clesacostat | Ligand Activity Charts | IUPHAR/BPS Guide to PHARMACOLOGY

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Ligand Activity Charts

clesacostat [Ligand Id: 12242] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4567446 (Clesacostat, Pf-05221304, PF-05221304, PF05221304)
Acetyl-CoA carboxylase 1 in Human [ChEMBL: CHEMBL3351] [GtoPdb: 1263] [UniProtKB: Q13085] Acetyl-CoA carboxylase 1 in Rat [ChEMBL: CHEMBL2397] [GtoPdb: 1263] [UniProtKB: P11497] There should be some charts here, you may need to enable JavaScript!
Acetyl-CoA carboxylase 2 in Human [ChEMBL: CHEMBL4829] [GtoPdb: 1264] [UniProtKB: O00763] There should be some charts here, you may need to enable JavaScript!
ABCG2/ATP-binding cassette sub-family G member 2 in Human [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] There should be some charts here, you may need to enable JavaScript!
ABCB11/Bile salt export pump in Human [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342] There should be some charts here, you may need to enable JavaScript!
ABCC1/Multidrug resistance-associated protein 1 in Human [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527] There should be some charts here, you may need to enable JavaScript!
Organic cation transporter 2/Solute carrier family 22 member 2 in Human [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244] There should be some charts here, you may need to enable JavaScript!
Organic anion transporter 1/Solute carrier family 22 member 6 in Human [ChEMBL: CHEMBL1641347] [GtoPdb: 1025] [UniProtKB: Q4U2R8] There should be some charts here, you may need to enable JavaScript!
Organic anion transporter 3/Solute carrier family 22 member 8 in Human [ChEMBL: CHEMBL1641348] [GtoPdb: 1027] [UniProtKB: Q8TCC7] There should be some charts here, you may need to enable JavaScript!
OATP1B1/Solute carrier organic anion transporter family member 1B1 in Human [ChEMBL: CHEMBL1697668] [GtoPdb: 1220] [UniProtKB: Q9Y6L6] 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
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]