 528 5 1 3 8.5 CCCC(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
CHEMBL4873587 186347 None 0 Mouse Functional pEC50 = 5.6 5.6 -31 2
Agonist activity at N-terminal HA-tagged mouse TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged mouse TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 528 5 1 3 8.5 CCCC(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
247732 96202 None 19 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 290 0 1 2 4.0 C[C@]12CC[C@H]3[C@@H](CC[C@@H]4C[C@@H](O)CC[C@]34C)[C@@H]1CCC2=O 10.1021/jm7015864
CHEMBL260526 96202 None 19 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 290 0 1 2 4.0 C[C@]12CC[C@H]3[C@@H](CC[C@@H]4C[C@@H](O)CC[C@]34C)[C@@H]1CCC2=O 10.1021/jm7015864
44457504 97589 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 388 5 1 1 7.2 CC[C@H]1C[C@@H]2CCCC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)O)[C@H]12 10.1021/jm7015864
CHEMBL270494 97589 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 388 5 1 1 7.2 CC[C@H]1C[C@@H]2CCCC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)O)[C@H]12 10.1021/jm7015864
1452577 109993 None 0 Mouse Functional pEC50 = 4.6 4.6 -4 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 324 5 1 4 2.4 Cc1ccnc(N2CCC[C@@H](C(=O)NCCc3ccccc3)C2)n1 10.1021/jm401731q
CHEMBL3234550 109993 None 0 Mouse Functional pEC50 = 4.6 4.6 -4 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 324 5 1 4 2.4 Cc1ccnc(N2CCC[C@@H](C(=O)NCCc3ccccc3)C2)n1 10.1021/jm401731q
137657436 159671 None 0 Mouse Functional pEC50 = 4.6 4.6 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 514 6 0 4 7.7 COc1cc(C2CCCc3nc(SCc4ccc(F)cc4F)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4102817 159671 None 0 Mouse Functional pEC50 = 4.6 4.6 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 514 6 0 4 7.7 COc1cc(C2CCCc3nc(SCc4ccc(F)cc4F)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
156017547 177892 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 359 2 2 3 4.5 C[C@H](CC#N)[C@H]1CC[C@H]2[C@@H]3C[C@H](O)[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/acsmedchemlett.9b00636
CHEMBL4643260 177892 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 359 2 2 3 4.5 C[C@H](CC#N)[C@H]1CC[C@H]2[C@@H]3C[C@H](O)[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/acsmedchemlett.9b00636
71459273 83018 None 0 Human Functional pEC50 = 7.6 7.6 1 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 405 4 0 4 5.2 O=C(c1cnccc1Oc1ccccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/jm301071h
CHEMBL2181221 83018 None 0 Human Functional pEC50 = 7.6 7.6 1 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 405 4 0 4 5.2 O=C(c1cnccc1Oc1ccccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/jm301071h
5283906 160220 None 35 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 374 4 1 2 5.7 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
CHEMBL410893 160220 None 35 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 374 4 1 2 5.7 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
168264807 197392 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human TGR5 expressed in HEK293 cells incubated for 30 mins by SEAP reporter gene based assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 30 mins by SEAP reporter gene based assay
ChEMBL 541 9 4 5 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@H](C)CCCC(=O)NCCS(=O)(=O)O)[C@H]3[C@H](C)C[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1016/j.ejmech.2023.115143
CHEMBL5403980 197392 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human TGR5 expressed in HEK293 cells incubated for 30 mins by SEAP reporter gene based assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 30 mins by SEAP reporter gene based assay
ChEMBL 541 9 4 5 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@H](C)CCCC(=O)NCCS(=O)(=O)O)[C@H]3[C@H](C)C[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1016/j.ejmech.2023.115143
CHEMBL5498864 197392 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human TGR5 expressed in HEK293 cells incubated for 30 mins by SEAP reporter gene based assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 30 mins by SEAP reporter gene based assay
ChEMBL 541 9 4 5 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@H](C)CCCC(=O)NCCS(=O)(=O)O)[C@H]3[C@H](C)C[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1016/j.ejmech.2023.115143
164626661 186700 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 614 6 3 5 7.5 CC(C)[C@@H]1CC[C@]2(NC(=O)OCC(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
CHEMBL4878597 186700 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 614 6 3 5 7.5 CC(C)[C@@H]1CC[C@]2(NC(=O)OCC(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
90654565 110020 None 0 Human Functional pEC50 = 6.6 6.6 -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 487 6 1 7 2.4 CN1CCN(c2cc(N3CCC[C@@H]3C(=O)NCCc3ccc(C#N)cc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
CHEMBL3234576 110020 None 0 Human Functional pEC50 = 6.6 6.6 -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 487 6 1 7 2.4 CN1CCN(c2cc(N3CCC[C@@H]3C(=O)NCCc3ccc(C#N)cc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
136166955 91646 None 0 Human Functional pEC50 = 5.6 5.6 3 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
ChEMBL 359 6 1 4 4.9 Cc1cccc(C(C/C(=N\O)c2ccncc2)c2ccc(N(C)C)cc2)c1 10.1016/j.bmcl.2013.06.017
CHEMBL2407945 91646 None 0 Human Functional pEC50 = 5.6 5.6 3 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
ChEMBL 359 6 1 4 4.9 Cc1cccc(C(C/C(=N\O)c2ccncc2)c2ccc(N(C)C)cc2)c1 10.1016/j.bmcl.2013.06.017
5994 4643 None 51 Human Functional pEC50 = 5.6 5.6 1 10
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 314 1 0 2 4.7 CC(=O)[C@H]1CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@H]3CC[C@]12C 10.1021/jm7015864
CHEMBL103 4643 None 51 Human Functional pEC50 = 5.6 5.6 1 10
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 314 1 0 2 4.7 CC(=O)[C@H]1CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@H]3CC[C@]12C 10.1021/jm7015864
155534680 172051 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 431 3 2 3 4.6 C[C@H](CC(=O)N1CCCC1)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/acs.jmedchem.9b00770
CHEMBL4470499 172051 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 431 3 2 3 4.6 C[C@H](CC(=O)N1CCCC1)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/acs.jmedchem.9b00770
118464823 158701 None 0 Mouse Functional pEC50 = 5.6 5.6 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 496 6 0 4 7.6 COc1cccc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)c1 10.1021/acsmedchemlett.7b00116
CHEMBL4092168 158701 None 0 Mouse Functional pEC50 = 5.6 5.6 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 496 6 0 4 7.6 COc1cccc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)c1 10.1021/acsmedchemlett.7b00116
156011298 177491 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 401 3 2 3 5.6 CC(C)[C@]1(O)C[C@H]2[C@@H]3CC[C@H]([C@H](C)CC#N)[C@@]3(C)CC[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1021/acsmedchemlett.9b00636
CHEMBL4638053 177491 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 401 3 2 3 5.6 CC(C)[C@]1(O)C[C@H]2[C@@H]3CC[C@H]([C@H](C)CC#N)[C@@]3(C)CC[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1021/acsmedchemlett.9b00636
71626492 112263 None 0 Mouse Functional pEC50 = 7.6 7.6 -2 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 411 4 0 5 5.2 O=C(c1cnccc1Oc1ccc2occc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
CHEMBL3290706 112263 None 0 Mouse Functional pEC50 = 7.6 7.6 -2 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 411 4 0 5 5.2 O=C(c1cnccc1Oc1ccc2occc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
145949879 162885 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay
ChEMBL 463 6 3 4 5.4 CCOC(=O)NCC[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1[C@@H](CC)[C@H]3O 10.1021/acsmedchemlett.7b00318
CHEMBL4172216 162885 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay
ChEMBL 463 6 3 4 5.4 CCOC(=O)NCC[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1[C@@H](CC)[C@H]3O 10.1021/acsmedchemlett.7b00318
1452520 109991 None 0 Mouse Functional pEC50 = 6.6 6.6 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 344 5 1 4 2.7 O=C(NCCc1ccc(Cl)cc1)[C@@H]1CCCN(c2ncccn2)C1 10.1021/jm401731q
CHEMBL3234547 109991 None 0 Mouse Functional pEC50 = 6.6 6.6 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 344 5 1 4 2.7 O=C(NCCc1ccc(Cl)cc1)[C@@H]1CCCN(c2ncccn2)C1 10.1021/jm401731q
17755103 201280 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 406 4 3 3 4.7 C[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O)C(=O)O 10.1016/j.bmc.2015.01.048
CHEMBL583611 201280 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 406 4 3 3 4.7 C[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O)C(=O)O 10.1016/j.bmc.2015.01.048
164622322 185943 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 569 4 2 3 8.8 CC(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CCCC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
CHEMBL4867540 185943 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 569 4 2 3 8.8 CC(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CCCC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
137660218 159324 None 0 Mouse Functional pEC50 = 6.5 6.5 16 2
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 527 9 0 7 6.8 COc1ccc(SCc2cnc(SCc3c(F)cc(C#N)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4098862 159324 None 0 Mouse Functional pEC50 = 6.5 6.5 16 2
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 527 9 0 7 6.8 COc1ccc(SCc2cnc(SCc3c(F)cc(C#N)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
92810 157402 None 38 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 316 1 0 2 4.8 CC(=O)[C@H]1CC[C@H]2[C@@H]3CC[C@H]4CC(=O)CC[C@]4(C)[C@H]3CC[C@]12C 10.1021/jm7015864
CHEMBL407717 157402 None 38 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 316 1 0 2 4.8 CC(=O)[C@H]1CC[C@H]2[C@@H]3CC[C@H]4CC(=O)CC[C@]4(C)[C@H]3CC[C@]12C 10.1021/jm7015864
439763 158218 None 15 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 483 7 3 4 4.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
CHEMBL408701 158218 None 15 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 483 7 3 4 4.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
136166859 91643 None 0 Human Functional pEC50 = 5.5 5.5 5 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
ChEMBL 345 6 1 4 4.5 CN(C)c1ccc(C(C/C(=N\O)c2ccncc2)c2ccccc2)cc1 10.1016/j.bmcl.2013.06.017
CHEMBL2407936 91643 None 0 Human Functional pEC50 = 5.5 5.5 5 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
ChEMBL 345 6 1 4 4.5 CN(C)c1ccc(C(C/C(=N\O)c2ccncc2)c2ccccc2)cc1 10.1016/j.bmcl.2013.06.017
71561499 87666 None 0 Human Functional pEC50 = 5.5 5.5 - 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 401 4 0 6 4.2 Cc1nn(C)c(Oc2ccccc2C#N)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336217 87666 None 0 Human Functional pEC50 = 5.5 5.5 - 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 401 4 0 6 4.2 Cc1nn(C)c(Oc2ccccc2C#N)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
11463847 97952 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 404 3 3 3 4.3 C[C@H]([C@@H]1C[C@H]1C(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
CHEMBL272426 97952 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 404 3 3 3 4.3 C[C@H]([C@@H]1C[C@H]1C(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
45483949 3582 None 33 Human Functional pEC50 = 6.5 6.5 -2 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.bmcl.2014.07.026
7048 3582 None 33 Human Functional pEC50 = 6.5 6.5 -2 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.bmcl.2014.07.026
CHEMBL567640 3582 None 33 Human Functional pEC50 = 6.5 6.5 -2 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.bmcl.2014.07.026
118464802 157616 None 0 Mouse Functional pEC50 = 5.5 5.5 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 524 5 0 5 7.3 Fc1ccc(-n2c(SCc3c(F)cccc3Cl)nc3c2C(c2ccc4c(c2)OCCO4)CCC3)cc1 10.1021/acsmedchemlett.7b00116
CHEMBL4079911 157616 None 0 Mouse Functional pEC50 = 5.5 5.5 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 524 5 0 5 7.3 Fc1ccc(-n2c(SCc3c(F)cccc3Cl)nc3c2C(c2ccc4c(c2)OCCO4)CCC3)cc1 10.1021/acsmedchemlett.7b00116
137630926 161229 None 0 Human Functional pEC50 = 4.5 4.5 -3 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 681 15 1 8 6.3 COc1ccc(SCc2cnc(SCc3c(F)cc(S(=O)(=O)NCCC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4086239 161229 None 0 Human Functional pEC50 = 4.5 4.5 -3 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 681 15 1 8 6.3 COc1ccc(SCc2cnc(SCc3c(F)cc(S(=O)(=O)NCCC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4117239 161229 None 0 Human Functional pEC50 = 4.5 4.5 -3 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 681 15 1 8 6.3 COc1ccc(SCc2cnc(SCc3c(F)cc(S(=O)(=O)NCCC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
387316 66790 None 37 Human Functional pEC50 = 4.5 4.5 - 1
Agonist activity at human TGR5 Y89A mutant expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assayAgonist activity at human TGR5 Y89A mutant expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assay
ChEMBL 499 7 4 5 3.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1016/j.ejmech.2015.09.024
CHEMBL185878 66790 None 37 Human Functional pEC50 = 4.5 4.5 - 1
Agonist activity at human TGR5 Y89A mutant expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assayAgonist activity at human TGR5 Y89A mutant expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assay
ChEMBL 499 7 4 5 3.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1016/j.ejmech.2015.09.024
118576916 157727 None 0 Human Functional pEC50 = 6.5 6.5 -7 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 477 8 0 6 6.7 COc1ccc(N(C)c2cnc(SCc3c(C)cccc3C)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4081298 157727 None 0 Human Functional pEC50 = 6.5 6.5 -7 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 477 8 0 6 6.7 COc1ccc(N(C)c2cnc(SCc3c(C)cccc3C)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
71540077 87329 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 418 7 2 6 2.0 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(C(C)(F)F)nc1)CC2 10.1021/ml300277t
CHEMBL2331652 87329 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 418 7 2 6 2.0 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(C(C)(F)F)nc1)CC2 10.1021/ml300277t
90654587 110011 None 0 Human Functional pEC50 = 8.5 8.5 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 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 Human Functional pEC50 = 8.5 8.5 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 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
90654584 110008 None 0 Mouse Functional pEC50 = 8.5 8.5 -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(C(F)(F)F)nc(N3CCC[C@@H](C(=O)NCCc4ccc(C#N)cc4)C3)n2)CC1 10.1021/jm401731q
CHEMBL3234565 110008 None 0 Mouse Functional pEC50 = 8.5 8.5 -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(C(F)(F)F)nc(N3CCC[C@@H](C(=O)NCCc4ccc(C#N)cc4)C3)n2)CC1 10.1021/jm401731q
90654590 110015 None 0 Mouse Functional pEC50 = 8.5 8.5 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 502 6 1 8 2.1 CN1CCN(c2cc(N3CCC[C@@H](C(=O)NCCc4ccc(C#N)nc4)C3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
CHEMBL3234571 110015 None 0 Mouse Functional pEC50 = 8.5 8.5 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 502 6 1 8 2.1 CN1CCN(c2cc(N3CCC[C@@H](C(=O)NCCc4ccc(C#N)nc4)C3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
118694559 1134 None 3 Mouse Functional pEC50 = 8.5 8.5 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COC1=C(C=CC=C1)COC(=O)C=2[C@@H](CC(N(C2C)C[C@@H]3OCCC3)=O)C=4C=NC(=CC4)Cl 10.1021/acs.jmedchem.2c01881
12906 1134 None 3 Mouse Functional pEC50 = 8.5 8.5 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COC1=C(C=CC=C1)COC(=O)C=2[C@@H](CC(N(C2C)C[C@@H]3OCCC3)=O)C=4C=NC(=CC4)Cl 10.1021/acs.jmedchem.2c01881
CHEMBL5434983 1134 None 3 Mouse Functional pEC50 = 8.5 8.5 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COC1=C(C=CC=C1)COC(=O)C=2[C@@H](CC(N(C2C)C[C@@H]3OCCC3)=O)C=4C=NC(=CC4)Cl 10.1021/acs.jmedchem.2c01881
71459275 83033 None 0 Human Functional pEC50 = 8.5 8.5 7 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 427 4 0 4 5.7 CCN1CCN(C(=O)c2cnccc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
CHEMBL2181235 83033 None 0 Human Functional pEC50 = 8.5 8.5 7 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 427 4 0 4 5.7 CCN1CCN(C(=O)c2cnccc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
118093582 164216 None 0 Mouse Functional pEC50 = 8.5 8.5 12 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 710 15 6 10 2.1 O=C(CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4209927 164216 None 0 Mouse Functional pEC50 = 8.5 8.5 12 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 710 15 6 10 2.1 O=C(CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
172439348 195035 None 0 Human Functional pEC50 = 8.5 8.5 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1293 40 3 17 6.6 CC1C(=O)N(CC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5395284 195035 None 0 Human Functional pEC50 = 8.5 8.5 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1293 40 3 17 6.6 CC1C(=O)N(CC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
53311869 83037 None 0 Mouse Functional pEC50 = 8.5 8.5 -3 2
Agonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assayAgonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay
ChEMBL 439 4 0 4 5.8 O=C(c1cnccc1Oc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
CHEMBL2181239 83037 None 0 Mouse Functional pEC50 = 8.5 8.5 -3 2
Agonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assayAgonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay
ChEMBL 439 4 0 4 5.8 O=C(c1cnccc1Oc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
71540174 87331 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 438 7 1 6 2.4 CCOc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1021/ml300277t
CHEMBL2331654 87331 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 438 7 1 6 2.4 CCOc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1021/ml300277t
172444413 195210 None 0 Mouse Functional pEC50 = 8.5 8.5 14 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1409 44 3 19 6.2 CC1C(=O)N(CC(=O)N(CCOCCOCCOCCOCCOCCOCCOCCOCCN(CC(=O)O)C(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CC(=O)O)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5398966 195210 None 0 Mouse Functional pEC50 = 8.5 8.5 14 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1409 44 3 19 6.2 CC1C(=O)N(CC(=O)N(CCOCCOCCOCCOCCOCCOCCOCCOCCN(CC(=O)O)C(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CC(=O)O)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
53311701 113626 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 414 3 0 5 4.7 CN1CCN(C(=O)c2cncnc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1016/j.bmcl.2014.07.026
CHEMBL3321845 113626 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 414 3 0 5 4.7 CN1CCN(C(=O)c2cncnc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1016/j.bmcl.2014.07.026
172442531 194984 None 0 Human Functional pEC50 = 8.4 8.4 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1325 39 3 16 7.8 N[C@@H](CC(=O)N1CCCN(CC(=O)NCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)C(=O)C1Cc1ccccc1)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5394421 194984 None 0 Human Functional pEC50 = 8.4 8.4 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1325 39 3 16 7.8 N[C@@H](CC(=O)N1CCCN(CC(=O)NCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)C(=O)C1Cc1ccccc1)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
172454739 196023 None 0 Human Functional pEC50 = 8.4 8.4 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1281 36 3 15 7.8 N[C@@H](CC(=O)N1CCCN(CC(=O)NCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)C(=O)C1Cc1ccccc1)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5415272 196023 None 0 Human Functional pEC50 = 8.4 8.4 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1281 36 3 15 7.8 N[C@@H](CC(=O)N1CCCN(CC(=O)NCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)C(=O)C1Cc1ccccc1)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
172454703 195937 None 0 Mouse Functional pEC50 = 8.4 8.4 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1149 27 3 12 7.7 N[C@@H](CC(=O)N1CCCN(CC(=O)NCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)C(=O)C1Cc1ccccc1)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5413666 195937 None 0 Mouse Functional pEC50 = 8.4 8.4 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1149 27 3 12 7.7 N[C@@H](CC(=O)N1CCCN(CC(=O)NCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)C(=O)C1Cc1ccccc1)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
172455948 196396 None 0 Human Functional pEC50 = 8.4 8.4 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1386 42 3 17 8.5 C.N[C@@H](CC(=O)N1CCCN(CC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)C(=O)C1Cc1ccccc1)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5422904 196396 None 0 Human Functional pEC50 = 8.4 8.4 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1386 42 3 17 8.5 C.N[C@@H](CC(=O)N1CCCN(CC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)C(=O)C1Cc1ccccc1)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
91758806 113627 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 430 3 1 6 4.4 CN1CCN(C(=O)c2cnc(O)nc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1016/j.bmcl.2014.07.026
CHEMBL3321846 113627 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 430 3 1 6 4.4 CN1CCN(C(=O)c2cnc(O)nc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1016/j.bmcl.2014.07.026
46232695 203371 None 0 Human Functional pEC50 = 8.4 8.4 - 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 386 4 0 3 5.8 CN(C(=O)c1c(-c2ccccc2Cl)noc1C1CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL601638 203371 None 0 Human Functional pEC50 = 8.4 8.4 - 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 386 4 0 3 5.8 CN(C(=O)c1c(-c2ccccc2Cl)noc1C1CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
46232659 203583 None 0 Human Functional pEC50 = 8.4 8.4 - 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 374 4 0 3 5.5 CCc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL603112 203583 None 0 Human Functional pEC50 = 8.4 8.4 - 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 374 4 0 3 5.5 CCc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
118103702 163795 None 0 Mouse Functional pEC50 = 8.4 8.4 - 1
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 724 15 6 10 2.2 O=C(CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)N[C@@H](C(=O)O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4204919 163795 None 0 Mouse Functional pEC50 = 8.4 8.4 - 1
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 724 15 6 10 2.2 O=C(CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)N[C@@H](C(=O)O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
145975890 163898 None 0 Mouse Functional pEC50 = 8.4 8.4 19 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 739 16 7 10 2.3 O=C(NCCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4206078 163898 None 0 Mouse Functional pEC50 = 8.4 8.4 19 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 739 16 7 10 2.3 O=C(NCCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
118103734 164745 None 0 Mouse Functional pEC50 = 8.4 8.4 25 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 761 14 6 12 2.0 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(OCc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)nc1 10.1021/acs.jmedchem.8b00308
CHEMBL4216584 164745 None 0 Mouse Functional pEC50 = 8.4 8.4 25 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 761 14 6 12 2.0 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(OCc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)nc1 10.1021/acs.jmedchem.8b00308
118104386 164787 None 0 Mouse Functional pEC50 = 8.4 8.4 - 1
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 760 15 4 8 4.2 C[C@@H](NC(=O)[C@@H](C)NC(=O)[C@@H](C)NC(=O)CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)C(=O)O 10.1021/acs.jmedchem.8b00308
CHEMBL4217133 164787 None 0 Mouse Functional pEC50 = 8.4 8.4 - 1
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 760 15 4 8 4.2 C[C@@H](NC(=O)[C@@H](C)NC(=O)[C@@H](C)NC(=O)CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)C(=O)O 10.1021/acs.jmedchem.8b00308
145967535 164888 None 0 Mouse Functional pEC50 = 8.4 8.4 15 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 739 15 6 10 2.3 CN(C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)C(=O)NCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4218315 164888 None 0 Mouse Functional pEC50 = 8.4 8.4 15 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 739 15 6 10 2.3 CN(C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)C(=O)NCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
145007569 195011 None 0 Mouse Functional pEC50 = 8.4 8.4 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(CC2CCCO2)C(=O)CC1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
CHEMBL5394911 195011 None 0 Mouse Functional pEC50 = 8.4 8.4 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(CC2CCCO2)C(=O)CC1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
90644447 112294 None 0 Human Functional pEC50 = 7.5 7.5 2 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 616 10 1 8 5.8 CCOC(=O)CNC(=O)CCc1oc2ccc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c2c1C 10.1016/j.ejmech.2014.05.031
CHEMBL3290737 112294 None 0 Human Functional pEC50 = 7.5 7.5 2 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 616 10 1 8 5.8 CCOC(=O)CNC(=O)CCc1oc2ccc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c2c1C 10.1016/j.ejmech.2014.05.031
71455636 83049 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 442 5 0 5 5.5 CCCN1CCN(C(=O)c2cncnc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
CHEMBL2181253 83049 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 442 5 0 5 5.5 CCCN1CCN(C(=O)c2cncnc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
71452079 83051 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 440 5 0 5 5.2 C=CCN1CCN(C(=O)c2cncnc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
CHEMBL2181255 83051 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 440 5 0 5 5.2 C=CCN1CCN(C(=O)c2cncnc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
90654596 110027 None 0 Human Functional pEC50 = 7.5 7.5 -15 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 608 10 2 8 4.0 N#Cc1ccc(CCNC(=O)[C@@H]2CCN2c2cc(N3CCC(Oc4ccc(CC(=O)O)cc4)CC3)nc(C(F)(F)F)n2)cc1 10.1021/jm401731q
CHEMBL3234583 110027 None 0 Human Functional pEC50 = 7.5 7.5 -15 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 608 10 2 8 4.0 N#Cc1ccc(CCNC(=O)[C@@H]2CCN2c2cc(N3CCC(Oc4ccc(CC(=O)O)cc4)CC3)nc(C(F)(F)F)n2)cc1 10.1021/jm401731q
118694573 196130 None 0 Human Functional pEC50 = 7.5 7.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5417359 196130 None 0 Human Functional pEC50 = 7.5 7.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
118694598 197051 None 0 Human Functional pEC50 = 7.5 7.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 457 7 0 6 3.9 COC(=O)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5437561 197051 None 0 Human Functional pEC50 = 7.5 7.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 457 7 0 6 3.9 COC(=O)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
71459273 83018 None 0 Mouse Functional pEC50 = 7.5 7.5 -1 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 405 4 0 4 5.2 O=C(c1cnccc1Oc1ccccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/jm301071h
CHEMBL2181221 83018 None 0 Mouse Functional pEC50 = 7.5 7.5 -1 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 405 4 0 4 5.2 O=C(c1cnccc1Oc1ccccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/jm301071h
71452080 83052 None 0 Mouse Functional pEC50 = 7.5 7.5 -10 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 440 4 0 5 5.2 O=C(c1cncnc1Oc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/jm301071h
CHEMBL2181256 83052 None 0 Mouse Functional pEC50 = 7.5 7.5 -10 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 440 4 0 5 5.2 O=C(c1cncnc1Oc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/jm301071h
164617886 184963 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 501 3 2 3 7.3 CC(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(N)=O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
CHEMBL4852436 184963 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 501 3 2 3 7.3 CC(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(N)=O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
118464664 157282 None 0 Mouse Functional pEC50 = 6.5 6.5 2 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 478 6 0 6 5.9 COc1cc(C2(C)CCCc3nc(SCc4ncccn4)n(-c4ccc(F)cc4)c32)ccc1F 10.1021/acsmedchemlett.7b00116
CHEMBL4075703 157282 None 0 Mouse Functional pEC50 = 6.5 6.5 2 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 478 6 0 6 5.9 COc1cc(C2(C)CCCc3nc(SCc4ncccn4)n(-c4ccc(F)cc4)c32)ccc1F 10.1021/acsmedchemlett.7b00116
156021144 178183 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 387 3 2 3 5.3 CC[C@]1(O)C[C@H]2[C@@H]3CC[C@H]([C@H](C)CC#N)[C@@]3(C)CC[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1021/acsmedchemlett.9b00636
CHEMBL4647613 178183 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 387 3 2 3 5.3 CC[C@]1(O)C[C@H]2[C@@H]3CC[C@H]([C@H](C)CC#N)[C@@]3(C)CC[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1021/acsmedchemlett.9b00636
118700248 194970 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5394284 194970 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694544 195184 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(F)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5398341 195184 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(F)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694377 195524 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(OC)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5405338 195524 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(OC)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694576 195995 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2Cl)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5414847 195995 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2Cl)=C1C 10.1021/acs.jmedchem.2c01881
118694463 196483 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 471 8 0 6 4.1 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C(=O)OC)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5424851 196483 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 471 8 0 6 4.1 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C(=O)OC)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694354 196663 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 423 6 0 3 5.5 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC1CCC1 10.1021/acs.jmedchem.2c01881
CHEMBL5429244 196663 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 423 6 0 3 5.5 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC1CCC1 10.1021/acs.jmedchem.2c01881
118694465 196755 None 0 Human Functional pEC50 = 6.5 6.5 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2F)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5431493 196755 None 0 Human Functional pEC50 = 6.5 6.5 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2F)=C1C 10.1021/acs.jmedchem.2c01881
118700250 197183 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2C)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5440622 197183 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2C)=C1C 10.1021/acs.jmedchem.2c01881
73350994 92781 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 520 6 0 3 7.7 O=C(c1cccs1)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
CHEMBL2435942 92781 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 520 6 0 3 7.7 O=C(c1cccs1)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
118694360 195298 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5400262 195298 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694361 195650 None 0 Mouse Functional pEC50 = 6.5 6.5 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 409 6 0 3 5.1 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC1CC1 10.1021/acs.jmedchem.2c01881
CHEMBL5408025 195650 None 0 Mouse Functional pEC50 = 6.5 6.5 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 409 6 0 3 5.1 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC1CC1 10.1021/acs.jmedchem.2c01881
118694348 196364 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(OC)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5422305 196364 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(OC)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694354 196663 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 423 6 0 3 5.5 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC1CCC1 10.1021/acs.jmedchem.2c01881
CHEMBL5429244 196663 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 423 6 0 3 5.5 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC1CCC1 10.1021/acs.jmedchem.2c01881
118694371 197143 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 455 7 0 4 5.2 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2c(C)cc(C)cc2C)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5439826 197143 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 455 7 0 4 5.2 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2c(C)cc(C)cc2C)=C1C 10.1021/acs.jmedchem.2c01881
14774173 189990 None 6 Human Functional pEC50 = 5.5 5.5 -1 2
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 279 4 1 3 3.5 O=C(O)c1cccc(OCc2ccc3ccccc3n2)c1 10.1021/acs.jmedchem.1c01078
CHEMBL5169385 189990 None 6 Human Functional pEC50 = 5.5 5.5 -1 2
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 279 4 1 3 3.5 O=C(O)c1cccc(OCc2ccc3ccccc3n2)c1 10.1021/acs.jmedchem.1c01078
101882290 114593 None 0 Human Functional pEC50 = 4.5 4.5 - 1
Activity at TGR5 in human NCI-H716 cells assessed as effect on intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assayActivity at TGR5 in human NCI-H716 cells assessed as effect on intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay
ChEMBL 446 6 3 4 5.2 COc1ccc(C(=O)Nc2cccc(C(=O)O)c2)c(NC(=O)c2ccc(C(C)(C)C)cc2)c1 10.1021/jm500937v
CHEMBL3335672 114593 None 0 Human Functional pEC50 = 4.5 4.5 - 1
Activity at TGR5 in human NCI-H716 cells assessed as effect on intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assayActivity at TGR5 in human NCI-H716 cells assessed as effect on intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay
ChEMBL 446 6 3 4 5.2 COc1ccc(C(=O)Nc2cccc(C(=O)O)c2)c(NC(=O)c2ccc(C(C)(C)C)cc2)c1 10.1021/jm500937v
9848818 97953 None 43 Human Functional pEC50 = 4.5 4.5 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 499 7 4 5 3.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
CHEMBL272427 97953 None 43 Human Functional pEC50 = 4.5 4.5 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 499 7 4 5 3.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
118735266 118896 None 0 Human Functional pEC50 = 4.5 4.5 -2 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 1178 26 2 13 10.8 O=C(CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NCCOCCOCCOCCNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421902 118896 None 0 Human Functional pEC50 = 4.5 4.5 -2 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 1178 26 2 13 10.8 O=C(CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NCCOCCOCCOCCNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
10133 910 None 49 Human Functional pEC50 = 4.5 4.5 -1 4
Agonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assayAgonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assay
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 10.1016/j.bmc.2011.03.004
145714624 910 None 49 Human Functional pEC50 = 4.5 4.5 -1 4
Agonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assayAgonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assay
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 10.1016/j.bmc.2011.03.004
4361 910 None 49 Human Functional pEC50 = 4.5 4.5 -1 4
Agonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assayAgonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assay
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 10.1016/j.bmc.2011.03.004
608 910 None 49 Human Functional pEC50 = 4.5 4.5 -1 4
Agonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assayAgonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assay
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 10.1016/j.bmc.2011.03.004
CHEMBL240597 910 None 49 Human Functional pEC50 = 4.5 4.5 -1 4
Agonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assayAgonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assay
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 10.1016/j.bmc.2011.03.004
DB06777 910 None 49 Human Functional pEC50 = 4.5 4.5 -1 4
Agonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assayAgonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assay
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 10.1016/j.bmc.2011.03.004
89707030 171871 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 391 4 3 3 3.9 C[C@H](CCC(N)=O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/acs.jmedchem.9b00770
CHEMBL4467588 171871 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 391 4 3 3 3.9 C[C@H](CCC(N)=O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/acs.jmedchem.9b00770
118464758 156487 None 0 Human Functional pEC50 = 4.5 4.5 -95 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 560 7 0 5 8.2 COc1cc(-n2c(SCc3c(F)cccc3Cl)nc3c2C(c2ccc(Cl)c(OC)c2)CCC3)ccc1F 10.1021/acsmedchemlett.7b00116
