clesacostat [Ligand Id: 12242] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4567446 (Clesacostat, Pf-05221304, PF-05221304, PF05221304) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Acetyl-CoA carboxylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3351] [GtoPdb: 1263] [UniProtKB: Q13085] | ||||||||
| ChEMBL | Inhibition of recombinant human ACC1 using acetyl coA as substrate incubated for 1 hr by transcreener fluorescence polarization assay | B | 7.48 | pIC50 | 33 | nM | IC50 | J Med Chem (2020) 63: 10879-10896 [PMID:32809824] |
| ChEMBL | Inhibition of recombinant human ACC1 using acetyl coA as substrate incubated for 1 hr by transcreener fluorescence polarization assay | B | 7.5 | pIC50 | 31.62 | nM | IC50 | J Med Chem (2020) 63: 10879-10896 [PMID:32809824] |
| ChEMBL | Inhibition of ACC1 (unknown origin) | B | 7.51 | pIC50 | 31 | nM | IC50 | J Med Chem (2020) 63: 5031-5073 [PMID:31930920] |
| ChEMBL | Uncompetitive inhibition of human ACC1 incubated for 15 mins in presence of ATP by Line weaver-Burk plot analysis | B | 7.91 | pIC50 | 12.4 | nM | IC50 | J Med Chem (2020) 63: 10879-10896 [PMID:32809824] |
| GtoPdb | - | - | 7.91 | pIC50 | 12.4 | nM | IC50 | J Med Chem (2020) 63: 10879-10896 [PMID:32809824] |
| Acetyl-CoA carboxylase 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2397] [GtoPdb: 1263] [UniProtKB: P11497] | ||||||||
| ChEMBL | Inhibition of rat ACC1 using acetyl-CoA as substrate incubated for 20 mins in presence of [14C]O3 by liquid scintillation counting method | B | 8.12 | pIC50 | 7.53 | nM | IC50 | J Med Chem (2020) 63: 10879-10896 [PMID:32809824] |
| Acetyl-CoA carboxylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4829] [GtoPdb: 1264] [UniProtKB: O00763] | ||||||||
| ChEMBL | Inhibition of ACC2 (unknown origin) | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2020) 63: 5031-5073 [PMID:31930920] |
| ChEMBL | Inhibition of recombinant human ACC2 using acetyl coA as substrate incubated for 1 hr by transcreener fluorescence polarization assay | B | 7.59 | pIC50 | 26 | nM | IC50 | J Med Chem (2020) 63: 10879-10896 [PMID:32809824] |
| ChEMBL | Inhibition of recombinant human ACC2 using acetyl coA as substrate incubated for 1 hr by transcreener fluorescence polarization assay | B | 7.6 | pIC50 | 25.12 | nM | IC50 | J Med Chem (2020) 63: 10879-10896 [PMID:32809824] |
| GtoPdb | - | - | 7.6 | pIC50 | 25.12 | nM | IC50 | J Med Chem (2020) 63: 10879-10896 [PMID:32809824] |
| ChEMBL | Uncompetitive inhibition of human ACC2 incubated for 15 mins in presence of ATP by Line weaver-Burk plot analysis | B | 8.06 | pIC50 | 8.66 | nM | IC50 | J Med Chem (2020) 63: 10879-10896 [PMID:32809824] |
| ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
| ChEMBL | Inhibition of human ABCG2 expressed in MDCK2-LE cells in presence of digoxin | B | 4.17 | pIC50 | 68000 | nM | IC50 | J Med Chem (2020) 63: 10879-10896 [PMID:32809824] |
| ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342] | ||||||||
| ChEMBL | Inhibition of human BSEP expressed in baculovirus infected Hi5 insect cells in presence of taurocholic acid by LC-MS/MS analysis | B | 4.03 | pIC50 | 94000 | nM | IC50 | J Med Chem (2020) 63: 10879-10896 [PMID:32809824] |
| ABCC1/Multidrug resistance-associated protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527] | ||||||||
| ChEMBL | Inhibition of human ABCC1 expressed in MDCK2-LE cells in presence of pitavastatin | B | 4.41 | pIC50 | 39000 | nM | IC50 | J Med Chem (2020) 63: 10879-10896 [PMID:32809824] |
| Organic cation transporter 2/Solute carrier family 22 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244] | ||||||||
| ChEMBL | Inhibition of human SLC22A2 expressed in HEK293 cells in presence of para-aminohippuric acid/metformin | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2020) 63: 10879-10896 [PMID:32809824] |
| Organic anion transporter 1/Solute carrier family 22 member 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1641347] [GtoPdb: 1025] [UniProtKB: Q4U2R8] | ||||||||
| ChEMBL | Inhibition of human SLC22A6 expressed in HEK293 cells in presence of para-aminohippuric acid/metformin | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2020) 63: 10879-10896 [PMID:32809824] |
| Organic anion transporter 3/Solute carrier family 22 member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1641348] [GtoPdb: 1027] [UniProtKB: Q8TCC7] | ||||||||
| ChEMBL | Inhibition of human SLC22A8 expressed in HEK293 cells in presence of para-aminohippuric acid/metformin | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2020) 63: 10879-10896 [PMID:32809824] |
| OATP1B1/Solute carrier organic anion transporter family member 1B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697668] [GtoPdb: 1220] [UniProtKB: Q9Y6L6] | ||||||||
| ChEMBL | Inhibition of human OATP1B1 expressed in HEK293 cells n presence of rosuvastatin | B | 4.93 | pIC50 | 11700 | nM | IC50 | J Med Chem (2020) 63: 10879-10896 [PMID:32809824] |
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]
