cholic acid [Ligand Id: 609] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL205596 (Cholalic acid, Cholbam, Cholic acid, Cholic Acid, E1000, Kolbam, NSC-6135, Orphacol) |
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| 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 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 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 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] |
| 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] |
| 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 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]