CHEMBL4066466 156487 None 0 Human Functional pEC50 = 4.5 4.5 -95 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 560 7 0 5 8.2 COc1cc(-n2c(SCc3c(F)cccc3Cl)nc3c2C(c2ccc(Cl)c(OC)c2)CCC3)ccc1F 10.1021/acsmedchemlett.7b00116
164618147 185471 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 599 6 2 5 7.6 CC(C)[C@@H]1CC[C@]2(C(=O)OCC(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
CHEMBL4860380 185471 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 599 6 2 5 7.6 CC(C)[C@@H]1CC[C@]2(C(=O)OCC(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
130361936 169961 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 430 5 2 5 4.4 CO[C@@H]1CC[C@]2(C)[C@H]3CC[C@@]4(C)[C@@H](CC[C@@H]4[C@H](C)CCc4nn[nH]n4)[C@@H]3[C@H](O)C[C@@H]2C1 10.1021/acs.jmedchem.9b00770
CHEMBL4440213 169961 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 430 5 2 5 4.4 CO[C@@H]1CC[C@]2(C)[C@H]3CC[C@@]4(C)[C@@H](CC[C@@H]4[C@H](C)CCc4nn[nH]n4)[C@@H]3[C@H](O)C[C@@H]2C1 10.1021/acs.jmedchem.9b00770
73353940 92772 None 0 Human Functional pEC50 = 7.5 7.5 27 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 582 6 0 4 7.0 O=C(c1ccccc1)N(Cc1cnccc1-c1ccccc1F)S(=O)(=O)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435932 92772 None 0 Human Functional pEC50 = 7.5 7.5 27 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 582 6 0 4 7.0 O=C(c1ccccc1)N(Cc1cnccc1-c1ccccc1F)S(=O)(=O)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
71459274 83019 None 0 Mouse Functional pEC50 = 7.5 7.5 -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 405 4 0 4 5.2 O=C(c1cnccc1Oc1cccc(Cl)c1)N1CCN(C2CC2)c2ccccc21 10.1021/jm301071h
CHEMBL2181222 83019 None 0 Mouse Functional pEC50 = 7.5 7.5 -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 405 4 0 4 5.2 O=C(c1cnccc1Oc1cccc(Cl)c1)N1CCN(C2CC2)c2ccccc21 10.1021/jm301071h
71450252 83038 None 0 Mouse Functional pEC50 = 7.5 7.5 -10 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 6.2 O=C(c1cnccc1Oc1cc(Cl)ccc1Cl)N1CCN(C2CCC2)c2ccccc21 10.1021/jm301071h
CHEMBL2181240 83038 None 0 Mouse Functional pEC50 = 7.5 7.5 -10 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 6.2 O=C(c1cnccc1Oc1cc(Cl)ccc1Cl)N1CCN(C2CCC2)c2ccccc21 10.1021/jm301071h
90654563 110018 None 0 Mouse Functional pEC50 = 7.5 7.5 -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 2.8 CN1CCN(c2cc(N3CCCC[C@H]3C(=O)NCCc3ccc(C#N)cc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
CHEMBL3234574 110018 None 0 Mouse Functional pEC50 = 7.5 7.5 -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 2.8 CN1CCN(c2cc(N3CCCC[C@H]3C(=O)NCCc3ccc(C#N)cc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
118093535 164541 None 0 Human Functional pEC50 = 7.5 7.5 -5 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 682 13 6 10 1.4 O=C(CCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4213844 164541 None 0 Human Functional pEC50 = 7.5 7.5 -5 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 682 13 6 10 1.4 O=C(CCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
118103672 164545 None 0 Human Functional pEC50 = 7.5 7.5 -31 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human 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 Human Functional pEC50 = 7.5 7.5 -31 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human 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
145974037 164849 None 0 Human Functional pEC50 = 7.5 7.5 -15 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 725 15 7 10 1.9 O=C(NCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4217797 164849 None 0 Human Functional pEC50 = 7.5 7.5 -15 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 725 15 7 10 1.9 O=C(NCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
44605616 200751 None 49 Human Functional pEC50 = 7.5 7.5 28 2
Agonist activity at human TGR5 expressed in melanophores assessed as melanosome dispersion by melanophore assayAgonist activity at human TGR5 expressed in melanophores assessed as melanosome dispersion by melanophore assay
ChEMBL 360 3 0 3 5.2 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(Cl)cc1 10.1021/jm901434t
CHEMBL575966 200751 None 49 Human Functional pEC50 = 7.5 7.5 28 2
Agonist activity at human TGR5 expressed in melanophores assessed as melanosome dispersion by melanophore assayAgonist activity at human TGR5 expressed in melanophores assessed as melanosome dispersion by melanophore assay
ChEMBL 360 3 0 3 5.2 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(Cl)cc1 10.1021/jm901434t
145007569 195011 None 0 Human Functional pEC50 = 7.5 7.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(CC2CCCO2)C(=O)CC1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
CHEMBL5394911 195011 None 0 Human Functional pEC50 = 7.5 7.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(CC2CCCO2)C(=O)CC1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
118694466 195057 None 0 Human Functional pEC50 = 7.5 7.5 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
CHEMBL5395730 195057 None 0 Human Functional pEC50 = 7.5 7.5 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
118694598 197051 None 0 Human Functional pEC50 = 7.5 7.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 457 7 0 6 3.9 COC(=O)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5437561 197051 None 0 Human Functional pEC50 = 7.5 7.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 457 7 0 6 3.9 COC(=O)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
44605616 200751 None 49 Human Functional pEC50 = 7.5 7.5 28 2
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 360 3 0 3 5.2 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL575966 200751 None 49 Human Functional pEC50 = 7.5 7.5 28 2
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 360 3 0 3 5.2 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
46232628 203273 None 0 Human Functional pEC50 = 7.5 7.5 - 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 374 4 0 3 5.6 CCN(C(=O)c1c(-c2ccccc2Cl)noc1C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL600833 203273 None 0 Human Functional pEC50 = 7.5 7.5 - 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 374 4 0 3 5.6 CCN(C(=O)c1c(-c2ccccc2Cl)noc1C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
46232595 203840 None 0 Human Functional pEC50 = 7.5 7.5 - 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 394 3 0 3 5.6 Cc1onc(-c2ccccc2C(F)(F)F)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL604543 203840 None 0 Human Functional pEC50 = 7.5 7.5 - 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 394 3 0 3 5.6 Cc1onc(-c2ccccc2C(F)(F)F)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
118103700 164078 None 0 Mouse Functional pEC50 = 7.5 7.5 3 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 764 14 6 13 1.4 Cn1nc(C(=O)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)cc1OCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4208057 164078 None 0 Mouse Functional pEC50 = 7.5 7.5 3 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 764 14 6 13 1.4 Cn1nc(C(=O)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)cc1OCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
118103673 164125 None 1 Mouse Functional pEC50 = 7.5 7.5 12 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 597 8 1 6 6.2 O=C(O)c1ccc(COc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)cc1 10.1021/acs.jmedchem.8b00308
CHEMBL4208726 164125 None 1 Mouse Functional pEC50 = 7.5 7.5 12 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 597 8 1 6 6.2 O=C(O)c1ccc(COc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)cc1 10.1021/acs.jmedchem.8b00308
118104381 164630 None 0 Mouse Functional pEC50 = 7.5 7.5 7 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 760 14 6 11 2.6 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1cccc(OCc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)c1 10.1021/acs.jmedchem.8b00308
CHEMBL4215045 164630 None 0 Mouse Functional pEC50 = 7.5 7.5 7 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 760 14 6 11 2.6 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1cccc(OCc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)c1 10.1021/acs.jmedchem.8b00308
137636348 155955 None 0 Human Functional pEC50 = 6.5 6.5 -12 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 524 7 0 5 7.2 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cccc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4060315 155955 None 0 Human Functional pEC50 = 6.5 6.5 -12 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 524 7 0 5 7.2 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cccc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
73353943 92784 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 518 6 0 3 7.8 CC(c1cc(C(F)(F)F)cc(C(F)(F)F)c1)N(Cc1cnccc1-c1ccccc1)C(=O)c1ccco1 10.1016/j.ejmech.2013.07.050
CHEMBL2435945 92784 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 518 6 0 3 7.8 CC(c1cc(C(F)(F)F)cc(C(F)(F)F)c1)N(Cc1cnccc1-c1ccccc1)C(=O)c1ccco1 10.1016/j.ejmech.2013.07.050
168264805 197367 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human TGR5 expressed in HEK293 cells incubated for 30 mins by SEAP reporter gene based assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 30 mins by SEAP reporter gene based assay
ChEMBL 527 8 4 5 3.9 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@H](C)CCC(=O)NCCS(=O)(=O)O)[C@H]3[C@H](C)C[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1016/j.ejmech.2023.115143
CHEMBL5402724 197367 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human TGR5 expressed in HEK293 cells incubated for 30 mins by SEAP reporter gene based assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 30 mins by SEAP reporter gene based assay
ChEMBL 527 8 4 5 3.9 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@H](C)CCC(=O)NCCS(=O)(=O)O)[C@H]3[C@H](C)C[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1016/j.ejmech.2023.115143
CHEMBL5498703 197367 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human TGR5 expressed in HEK293 cells incubated for 30 mins by SEAP reporter gene based assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 30 mins by SEAP reporter gene based assay
ChEMBL 527 8 4 5 3.9 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@H](C)CCC(=O)NCCS(=O)(=O)O)[C@H]3[C@H](C)C[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1016/j.ejmech.2023.115143
64980 207925 None 4 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 458 2 2 3 6.1 CC(=O)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@H](O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/jm900872z
CHEMBL80460 207925 None 4 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 458 2 2 3 6.1 CC(=O)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@H](O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/jm900872z
118464758 156487 None 0 Mouse Functional pEC50 = 6.5 6.5 95 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 560 7 0 5 8.2 COc1cc(-n2c(SCc3c(F)cccc3Cl)nc3c2C(c2ccc(Cl)c(OC)c2)CCC3)ccc1F 10.1021/acsmedchemlett.7b00116
CHEMBL4066466 156487 None 0 Mouse Functional pEC50 = 6.5 6.5 95 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 560 7 0 5 8.2 COc1cc(-n2c(SCc3c(F)cccc3Cl)nc3c2C(c2ccc(Cl)c(OC)c2)CCC3)ccc1F 10.1021/acsmedchemlett.7b00116
71561617 87672 None 0 Human Functional pEC50 = 5.5 5.5 - 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 444 4 0 5 5.6 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N1CCCCC1c1ccncc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336225 87672 None 0 Human Functional pEC50 = 5.5 5.5 - 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 444 4 0 5 5.6 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N1CCCCC1c1ccncc1 10.1016/j.bmcl.2012.12.076
71453902 83041 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 373 4 0 4 4.9 CN(C(=O)c1cncnc1Oc1cc(Cl)ccc1Cl)c1ccccc1 10.1021/jm301071h
CHEMBL2181243 83041 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 373 4 0 4 4.9 CN(C(=O)c1cncnc1Oc1cc(Cl)ccc1Cl)c1ccccc1 10.1021/jm301071h
44605617 200775 None 1 Human Functional pEC50 = 6.5 6.5 5 2
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 374 3 0 3 5.5 Cc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1Cl 10.1021/ml300277t
CHEMBL576138 200775 None 1 Human Functional pEC50 = 6.5 6.5 5 2
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 374 3 0 3 5.5 Cc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1Cl 10.1021/ml300277t
118093484 163618 None 0 Human Functional pEC50 = 6.5 6.5 -31 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 617 8 1 8 5.6 Cn1c(C(=O)O)cnc1SCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4202656 163618 None 0 Human Functional pEC50 = 6.5 6.5 -31 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 617 8 1 8 5.6 Cn1c(C(=O)O)cnc1SCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
71660822 164860 None 0 Human Functional pEC50 = 6.5 6.5 5 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 461 4 0 4 4.9 O=C([C@@H]1CSCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4217961 164860 None 0 Human Functional pEC50 = 6.5 6.5 5 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 461 4 0 4 4.9 O=C([C@@H]1CSCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118700248 194970 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5394284 194970 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694544 195184 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(F)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5398341 195184 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(F)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694377 195524 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(OC)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5405338 195524 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(OC)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694576 195995 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2Cl)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5414847 195995 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2Cl)=C1C 10.1021/acs.jmedchem.2c01881
118694353 196488 None 0 Human Functional pEC50 = 6.5 6.5 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 429 7 1 5 3.7 COc1ccccc1COC(=O)C1=C(C)N(CCO)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5425096 196488 None 0 Human Functional pEC50 = 6.5 6.5 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 429 7 1 5 3.7 COc1ccccc1COC(=O)C1=C(C)N(CCO)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
118694354 196663 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 423 6 0 3 5.5 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC1CCC1 10.1021/acs.jmedchem.2c01881
CHEMBL5429244 196663 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 423 6 0 3 5.5 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC1CCC1 10.1021/acs.jmedchem.2c01881
46232485 203071 None 0 Human Functional pEC50 = 6.5 6.5 - 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 410 4 0 4 5.5 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL599347 203071 None 0 Human Functional pEC50 = 6.5 6.5 - 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 410 4 0 4 5.5 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2010.01.003
46232596 203522 None 0 Human Functional pEC50 = 6.5 6.5 - 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 394 3 0 3 5.6 Cc1onc(-c2cccc(C(F)(F)F)c2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL602691 203522 None 0 Human Functional pEC50 = 6.5 6.5 - 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 394 3 0 3 5.6 Cc1onc(-c2cccc(C(F)(F)F)c2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
46232486 203994 None 0 Human Functional pEC50 = 6.5 6.5 - 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 351 3 0 4 4.5 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(C#N)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL605356 203994 None 0 Human Functional pEC50 = 6.5 6.5 - 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 351 3 0 4 4.5 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(C#N)cc1 10.1016/j.bmcl.2010.01.003
46232656 204558 None 0 Human Functional pEC50 = 6.5 6.5 - 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 388 5 0 3 6.0 CCCN(C(=O)c1c(-c2ccccc2Cl)noc1C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL608867 204558 None 0 Human Functional pEC50 = 6.5 6.5 - 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 388 5 0 3 6.0 CCCN(C(=O)c1c(-c2ccccc2Cl)noc1C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
71660823 164475 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 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 445 4 0 4 4.2 O=C([C@@H]1COCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4213036 164475 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 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 445 4 0 4 4.2 O=C([C@@H]1COCCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118093420 164640 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 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 459 5 0 4 4.6 CO[C@H]1C[C@@H](C(=O)N2CCN(C3CC3)c3ccccc32)N(Cc2cc(Cl)ccc2Cl)C1 10.1021/acs.jmedchem.8b00308
CHEMBL4215113 164640 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 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 459 5 0 4 4.6 CO[C@H]1C[C@@H](C(=O)N2CCN(C3CC3)c3ccccc32)N(Cc2cc(Cl)ccc2Cl)C1 10.1021/acs.jmedchem.8b00308
118700248 194970 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5394284 194970 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694360 195298 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5400262 195298 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694348 196364 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(OC)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5422305 196364 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(OC)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694354 196663 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 423 6 0 3 5.5 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC1CCC1 10.1021/acs.jmedchem.2c01881
CHEMBL5429244 196663 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 423 6 0 3 5.5 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC1CCC1 10.1021/acs.jmedchem.2c01881
5283820 98011 None 43 Human Functional pEC50 = 4.5 4.5 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 392 4 3 3 4.5 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@@H]3C[C@H](O)[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
CHEMBL272621 98011 None 43 Human Functional pEC50 = 4.5 4.5 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 392 4 3 3 4.5 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@@H]3C[C@H](O)[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
172462671 196608 None 0 Human Functional pEC50 = 4.5 4.5 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 448 6 1 5 4.8 CCOC(=O)CC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](OC)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC(=O)[C@]12C 10.1016/j.bmc.2023.117418
CHEMBL5427709 196608 None 0 Human Functional pEC50 = 4.5 4.5 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 448 6 1 5 4.8 CCOC(=O)CC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](OC)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC(=O)[C@]12C 10.1016/j.bmc.2023.117418
CHEMBL4581956 216495 None 7 Human Functional pEC50 = 5.5 5.5 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL None None None CC1=C(C(=O)OCc2ccccc2)C(c2ccccc2OC(C)C)CC(=O)N1 10.1021/acs.jmedchem.2c01881
46232657 203275 None 0 Human Functional pEC50 = 5.5 5.5 - 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 386 4 0 3 5.8 Cc1onc(-c2ccccc2Cl)c1C(=O)N(c1ccc(Cl)cc1)C1CC1 10.1016/j.bmcl.2010.01.003
CHEMBL600835 203275 None 0 Human Functional pEC50 = 5.5 5.5 - 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 386 4 0 3 5.8 Cc1onc(-c2ccccc2Cl)c1C(=O)N(c1ccc(Cl)cc1)C1CC1 10.1016/j.bmcl.2010.01.003
46232698 203307 None 0 Human Functional pEC50 = 5.5 5.5 - 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 372 2 0 3 5.2 Cc1onc(-c2ccccc2Cl)c1C(=O)N1CCc2cc(Cl)ccc21 10.1016/j.bmcl.2010.01.003
CHEMBL601218 203307 None 0 Human Functional pEC50 = 5.5 5.5 - 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 372 2 0 3 5.2 Cc1onc(-c2ccccc2Cl)c1C(=O)N1CCc2cc(Cl)ccc21 10.1016/j.bmcl.2010.01.003
723048 203381 None 16 Human Functional pEC50 = 5.5 5.5 - 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 346 3 1 3 5.2 Cc1onc(-c2ccccc2Cl)c1C(=O)Nc1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL601671 203381 None 16 Human Functional pEC50 = 5.5 5.5 - 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 346 3 1 3 5.2 Cc1onc(-c2ccccc2Cl)c1C(=O)Nc1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
44626599 200186 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 573 4 1 4 8.9 C=C(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC/C(=N\OC(=O)c6ccccc6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/jm900872z
CHEMBL571478 200186 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 573 4 1 4 8.9 C=C(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC/C(=N\OC(=O)c6ccccc6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/jm900872z
71561367 87661 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 412 4 0 5 4.6 Cc1nn(C)c(Oc2cccc(F)c2F)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336212 87661 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 412 4 0 5 4.6 Cc1nn(C)c(Oc2cccc(F)c2F)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
73353941 92773 None 0 Human Functional pEC50 = 7.5 7.5 28 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 572 6 0 5 6.6 O=C(c1ccco1)N(Cc1cnccc1-c1ccccc1F)S(=O)(=O)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435933 92773 None 0 Human Functional pEC50 = 7.5 7.5 28 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 572 6 0 5 6.6 O=C(c1ccco1)N(Cc1cnccc1-c1ccccc1F)S(=O)(=O)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
73357026 92780 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 504 6 0 3 7.2 O=C(c1ccoc1)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
CHEMBL2435941 92780 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 504 6 0 3 7.2 O=C(c1ccoc1)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
90654570 109994 None 0 Human Functional pEC50 = 6.5 6.5 2 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 342 5 1 4 2.5 Cc1ccnc(N2CCC[C@@H](C(=O)NCCc3ccc(F)cc3)C2)n1 10.1021/jm401731q
CHEMBL3234551 109994 None 0 Human Functional pEC50 = 6.5 6.5 2 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 342 5 1 4 2.5 Cc1ccnc(N2CCC[C@@H](C(=O)NCCc3ccc(F)cc3)C2)n1 10.1021/jm401731q
441302 97914 None 39 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 290 0 1 2 4.0 C[C@]12CC[C@H]3[C@@H](CC[C@H]4C[C@@H](O)CC[C@@]43C)[C@@H]1CCC2=O 10.1021/jm7015864
CHEMBL272195 97914 None 39 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 290 0 1 2 4.0 C[C@]12CC[C@H]3[C@@H](CC[C@H]4C[C@@H](O)CC[C@@]43C)[C@@H]1CCC2=O 10.1021/jm7015864
118464804 156634 None 0 Mouse Functional pEC50 = 6.5 6.5 4 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 568 9 1 6 6.8 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cc(CCO)cc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4068168 156634 None 0 Mouse Functional pEC50 = 6.5 6.5 4 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 568 9 1 6 6.8 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cc(CCO)cc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
24969872 17676 None 0 Human Functional pEC50 = 5.5 5.5 10 2
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 452 7 1 4 6.1 COc1ccc2cc(CNCCc3ccc(Br)cc3)c(-c3ccsc3)nc2c1 10.1021/ml300277t
CHEMBL1258423 17676 None 0 Human Functional pEC50 = 5.5 5.5 10 2
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 452 7 1 4 6.1 COc1ccc2cc(CNCCc3ccc(Br)cc3)c(-c3ccsc3)nc2c1 10.1021/ml300277t
126700765 156596 None 0 Human Functional pEC50 = 6.5 6.5 -8 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 499 9 0 6 6.2 COc1ccc(CN(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4067717 156596 None 0 Human Functional pEC50 = 6.5 6.5 -8 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 499 9 0 6 6.2 COc1ccc(CN(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
90654571 109995 None 0 Human Functional pEC50 = 7.5 7.5 2 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 402 5 1 4 3.1 Cc1ccnc(N2CCC[C@@H](C(=O)NCCc3ccc(Br)cc3)C2)n1 10.1021/jm401731q
CHEMBL3234552 109995 None 0 Human Functional pEC50 = 7.5 7.5 2 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 402 5 1 4 3.1 Cc1ccnc(N2CCC[C@@H](C(=O)NCCc3ccc(Br)cc3)C2)n1 10.1021/jm401731q
71561754 87678 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
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 = 7.5 7.5 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
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
155339374 181972 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 569 11 7 8 1.6 CO[C@@H]1C[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)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)[C@@H]21 10.1039/d0md00425a
CHEMBL4778769 181972 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 569 11 7 8 1.6 CO[C@@H]1C[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)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)[C@@H]21 10.1039/d0md00425a
118464724 159559 None 0 Mouse Functional pEC50 = 6.5 6.5 61 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 528 7 0 6 6.8 COc1ccc(C2OCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4101442 159559 None 0 Mouse Functional pEC50 = 6.5 6.5 61 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 528 7 0 6 6.8 COc1ccc(C2OCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
118694353 196488 None 0 Human Functional pEC50 = 6.5 6.5 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 429 7 1 5 3.7 COc1ccccc1COC(=O)C1=C(C)N(CCO)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5425096 196488 None 0 Human Functional pEC50 = 6.5 6.5 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 429 7 1 5 3.7 COc1ccccc1COC(=O)C1=C(C)N(CCO)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
439763 158218 None 15 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation in presence of 3-isobutyl-1-methylxanthine after 20 minsAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation in presence of 3-isobutyl-1-methylxanthine after 20 mins
ChEMBL 483 7 3 4 4.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/acs.jmedchem.9b00770
CHEMBL408701 158218 None 15 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation in presence of 3-isobutyl-1-methylxanthine after 20 minsAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation in presence of 3-isobutyl-1-methylxanthine after 20 mins
ChEMBL 483 7 3 4 4.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/acs.jmedchem.9b00770
CHEMBL4581956 216495 None 7 Human Functional pEC50 = 5.5 5.5 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL None None None CC1=C(C(=O)OCc2ccccc2)C(c2ccccc2OC(C)C)CC(=O)N1 10.1021/acs.jmedchem.2c01881
71626834 118894 None 0 Mouse Functional pEC50 = 5.5 5.5 2 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 582 10 2 6 5.3 O=C(O)CCNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421900 118894 None 0 Mouse Functional pEC50 = 5.5 5.5 2 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 582 10 2 6 5.3 O=C(O)CCNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
10133 910 None 49 Human Functional pEC50 = 4.5 4.5 -1 4
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 60 mins by HTR-FRET assay
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/acs.jmedchem.9b00770
145714624 910 None 49 Human Functional pEC50 = 4.5 4.5 -1 4
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 60 mins by HTR-FRET assay
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/acs.jmedchem.9b00770
4361 910 None 49 Human Functional pEC50 = 4.5 4.5 -1 4
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 60 mins by HTR-FRET assay
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/acs.jmedchem.9b00770
608 910 None 49 Human Functional pEC50 = 4.5 4.5 -1 4
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 60 mins by HTR-FRET assay
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/acs.jmedchem.9b00770
CHEMBL240597 910 None 49 Human Functional pEC50 = 4.5 4.5 -1 4
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 60 mins by HTR-FRET assay
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/acs.jmedchem.9b00770
DB06777 910 None 49 Human Functional pEC50 = 4.5 4.5 -1 4
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 60 mins by HTR-FRET assay
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/acs.jmedchem.9b00770
10133 910 None 49 Human Functional pEC50 = 4.5 4.5 -1 4
Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay
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/acs.jmedchem.6b01126
145714624 910 None 49 Human Functional pEC50 = 4.5 4.5 -1 4
Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay
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/acs.jmedchem.6b01126
4361 910 None 49 Human Functional pEC50 = 4.5 4.5 -1 4
Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay
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/acs.jmedchem.6b01126
608 910 None 49 Human Functional pEC50 = 4.5 4.5 -1 4
Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay
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/acs.jmedchem.6b01126
CHEMBL240597 910 None 49 Human Functional pEC50 = 4.5 4.5 -1 4
Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay
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/acs.jmedchem.6b01126
DB06777 910 None 49 Human Functional pEC50 = 4.5 4.5 -1 4
Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay
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/acs.jmedchem.6b01126
44627310 201236 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 474 3 3 3 6.1 CC(CO)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@H](O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/jm900872z
CHEMBL583203 201236 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 474 3 3 3 6.1 CC(CO)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@H](O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/jm900872z
5881 209308 None 39 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 288 0 1 2 3.9 C[C@]12CC[C@H]3[C@@H](CC=C4C[C@@H](O)CC[C@@]43C)[C@@H]1CCC2=O 10.1021/jm7015864
CHEMBL90593 209308 None 39 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 288 0 1 2 3.9 C[C@]12CC[C@H]3[C@@H](CC=C4C[C@@H](O)CC[C@@]43C)[C@@H]1CCC2=O 10.1021/jm7015864
71559936 87657 None 0 Human Functional pEC50 = 6.5 6.5 - 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 394 4 0 5 4.4 Cc1nn(C)c(Oc2ccccc2F)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336208 87657 None 0 Human Functional pEC50 = 6.5 6.5 - 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 394 4 0 5 4.4 Cc1nn(C)c(Oc2ccccc2F)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
126673445 157640 None 0 Human Functional pEC50 = 6.5 6.5 -47 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 499 8 0 6 6.7 COc1ccc(N(C)c2c(C)nc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4080290 157640 None 0 Human Functional pEC50 = 6.5 6.5 -47 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 499 8 0 6 6.7 COc1ccc(N(C)c2c(C)nc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
155669594 183240 None 0 Human Functional pEC50 = 6.5 6.5 - 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 394 4 0 4 3.8 O=C(c1cncn1Cc1ccc(F)cc1F)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
CHEMBL4795121 183240 None 0 Human Functional pEC50 = 6.5 6.5 - 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 394 4 0 4 3.8 O=C(c1cncn1Cc1ccc(F)cc1F)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
12310288 158818 None 36 Human Functional pEC50 = 4.5 4.5 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 449 6 4 4 3.6 C[C@H](CCC(=O)NCC(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
CHEMBL409348 158818 None 36 Human Functional pEC50 = 4.5 4.5 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 449 6 4 4 3.6 C[C@H](CCC(=O)NCC(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
90644457 112291 None 0 Human Functional pEC50 = 7.5 7.5 -2 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 614 8 2 8 4.9 Cc1c(/C=C/C(=O)NCC(=O)O)oc2ccc(Cl)c(C(=O)Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c12 10.1016/j.ejmech.2014.05.031
CHEMBL3290734 112291 None 0 Human Functional pEC50 = 7.5 7.5 -2 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 614 8 2 8 4.9 Cc1c(/C=C/C(=O)NCC(=O)O)oc2ccc(Cl)c(C(=O)Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c12 10.1016/j.ejmech.2014.05.031
118464680 158752 None 0 Human Functional pEC50 = 5.5 5.5 -46 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 526 7 0 5 7.6 COc1ccc([C@@H]2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4092785 158752 None 0 Human Functional pEC50 = 5.5 5.5 -46 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 526 7 0 5 7.6 COc1ccc([C@@H]2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
45483949 3582 None 33 Human Functional pEC50 = 5.5 5.5 -2 2
Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1021/jm901390p
7048 3582 None 33 Human Functional pEC50 = 5.5 5.5 -2 2
Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1021/jm901390p
CHEMBL567640 3582 None 33 Human Functional pEC50 = 5.5 5.5 -2 2
Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1021/jm901390p
156705120 181979 None 0 Mouse Functional pEC50 = 5.5 5.5 -41 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 503 6 0 7 5.6 O=C(OCCl)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4778884 181979 None 0 Mouse Functional pEC50 = 5.5 5.5 -41 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 503 6 0 7 5.6 O=C(OCCl)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
71559937 87658 None 0 Human Functional pEC50 = 6.5 6.5 - 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 410 4 0 5 4.9 Cc1nn(C)c(Oc2cccc(Cl)c2)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336209 87658 None 0 Human Functional pEC50 = 6.5 6.5 - 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 410 4 0 5 4.9 Cc1nn(C)c(Oc2cccc(Cl)c2)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
73352466 92764 None 0 Human Functional pEC50 = 7.5 7.5 4 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 453 5 1 3 6.3 N#CC(NCc1cnccc1-c1ccccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435924 92764 None 0 Human Functional pEC50 = 7.5 7.5 4 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 453 5 1 3 6.3 N#CC(NCc1cnccc1-c1ccccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
90644448 112293 None 0 Human Functional pEC50 = 7.5 7.5 2 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 531 7 1 6 6.2 Cc1c(CCC(=O)O)oc2ccc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c12 10.1016/j.ejmech.2014.05.031
CHEMBL3290736 112293 None 0 Human Functional pEC50 = 7.5 7.5 2 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 531 7 1 6 6.2 Cc1c(CCC(=O)O)oc2ccc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c12 10.1016/j.ejmech.2014.05.031
118694466 195057 None 0 Human Functional pEC50 = 7.5 7.5 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
CHEMBL5395730 195057 None 0 Human Functional pEC50 = 7.5 7.5 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
118576935 158042 None 0 Human Functional pEC50 = 7.5 7.5 -43 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human 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 Human Functional pEC50 = 7.5 7.5 -43 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human 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
118576958 158497 None 0 Human Functional pEC50 = 7.5 7.5 -17 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 519 8 0 6 7.0 COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)c(Cl)c2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4090147 158497 None 0 Human Functional pEC50 = 7.5 7.5 -17 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 519 8 0 6 7.0 COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)c(Cl)c2)cc1OC 10.1021/acs.jmedchem.6b01873
89501664 161545 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assay
ChEMBL 566 9 0 4 8.7 CC(C)(c1ccc(Cl)c(Cl)c1)c1cnc(SCCOCc2c(F)cccc2Cl)n1-c1ccc(F)cc1 10.1016/j.bmcl.2018.04.011
CHEMBL4127444 161545 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assay
ChEMBL 566 9 0 4 8.7 CC(C)(c1ccc(Cl)c(Cl)c1)c1cnc(SCCOCc2c(F)cccc2Cl)n1-c1ccc(F)cc1 10.1016/j.bmcl.2018.04.011
73355480 92776 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 514 6 0 2 7.6 O=C(c1ccccc1)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
CHEMBL2435937 92776 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 514 6 0 2 7.6 O=C(c1ccccc1)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
1452520 109991 None 0 Human Functional pEC50 = 6.5 6.5 -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 344 5 1 4 2.7 O=C(NCCc1ccc(Cl)cc1)[C@@H]1CCCN(c2ncccn2)C1 10.1021/jm401731q
CHEMBL3234547 109991 None 0 Human Functional pEC50 = 6.5 6.5 -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 344 5 1 4 2.7 O=C(NCCc1ccc(Cl)cc1)[C@@H]1CCCN(c2ncccn2)C1 10.1021/jm401731q
118464718 158342 None 0 Human Functional pEC50 = 5.5 5.5 -36 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 568 8 1 6 6.9 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cc(C(=O)O)cc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4088541 158342 None 0 Human Functional pEC50 = 5.5 5.5 -36 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 568 8 1 6 6.9 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cc(C(=O)O)cc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
155669596 180775 None 0 Mouse Functional pEC50 = 5.5 5.5 -1 2
Agonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assayAgonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay
ChEMBL 358 4 0 4 3.6 O=C(c1cncn1Cc1ccccc1)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
CHEMBL4755237 180775 None 0 Mouse Functional pEC50 = 5.5 5.5 -1 2
Agonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assayAgonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay
