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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 |
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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 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]