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]
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 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 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 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 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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]