ChEMBL 358 4 0 4 3.6 O=C(c1cncn1Cc1ccccc1)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
71626832 118889 None 0 Human Functional pEC50 = 4.5 4.5 2 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 511 7 1 5 5.8 O=C(O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421894 118889 None 0 Human Functional pEC50 = 4.5 4.5 2 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 511 7 1 5 5.8 O=C(O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
118464622 158963 None 0 Human Functional pEC50 = 4.5 4.5 -26 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 548 6 0 4 8.4 COc1cc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4F)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4095058 158963 None 0 Human Functional pEC50 = 4.5 4.5 -26 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 548 6 0 4 8.4 COc1cc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4F)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
71561614 87665 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 444 4 0 5 5.3 Cc1nn(C)c(Oc2ccccc2C(F)(F)F)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336216 87665 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 444 4 0 5 5.3 Cc1nn(C)c(Oc2ccccc2C(F)(F)F)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
90654567 110022 None 0 Mouse Functional pEC50 = 5.5 5.5 - 1
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 473 6 1 7 2.1 CN1CCN(c2cc(N3CC[C@@H]3C(=O)NCCc3ccc(C#N)cc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
CHEMBL3234578 110022 None 0 Mouse Functional pEC50 = 5.5 5.5 - 1
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 473 6 1 7 2.1 CN1CCN(c2cc(N3CC[C@@H]3C(=O)NCCc3ccc(C#N)cc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
44427760 93279 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 406 4 3 3 4.7 C[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)CC1C[C@H]3O)C(=O)O 10.1021/jm070633p
CHEMBL244783 93279 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 406 4 3 3 4.7 C[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)CC1C[C@H]3O)C(=O)O 10.1021/jm070633p
17755103 201280 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay
ChEMBL 406 4 3 3 4.7 C[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O)C(=O)O 10.1021/jm901390p
CHEMBL583611 201280 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay
ChEMBL 406 4 3 3 4.7 C[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O)C(=O)O 10.1021/jm901390p
136166852 91668 None 0 Human Functional pEC50 = 6.4 6.4 2 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
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 Functional pEC50 = 6.4 6.4 2 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
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
44457475 96248 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 509 9 2 3 6.5 CCC[C@H]1C[C@@H]2CCCC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)NCCS(=O)(=O)O)[C@H]12 10.1021/jm7015864
CHEMBL260737 96248 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 509 9 2 3 6.5 CCC[C@H]1C[C@@H]2CCCC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)NCCS(=O)(=O)O)[C@H]12 10.1021/jm7015864
45483949 3582 None 33 Mouse Functional pEC50 = 6.4 6.4 2 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2013.07.050
7048 3582 None 33 Mouse Functional pEC50 = 6.4 6.4 2 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2013.07.050
CHEMBL567640 3582 None 33 Mouse Functional pEC50 = 6.4 6.4 2 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2013.07.050
31401 48123 None 48 Human Functional pEC50 = 4.4 4.4 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 392 4 3 3 4.5 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
CHEMBL1551 48123 None 48 Human Functional pEC50 = 4.4 4.4 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 392 4 3 3 4.5 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
45485277 200189 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 553 4 1 4 8.7 C=C(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@](C)(CC[C@@H]4[C@@]5(C)CC/C(=N\OC(=O)C(C)C)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/jm900872z
CHEMBL571493 200189 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 553 4 1 4 8.7 C=C(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@](C)(CC[C@@H]4[C@@]5(C)CC/C(=N\OC(=O)C(C)C)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/jm900872z
118586279 155942 None 0 Mouse Functional pEC50 = 6.4 6.4 2 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 535 8 0 6 7.2 COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(C(F)(F)F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4060122 155942 None 0 Mouse Functional pEC50 = 6.4 6.4 2 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 535 8 0 6 7.2 COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(C(F)(F)F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
114611 97725 None 36 Human Functional pEC50 = 4.4 4.4 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 449 6 4 4 3.6 C[C@H](CCC(=O)NCC(=O)O)[C@H]1CC[C@H]2[C@@H]3C[C@H](O)[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
CHEMBL271208 97725 None 36 Human Functional pEC50 = 4.4 4.4 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 449 6 4 4 3.6 C[C@H](CCC(=O)NCC(=O)O)[C@H]1CC[C@H]2[C@@H]3C[C@H](O)[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
137653533 158855 None 0 Human Functional pEC50 = 4.4 4.4 -48 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 702 16 5 9 5.3 COc1ccc(SCc2cnc(SCc3c(F)cc(C(=O)NC(CCCNC(=N)N)C(=O)O)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4094009 158855 None 0 Human Functional pEC50 = 4.4 4.4 -48 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 702 16 5 9 5.3 COc1ccc(SCc2cnc(SCc3c(F)cc(C(=O)NC(CCCNC(=N)N)C(=O)O)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
155669593 183328 None 0 Mouse Functional pEC50 = 5.4 5.4 -31 2
Agonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assayAgonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay
ChEMBL 392 4 0 4 4.2 O=C(c1cncn1Cc1ccccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
CHEMBL4796107 183328 None 0 Mouse Functional pEC50 = 5.4 5.4 -31 2
Agonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assayAgonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay
ChEMBL 392 4 0 4 4.2 O=C(c1cncn1Cc1ccccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
164612607 185516 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 543 4 3 4 6.8 C[C@@H](O)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
CHEMBL4861151 185516 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 543 4 3 4 6.8 C[C@@H](O)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
73347897 92765 None 0 Mouse Functional pEC50 = 6.4 6.4 -6 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 435 5 1 3 6.1 N#CC(NCc1cnccc1-c1ccccc1)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435925 92765 None 0 Mouse Functional pEC50 = 6.4 6.4 -6 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 435 5 1 3 6.1 N#CC(NCc1cnccc1-c1ccccc1)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
71455635 83039 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 416 5 0 5 4.9 CN(C)c1ccccc1N(C)C(=O)c1cncnc1Oc1cc(Cl)ccc1Cl 10.1021/jm301071h
CHEMBL2181241 83039 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 416 5 0 5 4.9 CN(C)c1ccccc1N(C)C(=O)c1cncnc1Oc1cc(Cl)ccc1Cl 10.1021/jm301071h
118464811 156882 None 0 Human Functional pEC50 = 5.4 5.4 -5 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 703 16 0 8 7.9 COc1cc(C2(C)CCCc3nc(SCc4c(F)ccc(OCCOCCOCCN(C)C)c4F)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4070895 156882 None 0 Human Functional pEC50 = 5.4 5.4 -5 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 703 16 0 8 7.9 COc1cc(C2(C)CCCc3nc(SCc4c(F)ccc(OCCOCCOCCN(C)C)c4F)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
5880 208570 None 26 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 290 0 1 2 4.0 C[C@]12CC[C@H]3[C@@H](CC[C@@H]4C[C@H](O)CC[C@]34C)[C@@H]1CCC2=O 10.1021/jm7015864
CHEMBL85799 208570 None 26 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 290 0 1 2 4.0 C[C@]12CC[C@H]3[C@@H](CC[C@@H]4C[C@H](O)CC[C@]34C)[C@@H]1CCC2=O 10.1021/jm7015864
71541721 87321 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 367 6 2 5 1.8 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(C)cc1)CC2 10.1021/ml300277t
CHEMBL2331644 87321 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 367 6 2 5 1.8 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(C)cc1)CC2 10.1021/ml300277t
90644459 112276 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 531 6 0 7 6.4 CCOC(=O)c1oc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2c1C 10.1016/j.ejmech.2014.05.031
CHEMBL3290719 112276 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 531 6 0 7 6.4 CCOC(=O)c1oc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2c1C 10.1016/j.ejmech.2014.05.031
90654592 110017 None 0 Human Functional pEC50 = 7.4 7.4 -2 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 517 7 1 9 1.9 CCN1CCN(c2cc(N3CCC[C@@H](C(=O)NCCc4cnc(C#N)nc4)C3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
CHEMBL3234573 110017 None 0 Human Functional pEC50 = 7.4 7.4 -2 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 517 7 1 9 1.9 CCN1CCN(c2cc(N3CCC[C@@H](C(=O)NCCc4cnc(C#N)nc4)C3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
90644453 112278 None 0 Mouse Functional pEC50 = 7.4 7.4 -7 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 531 7 0 7 6.0 CCOC(=O)Cc1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
CHEMBL3290721 112278 None 0 Mouse Functional pEC50 = 7.4 7.4 -7 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 531 7 0 7 6.0 CCOC(=O)Cc1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
90654574 109998 None 0 Mouse Functional pEC50 = 7.4 7.4 -4 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 376 5 1 4 3.2 Cc1nc(N2CCC[C@@H](C(=O)NCCc3ccc(Cl)cc3)C2)ncc1F 10.1021/jm401731q
CHEMBL3234555 109998 None 0 Mouse Functional pEC50 = 7.4 7.4 -4 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 376 5 1 4 3.2 Cc1nc(N2CCC[C@@H](C(=O)NCCc3ccc(Cl)cc3)C2)ncc1F 10.1021/jm401731q
137661039 159583 None 0 Mouse Functional pEC50 = 6.4 6.4 21 2
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 653 13 2 9 5.5 COc1ccc(SCc2cnc(SCc3c(F)cc(C(=O)NCCS(=O)(=O)O)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4101738 159583 None 0 Mouse Functional pEC50 = 6.4 6.4 21 2
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 653 13 2 9 5.5 COc1ccc(SCc2cnc(SCc3c(F)cc(C(=O)NCCS(=O)(=O)O)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
164614522 185001 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 598 6 3 4 7.2 CC(C)[C@@H]1CC[C@]2(C(=O)NCC(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
CHEMBL4852971 185001 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 598 6 3 4 7.2 CC(C)[C@@H]1CC[C@]2(C(=O)NCC(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
71626765 118888 None 0 Human Functional pEC50 = 5.4 5.4 2 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 539 8 0 6 6.3 CCOC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421893 118888 None 0 Human Functional pEC50 = 5.4 5.4 2 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 539 8 0 6 6.3 CCOC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
172461858 196749 None 0 Human Functional pEC50 = 4.4 4.4 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 546 6 1 5 7.0 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC(=O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)Oc4cccc5ccccc45)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
CHEMBL5431401 196749 None 0 Human Functional pEC50 = 4.4 4.4 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 546 6 1 5 7.0 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC(=O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)Oc4cccc5ccccc45)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
118464620 159006 None 0 Mouse Functional pEC50 = 4.4 4.4 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 542 7 0 5 8.1 COc1ccc(-n2c(SCc3c(F)cccc3Cl)nc3c2C(c2ccc(Cl)c(OC)c2)CCC3)cc1 10.1021/acsmedchemlett.7b00116
CHEMBL4095497 159006 None 0 Mouse Functional pEC50 = 4.4 4.4 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 542 7 0 5 8.1 COc1ccc(-n2c(SCc3c(F)cccc3Cl)nc3c2C(c2ccc(Cl)c(OC)c2)CCC3)cc1 10.1021/acsmedchemlett.7b00116
71561370 87664 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 424 4 0 5 5.2 Cc1ccc(Oc2c(C(=O)N3CCCCC3c3cccnc3)c(C)nn2C)c(Cl)c1 10.1016/j.bmcl.2012.12.076
CHEMBL2336215 87664 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 424 4 0 5 5.2 Cc1ccc(Oc2c(C(=O)N3CCCCC3c3cccnc3)c(C)nn2C)c(Cl)c1 10.1016/j.bmcl.2012.12.076
73349425 92763 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 456 6 1 2 7.2 CCC(NCc1cnccc1-c1ccccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435922 92763 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 456 6 1 2 7.2 CCC(NCc1cnccc1-c1ccccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
1012 25 None 53 Human Functional pEC50 = 4.4 4.4 -22387 4
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 272 0 2 2 3.6 Oc1ccc2c(c1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2O)C 10.1021/jm7015864
1013 25 None 53 Human Functional pEC50 = 4.4 4.4 -22387 4
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 272 0 2 2 3.6 Oc1ccc2c(c1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2O)C 10.1021/jm7015864
1057 25 None 53 Human Functional pEC50 = 4.4 4.4 -22387 4
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 272 0 2 2 3.6 Oc1ccc2c(c1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2O)C 10.1021/jm7015864
5757 25 None 53 Human Functional pEC50 = 4.4 4.4 -22387 4
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 272 0 2 2 3.6 Oc1ccc2c(c1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2O)C 10.1021/jm7015864
CHEMBL135 25 None 53 Human Functional pEC50 = 4.4 4.4 -22387 4
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 272 0 2 2 3.6 Oc1ccc2c(c1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2O)C 10.1021/jm7015864
DB00783 25 None 53 Human Functional pEC50 = 4.4 4.4 -22387 4
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 272 0 2 2 3.6 Oc1ccc2c(c1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2O)C 10.1021/jm7015864
221493 921 None 58 Human Functional pEC50 = 4.4 4.4 -1 2
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1016/j.bmc.2023.117418
3096 921 None 58 Human Functional pEC50 = 4.4 4.4 -1 2
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1016/j.bmc.2023.117418
609 921 None 58 Human Functional pEC50 = 4.4 4.4 -1 2
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1016/j.bmc.2023.117418
CHEMBL205596 921 None 58 Human Functional pEC50 = 4.4 4.4 -1 2
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1016/j.bmc.2023.117418
DB02659 921 None 58 Human Functional pEC50 = 4.4 4.4 -1 2
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1016/j.bmc.2023.117418
71453905 83046 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 3 0 4 5.2 O=C(c1ncncc1Oc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 10.1021/jm301071h
CHEMBL2181250 83046 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 3 0 4 5.2 O=C(c1ncncc1Oc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 10.1021/jm301071h
162665892 182431 None 0 Mouse Functional pEC50 = 6.4 6.4 -16 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 537 6 0 7 6.0 O=C(OCC(F)(F)F)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4784355 182431 None 0 Mouse Functional pEC50 = 6.4 6.4 -16 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 537 6 0 7 6.0 O=C(OCC(F)(F)F)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
12544 48192 None 28 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 449 6 4 4 3.6 C[C@H](CCC(=O)NCC(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
CHEMBL1552 48192 None 28 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 449 6 4 4 3.6 C[C@H](CCC(=O)NCC(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
77845059 112277 None 0 Mouse Functional pEC50 = 7.4 7.4 -22 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 517 6 0 7 6.1 CCOC(=O)c1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
CHEMBL3290720 112277 None 0 Mouse Functional pEC50 = 7.4 7.4 -22 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 517 6 0 7 6.1 CCOC(=O)c1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
118093582 164216 None 0 Human Functional pEC50 = 7.4 7.4 -12 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 710 15 6 10 2.1 O=C(CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4209927 164216 None 0 Human Functional pEC50 = 7.4 7.4 -12 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 710 15 6 10 2.1 O=C(CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
145971348 164665 None 0 Human Functional pEC50 = 7.4 7.4 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 481 4 0 4 5.2 O=C([C@@H]1CSCN1Cc1cc(Cl)ccc1C(F)(F)F)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4215354 164665 None 0 Human Functional pEC50 = 7.4 7.4 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 481 4 0 4 5.2 O=C([C@@H]1CSCN1Cc1cc(Cl)ccc1C(F)(F)F)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
46232629 203274 None 0 Human Functional pEC50 = 7.4 7.4 - 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 388 4 0 3 6.0 Cc1onc(-c2ccccc2Cl)c1C(=O)N(c1ccc(Cl)cc1)C(C)C 10.1016/j.bmcl.2010.01.003
CHEMBL600834 203274 None 0 Human Functional pEC50 = 7.4 7.4 - 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 388 4 0 3 6.0 Cc1onc(-c2ccccc2Cl)c1C(=O)N(c1ccc(Cl)cc1)C(C)C 10.1016/j.bmcl.2010.01.003
118103669 164292 None 0 Mouse Functional pEC50 = 7.4 7.4 - 1
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 1047 28 13 18 -2.1 O=C(NCCCN(CCCNC(=O)[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)C(=O)NCCCCOc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4210783 164292 None 0 Mouse Functional pEC50 = 7.4 7.4 - 1
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 1047 28 13 18 -2.1 O=C(NCCCN(CCCNC(=O)[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)C(=O)NCCCCOc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
74766512 157539 None 0 Human Functional pEC50 = 6.4 6.4 -3 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 699 17 0 9 7.2 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cc(OCCOCCOCCN(C)C)cc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4079040 157539 None 0 Human Functional pEC50 = 6.4 6.4 -3 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 699 17 0 9 7.2 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cc(OCCOCCOCCN(C)C)cc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
71561619 87674 None 0 Human Functional pEC50 = 6.4 6.4 - 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 430 4 0 5 5.2 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N1CCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336227 87674 None 0 Human Functional pEC50 = 6.4 6.4 - 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 430 4 0 5 5.2 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N1CCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
71541719 87323 None 1 Rat Functional pEC50 = 5.4 5.4 -194 3
Agonist activity at rat TGR5 expressed in deoxycycline-induced CHO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at rat TGR5 expressed in deoxycycline-induced CHO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 395 7 2 5 2.6 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(C(C)C)cc1)CC2 10.1021/ml300277t
CHEMBL2331646 87323 None 1 Rat Functional pEC50 = 5.4 5.4 -194 3
Agonist activity at rat TGR5 expressed in deoxycycline-induced CHO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at rat TGR5 expressed in deoxycycline-induced CHO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 395 7 2 5 2.6 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(C(C)C)cc1)CC2 10.1021/ml300277t
118464639 158253 None 0 Mouse Functional pEC50 = 6.4 6.4 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 541 7 0 6 7.5 COc1cc(C2CCCc3nc(SCc4c(F)cccc4[N+](=O)[O-])n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4087370 158253 None 0 Mouse Functional pEC50 = 6.4 6.4 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 541 7 0 6 7.5 COc1cc(C2CCCc3nc(SCc4c(F)cccc4[N+](=O)[O-])n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
118103673 164125 None 1 Human Functional pEC50 = 6.4 6.4 -12 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 597 8 1 6 6.2 O=C(O)c1ccc(COc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)cc1 10.1021/acs.jmedchem.8b00308
CHEMBL4208726 164125 None 1 Human Functional pEC50 = 6.4 6.4 -12 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 597 8 1 6 6.2 O=C(O)c1ccc(COc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)cc1 10.1021/acs.jmedchem.8b00308
118103718 164616 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 682 13 6 9 1.4 O=C(CCc1cc(Cl)c(CN2C[C@@H](F)C[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4214838 164616 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 682 13 6 9 1.4 O=C(CCc1cc(Cl)c(CN2C[C@@H](F)C[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
118694489 195118 None 0 Human Functional pEC50 = 6.4 6.4 8 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 497 8 0 5 5.2 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC(F)(F)F)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5396998 195118 None 0 Human Functional pEC50 = 6.4 6.4 8 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 497 8 0 5 5.2 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC(F)(F)F)=C1C 10.1021/acs.jmedchem.2c01881
118694361 195650 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 409 6 0 3 5.1 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC1CC1 10.1021/acs.jmedchem.2c01881
CHEMBL5408025 195650 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 409 6 0 3 5.1 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC1CC1 10.1021/acs.jmedchem.2c01881
118694450 195753 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C(F)(F)F)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5410122 195753 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C(F)(F)F)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694501 196167 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(Cl)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5418039 196167 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(Cl)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694477 196545 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 463 7 0 4 5.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc3ccccc3c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5426387 196545 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 463 7 0 4 5.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc3ccccc3c2)=C1C 10.1021/acs.jmedchem.2c01881
118694385 196820 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
CHEMBL5432845 196820 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
46232982 203879 None 0 Human Functional pEC50 = 6.4 6.4 - 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 COc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL604751 203879 None 0 Human Functional pEC50 = 6.4 6.4 - 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 COc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2010.01.003
46233023 204106 None 0 Human Functional pEC50 = 6.4 6.4 - 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 340 3 0 3 4.9 Cc1ccccc1N(C)C(=O)c1c(-c2ccccc2Cl)noc1C 10.1016/j.bmcl.2010.01.003
CHEMBL605986 204106 None 0 Human Functional pEC50 = 6.4 6.4 - 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 340 3 0 3 4.9 Cc1ccccc1N(C)C(=O)c1c(-c2ccccc2Cl)noc1C 10.1016/j.bmcl.2010.01.003
118093493 163667 None 0 Mouse Functional pEC50 = 6.4 6.4 -3 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 664 13 6 9 1.5 O=C(CCc1cc(Cl)c(CN2CCC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4203191 163667 None 0 Mouse Functional pEC50 = 6.4 6.4 -3 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 664 13 6 9 1.5 O=C(CCc1cc(Cl)c(CN2CCC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
118093510 164281 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 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 475 4 0 4 5.7 CC1(C)SC[C@@H](C(=O)N2CCN(C3CC3)c3ccccc32)N1Cc1cc(Cl)ccc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4210686 164281 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 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 475 4 0 4 5.7 CC1(C)SC[C@@H](C(=O)N2CCN(C3CC3)c3ccccc32)N1Cc1cc(Cl)ccc1Cl 10.1021/acs.jmedchem.8b00308
118093506 164817 None 0 Mouse Functional pEC50 = 6.4 6.4 1 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 445 4 1 4 3.9 O=C([C@@H]1C[C@H](O)CN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4217450 164817 None 0 Mouse Functional pEC50 = 6.4 6.4 1 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 445 4 1 4 3.9 O=C([C@@H]1C[C@H](O)CN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118694377 195524 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(OC)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5405338 195524 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(OC)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694501 196167 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(Cl)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5418039 196167 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(Cl)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694463 196483 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 471 8 0 6 4.1 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C(=O)OC)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5424851 196483 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 471 8 0 6 4.1 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C(=O)OC)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694393 196611 None 0 Mouse Functional pEC50 = 6.4 6.4 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C(F)(F)F)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5427795 196611 None 0 Mouse Functional pEC50 = 6.4 6.4 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C(F)(F)F)cc2)=C1C 10.1021/acs.jmedchem.2c01881
5283932 97719 None 19 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 390 4 2 3 4.7 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CCC(=O)C[C@H]1C[C@H]3O 10.1021/jm7015864
CHEMBL271172 97719 None 19 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 390 4 2 3 4.7 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CCC(=O)C[C@H]1C[C@H]3O 10.1021/jm7015864
71660856 164301 None 0 Human Functional pEC50 = 5.4 5.4 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 406 3 0 3 5.1 O=C([C@@H]1CCCN1Cc1cc(Cl)ccc1Cl)N1CCSc2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4210879 164301 None 0 Human Functional pEC50 = 5.4 5.4 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 406 3 0 3 5.1 O=C([C@@H]1CCCN1Cc1cc(Cl)ccc1Cl)N1CCSc2ccccc21 10.1021/acs.jmedchem.8b00308
46232487 202865 None 0 Human Functional pEC50 = 5.4 5.4 - 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 369 4 0 4 4.6 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(N(C)C)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL598120 202865 None 0 Human Functional pEC50 = 5.4 5.4 - 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 369 4 0 4 4.6 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(N(C)C)cc1 10.1016/j.bmcl.2010.01.003
749179 205001 None 12 Human Functional pEC50 = 5.4 5.4 - 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 326 3 0 3 4.6 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccccc1 10.1016/j.bmcl.2010.01.003
CHEMBL611676 205001 None 12 Human Functional pEC50 = 5.4 5.4 - 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 326 3 0 3 4.6 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccccc1 10.1016/j.bmcl.2010.01.003
90654585 110009 None 0 Human Functional pEC50 = 8.4 8.4 2 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 465 6 1 7 2.1 Cc1nc(N2CCC[C@@H](C(=O)NCCc3ccc(C#N)cc3)C2)nc(N2CCN(C)CC2)c1F 10.1021/jm401731q
CHEMBL3234566 110009 None 0 Human Functional pEC50 = 8.4 8.4 2 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 465 6 1 7 2.1 Cc1nc(N2CCC[C@@H](C(=O)NCCc3ccc(C#N)cc3)C2)nc(N2CCN(C)CC2)c1F 10.1021/jm401731q
90654566 110021 None 0 Human Functional pEC50 = 8.4 8.4 -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 473 6 1 7 2.1 CN1CCN(c2cc(N3CC[C@H]3C(=O)NCCc3ccc(C#N)cc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
CHEMBL3234577 110021 None 0 Human Functional pEC50 = 8.4 8.4 -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 473 6 1 7 2.1 CN1CCN(c2cc(N3CC[C@H]3C(=O)NCCc3ccc(C#N)cc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
90654564 110019 None 0 Mouse Functional pEC50 = 8.4 8.4 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 487 6 1 7 2.4 CN1CCN(c2cc(N3CCC[C@H]3C(=O)NCCc3ccc(C#N)cc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
CHEMBL3234575 110019 None 0 Mouse Functional pEC50 = 8.4 8.4 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 487 6 1 7 2.4 CN1CCN(c2cc(N3CCC[C@H]3C(=O)NCCc3ccc(C#N)cc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
90654568 110023 None 0 Mouse Functional pEC50 = 8.4 8.4 4 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 488 7 1 8 1.8 CCN1CCN(c2cc(N3CC[C@H]3C(=O)NCCc3ccc(C#N)nc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
CHEMBL3234579 110023 None 0 Mouse Functional pEC50 = 8.4 8.4 4 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 488 7 1 8 1.8 CCN1CCN(c2cc(N3CC[C@H]3C(=O)NCCc3ccc(C#N)nc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
90654594 110025 None 0 Mouse Functional pEC50 = 8.4 8.4 3 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 544 7 2 7 3.6 CC1(C(=O)O)CCN(c2cc(N3CCC[C@@H](C(=O)NCCc4ccc(C#N)cc4)C3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
CHEMBL3234581 110025 None 0 Mouse Functional pEC50 = 8.4 8.4 3 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 544 7 2 7 3.6 CC1(C(=O)O)CCN(c2cc(N3CCC[C@@H](C(=O)NCCc4ccc(C#N)cc4)C3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
145007569 195011 None 0 Mouse Functional pEC50 = 8.4 8.4 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(CC2CCCO2)C(=O)CC1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
CHEMBL5394911 195011 None 0 Mouse Functional pEC50 = 8.4 8.4 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(CC2CCCO2)C(=O)CC1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
118576999 159799 None 0 Mouse Functional pEC50 = 8.4 8.4 17 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 566 9 0 7 6.3 COc1ccc(N(C)c2cnc(SCc3c(F)cc(C#CCN(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4104359 159799 None 0 Mouse Functional pEC50 = 8.4 8.4 17 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 566 9 0 7 6.3 COc1ccc(N(C)c2cnc(SCc3c(F)cc(C#CCN(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
172464689 196790 None 0 Mouse Functional pEC50 = 8.4 8.4 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1073 25 3 12 6.5 CC1C(=O)N(CC(=O)NCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5432337 196790 None 0 Mouse Functional pEC50 = 8.4 8.4 1 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1073 25 3 12 6.5 CC1C(=O)N(CC(=O)NCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
162657867 181135 None 0 Human Functional pEC50 = 8.4 8.4 - 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 390 5 0 5 3.5 COc1ccc(N2CCN(C(=O)c3cncn3[C@H](C)c3ccccc3)CC2)cc1 10.1016/j.bmc.2020.115972
CHEMBL4759282 181135 None 0 Human Functional pEC50 = 8.4 8.4 - 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 390 5 0 5 3.5 COc1ccc(N2CCN(C(=O)c3cncn3[C@H](C)c3ccccc3)CC2)cc1 10.1016/j.bmc.2020.115972
172464689 196790 None 0 Human Functional pEC50 = 8.4 8.4 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1073 25 3 12 6.5 CC1C(=O)N(CC(=O)NCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5432337 196790 None 0 Human Functional pEC50 = 8.4 8.4 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1073 25 3 12 6.5 CC1C(=O)N(CC(=O)NCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
156705119 183220 None 0 Human Functional pEC50 = 8.3 8.3 29 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 499 7 0 8 5.0 COCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4794753 183220 None 0 Human Functional pEC50 = 8.3 8.3 29 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 499 7 0 8 5.0 COCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
71540075 87327 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 435 7 2 5 2.6 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(CC(F)(F)F)cc1)CC2 10.1021/ml300277t
CHEMBL2331650 87327 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 435 7 2 5 2.6 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(CC(F)(F)F)cc1)CC2 10.1021/ml300277t
118586284 156638 None 0 Mouse Functional pEC50 = 8.3 8.3 9 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 503 8 0 6 6.5 COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2F)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4068227 156638 None 0 Mouse Functional pEC50 = 8.3 8.3 9 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 503 8 0 6 6.5 COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2F)cc1OC 10.1021/acs.jmedchem.6b01873
172470699 197151 None 0 Human Functional pEC50 = 8.3 8.3 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1237 33 3 14 7.8 N[C@@H](CC(=O)N1CCCN(CC(=O)NCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)C(=O)C1Cc1ccccc1)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5439914 197151 None 0 Human Functional pEC50 = 8.3 8.3 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1237 33 3 14 7.8 N[C@@H](CC(=O)N1CCCN(CC(=O)NCCOCCOCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)C(=O)C1Cc1ccccc1)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
71626557 112259 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 422 4 0 5 5.1 O=C(c1cnccc1Oc1cccc2ncccc12)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
CHEMBL3290702 112259 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 422 4 0 5 5.1 O=C(c1cnccc1Oc1cccc2ncccc12)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
126700765 156596 None 0 Mouse Functional pEC50 = 7.4 7.4 8 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 499 9 0 6 6.2 COc1ccc(CN(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4067717 156596 None 0 Mouse Functional pEC50 = 7.4 7.4 8 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 499 9 0 6 6.2 COc1ccc(CN(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
101886309 114975 None 29 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at GP-BAR1 (unknown origin) in human HEK293 cells assessed as receptor transactivation at 100 nM to 50 uM incubated for 16 hrs by CRE-driven luciferase reporter gene assayAgonist activity at GP-BAR1 (unknown origin) in human HEK293 cells assessed as receptor transactivation at 100 nM to 50 uM incubated for 16 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 392 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)CCO)[C@@H]2[C@@H]1O 10.1021/jm501273r
CHEMBL3342086 114975 None 29 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at GP-BAR1 (unknown origin) in human HEK293 cells assessed as receptor transactivation at 100 nM to 50 uM incubated for 16 hrs by CRE-driven luciferase reporter gene assayAgonist activity at GP-BAR1 (unknown origin) in human HEK293 cells assessed as receptor transactivation at 100 nM to 50 uM incubated for 16 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 392 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)CCO)[C@@H]2[C@@H]1O 10.1021/jm501273r
118694489 195118 None 0 Human Functional pEC50 = 6.4 6.4 8 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 497 8 0 5 5.2 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC(F)(F)F)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5396998 195118 None 0 Human Functional pEC50 = 6.4 6.4 8 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 497 8 0 5 5.2 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC(F)(F)F)=C1C 10.1021/acs.jmedchem.2c01881
118694361 195650 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 409 6 0 3 5.1 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC1CC1 10.1021/acs.jmedchem.2c01881
CHEMBL5408025 195650 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 409 6 0 3 5.1 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC1CC1 10.1021/acs.jmedchem.2c01881
118694450 195753 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C(F)(F)F)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5410122 195753 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C(F)(F)F)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694501 196167 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(Cl)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5418039 196167 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(Cl)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694477 196545 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 463 7 0 4 5.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc3ccccc3c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5426387 196545 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 463 7 0 4 5.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc3ccccc3c2)=C1C 10.1021/acs.jmedchem.2c01881
118700248 194970 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5394284 194970 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694377 195524 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(OC)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5405338 195524 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(OC)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694501 196167 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(Cl)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5418039 196167 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(Cl)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694463 196483 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 471 8 0 6 4.1 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C(=O)OC)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5424851 196483 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 471 8 0 6 4.1 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C(=O)OC)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694393 196611 None 0 Mouse Functional pEC50 = 6.4 6.4 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C(F)(F)F)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5427795 196611 None 0 Mouse Functional pEC50 = 6.4 6.4 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C(F)(F)F)cc2)=C1C 10.1021/acs.jmedchem.2c01881
