ChEMBL ligand: CHEMBL566315 (6-ecdca, 6-ethylchenodeoxycholic acid, DSP-1747, INT-747, Obeticholic acid, Ocaliva)
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] 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 (unknown origin) by coactivator recruitment assay	B	4	pEC50	99000	nM	EC50	J Med Chem (2014) 57: 8035-8055 [PMID:25255039]
ChEMBL	Agonist activity at FXR transfected in human HEK293T cells o-expressing pGL3/hBSEP/luc incubated for 24 hrs by Steady-Glo reagent based luciferase reporter gene assay	B	4.38	pEC50	42000	nM	EC50	J Med Chem (2020) 63: 3868-3880 [PMID:31940200]
ChEMBL	Agonist activity at GST-tagged human FXR-LBD (193 to 472 residues) using biotinylated SRC-1 peptide as substrate incubated for 1 hrs by HTRF assay	B	5	pEC50	10000	nM	EC50	J Med Chem (2020) 63: 3868-3880 [PMID:31940200]
ChEMBL	Agonist activity at human FXR expressed in HEK293 cells measured after 18 hrs by steady-glo luciferase reporter gene assay	B	6.15	pEC50	710	nM	EC50	J Med Chem (2020) 63: 12748-12772 [PMID:32991173]
ChEMBL	Transactivation of human FXR (unknown origin) expressed in HepG2 cells co-expressing pSG5RXR/pGL4.70 after 24 hrs post transfection by luciferase reporter gene assay	B	6.3	pEC50	500	nM	EC50	ACS Med Chem Lett (2019) 10: 407-412 [PMID:30996771]
ChEMBL	Agonist activity at human FXR expressed in COS1 cells after 5 hrs by CRE-driven luciferase reporter gene assay	F	6.44	pEC50	361	nM	EC50	J Med Chem (2007) 50: 4265-4268 [PMID:17685603]
ChEMBL	Agonist activity at GST-tagged human FXR LBD assessed as induction of biotinylated coactivator SRC-1 peptide recruitment measured after 2 hrs by streptavidin-conjugated AlphaScreen assay	B	6.54	pEC50	290	nM	EC50	J Med Chem (2020) 63: 12748-12772 [PMID:32991173]
ChEMBL	Agonist activity at human GST-fused FXR LBD assessed as coactivator interaction with receptor ligand binding domain by Alphascreen assay	B	6.7	pEC50	200	nM	EC50	Bioorg Med Chem (2011) 19: 2650-2658 [PMID:21459580]
ChEMBL	Agonist activity at recombinant human GST-tagged FXR LBD (193 to 472 residues) expressed in baculovirus-infected insect cells assessed as recruitment of biotinylated SRC1 peptide measured after 1 hr by Alphascreen assay	B	6.74	pEC50	180	nM	EC50	ACS Med Chem Lett (2017) 8: 1246-1251 [PMID:29259742]
ChEMBL	Agonist activity at human FXR expressed in human HeLa cells assessed as receptor activation by BSEP promoter-driven firefly luciferase reporter gene assay	B	6.8	pEC50	160	nM	EC50	J Med Chem (2014) 57: 8035-8055 [PMID:25255039]
ChEMBL	Agonist activity at human full length FXR expressed in HeLa cells cotransfected with pSG5-human RXR after 24 hrs by Dual-Glo luciferase reporter gene assay	B	6.8	pEC50	160	nM	EC50	Bioorg Med Chem (2015) 23: 3490-3498 [PMID:25934227]
ChEMBL	Agonist activity at glutathione transferase-tagged human FXR-LBD using biotinylated Src-1 peptide incubated for 30 mins by recruitment coactivator assay	B	6.82	pEC50	150	nM	EC50	J Med Chem (2016) 59: 9201-9214 [PMID:27652492]
GtoPdb	-	-	7	pEC50	99	nM	EC50	J Med Chem (2002) 45: 3569-72 [PMID:12166927]
ChEMBL	Agonist activity at FXR (unknown origin) assessed as recruitment of SRC1 peptide to FXR by FRET assay	B	7	pEC50	100	nM	EC50	J Med Chem (2017) 60: 5235-5266 [PMID:28252961]
ChEMBL	Agonist activity at FXR (unknown origin)	B	7	pEC50	99	nM	EC50	J Med Chem (2020) 63: 5031-5073 [PMID:31930920]
ChEMBL	Activation of human farnesoid X receptor	B	7	pEC50	99	nM	EC50	J Med Chem (2005) 48: 5383-5403 [PMID:16107136]
ChEMBL	Binding affinity for Farnesoid X Receptor (FXR)	B	7	pEC50	99	nM	EC50	Bioorg Med Chem Lett (2003) 13: 1865-1868 [PMID:12749886]
ChEMBL	Effective concentration against Farnesoid X receptor (FXR)	B	7	pEC50	99	nM	EC50	J Med Chem (2002) 45: 3569-3572 [PMID:12166927]
ChEMBL	Agonist activity at FXR expressed in COS1 cells by cell-based bioluminescence assay	F	7	pEC50	99	nM	EC50	J Med Chem (2009) 52: 7958-7961 [PMID:20014870]
ChEMBL	Binding affinity to FXR assessed as ligand-dependent SRC1 recruitment by FRET based co-activator assay	F	7.01	pEC50	98	nM	EC50	J Med Chem (2006) 49: 4208-4215 [PMID:16821780]
ChEMBL	Binding affinity for human Farnesoid X receptor in FRET assay	B	7.05	pEC50	90	nM	EC50	J Med Chem (2004) 47: 4559-4569 [PMID:15317466]
ChEMBL	Agonist activity at FXR (unknown origin) by reporter gene assay	B	7.07	pEC50	85	nM	EC50	J Med Chem (2014) 57: 8035-8055 [PMID:25255039]
ChEMBL	Agonist activity at FXR (unknown origin) by cell based assay	B	7.07	pEC50	85	nM	EC50	J Med Chem (2020) 63: 5031-5073 [PMID:31930920]
ChEMBL	Agonist activity at human FXR expressed in HEK293T cells assessed as BSEP promoter driven cellular transcriptional activity after 24 hrs by luciferase reporter gene assay	B	7.38	pEC50	42	nM	EC50	J Med Chem (2017) 60: 9960-9973 [PMID:29148806]
ChEMBL	Agonist activity at recombinant human GST-tagged FXR ligand binding domain (193 to 472 residues) expressed in baculovirus infected insect cells assessed as induction of interaction with biotin labelled SRC-1 after 1 hr by HTRF assay	B	8	pEC50	10	nM	EC50	J Med Chem (2017) 60: 9960-9973 [PMID:29148806]
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 human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assay	F	4.7	pEC50	20000	nM	EC50	Bioorg Med Chem (2011) 19: 2650-2658 [PMID:21459580]
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	4.82	pEC50	15000	nM	EC50	J Med Chem (2016) 59: 9201-9214 [PMID:27652492]
ChEMBL	Agonist activity at human TGR5 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 1 hr by TR-FRET assay	F	6.08	pEC50	840	nM	EC50	ACS Med Chem Lett (2017) 8: 1246-1251 [PMID:29259742]
ChEMBL	Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay	F	6.12	pEC50	755	nM	EC50	J Med Chem (2007) 50: 4265-4268 [PMID:17685603]
ChEMBL	Agonist activity at wild type TGR5 (unknown origin)	B	7	pEC50	100	nM	EC50	ACS Med Chem Lett (2013) 4: 1158-1162 [PMID:24900622]

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]