ChEMBL ligand: CHEMBL205596 (Cholalic acid, Cholbam, Cholic acid, Cholic Acid, E1000, Kolbam, NSC-6135, Orphacol)
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!
Plasmodium falciparum [ChEMBL: CHEMBL364] 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	Activation of GST-tagged FXR LBD (unknown origin) using biotinylated Src-1 peptide as substrate by AlphaScreen assay	B	4.14	pEC50	73000	nM	EC50	Eur J Med Chem (2023) 261: 115851-115851 [PMID:37813065]
ChEMBL	Agonist activity at GST-tagged FXR-LBD (unknown origin) assessed as biotin-labeled SRC-1 recruitment after 30 mins by Alpha Screen assay	B	4.35	pEC50	45000	nM	EC50	Eur J Med Chem (2018) 144: 349-358 [PMID:29275233]
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 HEK293 cells assessed as intracellular cAMP level	F	5.22	pIC50	6000	nM	IC50	Bioorg Med Chem Lett (2010) 20: 5718-5721 [PMID:20801037]
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	4.38	pEC50	41500	nM	EC50	Eur J Med Chem (2023) 261: 115851-115851 [PMID:37813065]
ChEMBL	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 assay	F	4.41	pEC50	38700	nM	EC50	Bioorg Med Chem (2023) 92: 117418-117418 [PMID:37536263]
ChEMBL	Agonist activity at wild type TGR5 (unknown origin)	B	4.7	pEC50	19830	nM	EC50	ACS Med Chem Lett (2013) 4: 1158-1162 [PMID:24900622]
ChEMBL	Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay	F	4.87	pEC50	13600	nM	EC50	J Med Chem (2007) 50: 4265-4268 [PMID:17685603]
ChEMBL	Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis	F	4.87	pEC50	13600	nM	EC50	ACS Med Chem Lett (2012) 3: 273-277 [PMID:24900463]
ChEMBL	Agonist activity at human TGR5 expressed in CHO cells by luciferase assay	F	4.87	pEC50	13600	nM	EC50	J Med Chem (2008) 51: 1831-1841 [PMID:18307294]
ChEMBL	Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay	F	4.87	pEC50	13600	nM	EC50	J Med Chem (2009) 52: 7958-7961 [PMID:20014870]
GtoPdb	-	-	5	pEC50	-	-	-	Biochem Biophys Res Commun (2002) 298: 714-9 [PMID:12419312]
GPBA receptor/G-protein coupled bile acid receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255150] [GtoPdb: 37] [UniProtKB: Q80SS6]
ChEMBL	Agonist activity at mouse TGR5 receptor expressed in HEK293 cells assessed as intracellular cAMP level	F	5.28	pIC50	5300	nM	IC50	Bioorg Med Chem Lett (2010) 20: 5718-5721 [PMID:20801037]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL	Antimalarial activity against Plasmodium falciparum NF54 infected in human erythrocytes assessed as reduction in [3H]hypoxanthine incorporation preincubated for 48 hrs followed by [3H]hypoxanthine addition measured after 24 hrs by liquid scintillation counting	F	4.7	pIC50	>20000	nM	IC50	Medchemcomm (2017) 8: 1152-1157 [PMID:30108825]

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]