91668293 136468 None 11 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at TGR5 (unknown origin) assessed as cAMP levelAgonist activity at TGR5 (unknown origin) assessed as cAMP level
ChEMBL 576 9 4 3 7.1 C[C@H](CCC(=O)N[C@H](CC(=O)O)Cc1c[nH]c2ccccc12)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/j.ejmech.2015.08.048
CHEMBL3735125 136468 None 11 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at TGR5 (unknown origin) assessed as cAMP levelAgonist activity at TGR5 (unknown origin) assessed as cAMP level
ChEMBL 576 9 4 3 7.1 C[C@H](CCC(=O)N[C@H](CC(=O)O)Cc1c[nH]c2ccccc12)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/j.ejmech.2015.08.048
168679763 195111 None 2 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 444 4 4 4 3.7 C[C@H](CC(F)(F)C(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@]12C 10.1016/j.ejmech.2023.115851
CHEMBL5396857 195111 None 2 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 444 4 4 4 3.7 C[C@H](CC(F)(F)C(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@]12C 10.1016/j.ejmech.2023.115851
172450323 196081 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 448 6 4 4 4.3 C=CC[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@]12C)C(=O)O 10.1016/j.ejmech.2023.115851
CHEMBL5416586 196081 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 448 6 4 4 4.3 C=CC[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@]12C)C(=O)O 10.1016/j.ejmech.2023.115851
73353938 92759 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 512 5 1 3 6.1 O=S(=O)(NCc1c(-c2ccccc2F)ccnc1Cl)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435915 92759 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 512 5 1 3 6.1 O=S(=O)(NCc1c(-c2ccccc2F)ccnc1Cl)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
73353942 92778 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 515 6 0 3 7.0 O=C(c1ccncc1)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
CHEMBL2435939 92778 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 515 6 0 3 7.0 O=C(c1ccncc1)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
118709773 113625 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 446 4 1 6 5.4 CSc1ncc(C(=O)N2CCNc3ccccc32)c(Oc2cc(Cl)ccc2Cl)n1 10.1016/j.bmcl.2014.07.026
CHEMBL3321844 113625 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 446 4 1 6 5.4 CSc1ncc(C(=O)N2CCNc3ccccc32)c(Oc2cc(Cl)ccc2Cl)n1 10.1016/j.bmcl.2014.07.026
71626490 112258 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 421 4 0 4 5.7 O=C(c1cnccc1Oc1ccc2ccccc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
CHEMBL3290701 112258 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 421 4 0 4 5.7 O=C(c1cnccc1Oc1ccc2ccccc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
118576916 157727 None 0 Mouse Functional pEC50 = 7.4 7.4 7 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 477 8 0 6 6.7 COc1ccc(N(C)c2cnc(SCc3c(C)cccc3C)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4081298 157727 None 0 Mouse Functional pEC50 = 7.4 7.4 7 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 477 8 0 6 6.7 COc1ccc(N(C)c2cnc(SCc3c(C)cccc3C)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
221493 921 None 58 Human Functional pEC50 = 4.4 4.4 -1 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1016/j.ejmech.2023.115851
3096 921 None 58 Human Functional pEC50 = 4.4 4.4 -1 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1016/j.ejmech.2023.115851
609 921 None 58 Human Functional pEC50 = 4.4 4.4 -1 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1016/j.ejmech.2023.115851
CHEMBL205596 921 None 58 Human Functional pEC50 = 4.4 4.4 -1 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1016/j.ejmech.2023.115851
DB02659 921 None 58 Human Functional pEC50 = 4.4 4.4 -1 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 408 4 4 4 3.4 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2C[C@H](O)[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1016/j.ejmech.2023.115851
162656549 181060 None 0 Human Functional pEC50 = 4.4 4.4 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay
ChEMBL 436 5 4 4 4.1 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@@H]2[C@H]([C@@H]3CC[C@H]([C@H](C)CCC(=O)O)[C@@]3(C)C[C@H]2O)[C@@H]1O 10.1021/acs.jmedchem.6b01126
CHEMBL4758363 181060 None 0 Human Functional pEC50 = 4.4 4.4 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay
ChEMBL 436 5 4 4 4.1 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@@H]2[C@H]([C@@H]3CC[C@H]([C@H](C)CCC(=O)O)[C@@]3(C)C[C@H]2O)[C@@H]1O 10.1021/acs.jmedchem.6b01126
44627314 200202 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 510 4 2 2 8.4 C=C(C)C[C@]1(O)CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(=C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/jm900872z
CHEMBL571592 200202 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 510 4 2 2 8.4 C=C(C)C[C@]1(O)CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(=C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/jm900872z
145955411 162493 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay
ChEMBL 474 6 4 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)CCNC(=O)NC3CC3)[C@@H]2[C@@H]1O 10.1021/acsmedchemlett.7b00318
CHEMBL4165830 162493 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay
ChEMBL 474 6 4 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)CCNC(=O)NC3CC3)[C@@H]2[C@@H]1O 10.1021/acsmedchemlett.7b00318
137651232 157460 None 0 Human Functional pEC50 = 4.4 4.4 -20 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 570 10 1 9 6.1 COc1ccc(SCc2cnc(SCc3c(F)cc(-c4nn[nH]n4)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4077972 157460 None 0 Human Functional pEC50 = 4.4 4.4 -20 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 570 10 1 9 6.1 COc1ccc(SCc2cnc(SCc3c(F)cc(-c4nn[nH]n4)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
118694385 196820 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
CHEMBL5432845 196820 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
71540077 87329 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 418 7 2 6 2.0 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(C(C)(F)F)nc1)CC2 10.1021/ml300277t
CHEMBL2331652 87329 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 418 7 2 6 2.0 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(C(C)(F)F)nc1)CC2 10.1021/ml300277t
71540175 87332 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 434 6 1 5 2.9 NC(=O)c1nc(C2CC2)nc2c1CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1021/ml300277t
CHEMBL2331655 87332 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 434 6 1 5 2.9 NC(=O)c1nc(C2CC2)nc2c1CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1021/ml300277t
71626556 112264 None 0 Mouse Functional pEC50 = 7.4 7.4 -1 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 411 4 0 5 5.2 O=C(c1cnccc1Oc1ccc2ccoc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
CHEMBL3290707 112264 None 0 Mouse Functional pEC50 = 7.4 7.4 -1 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 411 4 0 5 5.2 O=C(c1cnccc1Oc1ccc2ccoc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
90654572 109996 None 0 Human Functional pEC50 = 5.4 5.4 -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 324 5 1 4 2.4 Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3ncccn3)C2)cc1 10.1021/jm401731q
CHEMBL3234553 109996 None 0 Human Functional pEC50 = 5.4 5.4 -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 324 5 1 4 2.4 Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3ncccn3)C2)cc1 10.1021/jm401731q
118586282 159649 None 0 Human Functional pEC50 = 5.4 5.4 -23 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 486 8 0 7 5.8 COc1ccc(N(C)c2nnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4102610 159649 None 0 Human Functional pEC50 = 5.4 5.4 -23 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 486 8 0 7 5.8 COc1ccc(N(C)c2nnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
118464815 159610 None 0 Human Functional pEC50 = 5.4 5.4 -6 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 528 6 0 4 7.9 COc1cc(C2(C)CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)ccc1F 10.1021/acsmedchemlett.7b00116
CHEMBL4102107 159610 None 0 Human Functional pEC50 = 5.4 5.4 -6 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 528 6 0 4 7.9 COc1cc(C2(C)CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)ccc1F 10.1021/acsmedchemlett.7b00116
44427763 97026 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 422 4 4 4 3.7 C[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](C[C@H](O)[C@@]21C)[C@@]1(C)CC[C@@H](O)CC1C[C@H]3O)C(=O)O 10.1021/jm070633p
CHEMBL266356 97026 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 422 4 4 4 3.7 C[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](C[C@H](O)[C@@]21C)[C@@]1(C)CC[C@@H](O)CC1C[C@H]3O)C(=O)O 10.1021/jm070633p
11069533 98095 None 27 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 406 4 2 4 4.6 COC(=O)CC[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
CHEMBL273086 98095 None 27 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 406 4 2 4 4.6 COC(=O)CC[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
118725000 117124 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 392 4 3 3 4.5 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@@]4(C)[C@H]3C[C@H](O)[C@@]21C 10.1021/jm7015864
CHEMBL3391714 117124 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 392 4 3 3 4.5 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@@]4(C)[C@H]3C[C@H](O)[C@@]21C 10.1021/jm7015864
156705112 182970 None 0 Mouse Functional pEC50 = 7.4 7.4 -15 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 483 6 0 7 5.4 CCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4791709 182970 None 0 Mouse Functional pEC50 = 7.4 7.4 -15 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 483 6 0 7 5.4 CCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
118577011 157078 None 0 Mouse Functional pEC50 = 7.4 7.4 20 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 489 7 0 5 7.0 COc1cc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)ccc1Cl 10.1021/acs.jmedchem.6b01873
CHEMBL4073081 157078 None 0 Mouse Functional pEC50 = 7.4 7.4 20 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 489 7 0 5 7.0 COc1cc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)ccc1Cl 10.1021/acs.jmedchem.6b01873
91972025 156049 None 0 Human Functional pEC50 = 6.4 6.4 -43 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 540 7 0 5 7.8 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4061329 156049 None 0 Human Functional pEC50 = 6.4 6.4 -43 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 540 7 0 5 7.8 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
21121407 156726 None 1 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 442 5 3 4 4.3 C[C@H](CCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
CHEMBL406923 156726 None 1 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 442 5 3 4 4.3 C[C@H](CCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
73352462 92686 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 486 6 1 4 5.9 COC(=O)C(NCc1cnccc1-c1ccccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435835 92686 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 486 6 1 4 5.9 COC(=O)C(NCc1cnccc1-c1ccccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
90654586 110010 None 0 Human Functional pEC50 = 6.4 6.4 -2 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 447 6 1 7 2.0 Cc1nc(N2CCN(C)CC2)cc(N2CCC[C@@H](C(=O)NCCc3ccc(C#N)cc3)C2)n1 10.1021/jm401731q
CHEMBL3234567 110010 None 0 Human Functional pEC50 = 6.4 6.4 -2 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 447 6 1 7 2.0 Cc1nc(N2CCN(C)CC2)cc(N2CCC[C@@H](C(=O)NCCc3ccc(C#N)cc3)C2)n1 10.1021/jm401731q
172463946 196532 None 0 Human Functional pEC50 = 4.4 4.4 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 438 5 4 5 3.1 CO[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@]12C)C(=O)O 10.1016/j.ejmech.2023.115851
CHEMBL5426065 196532 None 0 Human Functional pEC50 = 4.4 4.4 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 438 5 4 5 3.1 CO[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@]12C)C(=O)O 10.1016/j.ejmech.2023.115851
10635 98766 None 25 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 290 0 1 2 4.0 C[C@]12CC[C@H]3[C@@H](CC[C@H]4CC(=O)CC[C@@]43C)[C@@H]1CC[C@@H]2O 10.1021/jm7015864
CHEMBL27769 98766 None 25 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 290 0 1 2 4.0 C[C@]12CC[C@H]3[C@@H](CC[C@H]4CC(=O)CC[C@@]43C)[C@@H]1CC[C@@H]2O 10.1021/jm7015864
137661958 159618 None 0 Mouse Functional pEC50 = 4.4 4.4 - 1
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 562 10 1 7 5.6 COc1ccc(SCc2cnc([S+]([O-])Cc3c(F)cc(C(=O)O)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4102235 159618 None 0 Mouse Functional pEC50 = 4.4 4.4 - 1
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 562 10 1 7 5.6 COc1ccc(SCc2cnc([S+]([O-])Cc3c(F)cc(C(=O)O)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
164620529 185798 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 551 5 2 4 6.7 CNS(=O)(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
CHEMBL4865346 185798 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 551 5 2 4 6.7 CNS(=O)(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
17756586 196765 None 1 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 422 4 4 4 3.7 C[C@H](C[C@H](C)C(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@]12C 10.1016/j.ejmech.2023.115851
CHEMBL5431752 196765 None 1 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 422 4 4 4 3.7 C[C@H](C[C@H](C)C(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@]12C 10.1016/j.ejmech.2023.115851
71461053 83016 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 406 4 0 3 6.1 CN(C(=O)c1cnccc1Oc1cc(Cl)ccc1Cl)c1ccccc1Cl 10.1021/jm301071h
CHEMBL2181219 83016 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 406 4 0 3 6.1 CN(C(=O)c1cnccc1Oc1cc(Cl)ccc1Cl)c1ccccc1Cl 10.1021/jm301071h
164610027 184837 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 571 3 1 4 7.6 CC(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)N6CCOCC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
CHEMBL4850654 184837 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 571 3 1 4 7.6 CC(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)N6CCOCC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
44605617 200775 None 1 Human Functional pEC50 = 6.3 6.3 5 2
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 374 3 0 3 5.5 Cc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1Cl 10.1016/j.bmcl.2012.12.076
CHEMBL576138 200775 None 1 Human Functional pEC50 = 6.3 6.3 5 2
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 374 3 0 3 5.5 Cc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1Cl 10.1016/j.bmcl.2012.12.076
73357023 92761 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 428 5 1 2 6.2 Fc1ccccc1-c1ccncc1CNCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435919 92761 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 428 5 1 2 6.2 Fc1ccccc1-c1ccncc1CNCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
156014273 177323 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 435 3 2 3 6.1 C[C@H](CC#N)[C@H]1CC[C@H]2[C@@H]3C[C@@](O)(c4ccccc4)[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/acsmedchemlett.9b00636
CHEMBL4635505 177323 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 435 3 2 3 6.1 C[C@H](CC#N)[C@H]1CC[C@H]2[C@@H]3C[C@@](O)(c4ccccc4)[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/acsmedchemlett.9b00636
56602333 91641 None 0 Human Functional pEC50 = 6.3 6.3 11 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
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 Human Functional pEC50 = 6.3 6.3 11 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
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
118464806 159150 None 0 Mouse Functional pEC50 = 6.3 6.3 34 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 703 16 0 8 7.9 COc1cc(C2(C)CCCc3nc(SCc4c(F)cc(OCCOCCOCCN(C)C)cc4F)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4097059 159150 None 0 Mouse Functional pEC50 = 6.3 6.3 34 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 703 16 0 8 7.9 COc1cc(C2(C)CCCc3nc(SCc4c(F)cc(OCCOCCOCCN(C)C)cc4F)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
73350993 92769 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 495 7 0 3 7.4 CCCN(Cc1cnccc1-c1ccccc1F)C(C#N)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435929 92769 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 495 7 0 3 7.4 CCCN(Cc1cnccc1-c1ccccc1F)C(C#N)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
71561615 87670 None 0 Human Functional pEC50 = 5.3 5.3 - 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 444 4 0 5 5.6 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N1CCCC[C@H]1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336223 87670 None 0 Human Functional pEC50 = 5.3 5.3 - 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 444 4 0 5 5.6 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N1CCCC[C@H]1c1cccnc1 10.1016/j.bmcl.2012.12.076
71452075 83017 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 371 4 0 4 4.5 O=C(c1cnccc1Oc1ccccc1)N1CCN(C2CC2)c2ccccc21 10.1021/jm301071h
CHEMBL2181220 83017 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 371 4 0 4 4.5 O=C(c1cnccc1Oc1ccccc1)N1CCN(C2CC2)c2ccccc21 10.1021/jm301071h
46232736 203765 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 340 4 0 4 3.8 CCc1nnn(-c2ccccc2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1021/ml300277t
CHEMBL604131 203765 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 340 4 0 4 3.8 CCc1nnn(-c2ccccc2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1021/ml300277t
118586284 156638 None 0 Human Functional pEC50 = 7.3 7.3 -9 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 503 8 0 6 6.5 COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2F)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4068227 156638 None 0 Human Functional pEC50 = 7.3 7.3 -9 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 503 8 0 6 6.5 COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2F)cc1OC 10.1021/acs.jmedchem.6b01873
73355481 92779 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 504 6 0 3 7.2 O=C(c1ccco1)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
CHEMBL2435940 92779 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 504 6 0 3 7.2 O=C(c1ccco1)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
66740913 158747 None 0 Human Functional pEC50 = 6.3 6.3 -22 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 471 8 0 6 5.6 COc1ccc(Cc2nnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4092629 158747 None 0 Human Functional pEC50 = 6.3 6.3 -22 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 471 8 0 6 5.6 COc1ccc(Cc2nnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
118694337 196734 None 0 Mouse Functional pEC50 = 5.3 5.3 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 426 7 0 4 4.2 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CCN(C)C 10.1021/acs.jmedchem.2c01881
CHEMBL5431170 196734 None 0 Mouse Functional pEC50 = 5.3 5.3 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 426 7 0 4 4.2 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CCN(C)C 10.1021/acs.jmedchem.2c01881
122844 168041 None 47 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 454 2 1 2 7.3 C=C(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CCC(=O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/jm900872z
CHEMBL431525 168041 None 47 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 454 2 1 2 7.3 C=C(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CCC(=O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/jm900872z
192254 17114 None 25 Human Functional pEC50 = 4.3 4.3 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 378 3 3 3 4.1 C[C@H](CC(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
CHEMBL1254990 17114 None 25 Human Functional pEC50 = 4.3 4.3 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 378 3 3 3 4.1 C[C@H](CC(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
440071 97588 None 7 Human Functional pEC50 = 4.3 4.3 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 563 9 3 6 4.3 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](OS(=O)(=O)O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
CHEMBL270493 97588 None 7 Human Functional pEC50 = 4.3 4.3 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 563 9 3 6 4.3 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](OS(=O)(=O)O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
9910920 199594 None 1 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay
ChEMBL 436 5 4 4 4.1 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)O)[C@@H]2[C@@H]1O 10.1021/jm901390p
CHEMBL567835 199594 None 1 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay
ChEMBL 436 5 4 4 4.1 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)O)[C@@H]2[C@@H]1O 10.1021/jm901390p
53311618 83047 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 399 3 0 4 5.2 O=C(c1cncnc1Oc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 10.1016/j.bmcl.2014.07.026
CHEMBL2181251 83047 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 399 3 0 4 5.2 O=C(c1cncnc1Oc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 10.1016/j.bmcl.2014.07.026
71540074 87326 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 453 7 2 6 3.1 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(SC(F)(F)F)cc1)CC2 10.1021/ml300277t
CHEMBL2331649 87326 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 453 7 2 6 3.1 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(SC(F)(F)F)cc1)CC2 10.1021/ml300277t
90654591 110016 None 0 Mouse Functional pEC50 = 7.3 7.3 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 488 6 2 8 1.7 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3cc(N4CCNCC4)nc(C(F)(F)F)n3)C2)cn1 10.1021/jm401731q
CHEMBL3234572 110016 None 0 Mouse Functional pEC50 = 7.3 7.3 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 488 6 2 8 1.7 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3cc(N4CCNCC4)nc(C(F)(F)F)n3)C2)cn1 10.1021/jm401731q
172444413 195210 None 0 Human Functional pEC50 = 7.3 7.3 -14 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1409 44 3 19 6.2 CC1C(=O)N(CC(=O)N(CCOCCOCCOCCOCCOCCOCCOCCOCCN(CC(=O)O)C(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CC(=O)O)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5398966 195210 None 0 Human Functional pEC50 = 7.3 7.3 -14 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1409 44 3 19 6.2 CC1C(=O)N(CC(=O)N(CCOCCOCCOCCOCCOCCOCCOCCOCCN(CC(=O)O)C(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CC(=O)O)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
118464629 156346 None 0 Mouse Functional pEC50 = 5.3 5.3 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 526 7 0 5 7.6 COc1cc(C2CCCc3nc(SCc4c(F)cccc4OC)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4064931 156346 None 0 Mouse Functional pEC50 = 5.3 5.3 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 526 7 0 5 7.6 COc1cc(C2CCCc3nc(SCc4c(F)cccc4OC)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
11069533 98095 None 27 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 406 4 2 4 4.6 COC(=O)CC[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/acs.jmedchem.9b00770
CHEMBL273086 98095 None 27 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 406 4 2 4 4.6 COC(=O)CC[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/acs.jmedchem.9b00770
172439843 195047 None 0 Human Functional pEC50 = 4.3 4.3 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 548 6 2 5 6.8 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)Oc4cccc5ccccc45)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
CHEMBL5395512 195047 None 0 Human Functional pEC50 = 4.3 4.3 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 548 6 2 5 6.8 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)Oc4cccc5ccccc45)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
71457417 83015 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 401 5 0 4 5.6 CCN(C(=O)c1cncnc1Oc1cc(Cl)ccc1Cl)c1ccccc1C 10.1021/jm301071h
CHEMBL2181218 83015 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 401 5 0 4 5.6 CCN(C(=O)c1cncnc1Oc1cc(Cl)ccc1Cl)c1ccccc1C 10.1021/jm301071h
5283821 98010 None 20 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 392 4 3 3 4.5 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@@H]3C[C@@H](O)[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
CHEMBL272620 98010 None 20 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 392 4 3 3 4.5 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@@H]3C[C@@H](O)[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
90654579 110003 None 0 Mouse Functional pEC50 = 5.3 5.3 -5 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 357 5 1 3 3.6 Cc1ccnc(N2CCC[C@@H](C(=O)NCCc3ccc(Cl)cc3)C2)c1 10.1021/jm401731q
CHEMBL3234560 110003 None 0 Mouse Functional pEC50 = 5.3 5.3 -5 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 357 5 1 3 3.6 Cc1ccnc(N2CCC[C@@H](C(=O)NCCc3ccc(Cl)cc3)C2)c1 10.1021/jm401731q
53311781 83031 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 398 3 0 3 5.8 O=C(c1cnccc1Oc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 10.1021/jm301071h
CHEMBL2181233 83031 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 398 3 0 3 5.8 O=C(c1cnccc1Oc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 10.1021/jm301071h
71561756 87679 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 446 6 0 5 5.6 Cc1ccc(CN(C(=O)c2c(C)nn(C)c2Oc2cccc(Cl)c2Cl)C(C)C)cn1 10.1016/j.bmcl.2012.12.076
CHEMBL2336233 87679 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 446 6 0 5 5.6 Cc1ccc(CN(C(=O)c2c(C)nn(C)c2Oc2cccc(Cl)c2Cl)C(C)C)cn1 10.1016/j.bmcl.2012.12.076
155339365 181114 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 507 11 2 5 4.8 COCCOCCNC(=O)CC[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3OC 10.1039/d0md00425a
CHEMBL4759021 181114 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 507 11 2 5 4.8 COCCOCCNC(=O)CC[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3OC 10.1039/d0md00425a
118464755 158597 None 0 Mouse Functional pEC50 = 6.3 6.3 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 544 6 0 4 8.5 COc1cc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)c(C)c4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4091129 158597 None 0 Mouse Functional pEC50 = 6.3 6.3 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 544 6 0 4 8.5 COc1cc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)c(C)c4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
71561500 87667 None 0 Human Functional pEC50 = 5.3 5.3 - 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 406 5 0 6 4.3 COc1cccc(Oc2c(C(=O)N3CCCCC3c3cccnc3)c(C)nn2C)c1 10.1016/j.bmcl.2012.12.076
CHEMBL2336218 87667 None 0 Human Functional pEC50 = 5.3 5.3 - 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 406 5 0 6 4.3 COc1cccc(Oc2c(C(=O)N3CCCCC3c3cccnc3)c(C)nn2C)c1 10.1016/j.bmcl.2012.12.076
137660218 159324 None 0 Human Functional pEC50 = 5.3 5.3 -16 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 527 9 0 7 6.8 COc1ccc(SCc2cnc(SCc3c(F)cc(C#N)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4098862 159324 None 0 Human Functional pEC50 = 5.3 5.3 -16 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 527 9 0 7 6.8 COc1ccc(SCc2cnc(SCc3c(F)cc(C#N)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
6675 85161 None 30 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 515 7 5 6 2.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](C[C@H](O)[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
CHEMBL224867 85161 None 30 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 515 7 5 6 2.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](C[C@H](O)[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
164611776 186321 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 543 4 3 4 6.8 C[C@H](O)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
CHEMBL4873170 186321 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 543 4 3 4 6.8 C[C@H](O)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
118709777 113629 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 403 3 1 3 4.2 CN1CCN(C(=O)C2(C(=O)Nc3cc(Cl)ccc3Cl)CC2)c2ccccc21 10.1016/j.bmcl.2014.07.026
CHEMBL3321850 113629 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 403 3 1 3 4.2 CN1CCN(C(=O)C2(C(=O)Nc3cc(Cl)ccc3Cl)CC2)c2ccccc21 10.1016/j.bmcl.2014.07.026
118586278 159828 None 0 Mouse Functional pEC50 = 8.3 8.3 50 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 467 8 0 6 6.2 COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccccc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4104779 159828 None 0 Mouse Functional pEC50 = 8.3 8.3 50 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 467 8 0 6 6.2 COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccccc2)cc1OC 10.1021/acs.jmedchem.6b01873
90644453 112278 None 0 Human Functional pEC50 = 8.3 8.3 7 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 531 7 0 7 6.0 CCOC(=O)Cc1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
CHEMBL3290721 112278 None 0 Human Functional pEC50 = 8.3 8.3 7 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 531 7 0 7 6.0 CCOC(=O)Cc1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
71718878 87684 None 0 Human Functional pEC50 = 8.3 8.3 - 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 373 5 0 6 3.3 COc1cccc(-n2nnc(C3CC3)c2C(=O)N(C)c2ccc(C#N)cc2)c1 10.1016/j.bmcl.2012.12.076
CHEMBL2336238 87684 None 0 Human Functional pEC50 = 8.3 8.3 - 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 373 5 0 6 3.3 COc1cccc(-n2nnc(C3CC3)c2C(=O)N(C)c2ccc(C#N)cc2)c1 10.1016/j.bmcl.2012.12.076
71718878 87684 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 373 5 0 6 3.3 COc1cccc(-n2nnc(C3CC3)c2C(=O)N(C)c2ccc(C#N)cc2)c1 10.1039/C2MD20174G
CHEMBL2336238 87684 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 373 5 0 6 3.3 COc1cccc(-n2nnc(C3CC3)c2C(=O)N(C)c2ccc(C#N)cc2)c1 10.1039/C2MD20174G
71626488 112270 None 0 Mouse Functional pEC50 = 8.3 8.3 -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 426 4 0 6 5.0 Cc1noc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
CHEMBL3290713 112270 None 0 Mouse Functional pEC50 = 8.3 8.3 -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 426 4 0 6 5.0 Cc1noc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
155339372 173173 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 444 5 1 5 5.6 CO[C@@H]1C[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)CCc3nnc(C)o3)[C@@H]21 10.1021/acs.jmedchem.9b00770
CHEMBL4519596 173173 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 444 5 1 5 5.6 CO[C@@H]1C[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)CCc3nnc(C)o3)[C@@H]21 10.1021/acs.jmedchem.9b00770
118464803 155874 None 0 Mouse Functional pEC50 = 7.3 7.3 15 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 525 7 0 6 6.6 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cncc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4059508 155874 None 0 Mouse Functional pEC50 = 7.3 7.3 15 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 525 7 0 6 6.6 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cncc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
118694598 197051 None 0 Mouse Functional pEC50 = 7.3 7.3 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 457 7 0 6 3.9 COC(=O)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5437561 197051 None 0 Mouse Functional pEC50 = 7.3 7.3 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 457 7 0 6 3.9 COC(=O)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
71661185 163905 None 0 Human Functional pEC50 = 7.3 7.3 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 447 4 0 3 4.9 O=C([C@@H]1C[C@H](F)CN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4206153 163905 None 0 Human Functional pEC50 = 7.3 7.3 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 447 4 0 3 4.9 O=C([C@@H]1C[C@H](F)CN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118093562 163982 None 0 Human Functional pEC50 = 7.3 7.3 -5 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 547 9 1 5 5.7 O=C(O)CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4207005 163982 None 0 Human Functional pEC50 = 7.3 7.3 -5 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 547 9 1 5 5.7 O=C(O)CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
71661185 163905 None 0 Mouse Functional pEC50 = 7.3 7.3 -1 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 447 4 0 3 4.9 O=C([C@@H]1C[C@H](F)CN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4206153 163905 None 0 Mouse Functional pEC50 = 7.3 7.3 -1 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 447 4 0 3 4.9 O=C([C@@H]1C[C@H](F)CN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118694598 197051 None 0 Mouse Functional pEC50 = 7.3 7.3 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 457 7 0 6 3.9 COC(=O)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5437561 197051 None 0 Mouse Functional pEC50 = 7.3 7.3 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 457 7 0 6 3.9 COC(=O)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
14650340 67205 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 307 7 0 3 5.0 CCCCOc1cccc(OCc2ccc3ccccc3n2)c1 10.1021/acs.jmedchem.1c01078
CHEMBL18775 67205 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 307 7 0 3 5.0 CCCCOc1cccc(OCc2ccc3ccccc3n2)c1 10.1021/acs.jmedchem.1c01078
136167006 91650 None 0 Human Functional pEC50 = 6.3 6.3 6 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
ChEMBL 408 5 1 3 5.9 Cc1cc(/C(CC(c2ccc(Br)cc2)c2ccccc2C)=N/O)ccn1 10.1016/j.bmcl.2013.06.017
CHEMBL2407950 91650 None 0 Human Functional pEC50 = 6.3 6.3 6 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
ChEMBL 408 5 1 3 5.9 Cc1cc(/C(CC(c2ccc(Br)cc2)c2ccccc2C)=N/O)ccn1 10.1016/j.bmcl.2013.06.017
73349428 92783 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 522 6 0 3 7.4 O=C(c1ccco1)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1F 10.1016/j.ejmech.2013.07.050
CHEMBL2435944 92783 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 522 6 0 3 7.4 O=C(c1ccco1)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1F 10.1016/j.ejmech.2013.07.050
118694374 194957 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 413 7 0 4 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5394113 194957 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 413 7 0 4 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694542 195285 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 489 8 0 4 6.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(-c3ccccc3)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5400104 195285 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 489 8 0 4 6.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(-c3ccccc3)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694455 196971 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 411 6 0 3 5.3 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC(C)C 10.1021/acs.jmedchem.2c01881
CHEMBL5435789 196971 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 411 6 0 3 5.3 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC(C)C 10.1021/acs.jmedchem.2c01881
118694370 197118 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 411 7 0 3 5.5 CCCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5439183 197118 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 411 7 0 3 5.5 CCCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694544 195184 None 0 Mouse Functional pEC50 = 6.3 6.3 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(F)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5398341 195184 None 0 Mouse Functional pEC50 = 6.3 6.3 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(F)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118700250 197183 None 0 Mouse Functional pEC50 = 6.3 6.3 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2C)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5440622 197183 None 0 Mouse Functional pEC50 = 6.3 6.3 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2C)=C1C 10.1021/acs.jmedchem.2c01881
12113821 199882 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 511 3 1 4 7.6 C=C(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC/C(=N\OC(C)=O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/jm900872z
CHEMBL569634 199882 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 511 3 1 4 7.6 C=C(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC/C(=N\OC(C)=O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/jm900872z
611 2327 None 52 Human Functional pEC50 = 5.3 5.3 50 2
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
ChEMBL 376 4 2 2 5.5 O[C@@H]1CC[C@]2([C@@H](C1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)C 10.1021/ml200256d
9903 2327 None 52 Human Functional pEC50 = 5.3 5.3 50 2
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
ChEMBL 376 4 2 2 5.5 O[C@@H]1CC[C@]2([C@@H](C1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)C 10.1021/ml200256d
CHEMBL1478 2327 None 52 Human Functional pEC50 = 5.3 5.3 50 2
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
ChEMBL 376 4 2 2 5.5 O[C@@H]1CC[C@]2([C@@H](C1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)C 10.1021/ml200256d
