ChEMBL ligand: CHEMBL567640
Farnesoid X receptor/Bile acid receptor FXR in Human [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1] There should be some charts here, you may need to enable JavaScript!
GPBA receptor/G-protein coupled bile acid receptor 1 in Human [ChEMBL: CHEMBL5409] [GtoPdb: 37] [UniProtKB: Q8TDU6] GPBA receptor/G-protein coupled bile acid receptor 1 in Mouse [ChEMBL: CHEMBL1255150] [GtoPdb: 37] [UniProtKB: Q80SS6] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
Farnesoid X receptor/Bile acid receptor FXR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1]
ChEMBL	Agonist activity at FXR expressed in COS1 cells by cell-based bioluminescence assay	F	4	pEC50	>100000	nM	EC50	J Med Chem (2009) 52: 7958-7961 [PMID:20014870]
ChEMBL	Agonist activity at GST-tagged FXR-LBD using biotinylated-SRC-1 peptide as substrate preincubated with compound for 30 mins measured after 4 hrs	F	4	pEC50	>100000	nM	EC50	ACS Med Chem Lett (2012) 3: 273-277 [PMID:24900463]
ChEMBL	Agonist activity at glutathione transferase-tagged human FXR-LBD using biotinylated Src-1 peptide incubated for 30 mins by recruitment coactivator assay	B	4	pEC50	>100000	nM	EC50	J Med Chem (2016) 59: 9201-9214 [PMID:27652492]
ChEMBL	Agonist activity at glutathione transferase-tagged human FXR ligand binding domain assessed as biotinylated Src1 peptide recruitment incubated for 30 mins by AlphaScreen assay	B	4	pEC50	>100000	nM	EC50	Eur J Med Chem (2022) 242: 114652-114652 [PMID:36049273]
ChEMBL	Activation of GST-tagged FXR LBD (unknown origin) using biotinylated Src-1 peptide as substrate by AlphaScreen assay	B	4	pEC50	>100000	nM	EC50	Eur J Med Chem (2023) 261: 115851-115851 [PMID:37813065]
GPBA receptor/G-protein coupled bile acid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5409] [GtoPdb: 37] [UniProtKB: Q8TDU6]
ChEMBL	Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production	F	4.89	pEC50	13000	nM	EC50	Bioorg Med Chem Lett (2013) 23: 4627-4632 [PMID:23831134]
ChEMBL	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 immunoassay	F	5.26	pEC50	5540	nM	EC50	ACS Med Chem Lett (2013) 4: 63-68 [PMID:24900564]
ChEMBL	Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay	F	5.46	pEC50	3440	nM	EC50	J Med Chem (2009) 52: 7958-7961 [PMID:20014870]
ChEMBL	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 assay	F	5.62	pEC50	2423	nM	EC50	Eur J Med Chem (2022) 242: 114697-114697 [PMID:36029562]
ChEMBL	Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay	F	5.91	pEC50	1230	nM	EC50	Eur J Med Chem (2013) 69: 55-68 [PMID:24007860]
ChEMBL	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 assay	F	6	pEC50	1004	nM	EC50	Eur J Med Chem (2020) 203: 112619-112619 [PMID:32682201]
ChEMBL	Agonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assay	F	6.05	pEC50	900	nM	EC50	Eur J Med Chem (2022) 242: 114652-114652 [PMID:36049273]
ChEMBL	Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay	F	6.05	pEC50	900	nM	EC50	J Med Chem (2016) 59: 9201-9214 [PMID:27652492]
ChEMBL	Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay	F	6.07	pEC50	850	nM	EC50	Eur J Med Chem (2023) 261: 115851-115851 [PMID:37813065]
ChEMBL	Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis	F	6.09	pEC50	820	nM	EC50	ACS Med Chem Lett (2012) 3: 273-277 [PMID:24900463]
ChEMBL	Agonist activity at human TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay	F	6.09	pEC50	820	nM	EC50	Bioorg Med Chem (2021) 32: 115972-115972 [PMID:33440321]
ChEMBL	Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay	F	6.53	pEC50	293	nM	EC50	Bioorg Med Chem Lett (2014) 24: 4271-4275 [PMID:25082126]
ChEMBL	Agonist activity at wild type TGR5 (unknown origin)	B	6.74	pEC50	180	nM	EC50	ACS Med Chem Lett (2013) 4: 1158-1162 [PMID:24900622]
ChEMBL	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 immunoassay	F	6.78	pEC50	166	nM	EC50	ACS Med Chem Lett (2013) 4: 63-68 [PMID:24900564]
GPBA receptor/G-protein coupled bile acid receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255150] [GtoPdb: 37] [UniProtKB: Q80SS6]
GtoPdb	-	-	6.09	pEC50	-	-	-	J Med Chem (2009) 52: 7958-61 [PMID:20014870]
ChEMBL	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 assay	F	6.23	pEC50	586	nM	EC50	Eur J Med Chem (2022) 242: 114697-114697 [PMID:36029562]
ChEMBL	Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay	F	6.44	pEC50	360	nM	EC50	Eur J Med Chem (2013) 69: 55-68 [PMID:24007860]
ChEMBL	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 assay	F	6.6	pEC50	251	nM	EC50	Eur J Med Chem (2020) 203: 112619-112619 [PMID:32682201]
ChEMBL	Agonist activity at mouse TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay	F	6.88	pEC50	132	nM	EC50	Bioorg Med Chem (2021) 32: 115972-115972 [PMID:33440321]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]