169450673 197107 None 3 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 464 7 4 4 5.0 CCCC[C@@]1(O)C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)O)CC[C@H]3[C@@H]21 10.1016/j.ejmech.2023.115851
CHEMBL5438844 197107 None 3 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 464 7 4 4 5.0 CCCC[C@@]1(O)C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)O)CC[C@H]3[C@@H]21 10.1016/j.ejmech.2023.115851
9910920 199594 None 1 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay
ChEMBL 436 5 4 4 4.1 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)O)[C@@H]2[C@@H]1O 10.1021/acs.jmedchem.6b01126
CHEMBL567835 199594 None 1 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay
ChEMBL 436 5 4 4 4.1 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)O)[C@@H]2[C@@H]1O 10.1021/acs.jmedchem.6b01126
172441617 197362 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assayAgonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assay
ChEMBL 470 6 2 5 4.7 CC[C@H]1[C@@H](O)[C@@H]2[C@H](CC[C@]3(C)[C@@H]([C@H](C)CCOS(=O)(=O)O)CC[C@@H]23)[C@@]2(C)CCC(=O)C[C@@H]12 10.1016/j.ejmech.2022.114652
CHEMBL5399923 197362 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assayAgonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assay
ChEMBL 470 6 2 5 4.7 CC[C@H]1[C@@H](O)[C@@H]2[C@H](CC[C@]3(C)[C@@H]([C@H](C)CCOS(=O)(=O)O)CC[C@@H]23)[C@@]2(C)CCC(=O)C[C@@H]12 10.1016/j.ejmech.2022.114652
CHEMBL5498670 197362 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assayAgonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assay
ChEMBL 470 6 2 5 4.7 CC[C@H]1[C@@H](O)[C@@H]2[C@H](CC[C@]3(C)[C@@H]([C@H](C)CCOS(=O)(=O)O)CC[C@@H]23)[C@@]2(C)CCC(=O)C[C@@H]12 10.1016/j.ejmech.2022.114652
71626228 118892 None 0 Human Functional pEC50 = 5.3 5.3 1 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 610 10 0 7 5.8 CCOC(=O)CN(C)C(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421898 118892 None 0 Human Functional pEC50 = 5.3 5.3 1 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 610 10 0 7 5.8 CCOC(=O)CN(C)C(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
44605617 200775 None 1 Human Functional pEC50 = 6.3 6.3 5 2
Agonist activity at TGR5 expressed in human U2-OS cells assessed as increase in MRE/CRE-driven gene expression by luciferase reporter gene assayAgonist activity at TGR5 expressed in human U2-OS cells assessed as increase in MRE/CRE-driven gene expression by luciferase reporter gene assay
ChEMBL 374 3 0 3 5.5 Cc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1Cl 10.1021/jm901434t
CHEMBL576138 200775 None 1 Human Functional pEC50 = 6.3 6.3 5 2
Agonist activity at TGR5 expressed in human U2-OS cells assessed as increase in MRE/CRE-driven gene expression by luciferase reporter gene assayAgonist activity at TGR5 expressed in human U2-OS cells assessed as increase in MRE/CRE-driven gene expression by luciferase reporter gene assay
ChEMBL 374 3 0 3 5.5 Cc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1Cl 10.1021/jm901434t
118103736 164331 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 453 5 0 4 5.1 O=C([C@@H]1CSCN1Cc1cc(C2CC2)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4211208 164331 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 453 5 0 4 5.1 O=C([C@@H]1CSCN1Cc1cc(C2CC2)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118694374 194957 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 413 7 0 4 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5394113 194957 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 413 7 0 4 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694542 195285 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 489 8 0 4 6.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(-c3ccccc3)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5400104 195285 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 489 8 0 4 6.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(-c3ccccc3)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694455 196971 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 411 6 0 3 5.3 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC(C)C 10.1021/acs.jmedchem.2c01881
CHEMBL5435789 196971 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 411 6 0 3 5.3 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC(C)C 10.1021/acs.jmedchem.2c01881
118694370 197118 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 411 7 0 3 5.5 CCCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5439183 197118 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 411 7 0 3 5.5 CCCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
46232531 201906 None 0 Human Functional pEC50 = 6.3 6.3 - 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 344 3 0 3 4.7 Cc1onc(-c2ccc(F)cc2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL591455 201906 None 0 Human Functional pEC50 = 6.3 6.3 - 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 344 3 0 3 4.7 Cc1onc(-c2ccc(F)cc2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
46232985 203346 None 0 Human Functional pEC50 = 6.3 6.3 - 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 344 3 0 3 4.7 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(F)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL601449 203346 None 0 Human Functional pEC50 = 6.3 6.3 - 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 344 3 0 3 4.7 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(F)cc1 10.1016/j.bmcl.2010.01.003
118694544 195184 None 0 Mouse Functional pEC50 = 6.3 6.3 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(F)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5398341 195184 None 0 Mouse Functional pEC50 = 6.3 6.3 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(F)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694542 195285 None 0 Mouse Functional pEC50 = 6.3 6.3 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 489 8 0 4 6.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(-c3ccccc3)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5400104 195285 None 0 Mouse Functional pEC50 = 6.3 6.3 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 489 8 0 4 6.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(-c3ccccc3)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118700250 197183 None 0 Mouse Functional pEC50 = 6.3 6.3 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2C)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5440622 197183 None 0 Mouse Functional pEC50 = 6.3 6.3 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 427 7 0 4 4.6 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2C)=C1C 10.1021/acs.jmedchem.2c01881
44605615 201228 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at TGR5 expressed in human U2-OS cells assessed as increase in MRE/CRE-driven gene expression by luciferase reporter gene assayAgonist activity at TGR5 expressed in human U2-OS cells assessed as increase in MRE/CRE-driven gene expression by luciferase reporter gene assay
ChEMBL 374 4 0 3 5.6 CCN(C(=O)c1c(-c2ccccc2Cl)noc1C)c1cccc(Cl)c1 10.1021/jm901434t
CHEMBL583110 201228 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at TGR5 expressed in human U2-OS cells assessed as increase in MRE/CRE-driven gene expression by luciferase reporter gene assayAgonist activity at TGR5 expressed in human U2-OS cells assessed as increase in MRE/CRE-driven gene expression by luciferase reporter gene assay
ChEMBL 374 4 0 3 5.6 CCN(C(=O)c1c(-c2ccccc2Cl)noc1C)c1cccc(Cl)c1 10.1021/jm901434t
44605615 201228 None 0 Human Functional pEC50 = 5.3 5.3 - 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 374 4 0 3 5.6 CCN(C(=O)c1c(-c2ccccc2Cl)noc1C)c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.003
CHEMBL583110 201228 None 0 Human Functional pEC50 = 5.3 5.3 - 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 374 4 0 3 5.6 CCN(C(=O)c1c(-c2ccccc2Cl)noc1C)c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.003
46232594 203521 None 0 Human Functional pEC50 = 5.3 5.3 - 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 COc1ccc(-c2noc(C)c2C(=O)N(C)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL602690 203521 None 0 Human Functional pEC50 = 5.3 5.3 - 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 COc1ccc(-c2noc(C)c2C(=O)N(C)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2010.01.003
71660856 164301 None 0 Mouse Functional pEC50 = 5.3 5.3 -1 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 406 3 0 3 5.1 O=C([C@@H]1CCCN1Cc1cc(Cl)ccc1Cl)N1CCSc2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4210879 164301 None 0 Mouse Functional pEC50 = 5.3 5.3 -1 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 406 3 0 3 5.1 O=C([C@@H]1CCCN1Cc1cc(Cl)ccc1Cl)N1CCSc2ccccc21 10.1021/acs.jmedchem.8b00308
118694337 196734 None 0 Mouse Functional pEC50 = 5.3 5.3 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 426 7 0 4 4.2 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CCN(C)C 10.1021/acs.jmedchem.2c01881
CHEMBL5431170 196734 None 0 Mouse Functional pEC50 = 5.3 5.3 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 426 7 0 4 4.2 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CCN(C)C 10.1021/acs.jmedchem.2c01881
10479586 106252 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 442 5 3 4 4.3 C[C@H](CCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
CHEMBL3138525 106252 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 442 5 3 4 4.3 C[C@H](CCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
9848818 97953 None 43 Human Functional pEC50 = 4.3 4.3 - 1
Agonist activity at wild type human TGR5 expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assayAgonist activity at wild type human TGR5 expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assay
ChEMBL 499 7 4 5 3.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/j.ejmech.2015.09.024
CHEMBL272427 97953 None 43 Human Functional pEC50 = 4.3 4.3 - 1
Agonist activity at wild type human TGR5 expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assayAgonist activity at wild type human TGR5 expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assay
ChEMBL 499 7 4 5 3.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3[C@@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1016/j.ejmech.2015.09.024
118586280 158379 None 0 Mouse Functional pEC50 = 6.3 6.3 1 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 493 6 0 4 7.7 CN(c1ccc(Cl)c(Cl)c1)c1cnc(SCc2c(F)cccc2F)n1-c1ccc(F)cc1 10.1021/acs.jmedchem.6b01873
CHEMBL4088938 158379 None 0 Mouse Functional pEC50 = 6.3 6.3 1 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 493 6 0 4 7.7 CN(c1ccc(Cl)c(Cl)c1)c1cnc(SCc2c(F)cccc2F)n1-c1ccc(F)cc1 10.1021/acs.jmedchem.6b01873
71691935 173352 None 5 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 461 4 3 4 4.0 C[C@H](CCC(=O)N1CCCC1)[C@H]1CC[C@H]2[C@H]3[C@H](C[C@H](O)[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/acs.jmedchem.9b00770
CHEMBL4524597 173352 None 5 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 461 4 3 4 4.0 C[C@H](CCC(=O)N1CCCC1)[C@H]1CC[C@H]2[C@H]3[C@H](C[C@H](O)[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/acs.jmedchem.9b00770
118464701 158282 None 0 Mouse Functional pEC50 = 6.3 6.3 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 548 6 0 4 8.4 COc1cc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)c(F)c4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4087791 158282 None 0 Mouse Functional pEC50 = 6.3 6.3 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 548 6 0 4 8.4 COc1cc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)c(F)c4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
73357024 92766 None 0 Human Functional pEC50 = 7.3 7.3 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 471 5 1 3 6.4 N#CC(NCc1cnccc1-c1c(F)cccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435926 92766 None 0 Human Functional pEC50 = 7.3 7.3 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 471 5 1 3 6.4 N#CC(NCc1cnccc1-c1c(F)cccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
71626697 112268 None 0 Mouse Functional pEC50 = 7.3 7.3 -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 427 4 0 5 5.7 O=C(c1cnccc1Oc1ccc2sccc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
CHEMBL3290711 112268 None 0 Mouse Functional pEC50 = 7.3 7.3 -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 427 4 0 5 5.7 O=C(c1cnccc1Oc1ccc2sccc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
137645502 157750 None 0 Mouse Functional pEC50 = 6.3 6.3 1 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 490 7 0 7 5.8 COc1ccc(C2(C)CCCc3nc(SCc4ncccn4)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4081476 157750 None 0 Mouse Functional pEC50 = 6.3 6.3 1 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 490 7 0 7 5.8 COc1ccc(C2(C)CCCc3nc(SCc4ncccn4)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
145973129 163126 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay
ChEMBL 459 5 3 5 5.6 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)CCc3cc(O)no3)[C@@H]2[C@@H]1O 10.1021/acsmedchemlett.7b00318
CHEMBL4175888 163126 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay
ChEMBL 459 5 3 5 5.6 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)CCc3cc(O)no3)[C@@H]2[C@@H]1O 10.1021/acsmedchemlett.7b00318
90644450 112286 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 616 9 1 9 4.6 CCOC(=O)CNC(=O)Cc1coc2cc(Cl)c(C(=O)Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
CHEMBL3290729 112286 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 616 9 1 9 4.6 CCOC(=O)CNC(=O)Cc1coc2cc(Cl)c(C(=O)Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
172471327 197573 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human TGR5 expressed in HEK293 cells incubated for 30 mins by SEAP reporter gene based assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 30 mins by SEAP reporter gene based assay
ChEMBL 527 8 4 5 3.9 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@H]([C@H](C)CCC(=O)NCCS(=O)(=O)O)[C@H]3[C@H](C)C[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1016/j.ejmech.2023.115143
CHEMBL5440876 197573 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human TGR5 expressed in HEK293 cells incubated for 30 mins by SEAP reporter gene based assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 30 mins by SEAP reporter gene based assay
ChEMBL 527 8 4 5 3.9 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@H]([C@H](C)CCC(=O)NCCS(=O)(=O)O)[C@H]3[C@H](C)C[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1016/j.ejmech.2023.115143
CHEMBL5500230 197573 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human TGR5 expressed in HEK293 cells incubated for 30 mins by SEAP reporter gene based assayAgonist activity at human TGR5 expressed in HEK293 cells incubated for 30 mins by SEAP reporter gene based assay
ChEMBL 527 8 4 5 3.9 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@H]([C@H](C)CCC(=O)NCCS(=O)(=O)O)[C@H]3[C@H](C)C[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1016/j.ejmech.2023.115143
73353937 92758 None 0 Human Functional pEC50 = 7.3 7.3 20 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 588 6 0 5 7.0 O=C(c1ccsc1)N(Cc1cnccc1-c1ccccc1F)S(=O)(=O)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435914 92758 None 0 Human Functional pEC50 = 7.3 7.3 20 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 588 6 0 5 7.0 O=C(c1ccsc1)N(Cc1cnccc1-c1ccccc1F)S(=O)(=O)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
46232736 203765 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 340 4 0 4 3.8 CCc1nnn(-c2ccccc2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1039/C2MD20174G
CHEMBL604131 203765 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 340 4 0 4 3.8 CCc1nnn(-c2ccccc2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1039/C2MD20174G
71626905 118890 None 0 Human Functional pEC50 = 5.3 5.3 1 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 596 10 1 7 5.4 CCOC(=O)CNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421896 118890 None 0 Human Functional pEC50 = 5.3 5.3 1 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 596 10 1 7 5.4 CCOC(=O)CNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
172470476 197129 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 434 5 1 5 4.4 COC(=O)CC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](OC)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC(=O)[C@]12C 10.1016/j.bmc.2023.117418
CHEMBL5439396 197129 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 434 5 1 5 4.4 COC(=O)CC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](OC)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC(=O)[C@]12C 10.1016/j.bmc.2023.117418
71461056 83040 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 387 4 0 4 5.2 Cc1ccccc1N(C)C(=O)c1cncnc1Oc1cc(Cl)ccc1Cl 10.1021/jm301071h
CHEMBL2181242 83040 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 387 4 0 4 5.2 Cc1ccccc1N(C)C(=O)c1cncnc1Oc1cc(Cl)ccc1Cl 10.1021/jm301071h
130361940 159401 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 447 7 3 3 5.3 CCCCNC(=O)CC[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/acs.jmedchem.9b00770
CHEMBL4099757 159401 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 447 7 3 3 5.3 CCCCNC(=O)CC[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/acs.jmedchem.9b00770
115245 95870 None 33 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 433 6 3 3 4.6 C[C@H](CCC(=O)NCC(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
CHEMBL258818 95870 None 33 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 433 6 3 3 4.6 C[C@H](CCC(=O)NCC(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
71453904 83045 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 3 0 4 5.2 O=C(c1nccnc1Oc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 10.1021/jm301071h
CHEMBL2181248 83045 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 3 0 4 5.2 O=C(c1nccnc1Oc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 10.1021/jm301071h
71561368 87662 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 444 4 0 5 5.6 Cc1nn(C)c(Oc2ccc(Cl)cc2Cl)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336213 87662 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 444 4 0 5 5.6 Cc1nn(C)c(Oc2ccc(Cl)cc2Cl)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
137656815 159832 None 0 Mouse Functional pEC50 = 6.3 6.3 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 514 6 0 4 7.7 COc1cc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)ccc1F 10.1021/acsmedchemlett.7b00116
CHEMBL4104842 159832 None 0 Mouse Functional pEC50 = 6.3 6.3 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 514 6 0 4 7.7 COc1cc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)ccc1F 10.1021/acsmedchemlett.7b00116
73352467 92768 None 0 Mouse Functional pEC50 = 6.3 6.3 -8 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 496 5 1 3 5.5 O=S(=O)(NCc1cnccc1-c1c(F)cccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435928 92768 None 0 Mouse Functional pEC50 = 6.3 6.3 -8 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 496 5 1 3 5.5 O=S(=O)(NCc1cnccc1-c1c(F)cccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
172451872 196068 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 496 6 1 5 5.8 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC(=O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)Oc4ccccc4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
CHEMBL5416364 196068 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 496 6 1 5 5.8 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC(=O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)Oc4ccccc4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
54586161 61187 None 0 Human Functional pEC50 = 4.3 4.3 - 1
Agonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assayAgonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assay
ChEMBL 551 8 3 4 7.1 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)CCNC(=O)OC/C=C/c3ccccc3)[C@@H]2[C@@H]1O 10.1016/j.bmc.2011.03.004
CHEMBL1765565 61187 None 0 Human Functional pEC50 = 4.3 4.3 - 1
Agonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assayAgonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assay
ChEMBL 551 8 3 4 7.1 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)CCNC(=O)OC/C=C/c3ccccc3)[C@@H]2[C@@H]1O 10.1016/j.bmc.2011.03.004
45483949 3582 None 33 Human Functional pEC50 = 5.3 5.3 -2 2
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1021/ml300277t
7048 3582 None 33 Human Functional pEC50 = 5.3 5.3 -2 2
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1021/ml300277t
CHEMBL567640 3582 None 33 Human Functional pEC50 = 5.3 5.3 -2 2
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1021/ml300277t
118464805 157890 None 0 Mouse Functional pEC50 = 6.3 6.3 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 544 6 0 4 8.4 COc1cc(C2(C)CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4083189 157890 None 0 Mouse Functional pEC50 = 6.3 6.3 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 544 6 0 4 8.4 COc1cc(C2(C)CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
611 2327 None 52 Human Functional pEC50 = 5.3 5.3 50 2
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 376 4 2 2 5.5 O[C@@H]1CC[C@]2([C@@H](C1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)C 10.1021/jm900872z
9903 2327 None 52 Human Functional pEC50 = 5.3 5.3 50 2
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 376 4 2 2 5.5 O[C@@H]1CC[C@]2([C@@H](C1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)C 10.1021/jm900872z
CHEMBL1478 2327 None 52 Human Functional pEC50 = 5.3 5.3 50 2
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 376 4 2 2 5.5 O[C@@H]1CC[C@]2([C@@H](C1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)C 10.1021/jm900872z
172467969 197003 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 420 4 4 4 3.6 C=C(C[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@]12C)C(=O)O 10.1016/j.ejmech.2023.115851
CHEMBL5436516 197003 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 420 4 4 4 3.6 C=C(C[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](O)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@]12C)C(=O)O 10.1016/j.ejmech.2023.115851
156705115 182225 None 0 Mouse Functional pEC50 = 6.3 6.3 -3 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 527 7 0 9 4.9 CC(=O)OCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4782069 182225 None 0 Mouse Functional pEC50 = 6.3 6.3 -3 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 527 7 0 9 4.9 CC(=O)OCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
71541719 87323 None 1 Mouse Functional pEC50 = 5.3 5.3 -281 3
Agonist activity at mouse TGR5 expressed in deoxycycline-induced CHO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at mouse TGR5 expressed in deoxycycline-induced CHO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 395 7 2 5 2.6 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(C(C)C)cc1)CC2 10.1021/ml300277t
CHEMBL2331646 87323 None 1 Mouse Functional pEC50 = 5.3 5.3 -281 3
Agonist activity at mouse TGR5 expressed in deoxycycline-induced CHO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at mouse TGR5 expressed in deoxycycline-induced CHO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 395 7 2 5 2.6 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(C(C)C)cc1)CC2 10.1021/ml300277t
130361815 170581 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 447 8 1 5 4.2 C[C@H](CCC(N)=O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](OC=O)C[C@H]1C[C@H]3OC=O 10.1021/acs.jmedchem.9b00770
CHEMBL4449000 170581 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 447 8 1 5 4.2 C[C@H](CCC(N)=O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](OC=O)C[C@H]1C[C@H]3OC=O 10.1021/acs.jmedchem.9b00770
162671787 182948 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 876 23 13 15 -2.2 CO[C@@H]1C[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)N(CCCNC(=O)[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)CCCNC(=O)[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)[C@@H]21 10.1039/d0md00425a
CHEMBL4791399 182948 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 876 23 13 15 -2.2 CO[C@@H]1C[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)N(CCCNC(=O)[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)CCCNC(=O)[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)[C@@H]21 10.1039/d0md00425a
155669591 182802 None 0 Human Functional pEC50 = 6.3 6.3 - 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 376 4 0 4 3.7 O=C(c1cncn1Cc1ccc(F)cc1)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
CHEMBL4789395 182802 None 0 Human Functional pEC50 = 6.3 6.3 - 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 376 4 0 4 3.7 O=C(c1cncn1Cc1ccc(F)cc1)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
137646061 157907 None 0 Mouse Functional pEC50 = 5.3 5.3 3 2
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 502 9 0 6 6.7 COc1ccc(OCc2cnc(SCc3c(F)cccc3Cl)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4083324 157907 None 0 Mouse Functional pEC50 = 5.3 5.3 3 2
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 502 9 0 6 6.7 COc1ccc(OCc2cnc(SCc3c(F)cccc3Cl)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
137634612 156206 None 0 Human Functional pEC50 = 5.3 5.3 -35 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 518 9 0 6 7.4 COc1ccc(SCc2cnc(SCc3c(F)cccc3Cl)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4063237 156206 None 0 Human Functional pEC50 = 5.3 5.3 -35 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 518 9 0 6 7.4 COc1ccc(SCc2cnc(SCc3c(F)cccc3Cl)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
156018264 177896 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 373 2 2 3 4.9 C[C@H](CC#N)[C@H]1CC[C@H]2[C@@H]3C[C@@](C)(O)[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/acsmedchemlett.9b00636
CHEMBL4643368 177896 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 373 2 2 3 4.9 C[C@H](CC#N)[C@H]1CC[C@H]2[C@@H]3C[C@@](C)(O)[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/acsmedchemlett.9b00636
5306292 196577 None 8 Human Functional pEC50 = 5.2 5.2 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 293 2 0 3 2.7 COC(=O)C1=C(C)N(C)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5427123 196577 None 8 Human Functional pEC50 = 5.2 5.2 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 293 2 0 3 2.7 COC(=O)C1=C(C)N(C)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
118694580 196916 None 0 Human Functional pEC50 = 5.2 5.2 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 341 4 1 3 3.6 O=C1CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=CN1 10.1021/acs.jmedchem.2c01881
CHEMBL5434777 196916 None 0 Human Functional pEC50 = 5.2 5.2 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 341 4 1 3 3.6 O=C1CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=CN1 10.1021/acs.jmedchem.2c01881
71626905 118890 None 0 Mouse Functional pEC50 = 5.2 5.2 -1 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 596 10 1 7 5.4 CCOC(=O)CNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421896 118890 None 0 Mouse Functional pEC50 = 5.2 5.2 -1 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 596 10 1 7 5.4 CCOC(=O)CNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
118694469 194962 None 0 Mouse Functional pEC50 = 6.2 6.2 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
CHEMBL5394197 194962 None 0 Mouse Functional pEC50 = 6.2 6.2 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
71720725 87685 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 428 4 0 5 5.1 Cc1nn(C)c(Oc2cccc(Cl)c2F)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336239 87685 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 428 4 0 5 5.1 Cc1nn(C)c(Oc2cccc(Cl)c2F)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
136167037 91654 None 0 Human Functional pEC50 = 6.2 6.2 -1 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
ChEMBL 450 7 2 4 6.5 Cc1cc(/C(CC(c2ccc(-c3ccc(C(=O)O)cc3)cc2)c2ccccc2C)=N/O)ccn1 10.1016/j.bmcl.2013.06.017
CHEMBL2407954 91654 None 0 Human Functional pEC50 = 6.2 6.2 -1 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
ChEMBL 450 7 2 4 6.5 Cc1cc(/C(CC(c2ccc(-c3ccc(C(=O)O)cc3)cc2)c2ccccc2C)=N/O)ccn1 10.1016/j.bmcl.2013.06.017
90284086 117741 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 418 5 2 2 6.4 CC[C@H]1C[C@@H]2[C@H](CC[C@@]3(C)[C@H]2CC[C@@H]3[C@H](C)C[C@H](C)C(=O)O)[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1016/j.bmc.2015.01.048
CHEMBL3401354 117741 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 418 5 2 2 6.4 CC[C@H]1C[C@@H]2[C@H](CC[C@@]3(C)[C@H]2CC[C@@H]3[C@H](C)C[C@H](C)C(=O)O)[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1016/j.bmc.2015.01.048
611 2327 None 52 Human Functional pEC50 = 6.2 6.2 50 2
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 376 4 2 2 5.5 O[C@@H]1CC[C@]2([C@@H](C1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)C 10.1021/jm7015864
9903 2327 None 52 Human Functional pEC50 = 6.2 6.2 50 2
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 376 4 2 2 5.5 O[C@@H]1CC[C@]2([C@@H](C1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)C 10.1021/jm7015864
CHEMBL1478 2327 None 52 Human Functional pEC50 = 6.2 6.2 50 2
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 376 4 2 2 5.5 O[C@@H]1CC[C@]2([C@@H](C1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)C 10.1021/jm7015864
73352464 92760 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 410 5 1 2 6.1 FC(F)(F)c1cc(CNCc2cnccc2-c2ccccc2)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435918 92760 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 410 5 1 2 6.1 FC(F)(F)c1cc(CNCc2cnccc2-c2ccccc2)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
1452577 109993 None 0 Human Functional pEC50 = 5.2 5.2 4 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 324 5 1 4 2.4 Cc1ccnc(N2CCC[C@@H](C(=O)NCCc3ccccc3)C2)n1 10.1021/jm401731q
CHEMBL3234550 109993 None 0 Human Functional pEC50 = 5.2 5.2 4 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 324 5 1 4 2.4 Cc1ccnc(N2CCC[C@@H](C(=O)NCCc3ccccc3)C2)n1 10.1021/jm401731q
71626229 118895 None 0 Mouse Functional pEC50 = 5.2 5.2 2 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 582 9 1 6 5.3 CN(CC(=O)O)C(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421901 118895 None 0 Mouse Functional pEC50 = 5.2 5.2 2 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 582 9 1 6 5.3 CN(CC(=O)O)C(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
45483949 3582 None 33 Mouse Functional pEC50 = 6.2 6.2 2 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2022.114697
7048 3582 None 33 Mouse Functional pEC50 = 6.2 6.2 2 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2022.114697
CHEMBL567640 3582 None 33 Mouse Functional pEC50 = 6.2 6.2 2 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2022.114697
71626493 112261 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 422 4 0 5 5.1 O=C(c1cnccc1Oc1ccc2cccnc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
CHEMBL3290704 112261 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 422 4 0 5 5.1 O=C(c1cnccc1Oc1ccc2cccnc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
137641119 157101 None 0 Mouse Functional pEC50 = 6.2 6.2 28 2
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 636 12 0 8 6.2 COc1ccc(SCc2cnc(SCc3c(F)cc(S(=O)(=O)/N=C/N(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4073356 157101 None 0 Mouse Functional pEC50 = 6.2 6.2 28 2
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 636 12 0 8 6.2 COc1ccc(SCc2cnc(SCc3c(F)cc(S(=O)(=O)/N=C/N(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
92880 96247 None 10 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 390 4 1 3 5.6 COC(=O)CC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
CHEMBL260735 96247 None 10 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 390 4 1 3 5.6 COC(=O)CC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
71461058 83053 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 456 6 0 5 5.8 CCCCN1CCN(C(=O)c2cncnc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
CHEMBL2181257 83053 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 456 6 0 5 5.8 CCCCN1CCN(C(=O)c2cncnc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
156705100 182355 None 0 Mouse Functional pEC50 = 5.2 5.2 -4 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 567 7 0 10 5.5 Cc1oc(=O)oc1COC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4783601 182355 None 0 Mouse Functional pEC50 = 5.2 5.2 -4 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 567 7 0 10 5.5 Cc1oc(=O)oc1COC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
90654590 110015 None 0 Human Functional pEC50 = 8.2 8.2 -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 502 6 1 8 2.1 CN1CCN(c2cc(N3CCC[C@@H](C(=O)NCCc4ccc(C#N)nc4)C3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
CHEMBL3234571 110015 None 0 Human Functional pEC50 = 8.2 8.2 -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 502 6 1 8 2.1 CN1CCN(c2cc(N3CCC[C@@H](C(=O)NCCc4ccc(C#N)nc4)C3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
172433366 197250 None 0 Mouse Functional pEC50 = 8.2 8.2 2 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 955 16 2 9 6.8 CC1C(=O)N(CC(=O)NCCN(C)C(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5483060 197250 None 0 Mouse Functional pEC50 = 8.2 8.2 2 2
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 955 16 2 9 6.8 CC1C(=O)N(CC(=O)NCCN(C)C(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)CCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
45273910 113623 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 413 3 0 4 5.3 CN1CCN(C(=O)c2cccnc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1016/j.bmcl.2014.07.026
CHEMBL3321841 113623 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
ChEMBL 413 3 0 4 5.3 CN1CCN(C(=O)c2cccnc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1016/j.bmcl.2014.07.026
172454703 195937 None 0 Human Functional pEC50 = 8.2 8.2 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1149 27 3 12 7.7 N[C@@H](CC(=O)N1CCCN(CC(=O)NCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)C(=O)C1Cc1ccccc1)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
CHEMBL5413666 195937 None 0 Human Functional pEC50 = 8.2 8.2 -1 2
Agonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assayAgonist activity at human TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase assay
ChEMBL 1149 27 3 12 7.7 N[C@@H](CC(=O)N1CCCN(CC(=O)NCCOCCOCCOCCNC(=O)CCc2cc(Cl)c(Oc3ccsc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)C(=O)C1Cc1ccccc1)Cc1cc(F)c(F)cc1F 10.1016/j.ejmech.2022.114697
90644455 112290 None 0 Mouse Functional pEC50 = 8.2 8.2 1 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 614 9 1 8 5.9 CCOC(=O)CNC(=O)/C=C/c1oc2ccc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c2c1C 10.1016/j.ejmech.2014.05.031
CHEMBL3290733 112290 None 0 Mouse Functional pEC50 = 8.2 8.2 1 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 614 9 1 8 5.9 CCOC(=O)CNC(=O)/C=C/c1oc2ccc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c2c1C 10.1016/j.ejmech.2014.05.031
71453901 83036 None 0 Human Functional pEC50 = 8.2 8.2 10 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 439 5 0 4 5.8 C=CCN1CCN(C(=O)c2cnccc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
CHEMBL2181238 83036 None 0 Human Functional pEC50 = 8.2 8.2 10 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 439 5 0 4 5.8 C=CCN1CCN(C(=O)c2cnccc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
71450251 83023 None 29 Mouse Functional pEC50 = 8.2 8.2 -8 3
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 399 4 0 4 5.1 Cc1ccc(C)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)c1 10.1021/jm301071h
CHEMBL2181226 83023 None 29 Mouse Functional pEC50 = 8.2 8.2 -8 3
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 399 4 0 4 5.1 Cc1ccc(C)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)c1 10.1021/jm301071h
118103729 164326 None 0 Mouse Functional pEC50 = 8.2 8.2 - 1
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 676 14 3 7 5.0 O=C(O)CC[C@H](NC(=O)CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)C(=O)O 10.1021/acs.jmedchem.8b00308
CHEMBL4211123 164326 None 0 Mouse Functional pEC50 = 8.2 8.2 - 1
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 676 14 3 7 5.0 O=C(O)CC[C@H](NC(=O)CCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)C(=O)O 10.1021/acs.jmedchem.8b00308
118093535 164541 None 0 Mouse Functional pEC50 = 8.2 8.2 5 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 682 13 6 10 1.4 O=C(CCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4213844 164541 None 0 Mouse Functional pEC50 = 8.2 8.2 5 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 682 13 6 10 1.4 O=C(CCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
118093557 164754 None 0 Mouse Functional pEC50 = 8.2 8.2 3 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 477 5 1 5 4.4 O=C([C@@H]1CSCN1Cc1cc(Cl)c(CO)cc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4216682 164754 None 0 Mouse Functional pEC50 = 8.2 8.2 3 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 477 5 1 5 4.4 O=C([C@@H]1CSCN1Cc1cc(Cl)c(CO)cc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
71561504 87669 None 0 Human Functional pEC50 = 8.2 8.2 - 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 444 4 0 5 5.6 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N1CCCC[C@@H]1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336222 87669 None 0 Human Functional pEC50 = 8.2 8.2 - 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 444 4 0 5 5.6 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N1CCCC[C@@H]1c1cccnc1 10.1016/j.bmcl.2012.12.076
155669601 181115 None 0 Human Functional pEC50 = 8.2 8.2 91 2
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 426 4 0 4 4.9 O=C(c1cncn1Cc1ccc(Cl)cc1Cl)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
CHEMBL4759025 181115 None 0 Human Functional pEC50 = 8.2 8.2 91 2
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 426 4 0 4 4.9 O=C(c1cncn1Cc1ccc(Cl)cc1Cl)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
90654569 109992 None 0 Human Functional pEC50 = 7.2 7.2 2 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 358 5 1 4 3.0 Cc1ccnc(N2CCC[C@@H](C(=O)NCCc3ccc(Cl)cc3)C2)n1 10.1021/jm401731q
CHEMBL3234549 109992 None 0 Human Functional pEC50 = 7.2 7.2 2 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 358 5 1 4 3.0 Cc1ccnc(N2CCC[C@@H](C(=O)NCCc3ccc(Cl)cc3)C2)n1 10.1021/jm401731q
71561755 87317 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 438 6 0 6 5.3 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N(Cc1cncs1)C(C)C 10.1016/j.bmcl.2012.12.076
CHEMBL2331604 87317 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 438 6 0 6 5.3 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N(Cc1cncs1)C(C)C 10.1016/j.bmcl.2012.12.076
71626560 112269 None 0 Mouse Functional pEC50 = 7.2 7.2 -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 428 4 0 6 5.1 O=C(c1cnccc1Oc1ccc2ncsc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
CHEMBL3290712 112269 None 0 Mouse Functional pEC50 = 7.2 7.2 -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 428 4 0 6 5.1 O=C(c1cnccc1Oc1ccc2ncsc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
118694404 196503 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 397 6 0 3 5.1 CCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5425461 196503 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 397 6 0 3 5.1 CCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694537 197046 None 0 Human Functional pEC50 = 6.2 6.2 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 369 4 0 3 4.3 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1C 10.1021/acs.jmedchem.2c01881
CHEMBL5437459 197046 None 0 Human Functional pEC50 = 6.2 6.2 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 369 4 0 3 4.3 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1C 10.1021/acs.jmedchem.2c01881
118694542 195285 None 0 Mouse Functional pEC50 = 6.2 6.2 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 489 8 0 4 6.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(-c3ccccc3)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5400104 195285 None 0 Mouse Functional pEC50 = 6.2 6.2 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 489 8 0 4 6.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(-c3ccccc3)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694528 195681 None 0 Mouse Functional pEC50 = 6.2 6.2 -3 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(Cl)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5408901 195681 None 0 Mouse Functional pEC50 = 6.2 6.2 -3 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(Cl)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694465 196755 None 0 Mouse Functional pEC50 = 6.2 6.2 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2F)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5431493 196755 None 0 Mouse Functional pEC50 = 6.2 6.2 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2F)=C1C 10.1021/acs.jmedchem.2c01881
156705111 183036 None 0 Mouse Functional pEC50 = 5.2 5.2 -2 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 455 5 1 6 4.9 O=C(O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4792593 183036 None 0 Mouse Functional pEC50 = 5.2 5.2 -2 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
ChEMBL 455 5 1 6 4.9 O=C(O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
137638975 156967 None 0 Mouse Functional pEC50 = 5.2 5.2 - 1
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 546 10 1 7 6.6 COc1ccc(SCc2cnc(SCc3c(F)cc(C(=O)O)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4071870 156967 None 0 Mouse Functional pEC50 = 5.2 5.2 - 1
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 546 10 1 7 6.6 COc1ccc(SCc2cnc(SCc3c(F)cc(C(=O)O)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
92803 167428 None 28 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 360 4 1 1 6.5 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4CCCC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
CHEMBL429432 167428 None 28 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 360 4 1 1 6.5 C[C@H](CCC(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4CCCC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
73347897 92765 None 0 Human Functional pEC50 = 7.2 7.2 6 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 435 5 1 3 6.1 N#CC(NCc1cnccc1-c1ccccc1)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435925 92765 None 0 Human Functional pEC50 = 7.2 7.2 6 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 435 5 1 3 6.1 N#CC(NCc1cnccc1-c1ccccc1)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
10133 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
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 10.1016/j.bmc.2015.01.048
145714624 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
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 10.1016/j.bmc.2015.01.048
4361 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
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 10.1016/j.bmc.2015.01.048
608 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
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 10.1016/j.bmc.2015.01.048
CHEMBL240597 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
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 10.1016/j.bmc.2015.01.048
DB06777 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
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 10.1016/j.bmc.2015.01.048
155669601 181115 None 0 Mouse Functional pEC50 = 6.2 6.2 -91 2
Agonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assayAgonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay
ChEMBL 426 4 0 4 4.9 O=C(c1cncn1Cc1ccc(Cl)cc1Cl)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
CHEMBL4759025 181115 None 0 Mouse Functional pEC50 = 6.2 6.2 -91 2
Agonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assayAgonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay
ChEMBL 426 4 0 4 4.9 O=C(c1cncn1Cc1ccc(Cl)cc1Cl)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
76318386 106081 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human recombinant TGR5 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 391 4 0 5 4.3 COc1cccc(-c2noc(C)c2C(=O)N(C)c2ccc(C(F)(F)F)nc2)c1 10.1039/C2MD20174G
CHEMBL3132969 106081 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human recombinant TGR5 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 391 4 0 5 4.3 COc1cccc(-c2noc(C)c2C(=O)N(C)c2ccc(C(F)(F)F)nc2)c1 10.1039/C2MD20174G
44457506 157398 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 374 4 1 1 6.8 C[C@H]1C[C@@H]2CCCC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)O)[C@H]12 10.1021/jm7015864
CHEMBL407713 157398 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 374 4 1 1 6.8 C[C@H]1C[C@@H]2CCCC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)O)[C@H]12 10.1021/jm7015864
73352467 92768 None 0 Human Functional pEC50 = 7.2 7.2 8 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 496 5 1 3 5.5 O=S(=O)(NCc1cnccc1-c1c(F)cccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435928 92768 None 0 Human Functional pEC50 = 7.2 7.2 8 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 496 5 1 3 5.5 O=S(=O)(NCc1cnccc1-c1c(F)cccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
155339364 182822 None 0 Human Functional pEC50 = 7.2 7.2 1 2
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 583 11 6 8 1.9 CO[C@@H]1C[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)N(C)C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)[C@@H]21 10.1039/d0md00425a
CHEMBL4789628 182822 None 0 Human Functional pEC50 = 7.2 7.2 1 2
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 583 11 6 8 1.9 CO[C@@H]1C[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)N(C)C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)[C@@H]21 10.1039/d0md00425a
118464749 158671 None 0 Mouse Functional pEC50 = 5.2 5.2 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 562 7 0 4 8.4 COc1cc(C2(CF)CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4091882 158671 None 0 Mouse Functional pEC50 = 5.2 5.2 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 562 7 0 4 8.4 COc1cc(C2(CF)CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
162646016 179577 None 0 Human Functional pEC50 = 4.2 4.2 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay
ChEMBL 436 5 4 4 4.1 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@@H](O)[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)O)[C@@H]2[C@@H]1O 10.1021/acs.jmedchem.6b01126
CHEMBL4740844 179577 None 0 Human Functional pEC50 = 4.2 4.2 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay
ChEMBL 436 5 4 4 4.1 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@@H](O)[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)O)[C@@H]2[C@@H]1O 10.1021/acs.jmedchem.6b01126
172456318 196370 None 0 Human Functional pEC50 = 4.2 4.2 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 502 7 1 5 6.0 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC(=O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)OCC4CCCC4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
CHEMBL5422399 196370 None 0 Human Functional pEC50 = 4.2 4.2 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 502 7 1 5 6.0 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC(=O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)OCC4CCCC4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
118464630 158746 None 0 Mouse Functional pEC50 = 6.2 6.2 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 574 6 0 4 8.3 COc1cc(C2CCCc3nc(SCc4c(F)cccc4Br)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4092628 158746 None 0 Mouse Functional pEC50 = 6.2 6.2 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 574 6 0 4 8.3 COc1cc(C2CCCc3nc(SCc4c(F)cccc4Br)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
5879 208789 None 34 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 290 0 1 2 4.0 C[C@]12CC[C@H]3[C@@H](CC[C@H]4C[C@H](O)CC[C@@]43C)[C@@H]1CCC2=O 10.1021/jm7015864
CHEMBL87285 208789 None 34 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 290 0 1 2 4.0 C[C@]12CC[C@H]3[C@@H](CC[C@H]4C[C@H](O)CC[C@@]43C)[C@@H]1CCC2=O 10.1021/jm7015864
44627313 200217 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 510 4 2 2 8.4 C=C(C)C[C@@]1(O)CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(=C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/jm900872z
CHEMBL571735 200217 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 510 4 2 2 8.4 C=C(C)C[C@@]1(O)CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(=C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/jm900872z
73349426 92767 None 0 Human Functional pEC50 = 7.2 7.2 12 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 478 5 1 3 5.4 O=S(=O)(NCc1cnccc1-c1ccccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435927 92767 None 0 Human Functional pEC50 = 7.2 7.2 12 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 478 5 1 3 5.4 O=S(=O)(NCc1cnccc1-c1ccccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
90327488 112280 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 503 5 1 6 5.9 Cc1c(C(=O)O)oc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
CHEMBL3290723 112280 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 503 5 1 6 5.9 Cc1c(C(=O)O)oc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
90654591 110016 None 0 Human Functional pEC50 = 7.2 7.2 -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 488 6 2 8 1.7 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3cc(N4CCNCC4)nc(C(F)(F)F)n3)C2)cn1 10.1021/jm401731q
CHEMBL3234572 110016 None 0 Human Functional pEC50 = 7.2 7.2 -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 488 6 2 8 1.7 N#Cc1ccc(CCNC(=O)[C@@H]2CCCN(c3cc(N4CCNCC4)nc(C(F)(F)F)n3)C2)cn1 10.1021/jm401731q
90654580 110004 None 0 Mouse Functional pEC50 = 7.2 7.2 -4 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 367 5 1 5 2.4 Cc1nc(N2CCC[C@@H](C(=O)NCCc3ccc(C#N)cc3)C2)ncc1F 10.1021/jm401731q
CHEMBL3234561 110004 None 0 Mouse Functional pEC50 = 7.2 7.2 -4 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 367 5 1 5 2.4 Cc1nc(N2CCC[C@@H](C(=O)NCCc3ccc(C#N)cc3)C2)ncc1F 10.1021/jm401731q
118093541 163614 None 0 Human Functional pEC50 = 7.2 7.2 -7 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 696 13 5 10 1.7 CN(C[C@H](O)[C@@H](O)[C@@H](O)[C@H](O)CO)C(=O)CCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4202603 163614 None 0 Human Functional pEC50 = 7.2 7.2 -7 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 696 13 5 10 1.7 CN(C[C@H](O)[C@@H](O)[C@@H](O)[C@H](O)CO)C(=O)CCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
71660979 163638 None 0 Human Functional pEC50 = 7.2 7.2 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 447 4 0 3 4.9 O=C([C@@H]1C[C@@H](F)CN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4202908 163638 None 0 Human Functional pEC50 = 7.2 7.2 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 447 4 0 3 4.9 O=C([C@@H]1C[C@@H](F)CN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
145967535 164888 None 0 Human Functional pEC50 = 7.2 7.2 -15 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 739 15 6 10 2.3 CN(C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)C(=O)NCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4218315 164888 None 0 Human Functional pEC50 = 7.2 7.2 -15 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 739 15 6 10 2.3 CN(C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)C(=O)NCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
46233054 203178 None 0 Human Functional pEC50 = 7.2 7.2 - 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 374 3 0 3 5.5 Cc1cc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)ccc1Cl 10.1016/j.bmcl.2010.01.003
CHEMBL600020 203178 None 0 Human Functional pEC50 = 7.2 7.2 - 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 374 3 0 3 5.5 Cc1cc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)ccc1Cl 10.1016/j.bmcl.2010.01.003
46232737 203337 None 0 Human Functional pEC50 = 7.2 7.2 - 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 340 4 0 3 4.8 CCc1onc(-c2ccccc2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL601428 203337 None 0 Human Functional pEC50 = 7.2 7.2 - 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 340 4 0 3 4.8 CCc1onc(-c2ccccc2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
46232570 203654 None 0 Human Functional pEC50 = 7.2 7.2 - 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 COc1ccccc1-c1noc(C)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL603500 203654 None 0 Human Functional pEC50 = 7.2 7.2 - 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 COc1ccccc1-c1noc(C)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
71661186 164377 None 0 Mouse Functional pEC50 = 7.2 7.2 3 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 532 9 1 5 5.6 NCCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4211892 164377 None 0 Mouse Functional pEC50 = 7.2 7.2 3 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 532 9 1 5 5.6 NCCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
145971348 164665 None 0 Mouse Functional pEC50 = 7.2 7.2 -1 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 481 4 0 4 5.2 O=C([C@@H]1CSCN1Cc1cc(Cl)ccc1C(F)(F)F)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4215354 164665 None 0 Mouse Functional pEC50 = 7.2 7.2 -1 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 481 4 0 4 5.2 O=C([C@@H]1CSCN1Cc1cc(Cl)ccc1C(F)(F)F)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
145007569 195011 None 0 Mouse Functional pEC50 = 7.2 7.2 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(CC2CCCO2)C(=O)CC1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
CHEMBL5394911 195011 None 0 Mouse Functional pEC50 = 7.2 7.2 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(CC2CCCO2)C(=O)CC1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
10198 2054 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at TGR5 (unknown origin)Agonist activity at TGR5 (unknown origin)
ChEMBL 471 6 2 6 4.1 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)CC[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)[C@@H](CCOS(=O)(=O)[O-])C 10.1016/j.ejmech.2023.115143
137321169 2054 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at TGR5 (unknown origin)Agonist activity at TGR5 (unknown origin)
ChEMBL 471 6 2 6 4.1 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)CC[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)[C@@H](CCOS(=O)(=O)[O-])C 10.1016/j.ejmech.2023.115143
23642339 2054 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at TGR5 (unknown origin)Agonist activity at TGR5 (unknown origin)
ChEMBL 471 6 2 6 4.1 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)CC[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)[C@@H](CCOS(=O)(=O)[O-])C 10.1016/j.ejmech.2023.115143
CHEMBL3306873 2054 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at TGR5 (unknown origin)Agonist activity at TGR5 (unknown origin)
ChEMBL 471 6 2 6 4.1 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)CC[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)[C@@H](CCOS(=O)(=O)[O-])C 10.1016/j.ejmech.2023.115143
118694430 195107 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 383 5 0 3 4.7 CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5396796 195107 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 383 5 0 3 4.7 CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694404 196503 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 397 6 0 3 5.1 CCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5425461 196503 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 397 6 0 3 5.1 CCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694537 197046 None 0 Human Functional pEC50 = 6.2 6.2 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 369 4 0 3 4.3 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1C 10.1021/acs.jmedchem.2c01881
CHEMBL5437459 197046 None 0 Human Functional pEC50 = 6.2 6.2 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 369 4 0 3 4.3 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1C 10.1021/acs.jmedchem.2c01881
46233020 201803 None 0 Human Functional pEC50 = 6.2 6.2 - 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 360 3 0 3 5.2 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.003
CHEMBL590739 201803 None 0 Human Functional pEC50 = 6.2 6.2 - 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 360 3 0 3 5.2 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.003
46232626 201960 None 0 Human Functional pEC50 = 6.2 6.2 - 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 394 3 0 3 5.9 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL591927 201960 None 0 Human Functional pEC50 = 6.2 6.2 - 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 394 3 0 3 5.9 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
46232627 203380 None 0 Human Functional pEC50 = 6.2 6.2 - 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 378 3 0 3 5.4 Cc1onc(-c2c(F)cccc2Cl)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL601670 203380 None 0 Human Functional pEC50 = 6.2 6.2 - 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 378 3 0 3 5.4 Cc1onc(-c2c(F)cccc2Cl)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
46232984 203880 None 0 Human Functional pEC50 = 6.2 6.2 - 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 344 3 0 3 4.7 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1cccc(F)c1 10.1016/j.bmcl.2010.01.003
CHEMBL604752 203880 None 0 Human Functional pEC50 = 6.2 6.2 - 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 344 3 0 3 4.7 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1cccc(F)c1 10.1016/j.bmcl.2010.01.003
71661224 164235 None 0 Mouse Functional pEC50 = 6.2 6.2 1 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 415 4 0 3 4.6 O=C([C@@H]1CCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4210112 164235 None 0 Mouse Functional pEC50 = 6.2 6.2 1 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 415 4 0 3 4.6 O=C([C@@H]1CCN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118103718 164616 None 0 Mouse Functional pEC50 = 6.2 6.2 -1 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 682 13 6 9 1.4 O=C(CCc1cc(Cl)c(CN2C[C@@H](F)C[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4214838 164616 None 0 Mouse Functional pEC50 = 6.2 6.2 -1 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 682 13 6 9 1.4 O=C(CCc1cc(Cl)c(CN2C[C@@H](F)C[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
118694469 194962 None 0 Mouse Functional pEC50 = 6.2 6.2 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
CHEMBL5394197 194962 None 0 Mouse Functional pEC50 = 6.2 6.2 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
118700253 195316 None 0 Mouse Functional pEC50 = 6.2 6.2 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 414 7 0 5 3.7 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccncc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5400773 195316 None 0 Mouse Functional pEC50 = 6.2 6.2 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 414 7 0 5 3.7 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccncc2)=C1C 10.1021/acs.jmedchem.2c01881
118694528 195681 None 0 Mouse Functional pEC50 = 6.2 6.2 -3 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(Cl)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5408901 195681 None 0 Mouse Functional pEC50 = 6.2 6.2 -3 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 447 7 0 4 5.0 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(Cl)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694465 196755 None 0 Mouse Functional pEC50 = 6.2 6.2 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2F)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5431493 196755 None 0 Mouse Functional pEC50 = 6.2 6.2 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2F)=C1C 10.1021/acs.jmedchem.2c01881
118694455 196971 None 0 Mouse Functional pEC50 = 6.2 6.2 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 411 6 0 3 5.3 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC(C)C 10.1021/acs.jmedchem.2c01881
CHEMBL5435789 196971 None 0 Mouse Functional pEC50 = 6.2 6.2 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 411 6 0 3 5.3 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC(C)C 10.1021/acs.jmedchem.2c01881
44605617 200775 None 1 Rat Functional pEC50 = 6.2 6.2 -5 2
Agonist activity at rat TGR5 expressed in melanophores assessed as melanosome dispersion by melanophore assayAgonist activity at rat TGR5 expressed in melanophores assessed as melanosome dispersion by melanophore assay
ChEMBL 374 3 0 3 5.5 Cc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1Cl 10.1021/jm901434t
CHEMBL576138 200775 None 1 Rat Functional pEC50 = 6.2 6.2 -5 2
Agonist activity at rat TGR5 expressed in melanophores assessed as melanosome dispersion by melanophore assayAgonist activity at rat TGR5 expressed in melanophores assessed as melanosome dispersion by melanophore assay
ChEMBL 374 3 0 3 5.5 Cc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1Cl 10.1021/jm901434t
118694343 197048 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 335 4 1 3 3.6 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(C)cc2)CC(=O)N1 10.1021/acs.jmedchem.2c01881
CHEMBL5437536 197048 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 335 4 1 3 3.6 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(C)cc2)CC(=O)N1 10.1021/acs.jmedchem.2c01881
172471761 197158 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 460 6 1 5 4.9 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC(=O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)OC4CC4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
CHEMBL5440059 197158 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 460 6 1 5 4.9 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC(=O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)OC4CC4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
5306292 196577 None 8 Human Functional pEC50 = 5.2 5.2 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 293 2 0 3 2.7 COC(=O)C1=C(C)N(C)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5427123 196577 None 8 Human Functional pEC50 = 5.2 5.2 2 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 293 2 0 3 2.7 COC(=O)C1=C(C)N(C)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
118694580 196916 None 0 Human Functional pEC50 = 5.2 5.2 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 341 4 1 3 3.6 O=C1CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=CN1 10.1021/acs.jmedchem.2c01881
CHEMBL5434777 196916 None 0 Human Functional pEC50 = 5.2 5.2 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 341 4 1 3 3.6 O=C1CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=CN1 10.1021/acs.jmedchem.2c01881
118694343 197048 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 335 4 1 3 3.6 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(C)cc2)CC(=O)N1 10.1021/acs.jmedchem.2c01881
CHEMBL5437536 197048 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 335 4 1 3 3.6 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(C)cc2)CC(=O)N1 10.1021/acs.jmedchem.2c01881
46232411 203834 None 0 Human Functional pEC50 = 5.2 5.2 - 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 368 5 0 3 5.5 CCCc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL604524 203834 None 0 Human Functional pEC50 = 5.2 5.2 - 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 368 5 0 3 5.5 CCCc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2010.01.003
71626555 112260 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 422 4 0 5 5.1 O=C(c1cnccc1Oc1ccc2ncccc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
CHEMBL3290703 112260 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 422 4 0 5 5.1 O=C(c1cnccc1Oc1ccc2ncccc2c1)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
58043236 91640 None 0 Human Functional pEC50 = 5.2 5.2 -2 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
ChEMBL 466 7 2 5 5.5 Cc1ccccc1[C@@H](C/C(=N\O)c1ccc(=O)n(C)c1)c1ccc(-c2ccc(C(=O)O)cc2)cc1 10.1016/j.bmcl.2013.06.017
CHEMBL2407933 91640 None 0 Human Functional pEC50 = 5.2 5.2 -2 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
ChEMBL 466 7 2 5 5.5 Cc1ccccc1[C@@H](C/C(=N\O)c1ccc(=O)n(C)c1)c1ccc(-c2ccc(C(=O)O)cc2)cc1 10.1016/j.bmcl.2013.06.017
71561881 87675 None 0 Human Functional pEC50 = 5.2 5.2 - 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 447 4 0 6 4.9 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N1CCCCC1c1nccn1C 10.1016/j.bmcl.2012.12.076
CHEMBL2336228 87675 None 0 Human Functional pEC50 = 5.2 5.2 - 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 447 4 0 6 4.9 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N1CCCCC1c1nccn1C 10.1016/j.bmcl.2012.12.076
71561367 87661 None 0 Human Functional pEC50 = 7.2 7.2 - 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 412 4 0 5 4.6 Cc1nn(C)c(Oc2cccc(F)c2F)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336212 87661 None 0 Human Functional pEC50 = 7.2 7.2 - 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 412 4 0 5 4.6 Cc1nn(C)c(Oc2cccc(F)c2F)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
46196449 77239 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
ChEMBL 436 5 4 4 4.1 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](C[C@H](O)[C@@H]3[C@H](C)CCC(=O)O)[C@@H]2[C@@H]1O 10.1021/ml200256d
CHEMBL2062554 77239 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
ChEMBL 436 5 4 4 4.1 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](C[C@H](O)[C@@H]3[C@H](C)CCC(=O)O)[C@@H]2[C@@H]1O 10.1021/ml200256d
CHEMBL2079386 77239 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
ChEMBL 436 5 4 4 4.1 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](C[C@H](O)[C@@H]3[C@H](C)CCC(=O)O)[C@@H]2[C@@H]1O 10.1021/ml200256d
71626489 112257 None 0 Mouse Functional pEC50 = 7.2 7.2 -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 421 4 0 4 5.7 O=C(c1cnccc1Oc1cccc2ccccc12)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
CHEMBL3290700 112257 None 0 Mouse Functional pEC50 = 7.2 7.2 -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 421 4 0 4 5.7 O=C(c1cnccc1Oc1cccc2ccccc12)N1CCN(C2CC2)c2ccccc21 10.1016/j.ejmech.2014.05.031
77846087 112275 None 0 Mouse Functional pEC50 = 7.2 7.2 -8 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 537 4 0 5 7.0 Cc1c(Br)oc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
CHEMBL3290718 112275 None 0 Mouse Functional pEC50 = 7.2 7.2 -8 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 537 4 0 5 7.0 Cc1c(Br)oc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
71453901 83036 None 0 Mouse Functional pEC50 = 7.2 7.2 -10 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 439 5 0 4 5.8 C=CCN1CCN(C(=O)c2cnccc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
CHEMBL2181238 83036 None 0 Mouse Functional pEC50 = 7.2 7.2 -10 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 439 5 0 4 5.8 C=CCN1CCN(C(=O)c2cnccc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
156019635 178094 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 387 3 2 3 5.3 CC[C@@]1(O)C[C@H]2[C@@H]3CC[C@H]([C@H](C)CC#N)[C@@]3(C)CC[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1021/acsmedchemlett.9b00636
CHEMBL4646200 178094 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 387 3 2 3 5.3 CC[C@@]1(O)C[C@H]2[C@@H]3CC[C@H]([C@H](C)CC#N)[C@@]3(C)CC[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1021/acsmedchemlett.9b00636
89501425 161642 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assay
ChEMBL 539 9 0 5 7.8 CC(C)(c1ccc(Cl)c(Cl)c1)c1cnc(SCCOCc2ccc(C#N)cc2)n1-c1ccc(F)cc1 10.1016/j.bmcl.2018.04.011
CHEMBL4128688 161642 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHOK1 cells after 5 hrs by luciferase reporter gene assay
ChEMBL 539 9 0 5 7.8 CC(C)(c1ccc(Cl)c(Cl)c1)c1cnc(SCCOCc2ccc(C#N)cc2)n1-c1ccc(F)cc1 10.1016/j.bmcl.2018.04.011
10133 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
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/ml200256d
145714624 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
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/ml200256d
4361 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
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/ml200256d
608 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
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/ml200256d
CHEMBL240597 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
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/ml200256d
DB06777 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
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/ml200256d
10133 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
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/jm070633p
145714624 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
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/jm070633p
4361 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
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/jm070633p
608 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
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/jm070633p
CHEMBL240597 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
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/jm070633p
DB06777 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
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/jm070633p
10133 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
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/jm7015864
145714624 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
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/jm7015864
4361 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
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/jm7015864
608 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
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/jm7015864
CHEMBL240597 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
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/jm7015864
DB06777 910 None 49 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
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/jm7015864
77845284 112283 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 517 7 1 6 5.9 O=C(O)CCc1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
CHEMBL3290726 112283 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 517 7 1 6 5.9 O=C(O)CCc1coc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
118464815 159610 None 0 Mouse Functional pEC50 = 6.2 6.2 6 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 528 6 0 4 7.9 COc1cc(C2(C)CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)ccc1F 10.1021/acsmedchemlett.7b00116
CHEMBL4102107 159610 None 0 Mouse Functional pEC50 = 6.2 6.2 6 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 528 6 0 4 7.9 COc1cc(C2(C)CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)ccc1F 10.1021/acsmedchemlett.7b00116
118586298 158118 None 0 Mouse Functional pEC50 = 7.2 7.2 2 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 449 8 0 6 6.1 COc1ccc(N(C)c2cnc(SCc3ccccc3)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4085664 158118 None 0 Mouse Functional pEC50 = 7.2 7.2 2 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 449 8 0 6 6.1 COc1ccc(N(C)c2cnc(SCc3ccccc3)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
164620833 185664 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 565 6 2 4 7.0 CCNS(=O)(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
CHEMBL4863256 185664 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 565 6 2 4 7.0 CCNS(=O)(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
118464664 157282 None 0 Human Functional pEC50 = 6.2 6.2 -2 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 478 6 0 6 5.9 COc1cc(C2(C)CCCc3nc(SCc4ncccn4)n(-c4ccc(F)cc4)c32)ccc1F 10.1021/acsmedchemlett.7b00116
CHEMBL4075703 157282 None 0 Human Functional pEC50 = 6.2 6.2 -2 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 478 6 0 6 5.9 COc1cc(C2(C)CCCc3nc(SCc4ncccn4)n(-c4ccc(F)cc4)c32)ccc1F 10.1021/acsmedchemlett.7b00116
118464811 156882 None 0 Mouse Functional pEC50 = 6.2 6.2 5 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 703 16 0 8 7.9 COc1cc(C2(C)CCCc3nc(SCc4c(F)ccc(OCCOCCOCCN(C)C)c4F)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4070895 156882 None 0 Mouse Functional pEC50 = 6.2 6.2 5 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 703 16 0 8 7.9 COc1cc(C2(C)CCCc3nc(SCc4c(F)ccc(OCCOCCOCCN(C)C)c4F)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
10198 2054 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assayAgonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assay
ChEMBL 471 6 2 6 4.1 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)CC[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)[C@@H](CCOS(=O)(=O)[O-])C 10.1016/j.ejmech.2022.114652
137321169 2054 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assayAgonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assay
ChEMBL 471 6 2 6 4.1 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)CC[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)[C@@H](CCOS(=O)(=O)[O-])C 10.1016/j.ejmech.2022.114652
23642339 2054 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assayAgonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assay
ChEMBL 471 6 2 6 4.1 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)CC[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)[C@@H](CCOS(=O)(=O)[O-])C 10.1016/j.ejmech.2022.114652
CHEMBL3306873 2054 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assayAgonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assay
ChEMBL 471 6 2 6 4.1 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)CC[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)[C@@H](CCOS(=O)(=O)[O-])C 10.1016/j.ejmech.2022.114652
611 2327 None 52 Human Functional pEC50 = 6.2 6.2 50 2
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 376 4 2 2 5.5 O[C@@H]1CC[C@]2([C@@H](C1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)C 10.1016/j.bmc.2015.01.048
9903 2327 None 52 Human Functional pEC50 = 6.2 6.2 50 2
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 376 4 2 2 5.5 O[C@@H]1CC[C@]2([C@@H](C1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)C 10.1016/j.bmc.2015.01.048
CHEMBL1478 2327 None 52 Human Functional pEC50 = 6.2 6.2 50 2
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 376 4 2 2 5.5 O[C@@H]1CC[C@]2([C@@H](C1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)C 10.1016/j.bmc.2015.01.048
2733768 161394 None 21 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at wild type human TGR5 expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assayAgonist activity at wild type human TGR5 expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assay
ChEMBL 499 7 4 5 3.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@@]21C 10.1016/j.ejmech.2015.09.024
CHEMBL412272 161394 None 21 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at wild type human TGR5 expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assayAgonist activity at wild type human TGR5 expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assay
ChEMBL 499 7 4 5 3.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@@]21C 10.1016/j.ejmech.2015.09.024
172448835 195687 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 472 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@@H]2[C@H](C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CC(F)(F)C(=O)O)CC[C@@H]23)[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1016/j.ejmech.2023.115851
CHEMBL5409189 195687 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 472 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@@H]2[C@H](C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CC(F)(F)C(=O)O)CC[C@@H]23)[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1016/j.ejmech.2023.115851
71461055 83035 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 441 4 0 4 6.1 CC(C)N1CCN(C(=O)c2cnccc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
CHEMBL2181237 83035 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 441 4 0 4 6.1 CC(C)N1CCN(C(=O)c2cnccc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
145007569 195011 None 0 Mouse Functional pEC50 = 7.2 7.2 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(CC2CCCO2)C(=O)CC1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
CHEMBL5394911 195011 None 0 Mouse Functional pEC50 = 7.2 7.2 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(CC2CCCO2)C(=O)CC1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
118455251 156450 None 0 Mouse Functional pEC50 = 6.2 6.2 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 514 6 0 4 7.7 COc1cc(C2CCCc3nc(SCc4c(F)cccc4F)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4065966 156450 None 0 Mouse Functional pEC50 = 6.2 6.2 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 514 6 0 4 7.7 COc1cc(C2CCCc3nc(SCc4c(F)cccc4F)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
156014434 177336 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 373 2 2 3 4.9 C[C@H](CC#N)[C@H]1CC[C@H]2[C@@H]3C[C@](C)(O)[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/acsmedchemlett.9b00636
CHEMBL4635684 177336 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 373 2 2 3 4.9 C[C@H](CC#N)[C@H]1CC[C@H]2[C@@H]3C[C@](C)(O)[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/acsmedchemlett.9b00636
44479724 199549 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 472 2 2 3 6.3 CC1(C)[C@@H](O)CC[C@@]2(C)[C@H]1CC[C@]1(C)[C@@H]2CC[C@@H]2[C@H]3[C@H]([C@]4(C)CO4)CC[C@]3(C(=O)O)CC[C@]21C 10.1021/jm900872z
CHEMBL567578 199549 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 472 2 2 3 6.3 CC1(C)[C@@H](O)CC[C@@]2(C)[C@H]1CC[C@]1(C)[C@@H]2CC[C@@H]2[C@H]3[C@H]([C@]4(C)CO4)CC[C@]3(C(=O)O)CC[C@]21C 10.1021/jm900872z
156705091 182313 None 0 Human Functional pEC50 = 8.2 8.2 20 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 515 7 0 8 5.7 CSCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4783037 182313 None 0 Human Functional pEC50 = 8.2 8.2 20 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 515 7 0 8 5.7 CSCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
126673445 157640 None 0 Mouse Functional pEC50 = 8.2 8.2 47 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 499 8 0 6 6.7 COc1ccc(N(C)c2c(C)nc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4080290 157640 None 0 Mouse Functional pEC50 = 8.2 8.2 47 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 499 8 0 6 6.7 COc1ccc(N(C)c2c(C)nc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
71459276 83034 None 0 Human Functional pEC50 = 8.2 8.2 10 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 441 5 0 4 6.1 CCCN1CCN(C(=O)c2cnccc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
CHEMBL2181236 83034 None 0 Human Functional pEC50 = 8.2 8.2 10 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 441 5 0 4 6.1 CCCN1CCN(C(=O)c2cnccc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
118577298 161080 None 0 Mouse Functional pEC50 = 8.1 8.1 18 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 581 9 0 6 6.4 COc1ccc(N(C)c2cnc(SCc3c(F)cc(C#CC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4086463 161080 None 0 Mouse Functional pEC50 = 8.1 8.1 18 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 581 9 0 6 6.4 COc1ccc(N(C)c2cnc(SCc3c(F)cc(C#CC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4096633 161080 None 0 Mouse Functional pEC50 = 8.1 8.1 18 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 581 9 0 6 6.4 COc1ccc(N(C)c2cnc(SCc3c(F)cc(C#CC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4116110 161080 None 0 Mouse Functional pEC50 = 8.1 8.1 18 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 581 9 0 6 6.4 COc1ccc(N(C)c2cnc(SCc3c(F)cc(C#CC[N+](C)(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
77846087 112275 None 0 Human Functional pEC50 = 8.1 8.1 8 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 537 4 0 5 7.0 Cc1c(Br)oc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
CHEMBL3290718 112275 None 0 Human Functional pEC50 = 8.1 8.1 8 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 537 4 0 5 7.0 Cc1c(Br)oc2cc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
126673504 157707 None 0 Mouse Functional pEC50 = 8.1 8.1 10 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 511 10 0 6 6.9 C=CCN(c1ccc(OC)c(OC)c1)c1cnc(SCc2c(F)cccc2F)n1-c1ccc(F)cc1 10.1021/acs.jmedchem.6b01873
CHEMBL4081050 157707 None 0 Mouse Functional pEC50 = 8.1 8.1 10 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 511 10 0 6 6.9 C=CCN(c1ccc(OC)c(OC)c1)c1cnc(SCc2c(F)cccc2F)n1-c1ccc(F)cc1 10.1021/acs.jmedchem.6b01873
71561366 87660 None 0 Human Functional pEC50 = 8.1 8.1 - 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 444 4 0 5 5.6 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336211 87660 None 0 Human Functional pEC50 = 8.1 8.1 - 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 444 4 0 5 5.6 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
71561884 87682 None 0 Human Functional pEC50 = 8.1 8.1 - 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 430 6 0 5 5.0 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N(Cc1cccnc1)C1CC1 10.1016/j.bmcl.2012.12.076
CHEMBL2336236 87682 None 0 Human Functional pEC50 = 8.1 8.1 - 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 430 6 0 5 5.0 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N(Cc1cccnc1)C1CC1 10.1016/j.bmcl.2012.12.076
71459274 83019 None 0 Human Functional pEC50 = 8.1 8.1 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 405 4 0 4 5.2 O=C(c1cnccc1Oc1cccc(Cl)c1)N1CCN(C2CC2)c2ccccc21 10.1021/jm301071h
CHEMBL2181222 83019 None 0 Human Functional pEC50 = 8.1 8.1 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 405 4 0 4 5.2 O=C(c1cnccc1Oc1cccc(Cl)c1)N1CCN(C2CC2)c2ccccc21 10.1021/jm301071h
46232530 203342 None 0 Human Functional pEC50 = 8.1 8.1 - 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 344 3 0 3 4.7 Cc1onc(-c2cccc(F)c2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL601440 203342 None 0 Human Functional pEC50 = 8.1 8.1 - 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 344 3 0 3 4.7 Cc1onc(-c2cccc(F)c2)c1C(=O)N(C)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.01.003
118093541 163614 None 0 Mouse Functional pEC50 = 8.1 8.1 7 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 696 13 5 10 1.7 CN(C[C@H](O)[C@@H](O)[C@@H](O)[C@H](O)CO)C(=O)CCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4202603 163614 None 0 Mouse Functional pEC50 = 8.1 8.1 7 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 696 13 5 10 1.7 CN(C[C@H](O)[C@@H](O)[C@@H](O)[C@H](O)CO)C(=O)CCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
118103740 163649 None 0 Mouse Functional pEC50 = 8.1 8.1 25 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 761 14 6 12 2.0 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(OCc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)cn1 10.1021/acs.jmedchem.8b00308
CHEMBL4202994 163649 None 0 Mouse Functional pEC50 = 8.1 8.1 25 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 761 14 6 12 2.0 O=C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)c1ccc(OCc2cc(Cl)c(CN3CSC[C@H]3C(=O)N3CCN(C4CC4)c4ccccc43)cc2Cl)cn1 10.1021/acs.jmedchem.8b00308
71561882 87680 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 446 7 0 5 5.7 CCC(C)N(Cc1cccnc1)C(=O)c1c(C)nn(C)c1Oc1cccc(Cl)c1Cl 10.1016/j.bmcl.2012.12.076
CHEMBL2336234 87680 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 446 7 0 5 5.7 CCC(C)N(Cc1cccnc1)C(=O)c1c(C)nn(C)c1Oc1cccc(Cl)c1Cl 10.1016/j.bmcl.2012.12.076
121322331 162982 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay
ChEMBL 497 6 3 5 4.1 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)NS(C)(=O)=O)[C@@H]2[C@@H]1O 10.1021/acsmedchemlett.7b00318
CHEMBL4173597 162982 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay
ChEMBL 497 6 3 5 4.1 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)NS(C)(=O)=O)[C@@H]2[C@@H]1O 10.1021/acsmedchemlett.7b00318
118694581 194966 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 393 5 0 3 4.3 C#CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5394245 194966 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 393 5 0 3 4.3 C#CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694430 195107 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 383 5 0 3 4.7 CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5396796 195107 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 383 5 0 3 4.7 CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694393 196611 None 0 Human Functional pEC50 = 6.2 6.2 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C(F)(F)F)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5427795 196611 None 0 Human Functional pEC50 = 6.2 6.2 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C(F)(F)F)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694423 197114 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 419 7 0 4 4.7 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCC2CCCCC2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5439109 197114 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 419 7 0 4 4.7 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCC2CCCCC2)=C1C 10.1021/acs.jmedchem.2c01881
118700253 195316 None 0 Mouse Functional pEC50 = 6.2 6.2 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 414 7 0 5 3.7 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccncc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5400773 195316 None 0 Mouse Functional pEC50 = 6.2 6.2 1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 414 7 0 5 3.7 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccncc2)=C1C 10.1021/acs.jmedchem.2c01881
118694455 196971 None 0 Mouse Functional pEC50 = 6.2 6.2 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 411 6 0 3 5.3 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC(C)C 10.1021/acs.jmedchem.2c01881
CHEMBL5435789 196971 None 0 Mouse Functional pEC50 = 6.2 6.2 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 411 6 0 3 5.3 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1CC(C)C 10.1021/acs.jmedchem.2c01881
15818 115500 None 14 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 292 0 2 2 3.8 C[C@]12CC[C@H]3[C@@H](CC[C@H]4C[C@H](O)CC[C@@]43C)[C@@H]1CC[C@@H]2O 10.1021/jm7015864
CHEMBL335062 115500 None 14 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 292 0 2 2 3.8 C[C@]12CC[C@H]3[C@@H](CC[C@H]4C[C@H](O)CC[C@@]43C)[C@@H]1CC[C@@H]2O 10.1021/jm7015864
118576999 159799 None 0 Human Functional pEC50 = 7.2 7.2 -17 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 566 9 0 7 6.3 COc1ccc(N(C)c2cnc(SCc3c(F)cc(C#CCN(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4104359 159799 None 0 Human Functional pEC50 = 7.2 7.2 -17 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 566 9 0 7 6.3 COc1ccc(N(C)c2cnc(SCc3c(F)cc(C#CCN(C)C)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
71453906 83050 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 442 4 0 5 5.5 CC(C)N1CCN(C(=O)c2cncnc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
CHEMBL2181254 83050 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 442 4 0 5 5.5 CC(C)N1CCN(C(=O)c2cncnc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
71626832 118889 None 0 Mouse Functional pEC50 = 4.2 4.2 -2 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 511 7 1 5 5.8 O=C(O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421894 118889 None 0 Mouse Functional pEC50 = 4.2 4.2 -2 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 511 7 1 5 5.8 O=C(O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
90644444 112292 None 0 Mouse Functional pEC50 = 7.1 7.1 -4 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 587 8 0 8 6.1 CCOC(=O)CCc1oc2ccc(Cl)c(C(=O)Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c2c1C 10.1016/j.ejmech.2014.05.031
CHEMBL3290735 112292 None 0 Mouse Functional pEC50 = 7.1 7.1 -4 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 587 8 0 8 6.1 CCOC(=O)CCc1oc2ccc(Cl)c(C(=O)Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c2c1C 10.1016/j.ejmech.2014.05.031
90654578 110002 None 0 Mouse Functional pEC50 = 6.1 6.1 -3 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 357 5 1 3 3.6 Cc1cccc(N2CCC[C@@H](C(=O)NCCc3ccc(Cl)cc3)C2)n1 10.1021/jm401731q
CHEMBL3234559 110002 None 0 Mouse Functional pEC50 = 6.1 6.1 -3 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 357 5 1 3 3.6 Cc1cccc(N2CCC[C@@H](C(=O)NCCc3ccc(Cl)cc3)C2)n1 10.1021/jm401731q
118464680 158752 None 0 Mouse Functional pEC50 = 7.1 7.1 46 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 526 7 0 5 7.6 COc1ccc([C@@H]2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4092785 158752 None 0 Mouse Functional pEC50 = 7.1 7.1 46 2
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 526 7 0 5 7.6 COc1ccc([C@@H]2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
90284520 117743 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 434 5 3 3 5.4 CC[C@H]1[C@H](O)[C@@H]2[C@H](CC[C@@]3(C)[C@H]2CC[C@@H]3[C@H](C)C[C@H](C)C(=O)O)[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1016/j.bmc.2015.01.048
CHEMBL3401356 117743 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 434 5 3 3 5.4 CC[C@H]1[C@H](O)[C@@H]2[C@H](CC[C@@]3(C)[C@H]2CC[C@@H]3[C@H](C)C[C@H](C)C(=O)O)[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1016/j.bmc.2015.01.048
44457480 158055 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 495 8 2 3 6.1 CC[C@H]1C[C@@H]2CCCC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)NCCS(=O)(=O)O)[C@H]12 10.1021/jm7015864
CHEMBL408477 158055 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 495 8 2 3 6.1 CC[C@H]1C[C@@H]2CCCC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)NCCS(=O)(=O)O)[C@H]12 10.1021/jm7015864
118694352 195534 None 0 Mouse Functional pEC50 = 6.1 6.1 -3 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 457 9 0 5 4.7 COCCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5405469 195534 None 0 Mouse Functional pEC50 = 6.1 6.1 -3 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 457 9 0 5 4.7 COCCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
14650410 190308 None 13 Human Functional pEC50 = 5.1 5.1 -6 2
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 265 4 1 3 3.3 OCc1cccc(OCc2ccc3ccccc3n2)c1 10.1021/acs.jmedchem.1c01078
CHEMBL5174405 190308 None 13 Human Functional pEC50 = 5.1 5.1 -6 2
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysisAgonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
ChEMBL 265 4 1 3 3.3 OCc1cccc(OCc2ccc3ccccc3n2)c1 10.1021/acs.jmedchem.1c01078
118464628 158065 None 0 Mouse Functional pEC50 = 5.1 5.1 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 514 6 0 4 7.7 COc1cc(C2CCCc3nc(SCc4cc(F)ccc4F)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4084863 158065 None 0 Mouse Functional pEC50 = 5.1 5.1 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 514 6 0 4 7.7 COc1cc(C2CCCc3nc(SCc4cc(F)ccc4F)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
73346391 92777 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 548 6 0 2 8.3 O=C(c1ccc(Cl)cc1)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
CHEMBL2435938 92777 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 548 6 0 2 8.3 O=C(c1ccc(Cl)cc1)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
71540073 87325 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 437 7 2 6 2.4 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1021/ml300277t
CHEMBL2331648 87325 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 437 7 2 6 2.4 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1021/ml300277t
118694344 195706 None 0 Human Functional pEC50 = 7.1 7.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5409356 195706 None 0 Human Functional pEC50 = 7.1 7.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 443 8 0 5 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
71540073 87325 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 437 7 2 6 2.4 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1016/j.bmcl.2012.12.076
CHEMBL2331648 87325 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 437 7 2 6 2.4 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1016/j.bmcl.2012.12.076
136166936 91638 None 0 Human Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
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 Human Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
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
137645502 157750 None 0 Human Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 490 7 0 7 5.8 COc1ccc(C2(C)CCCc3nc(SCc4ncccn4)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4081476 157750 None 0 Human Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 490 7 0 7 5.8 COc1ccc(C2(C)CCCc3nc(SCc4ncccn4)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
118728411 117740 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 404 5 2 2 6.1 CC[C@H]1C[C@@H]2[C@H](CC[C@@]3(C)[C@H]2CC[C@@H]3[C@H](C)CCC(=O)O)[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1016/j.bmc.2015.01.048
CHEMBL3401353 117740 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 404 5 2 2 6.1 CC[C@H]1C[C@@H]2[C@H](CC[C@@]3(C)[C@H]2CC[C@@H]3[C@H](C)CCC(=O)O)[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1016/j.bmc.2015.01.048
118586280 158379 None 0 Human Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 493 6 0 4 7.7 CN(c1ccc(Cl)c(Cl)c1)c1cnc(SCc2c(F)cccc2F)n1-c1ccc(F)cc1 10.1021/acs.jmedchem.6b01873
CHEMBL4088938 158379 None 0 Human Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 493 6 0 4 7.7 CN(c1ccc(Cl)c(Cl)c1)c1cnc(SCc2c(F)cccc2F)n1-c1ccc(F)cc1 10.1021/acs.jmedchem.6b01873
90654570 109994 None 0 Mouse Functional pEC50 = 6.1 6.1 -2 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 342 5 1 4 2.5 Cc1ccnc(N2CCC[C@@H](C(=O)NCCc3ccc(F)cc3)C2)n1 10.1021/jm401731q
CHEMBL3234551 109994 None 0 Mouse Functional pEC50 = 6.1 6.1 -2 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 342 5 1 4 2.5 Cc1ccnc(N2CCC[C@@H](C(=O)NCCc3ccc(F)cc3)C2)n1 10.1021/jm401731q
447715 199383 None 50 Human Functional pEC50 = 6.1 6.1 6 7
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
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/jm070633p
CHEMBL566315 199383 None 50 Human Functional pEC50 = 6.1 6.1 6 7
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
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/jm070633p
118694385 196820 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
CHEMBL5432845 196820 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
11258221 158968 None 0 Human Functional pEC50 = 4.1 4.1 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 404 3 3 3 4.3 C[C@H]([C@H]1C[C@H]1C(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
CHEMBL409510 158968 None 0 Human Functional pEC50 = 4.1 4.1 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 404 3 3 3 4.3 C[C@H]([C@H]1C[C@H]1C(=O)O)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
126016 97504 None 4 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 390 4 2 2 5.8 CC1C[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]12 10.1021/jm7015864
CHEMBL270105 97504 None 4 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 390 4 2 2 5.8 CC1C[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]12 10.1021/jm7015864
90654583 110007 None 0 Human Functional pEC50 = 7.1 7.1 2 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 447 6 1 7 2.0 Cc1cc(N2CCN(C)CC2)nc(N2CCC[C@@H](C(=O)NCCc3ccc(C#N)cc3)C2)n1 10.1021/jm401731q
CHEMBL3234564 110007 None 0 Human Functional pEC50 = 7.1 7.1 2 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 447 6 1 7 2.0 Cc1cc(N2CCN(C)CC2)nc(N2CCC[C@@H](C(=O)NCCc3ccc(C#N)cc3)C2)n1 10.1021/jm401731q
71459276 83034 None 0 Mouse Functional pEC50 = 7.1 7.1 -10 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 441 5 0 4 6.1 CCCN1CCN(C(=O)c2cnccc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
CHEMBL2181236 83034 None 0 Mouse Functional pEC50 = 7.1 7.1 -10 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 441 5 0 4 6.1 CCCN1CCN(C(=O)c2cnccc2Oc2cc(Cl)ccc2Cl)c2ccccc21 10.1021/jm301071h
155339369 182888 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 406 5 2 3 5.1 CO[C@@H]1C[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]21 10.1039/d0md00425a
CHEMBL4790399 182888 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 406 5 2 3 5.1 CO[C@@H]1C[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]21 10.1039/d0md00425a
447715 199383 None 50 Human Functional pEC50 = 6.1 6.1 6 7
Agonist activity at TGR5 (unknown origin)Agonist activity at 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 10.1016/j.ejmech.2023.115143
CHEMBL566315 199383 None 50 Human Functional pEC50 = 6.1 6.1 6 7
Agonist activity at TGR5 (unknown origin)Agonist activity at 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 10.1016/j.ejmech.2023.115143
137653533 158855 None 0 Mouse Functional pEC50 = 6.1 6.1 48 2
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 702 16 5 9 5.3 COc1ccc(SCc2cnc(SCc3c(F)cc(C(=O)NC(CCCNC(=N)N)C(=O)O)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4094009 158855 None 0 Mouse Functional pEC50 = 6.1 6.1 48 2
Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 702 16 5 9 5.3 COc1ccc(SCc2cnc(SCc3c(F)cc(C(=O)NC(CCCNC(=N)N)C(=O)O)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
172444492 195338 None 0 Human Functional pEC50 = 4.1 4.1 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 510 7 1 5 6.0 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC(=O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)OCc4ccccc4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
CHEMBL5401550 195338 None 0 Human Functional pEC50 = 4.1 4.1 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 510 7 1 5 6.0 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC(=O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)OCc4ccccc4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
126673452 161247 None 0 Human Functional pEC50 = 7.1 7.1 -257 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human 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 Human Functional pEC50 = 7.1 7.1 -257 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human 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 Human Functional pEC50 = 7.1 7.1 -257 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human 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
164613452 185047 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 564 6 1 4 7.9 CCCS(=O)(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
CHEMBL4853647 185047 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 564 6 1 4 7.9 CCCS(=O)(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
118464803 155874 None 0 Human Functional pEC50 = 6.1 6.1 -15 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 525 7 0 6 6.6 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cncc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4059508 155874 None 0 Human Functional pEC50 = 6.1 6.1 -15 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 525 7 0 6 6.6 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cncc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
44372731 54412 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 362 3 2 2 5.1 CC(CC(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
CHEMBL160902 54412 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 362 3 2 2 5.1 CC(CC(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/jm7015864
118694353 196488 None 0 Mouse Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 429 7 1 5 3.7 COc1ccccc1COC(=O)C1=C(C)N(CCO)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5425096 196488 None 0 Mouse Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 429 7 1 5 3.7 COc1ccccc1COC(=O)C1=C(C)N(CCO)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
44626704 200187 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 525 4 1 4 8.0 C=C(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC/C(=N\OC(=O)CC)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/jm900872z
CHEMBL571482 200187 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 525 4 1 4 8.0 C=C(C)[C@@H]1CC[C@]2(C(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC/C(=N\OC(=O)CC)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/jm900872z
118577093 158129 None 0 Human Functional pEC50 = 5.1 5.1 -8 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 497 9 0 7 6.2 COc1ccc(-n2c(N(C)c3ccc(OC)c(OC)c3)cnc2SCc2c(F)cccc2F)cc1 10.1021/acs.jmedchem.6b01873
CHEMBL4085777 158129 None 0 Human Functional pEC50 = 5.1 5.1 -8 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 497 9 0 7 6.2 COc1ccc(-n2c(N(C)c3ccc(OC)c(OC)c3)cnc2SCc2c(F)cccc2F)cc1 10.1021/acs.jmedchem.6b01873
118464729 157041 None 0 Mouse Functional pEC50 = 6.1 6.1 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 532 6 0 5 7.4 COc1cc(C2OCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4072719 157041 None 0 Mouse Functional pEC50 = 6.1 6.1 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 532 6 0 5 7.4 COc1cc(C2OCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
90644445 112284 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 616 8 1 9 4.9 CCOC(=O)CNC(=O)c1oc2cc(Cl)c(C(=O)Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2c1C 10.1016/j.ejmech.2014.05.031
CHEMBL3290727 112284 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 616 8 1 9 4.9 CCOC(=O)CNC(=O)c1oc2cc(Cl)c(C(=O)Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc2c1C 10.1016/j.ejmech.2014.05.031
71541721 87321 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 367 6 2 5 1.8 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(C)cc1)CC2 10.1021/ml300277t
CHEMBL2331644 87321 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 367 6 2 5 1.8 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(C)cc1)CC2 10.1021/ml300277t
156011870 177425 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 427 6 2 3 6.3 C=CCCC[C@]1(O)C[C@H]2[C@@H]3CC[C@H]([C@H](C)CC#N)[C@@]3(C)CC[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1021/acsmedchemlett.9b00636
CHEMBL4637054 177425 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assayAgonist activity at human GPBAR1 receptor expressed in HEK293T cells after 18 hrs by cAMP response element driven renilla-luciferase dual reporter gene assay
ChEMBL 427 6 2 3 6.3 C=CCCC[C@]1(O)C[C@H]2[C@@H]3CC[C@H]([C@H](C)CC#N)[C@@]3(C)CC[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 10.1021/acsmedchemlett.9b00636
44457500 155864 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 402 6 1 1 7.6 CCC[C@H]1C[C@@H]2CCCC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)O)[C@H]12 10.1021/jm7015864
CHEMBL405879 155864 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 402 6 1 1 7.6 CCC[C@H]1C[C@@H]2CCCC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)O)[C@H]12 10.1021/jm7015864
71626228 118892 None 0 Mouse Functional pEC50 = 5.1 5.1 -1 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 610 10 0 7 5.8 CCOC(=O)CN(C)C(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421898 118892 None 0 Mouse Functional pEC50 = 5.1 5.1 -1 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 610 10 0 7 5.8 CCOC(=O)CN(C)C(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
44626600 200191 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 551 6 1 4 8.6 C=CCCC(=O)O/N=C1\CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(=C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/jm900872z
CHEMBL571515 200191 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assayAgonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
ChEMBL 551 6 1 4 8.6 C=CCCC(=O)O/N=C1\CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(=C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/jm900872z
145975890 163898 None 0 Human Functional pEC50 = 7.1 7.1 -19 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 739 16 7 10 2.3 O=C(NCCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4206078 163898 None 0 Human Functional pEC50 = 7.1 7.1 -19 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 739 16 7 10 2.3 O=C(NCCCCCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
118103697 164052 None 0 Human Functional pEC50 = 7.1 7.1 -7 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 696 13 5 10 1.7 CN(C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)C(=O)CCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4207801 164052 None 0 Human Functional pEC50 = 7.1 7.1 -7 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 696 13 5 10 1.7 CN(C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)C(=O)CCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
118093476 164198 None 0 Human Functional pEC50 = 7.1 7.1 -39 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 780 14 6 13 2.1 Cn1c(C(=O)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)cnc1SCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
CHEMBL4209669 164198 None 0 Human Functional pEC50 = 7.1 7.1 -39 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 780 14 6 13 2.1 Cn1c(C(=O)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)cnc1SCc1cc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/acs.jmedchem.8b00308
44605617 200775 None 1 Human Functional pEC50 = 7.1 7.1 5 2
Agonist activity at human TGR5 expressed in melanophores assessed as melanosome dispersion by melanophore assayAgonist activity at human TGR5 expressed in melanophores assessed as melanosome dispersion by melanophore assay
ChEMBL 374 3 0 3 5.5 Cc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1Cl 10.1021/jm901434t
CHEMBL576138 200775 None 1 Human Functional pEC50 = 7.1 7.1 5 2
Agonist activity at human TGR5 expressed in melanophores assessed as melanosome dispersion by melanophore assayAgonist activity at human TGR5 expressed in melanophores assessed as melanosome dispersion by melanophore assay
ChEMBL 374 3 0 3 5.5 Cc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1Cl 10.1021/jm901434t
145007569 195011 None 0 Human Functional pEC50 = 7.1 7.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(CC2CCCO2)C(=O)CC1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
CHEMBL5394911 195011 None 0 Human Functional pEC50 = 7.1 7.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(CC2CCCO2)C(=O)CC1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
44605617 200775 None 1 Human Functional pEC50 = 7.1 7.1 5 2
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 374 3 0 3 5.5 Cc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1Cl 10.1016/j.bmcl.2010.01.003
CHEMBL576138 200775 None 1 Human Functional pEC50 = 7.1 7.1 5 2
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 374 3 0 3 5.5 Cc1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1Cl 10.1016/j.bmcl.2010.01.003
46232568 203555 None 0 Human Functional pEC50 = 7.1 7.1 - 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 340 3 0 3 4.9 Cc1cccc(-c2noc(C)c2C(=O)N(C)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2010.01.003
CHEMBL602892 203555 None 0 Human Functional pEC50 = 7.1 7.1 - 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 340 3 0 3 4.9 Cc1cccc(-c2noc(C)c2C(=O)N(C)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2010.01.003
118694573 196130 None 0 Mouse Functional pEC50 = 7.1 7.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5417359 196130 None 0 Mouse Functional pEC50 = 7.1 7.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
2733768 161394 None 21 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 499 7 4 5 3.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@@]21C 10.1021/jm7015864
CHEMBL412272 161394 None 21 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 499 7 4 5 3.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@@]21C 10.1021/jm7015864
118104385 163678 None 0 Human Functional pEC50 = 6.1 6.1 -5 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 648 13 6 10 0.7 O=C(CCc1ccc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)c1)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
CHEMBL4203321 163678 None 0 Human Functional pEC50 = 6.1 6.1 -5 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 648 13 6 10 0.7 O=C(CCc1ccc(Cl)c(CN2CSC[C@H]2C(=O)N2CCN(C3CC3)c3ccccc32)c1)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO 10.1021/acs.jmedchem.8b00308
89651284 164741 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 432 6 0 3 5.6 CN(C(=O)[C@@H]1CCCN1Cc1cc(Cl)ccc1Cl)c1ccccc1OC1CCC1 10.1021/acs.jmedchem.8b00308
CHEMBL4216520 164741 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 432 6 0 3 5.6 CN(C(=O)[C@@H]1CCCN1Cc1cc(Cl)ccc1Cl)c1ccccc1OC1CCC1 10.1021/acs.jmedchem.8b00308
118093506 164817 None 0 Human Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 445 4 1 4 3.9 O=C([C@@H]1C[C@H](O)CN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4217450 164817 None 0 Human Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 445 4 1 4 3.9 O=C([C@@H]1C[C@H](O)CN1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118694581 194966 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 393 5 0 3 4.3 C#CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5394245 194966 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 393 5 0 3 4.3 C#CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
42854553 195752 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 445 6 0 3 5.9 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1Cc1ccccc1 10.1021/acs.jmedchem.2c01881
CHEMBL5410102 195752 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 445 6 0 3 5.9 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1Cc1ccccc1 10.1021/acs.jmedchem.2c01881
118694569 196448 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 441 9 0 4 4.8 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCCCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5424150 196448 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 441 9 0 4 4.8 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCCCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694570 196470 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 471 8 0 6 4.1 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C(=O)OC)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5424612 196470 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 471 8 0 6 4.1 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C(=O)OC)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694393 196611 None 0 Human Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C(F)(F)F)cc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5427795 196611 None 0 Human Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccc(C(F)(F)F)cc2)=C1C 10.1021/acs.jmedchem.2c01881
118694453 196864 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 409 6 0 3 5.2 C=C(C)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5433643 196864 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 409 6 0 3 5.2 C=C(C)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
42854551 196992 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 395 6 0 3 4.9 C=CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5436242 196992 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 395 6 0 3 4.9 C=CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694423 197114 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 419 7 0 4 4.7 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCC2CCCCC2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5439109 197114 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 419 7 0 4 4.7 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCC2CCCCC2)=C1C 10.1021/acs.jmedchem.2c01881
46232697 202051 None 0 Human Functional pEC50 = 6.1 6.1 - 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 416 5 0 3 6.8 CC(C)c1onc(-c2ccccc2Cl)c1C(=O)N(c1ccc(Cl)cc1)C(C)C 10.1016/j.bmcl.2010.01.003
CHEMBL592645 202051 None 0 Human Functional pEC50 = 6.1 6.1 - 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 416 5 0 3 6.8 CC(C)c1onc(-c2ccccc2Cl)c1C(=O)N(c1ccc(Cl)cc1)C(C)C 10.1016/j.bmcl.2010.01.003
118103736 164331 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 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 453 5 0 4 5.1 O=C([C@@H]1CSCN1Cc1cc(C2CC2)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4211208 164331 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 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 453 5 0 4 5.1 O=C([C@@H]1CSCN1Cc1cc(C2CC2)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1021/acs.jmedchem.8b00308
118694352 195534 None 0 Mouse Functional pEC50 = 6.1 6.1 -3 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 457 9 0 5 4.7 COCCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5405469 195534 None 0 Mouse Functional pEC50 = 6.1 6.1 -3 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 457 9 0 5 4.7 COCCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2OC)=C1C 10.1021/acs.jmedchem.2c01881
42854553 195752 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 445 6 0 3 5.9 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1Cc1ccccc1 10.1021/acs.jmedchem.2c01881
CHEMBL5410102 195752 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 445 6 0 3 5.9 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1Cc1ccccc1 10.1021/acs.jmedchem.2c01881
118694450 195753 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C(F)(F)F)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5410122 195753 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C(F)(F)F)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694566 195890 None 0 Mouse Functional pEC50 = 6.1 6.1 -3 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(F)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5412722 195890 None 0 Mouse Functional pEC50 = 6.1 6.1 -3 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(F)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694570 196470 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 471 8 0 6 4.1 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C(=O)OC)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5424612 196470 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 471 8 0 6 4.1 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C(=O)OC)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694353 196488 None 0 Mouse Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 429 7 1 5 3.7 COc1ccccc1COC(=O)C1=C(C)N(CCO)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5425096 196488 None 0 Mouse Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 429 7 1 5 3.7 COc1ccccc1COC(=O)C1=C(C)N(CCO)C(=O)CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
118694404 196503 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 397 6 0 3 5.1 CCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5425461 196503 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 397 6 0 3 5.1 CCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694385 196820 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
CHEMBL5432845 196820 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(C[C@@H]2CCCO2)C(=O)C[C@@H]1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
118093511 164120 None 0 Human Functional pEC50 = 5.1 5.1 -3 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 388 3 0 2 4.9 O=C([C@@H]1CCCN1Cc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 10.1021/acs.jmedchem.8b00308
CHEMBL4208655 164120 None 0 Human Functional pEC50 = 5.1 5.1 -3 2
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level by HTRF assay
ChEMBL 388 3 0 2 4.9 O=C([C@@H]1CCCN1Cc1cc(Cl)ccc1Cl)N1CCCc2ccccc21 10.1021/acs.jmedchem.8b00308
46232528 203473 None 0 Human Functional pEC50 = 5.1 5.1 - 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 384 4 0 5 4.4 COC(=O)c1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL602273 203473 None 0 Human Functional pEC50 = 5.1 5.1 - 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 384 4 0 5 4.4 COC(=O)c1ccc(N(C)C(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2010.01.003
46232413 203876 None 0 Human Functional pEC50 = 5.1 5.1 - 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 382 3 0 3 5.9 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(C(C)(C)C)cc1 10.1016/j.bmcl.2010.01.003
CHEMBL604734 203876 None 0 Human Functional pEC50 = 5.1 5.1 - 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 382 3 0 3 5.9 Cc1onc(-c2ccccc2Cl)c1C(=O)N(C)c1ccc(C(C)(C)C)cc1 10.1016/j.bmcl.2010.01.003
118694580 196916 None 0 Mouse Functional pEC50 = 5.1 5.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 341 4 1 3 3.6 O=C1CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=CN1 10.1021/acs.jmedchem.2c01881
CHEMBL5434777 196916 None 0 Mouse Functional pEC50 = 5.1 5.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 341 4 1 3 3.6 O=C1CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=CN1 10.1021/acs.jmedchem.2c01881
90654574 109998 None 0 Human Functional pEC50 = 8.1 8.1 4 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 376 5 1 4 3.2 Cc1nc(N2CCC[C@@H](C(=O)NCCc3ccc(Cl)cc3)C2)ncc1F 10.1021/jm401731q
CHEMBL3234555 109998 None 0 Human Functional pEC50 = 8.1 8.1 4 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 376 5 1 4 3.2 Cc1nc(N2CCC[C@@H](C(=O)NCCc3ccc(Cl)cc3)C2)ncc1F 10.1021/jm401731q
90654564 110019 None 0 Human Functional pEC50 = 8.1 8.1 -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 487 6 1 7 2.4 CN1CCN(c2cc(N3CCC[C@H]3C(=O)NCCc3ccc(C#N)cc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
CHEMBL3234575 110019 None 0 Human Functional pEC50 = 8.1 8.1 -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 487 6 1 7 2.4 CN1CCN(c2cc(N3CCC[C@H]3C(=O)NCCc3ccc(C#N)cc3)nc(C(F)(F)F)n2)CC1 10.1021/jm401731q
76318387 106084 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 417 5 0 5 4.9 COc1cccc(-c2noc(C3CC3)c2C(=O)N(C)c2ccc(C(F)(F)F)nc2)c1 10.1039/C2MD20174G
CHEMBL3132971 106084 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometryAgonist activity at human recombinant TGR5 receptor expressed in doxycycline-induced CHO cells assessed as cAMP accumulation after 30 mins by spectrophotometry
ChEMBL 417 5 0 5 4.9 COc1cccc(-c2noc(C3CC3)c2C(=O)N(C)c2ccc(C(F)(F)F)nc2)c1 10.1039/C2MD20174G
90644455 112290 None 0 Human Functional pEC50 = 8.1 8.1 -1 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 614 9 1 8 5.9 CCOC(=O)CNC(=O)/C=C/c1oc2ccc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c2c1C 10.1016/j.ejmech.2014.05.031
CHEMBL3290733 112290 None 0 Human Functional pEC50 = 8.1 8.1 -1 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 614 9 1 8 5.9 CCOC(=O)CNC(=O)/C=C/c1oc2ccc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c2c1C 10.1016/j.ejmech.2014.05.031
90644456 112288 None 0 Human Functional pEC50 = 8.1 8.1 1 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 557 7 0 7 6.8 CCOC(=O)/C=C/c1oc2ccc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c2c1C 10.1016/j.ejmech.2014.05.031
CHEMBL3290731 112288 None 0 Human Functional pEC50 = 8.1 8.1 1 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 557 7 0 7 6.8 CCOC(=O)/C=C/c1oc2ccc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c2c1C 10.1016/j.ejmech.2014.05.031
136167004 91637 None 4 Human Functional pEC50 = 7.1 7.1 1 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
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
CHEMBL2407930 91637 None 4 Human Functional pEC50 = 7.1 7.1 1 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
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
164618838 185892 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 530 4 1 4 8.4 CCOC(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
CHEMBL4866697 185892 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 530 4 1 4 8.4 CCOC(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
42854553 195752 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 445 6 0 3 5.9 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1Cc1ccccc1 10.1021/acs.jmedchem.2c01881
CHEMBL5410102 195752 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 445 6 0 3 5.9 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1Cc1ccccc1 10.1021/acs.jmedchem.2c01881
118694569 196448 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 441 9 0 4 4.8 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCCCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5424150 196448 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 441 9 0 4 4.8 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCCCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694570 196470 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 471 8 0 6 4.1 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C(=O)OC)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5424612 196470 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 471 8 0 6 4.1 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C(=O)OC)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694453 196864 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 409 6 0 3 5.2 C=C(C)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5433643 196864 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 409 6 0 3 5.2 C=C(C)CN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
42854551 196992 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 395 6 0 3 4.9 C=CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5436242 196992 None 0 Human Functional pEC50 = 6.1 6.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 395 6 0 3 4.9 C=CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694450 195753 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C(F)(F)F)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5410122 195753 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 481 7 0 4 5.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C(F)(F)F)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694566 195890 None 0 Mouse Functional pEC50 = 6.1 6.1 -3 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(F)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5412722 195890 None 0 Mouse Functional pEC50 = 6.1 6.1 -3 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 431 7 0 4 4.5 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(F)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694570 196470 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 471 8 0 6 4.1 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C(=O)OC)c2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5424612 196470 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 471 8 0 6 4.1 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2cccc(C(=O)OC)c2)=C1C 10.1021/acs.jmedchem.2c01881
118694404 196503 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 397 6 0 3 5.1 CCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5425461 196503 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 397 6 0 3 5.1 CCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
71626834 118894 None 0 Human Functional pEC50 = 5.1 5.1 -2 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 582 10 2 6 5.3 O=C(O)CCNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421900 118894 None 0 Human Functional pEC50 = 5.1 5.1 -2 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 582 10 2 6 5.3 O=C(O)CCNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
118735265 118893 None 0 Mouse Functional pEC50 = 5.1 5.1 1 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 568 9 2 6 4.9 O=C(O)CNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
CHEMBL3421899 118893 None 0 Mouse Functional pEC50 = 5.1 5.1 1 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 568 9 2 6 4.9 O=C(O)CNC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc32)cc1Cl 10.1021/jm500829b
172450361 195585 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 436 5 2 5 4.2 COC(=O)CC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](OC)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@]12C 10.1016/j.bmc.2023.117418
CHEMBL5406515 195585 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 436 5 2 5 4.2 COC(=O)CC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](OC)C[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@]12C 10.1016/j.bmc.2023.117418
156705085 183093 None 0 Human Functional pEC50 = 7.1 7.1 2 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 543 10 0 9 5.0 COCCOCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4793377 183093 None 0 Human Functional pEC50 = 7.1 7.1 2 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 543 10 0 9 5.0 COCCOCOC(=O)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
118464738 156806 None 0 Mouse Functional pEC50 = 6.1 6.1 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 564 6 0 4 8.9 COc1cc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)c(Cl)c4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4070183 156806 None 0 Mouse Functional pEC50 = 6.1 6.1 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 564 6 0 4 8.9 COc1cc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)c(Cl)c4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
90654576 110000 None 0 Mouse Functional pEC50 = 5.1 5.1 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 344 5 1 4 2.7 O=C(NCCc1ccc(Cl)cc1)[C@@H]1CCCN(c2ccncn2)C1 10.1021/jm401731q
CHEMBL3234557 110000 None 0 Mouse Functional pEC50 = 5.1 5.1 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 344 5 1 4 2.7 O=C(NCCc1ccc(Cl)cc1)[C@@H]1CCCN(c2ccncn2)C1 10.1021/jm401731q
90644446 112279 None 0 Mouse Functional pEC50 = 7.1 7.1 -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 559 7 0 8 5.4 COC(=O)CCc1coc2cc(Cl)c(C(=O)Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
CHEMBL3290722 112279 None 0 Mouse Functional pEC50 = 7.1 7.1 -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 559 7 0 8 5.4 COC(=O)CCc1coc2cc(Cl)c(C(=O)Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2014.05.031
126673489 156763 None 0 Mouse Functional pEC50 = 7.1 7.1 13 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 571 11 0 8 6.5 COC(=O)CCc1nc(SCc2c(F)cccc2F)n(-c2ccc(F)cc2)c1N(C)c1ccc(OC)c(OC)c1 10.1021/acs.jmedchem.6b01873
CHEMBL4069569 156763 None 0 Mouse Functional pEC50 = 7.1 7.1 13 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 571 11 0 8 6.5 COC(=O)CCc1nc(SCc2c(F)cccc2F)n(-c2ccc(F)cc2)c1N(C)c1ccc(OC)c(OC)c1 10.1021/acs.jmedchem.6b01873
45483949 3582 None 33 Human Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1021/ml200256d
7048 3582 None 33 Human Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1021/ml200256d
CHEMBL567640 3582 None 33 Human Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1021/ml200256d
44605418 199214 None 23 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay
ChEMBL 450 5 4 4 4.3 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)C[C@@H](C)C(=O)O)[C@@H]2[C@@H]1O 10.1021/jm901390p
CHEMBL565278 199214 None 23 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assayAgonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay
ChEMBL 450 5 4 4 4.3 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)C[C@@H](C)C(=O)O)[C@@H]2[C@@H]1O 10.1021/jm901390p
45483949 3582 None 33 Human Functional pEC50 = 6.1 6.1 -2 2
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 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.bmc.2020.115972
7048 3582 None 33 Human Functional pEC50 = 6.1 6.1 -2 2
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 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.bmc.2020.115972
CHEMBL567640 3582 None 33 Human Functional pEC50 = 6.1 6.1 -2 2
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 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.bmc.2020.115972
73349426 92767 None 0 Mouse Functional pEC50 = 6.1 6.1 -12 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 478 5 1 3 5.4 O=S(=O)(NCc1cnccc1-c1ccccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435927 92767 None 0 Mouse Functional pEC50 = 6.1 6.1 -12 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 478 5 1 3 5.4 O=S(=O)(NCc1cnccc1-c1ccccc1F)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
137661039 159583 None 0 Human Functional pEC50 = 5.1 5.1 -21 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 653 13 2 9 5.5 COc1ccc(SCc2cnc(SCc3c(F)cc(C(=O)NCCS(=O)(=O)O)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
CHEMBL4101738 159583 None 0 Human Functional pEC50 = 5.1 5.1 -21 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric methodAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level after 40 mins by mass spectrometric method
ChEMBL 653 13 2 9 5.5 COc1ccc(SCc2cnc(SCc3c(F)cc(C(=O)NCCS(=O)(=O)O)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2017.02.069
71540078 87330 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 422 6 1 5 2.6 CCc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1021/ml300277t
CHEMBL2331653 87330 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 422 6 1 5 2.6 CCc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(OC(F)(F)F)cc1)CC2 10.1021/ml300277t
118694573 196130 None 0 Mouse Functional pEC50 = 7.1 7.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
CHEMBL5417359 196130 None 0 Mouse Functional pEC50 = 7.1 7.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 469 7 0 5 4.9 COc1ccccc1COC(=O)C1=C(C)N(C[C@H]2CCCO2)C(=O)C[C@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c01881
164623929 186347 None 0 Human Functional pEC50 = 7.1 7.1 31 2
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 528 5 1 3 8.5 CCCC(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
CHEMBL4873587 186347 None 0 Human Functional pEC50 = 7.1 7.1 31 2
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 528 5 1 3 8.5 CCCC(=O)O[C@@H]1CC[C@@]2(C)[C@@H](CC[C@]3(C)[C@@H]2CC[C@@H]2[C@H]4[C@H](C(C)C)CC[C@]4(C(=O)O)CC[C@]23C)C1(C)C 10.1021/acs.jmedchem.1c00851
156705120 181979 None 0 Human Functional pEC50 = 7.1 7.1 41 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 503 6 0 7 5.6 O=C(OCCl)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
CHEMBL4778884 181979 None 0 Human Functional pEC50 = 7.1 7.1 41 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 503 6 0 7 5.6 O=C(OCCl)c1coc2ccc(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)cc12 10.1016/j.ejmech.2020.112619
155669600 179882 None 0 Mouse Functional pEC50 = 6.1 6.1 -87 2
Agonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assayAgonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay
ChEMBL 426 4 0 4 4.9 O=C(c1cncn1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
CHEMBL4744582 179882 None 0 Mouse Functional pEC50 = 6.1 6.1 -87 2
Agonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assayAgonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay
ChEMBL 426 4 0 4 4.9 O=C(c1cncn1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
71541720 87320 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 353 6 2 5 1.5 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccccc1)CC2 10.1021/ml300277t
CHEMBL2331643 87320 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 353 6 2 5 1.5 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccccc1)CC2 10.1021/ml300277t
447715 199383 None 50 Human Functional pEC50 = 6.1 6.1 6 7
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay
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/acsmedchemlett.7b00318
CHEMBL566315 199383 None 50 Human Functional pEC50 = 6.1 6.1 6 7
Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assayAgonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay
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/acsmedchemlett.7b00318
172471915 197194 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 492 8 4 4 5.6 CCCC[C@]1(O)[C@@H]2[C@H](C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)O)CC[C@@H]23)[C@@]2(C)CC[C@@H](O)C[C@H]2[C@H]1CC 10.1016/j.ejmech.2023.115851
CHEMBL5440980 197194 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 492 8 4 4 5.6 CCCC[C@]1(O)[C@@H]2[C@H](C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)O)CC[C@@H]23)[C@@]2(C)CC[C@@H](O)C[C@H]2[C@H]1CC 10.1016/j.ejmech.2023.115851
130361991 169799 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 430 4 2 5 4.9 Cc1noc(CC[C@@H](C)[C@H]2CC[C@H]3[C@H]4[C@H](CC[C@@]32C)[C@@]2(C)CC[C@@H](O)C[C@H]2C[C@H]4O)n1 10.1021/acs.jmedchem.9b00770
CHEMBL4437850 169799 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 430 4 2 5 4.9 Cc1noc(CC[C@@H](C)[C@H]2CC[C@H]3[C@H]4[C@H](CC[C@@]32C)[C@@]2(C)CC[C@@H](O)C[C@H]2C[C@H]4O)n1 10.1021/acs.jmedchem.9b00770
71561619 87674 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 430 4 0 5 5.2 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N1CCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336227 87674 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 430 4 0 5 5.2 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N1CCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
439763 158218 None 15 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 483 7 3 4 4.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/acs.jmedchem.9b00770
CHEMBL408701 158218 None 15 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assayAgonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
ChEMBL 483 7 3 4 4.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1021/acs.jmedchem.9b00770
90644447 112294 None 0 Mouse Functional pEC50 = 7.1 7.1 -2 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 616 10 1 8 5.8 CCOC(=O)CNC(=O)CCc1oc2ccc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c2c1C 10.1016/j.ejmech.2014.05.031
CHEMBL3290737 112294 None 0 Mouse Functional pEC50 = 7.1 7.1 -2 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 616 10 1 8 5.8 CCOC(=O)CNC(=O)CCc1oc2ccc(Cl)c(Oc3ccncc3C(=O)N3CCN(C4CC4)c4ccccc43)c2c1C 10.1016/j.ejmech.2014.05.031
45483949 3582 None 33 Human Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2023.115851
7048 3582 None 33 Human Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2023.115851
CHEMBL567640 3582 None 33 Human Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2023.115851
219833 97463 None 33 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 320 1 2 2 4.4 C[C@H](O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@]12C 10.1021/jm7015864
CHEMBL269897 97463 None 33 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 320 1 2 2 4.4 C[C@H](O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@]12C 10.1021/jm7015864
73353940 92772 None 0 Mouse Functional pEC50 = 6.1 6.1 -27 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 582 6 0 4 7.0 O=C(c1ccccc1)N(Cc1cnccc1-c1ccccc1F)S(=O)(=O)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435932 92772 None 0 Mouse Functional pEC50 = 6.1 6.1 -27 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 582 6 0 4 7.0 O=C(c1ccccc1)N(Cc1cnccc1-c1ccccc1F)S(=O)(=O)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
126673504 157707 None 0 Human Functional pEC50 = 7.1 7.1 -10 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 511 10 0 6 6.9 C=CCN(c1ccc(OC)c(OC)c1)c1cnc(SCc2c(F)cccc2F)n1-c1ccc(F)cc1 10.1021/acs.jmedchem.6b01873
CHEMBL4081050 157707 None 0 Human Functional pEC50 = 7.1 7.1 -10 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 511 10 0 6 6.9 C=CCN(c1ccc(OC)c(OC)c1)c1cnc(SCc2c(F)cccc2F)n1-c1ccc(F)cc1 10.1021/acs.jmedchem.6b01873
118694580 196916 None 0 Mouse Functional pEC50 = 5.1 5.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 341 4 1 3 3.6 O=C1CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=CN1 10.1021/acs.jmedchem.2c01881
CHEMBL5434777 196916 None 0 Mouse Functional pEC50 = 5.1 5.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 341 4 1 3 3.6 O=C1CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=CN1 10.1021/acs.jmedchem.2c01881
164612114 184736 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 512 3 2 3 7.7 CC(C)[C@@H]1CC[C@]2(N)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
CHEMBL4849469 184736 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assayAgonist activity at N-terminal HA-tagged human TGR5 expressed in HEK293 cells assessed as reduction in intracellular cAMP levels incubated for 30 mins by Lance Ultra cAMP assay
ChEMBL 512 3 2 3 7.7 CC(C)[C@@H]1CC[C@]2(N)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@@H](OC(=O)NC6CC6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12 10.1021/acs.jmedchem.1c00851
5284055 97627 None 2 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 394 4 4 4 3.4 C[C@H](CCCO)[C@H]1CC[C@H]2[C@H]3[C@H](C[C@H](O)[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
CHEMBL270703 97627 None 2 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human TGR5 expressed in CHO cells by luciferase assayAgonist activity at human TGR5 expressed in CHO cells by luciferase assay
ChEMBL 394 4 4 4 3.4 C[C@H](CCCO)[C@H]1CC[C@H]2[C@H]3[C@H](C[C@H](O)[C@@]21C)[C@@]1(C)CC[C@@H](O)C[C@H]1C[C@H]3O 10.1021/jm7015864
70686470 77238 None 0 Human Functional pEC50 = 4.1 4.1 - 1
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
ChEMBL 436 5 4 4 4.1 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](C[C@@H](O)[C@@H]3[C@H](C)CCC(=O)O)[C@@H]2[C@@H]1O 10.1021/ml200256d
CHEMBL2062553 77238 None 0 Human Functional pEC50 = 4.1 4.1 - 1
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
ChEMBL 436 5 4 4 4.1 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](C[C@@H](O)[C@@H]3[C@H](C)CCC(=O)O)[C@@H]2[C@@H]1O 10.1021/ml200256d
CHEMBL2079385 77238 None 0 Human Functional pEC50 = 4.1 4.1 - 1
Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysisAgonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
ChEMBL 436 5 4 4 4.1 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](C[C@@H](O)[C@@H]3[C@H](C)CCC(=O)O)[C@@H]2[C@@H]1O 10.1021/ml200256d
145007569 195011 None 0 Human Functional pEC50 = 7.1 7.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(CC2CCCO2)C(=O)CC1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
CHEMBL5394911 195011 None 0 Human Functional pEC50 = 7.1 7.1 1 2
Agonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at human TGR5 receptor expressed in HEK293 cells cotransfected with pCMV tag4b-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 470 7 0 6 4.3 COc1ccccc1COC(=O)C1=C(C)N(CC2CCCO2)C(=O)CC1c1ccc(Cl)nc1 10.1021/acs.jmedchem.2c01881
90654571 109995 None 0 Mouse Functional pEC50 = 7.1 7.1 -2 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 402 5 1 4 3.1 Cc1ccnc(N2CCC[C@@H](C(=O)NCCc3ccc(Br)cc3)C2)n1 10.1021/jm401731q
CHEMBL3234552 109995 None 0 Mouse Functional pEC50 = 7.1 7.1 -2 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 402 5 1 4 3.1 Cc1ccnc(N2CCC[C@@H](C(=O)NCCc3ccc(Br)cc3)C2)n1 10.1021/jm401731q
136166933 91649 None 0 Human Functional pEC50 = 6.1 6.1 3 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
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 Functional pEC50 = 6.1 6.1 3 2
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP productionAgonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
ChEMBL 394 5 1 3 5.6 Cc1ccccc1C(C/C(=N\O)c1ccncc1)c1ccc(Br)cc1 10.1016/j.bmcl.2013.06.017
3223370 109990 None 0 Human Functional pEC50 = 6.1 6.1 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 344 5 1 4 2.7 O=C(NCCc1ccc(Cl)cc1)C1CCCN(c2ncccn2)C1 10.1021/jm401731q
CHEMBL3234546 109990 None 0 Human Functional pEC50 = 6.1 6.1 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 344 5 1 4 2.7 O=C(NCCc1ccc(Cl)cc1)C1CCCN(c2ncccn2)C1 10.1021/jm401731q
118577011 157078 None 0 Human Functional pEC50 = 6.1 6.1 -20 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 489 7 0 5 7.0 COc1cc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)ccc1Cl 10.1021/acs.jmedchem.6b01873
CHEMBL4073081 157078 None 0 Human Functional pEC50 = 6.1 6.1 -20 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 489 7 0 5 7.0 COc1cc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)ccc1Cl 10.1021/acs.jmedchem.6b01873
118455249 156789 None 0 Mouse Functional pEC50 = 6.1 6.1 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 530 6 0 4 8.2 COc1cc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
CHEMBL4069934 156789 None 0 Mouse Functional pEC50 = 6.1 6.1 - 1
Agonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric methodAgonist activity at TGR5 in mouse STC1 cells assessed as increase in cAMP accumulation after 40 mins by mass spectrometric method
ChEMBL 530 6 0 4 8.2 COc1cc(C2CCCc3nc(SCc4c(F)cccc4Cl)n(-c4ccc(F)cc4)c32)ccc1Cl 10.1021/acsmedchemlett.7b00116
2733768 161394 None 21 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human TGR5 Y89A mutant expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assayAgonist activity at human TGR5 Y89A mutant expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assay
ChEMBL 499 7 4 5 3.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@@]21C 10.1016/j.ejmech.2015.09.024
CHEMBL412272 161394 None 21 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human TGR5 Y89A mutant expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assayAgonist activity at human TGR5 Y89A mutant expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assay
ChEMBL 499 7 4 5 3.4 C[C@H](CCC(=O)NCCS(=O)(=O)O)[C@H]1CC[C@H]2[C@@H]3CC[C@@H]4C[C@H](O)CC[C@]4(C)[C@H]3C[C@H](O)[C@@]21C 10.1016/j.ejmech.2015.09.024
172457880 196398 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 462 6 2 5 4.7 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)OC4CC4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
CHEMBL5422935 196398 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 462 6 2 5 4.7 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)OC4CC4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
73346390 92770 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 533 7 0 4 7.8 N#CC(c1cc(C(F)(F)F)cc(C(F)(F)F)c1)N(Cc1ccco1)Cc1cnccc1-c1ccccc1F 10.1016/j.ejmech.2013.07.050
CHEMBL2435930 92770 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 533 7 0 4 7.8 N#CC(c1cc(C(F)(F)F)cc(C(F)(F)F)c1)N(Cc1ccco1)Cc1cnccc1-c1ccccc1F 10.1016/j.ejmech.2013.07.050
71541722 87322 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 381 7 2 5 2.1 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(CC)cc1)CC2 10.1021/ml300277t
CHEMBL2331645 87322 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassayAgonist activity at human TGR5 expressed in deoxycycline-induced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
ChEMBL 381 7 2 5 2.1 CCNc1nc2c(c(C(N)=O)n1)CN(C(=O)CCc1ccc(CC)cc1)CC2 10.1021/ml300277t
155669600 179882 None 0 Human Functional pEC50 = 8.0 8.0 87 2
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 426 4 0 4 4.9 O=C(c1cncn1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
CHEMBL4744582 179882 None 0 Human Functional pEC50 = 8.0 8.0 87 2
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 426 4 0 4 4.9 O=C(c1cncn1Cc1cc(Cl)ccc1Cl)N1CCN(C2CC2)c2ccccc21 10.1016/j.bmc.2020.115972
118576918 161225 None 0 Mouse Functional pEC50 = 8.0 8.0 24 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 654 13 0 8 6.3 COc1ccc(N(C)c2cnc(SCc3c(F)cc(OCCC[N+]45CCN(CC4)CC5)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4078612 161225 None 0 Mouse Functional pEC50 = 8.0 8.0 24 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 654 13 0 8 6.3 COc1ccc(N(C)c2cnc(SCc3c(F)cc(OCCC[N+]45CCN(CC4)CC5)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4117224 161225 None 0 Mouse Functional pEC50 = 8.0 8.0 24 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 654 13 0 8 6.3 COc1ccc(N(C)c2cnc(SCc3c(F)cc(OCCC[N+]45CCN(CC4)CC5)cc3F)n2-c2ccc(F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
45483949 3582 None 33 Human Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1021/acs.jmedchem.6b01126
7048 3582 None 33 Human Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1021/acs.jmedchem.6b01126
CHEMBL567640 3582 None 33 Human Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1021/acs.jmedchem.6b01126
45483949 3582 None 33 Human Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assayAgonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2022.114652
7048 3582 None 33 Human Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assayAgonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2022.114652
CHEMBL567640 3582 None 33 Human Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assayAgonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assay
ChEMBL 450 5 4 4 4.3 CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@@H]([C@@]3(C)[C@H](C[C@@H]2[C@@]2([C@H]1C[C@H](O)CC2)C)O)[C@@H](C[C@@H](C(=O)O)C)C 10.1016/j.ejmech.2022.114652
118586279 155942 None 0 Human Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 535 8 0 6 7.2 COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(C(F)(F)F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
CHEMBL4060122 155942 None 0 Human Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assayAgonist activity at human TGR5 transfected in HEK293 cells assessed as cAMP accumulation after overnight incubation by luciferase reporter gene assay
ChEMBL 535 8 0 6 7.2 COc1ccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(C(F)(F)F)cc2)cc1OC 10.1021/acs.jmedchem.6b01873
118694374 194957 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 413 7 0 4 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5394113 194957 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 413 7 0 4 4.3 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694430 195107 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 383 5 0 3 4.7 CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5396796 195107 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 383 5 0 3 4.7 CCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
42854553 195752 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 445 6 0 3 5.9 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1Cc1ccccc1 10.1021/acs.jmedchem.2c01881
CHEMBL5410102 195752 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 445 6 0 3 5.9 CC1=C(C(=O)OCc2ccccc2)C(c2ccc(Cl)cc2)CC(=O)N1Cc1ccccc1 10.1021/acs.jmedchem.2c01881
118694569 196448 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 441 9 0 4 4.8 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCCCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5424150 196448 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 441 9 0 4 4.8 COCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCCCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
118694370 197118 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 411 7 0 3 5.5 CCCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
CHEMBL5439183 197118 None 0 Mouse Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assayAgonist activity at mouse TGR5 receptor expressed in HEK293 cells cotransfected with pCMV AC6-TGR5 assessed as activation of intracellular cAMP production incubated overnight by luciferase reporter gene assay
ChEMBL 411 7 0 3 5.5 CCCCN1C(=O)CC(c2ccc(Cl)cc2)C(C(=O)OCc2ccccc2)=C1C 10.1021/acs.jmedchem.2c01881
172460571 196505 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 450 6 4 4 4.6 CCC[C@@]1(O)C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)O)CC[C@H]3[C@@H]21 10.1016/j.ejmech.2023.115851
CHEMBL5425544 196505 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 450 6 4 4 4.6 CCC[C@@]1(O)C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)O)CC[C@H]3[C@@H]21 10.1016/j.ejmech.2023.115851
172458681 196469 None 0 Human Functional pEC50 = 4.1 4.1 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 434 5 4 4 4.0 C=C[C@@]1(O)C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)O)CC[C@H]3[C@@H]21 10.1016/j.ejmech.2023.115851
CHEMBL5424602 196469 None 0 Human Functional pEC50 = 4.1 4.1 - 1
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
ChEMBL 434 5 4 4 4.0 C=C[C@@]1(O)C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)O)CC[C@H]3[C@@H]21 10.1016/j.ejmech.2023.115851
118586276 156263 None 0 Mouse Functional pEC50 = 7.0 7.0 10 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 455 7 0 5 6.4 COc1cccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)c1 10.1021/acs.jmedchem.6b01873
CHEMBL4063932 156263 None 0 Mouse Functional pEC50 = 7.0 7.0 10 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 455 7 0 5 6.4 COc1cccc(N(C)c2cnc(SCc3c(F)cccc3F)n2-c2ccc(F)cc2)c1 10.1021/acs.jmedchem.6b01873
73355479 92774 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 452 5 0 2 6.3 CC(=O)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
CHEMBL2435934 92774 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 452 5 0 2 6.3 CC(=O)N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)Cc1cnccc1-c1ccccc1 10.1016/j.ejmech.2013.07.050
73353941 92773 None 0 Mouse Functional pEC50 = 6.0 6.0 -28 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 572 6 0 5 6.6 O=C(c1ccco1)N(Cc1cnccc1-c1ccccc1F)S(=O)(=O)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
CHEMBL2435933 92773 None 0 Mouse Functional pEC50 = 6.0 6.0 -28 2
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assayAgonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
ChEMBL 572 6 0 5 6.6 O=C(c1ccco1)N(Cc1cnccc1-c1ccccc1F)S(=O)(=O)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.ejmech.2013.07.050
90283905 117744 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 402 4 1 3 5.1 C[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@@H]3C(=O)C[C@@H]4CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C)C(=O)O 10.1016/j.bmc.2015.01.048
CHEMBL3401357 117744 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assayAgonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
ChEMBL 402 4 1 3 5.1 C[C@@H](C[C@@H](C)[C@H]1CC[C@H]2[C@@H]3C(=O)C[C@@H]4CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C)C(=O)O 10.1016/j.bmc.2015.01.048
71561502 87668 None 0 Human Functional pEC50 = 6.0 6.0 - 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 376 4 0 5 4.3 Cc1nn(C)c(Oc2ccccc2)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336220 87668 None 0 Human Functional pEC50 = 6.0 6.0 - 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 376 4 0 5 4.3 Cc1nn(C)c(Oc2ccccc2)c1C(=O)N1CCCCC1c1cccnc1 10.1016/j.bmcl.2012.12.076
71561883 87681 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 404 5 0 5 4.5 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N(C)Cc1cccnc1 10.1016/j.bmcl.2012.12.076
CHEMBL2336235 87681 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycyclineAgonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
ChEMBL 404 5 0 5 4.5 Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N(C)Cc1cccnc1 10.1016/j.bmcl.2012.12.076
172471284 197164 None 0 Human Functional pEC50 = 4.0 4.0 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 512 7 2 5 5.8 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)OCc4ccccc4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
CHEMBL5440153 197164 None 0 Human Functional pEC50 = 4.0 4.0 - 1
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assayPositive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
ChEMBL 512 7 2 5 5.8 CO[C@@H]1C[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2C[C@H](O)[C@]3(C)[C@@H]([C@H](C)CCC(=O)OCc4ccccc4)CC[C@H]3[C@H]12 10.1016/j.bmc.2023.117418
118464747 158426 None 0 Human Functional pEC50 = 6.0 6.0 -4 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 743 19 2 10 6.0 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cc(C(=O)NCCOCCOCCOCCO)cc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
CHEMBL4089352 158426 None 0 Human Functional pEC50 = 6.0 6.0 -4 2
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assayAgonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 40 mins by HTRF assay
ChEMBL 743 19 2 10 6.0 COc1ccc(C2(C)CCCc3nc(SCc4c(F)cc(C(=O)NCCOCCOCCOCCO)cc4F)n(-c4ccc(F)cc4)c32)cc1OC 10.1021/acsmedchemlett.7b00116
90654575 109999 None 0 Human Functional pEC50 = 6.0 6.0 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 343 5 1 3 3.3 O=C(NCCc1ccc(Cl)cc1)[C@@H]1CCCN(c2ccccn2)C1 10.1021/jm401731q
CHEMBL3234556