T863 [Ligand Id: 7828] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL473967
  • Acyl coenzyme A:cholesterol acyltransferase 1 in Human [ChEMBL: CHEMBL2782] [UniProtKB: P35610]
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  • diacylglycerol O-acyltransferase 1/Diacylglycerol O-acyltransferase 1 in Human [ChEMBL: CHEMBL6009] [GtoPdb: 2821] [UniProtKB: O75907]
  • diacylglycerol O-acyltransferase 1/Diacylglycerol O-acyltransferase 1 in Rat [ChEMBL: CHEMBL6129] [GtoPdb: 2821] [UniProtKB: Q9ERM3]
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  • diacylglycerol O-acyltransferase 2/Diacylglycerol O-acyltransferase 2 in Human [ChEMBL: CHEMBL5853] [GtoPdb: 3211] [UniProtKB: Q96PD7]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acyl coenzyme A:cholesterol acyltransferase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2782] [UniProtKB: P35610]
ChEMBL Inhibition of human ACAT1 at 10 uM by liquid scintillography B 4.92 pIC50 12000 nM IC50 J Med Chem (2009) 52: 1558-1568 [PMID:19256504]
diacylglycerol O-acyltransferase 1/Diacylglycerol O-acyltransferase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6009] [GtoPdb: 2821] [UniProtKB: O75907]
ChEMBL Inhibition of human DGAT1 expressed in baculovirus infected insect cells after 1 hr using palmitoyl-1-14C-coenzyme A by phospholipid flashplate assay B 6.95 pIC50 113 nM IC50 J Med Chem (2011) 54: 2433-2446 [PMID:21413799]
ChEMBL Inhibition of full length human microsomal DGAT-1 expressed in baculovirus infected insect Sf9 cells using [14C]decanoylCoA as substrate after 1.5 hrs by scintillation counting B 7.14 pIC50 72 nM IC50 ACS Med Chem Lett (2011) 2: 407-412 [PMID:24900321]
ChEMBL Inhibition of human DGAT1 B 7.14 pIC50 72 nM IC50 Bioorg Med Chem Lett (2011) 21: 6122-6125 [PMID:21908190]
ChEMBL Inhibition of DGAT1-mediated triglyceride synthesis in human HT-29 cells using [3H]glycerol as substrate after 6 hrs by beta counting B 7.8 pIC50 16 nM IC50 ACS Med Chem Lett (2011) 2: 407-412 [PMID:24900321]
GtoPdb - - 7.82 pIC50 15 nM IC50 J Med Chem (2009) 52: 1558-68 [PMID:19256504]
ChEMBL Inhibition of human recombinant DGAT1 expressed in Sf9 cells by liquid scintillography B 7.82 pIC50 15 nM IC50 J Med Chem (2009) 52: 1558-1568 [PMID:19256504]
ChEMBL Inhibition of human DGAT-1-mediated triglyceride synthesis in the HT-29 cells by whole cell assay B 8.1 pIC50 8 nM IC50 Bioorg Med Chem Lett (2011) 21: 6122-6125 [PMID:21908190]
ChEMBL Inhibition of human liver flag-tagged DGAT1 expressed in baculovirus infected insect cells after 2 hrs by SPA B 8.22 pIC50 6 nM IC50 J Med Chem (2014) 57: 3464-3483 [PMID:24670009]
ChEMBL Inhibition of DGAT1 (unknown origin) by cell-based assay B 8.4 pIC50 4 nM IC50 J Med Chem (2014) 57: 3464-3483 [PMID:24670009]
ChEMBL Inhibition of human DGAT1 expressed in CHO-K1 cells after 1 hr using palmitoyl-1-14C-coenzyme A by phospholipid flashplate assay B 5.84 pEC50 1436 nM EC50 J Med Chem (2011) 54: 2433-2446 [PMID:21413799]
diacylglycerol O-acyltransferase 1/Diacylglycerol O-acyltransferase 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6129] [GtoPdb: 2821] [UniProtKB: Q9ERM3]
ChEMBL Inhibition of DGAT in rat liver microsomes B 5.51 pIC50 3100 nM IC50 Bioorg Med Chem Lett (2012) 22: 7456-7460 [PMID:23141914]
ChEMBL Inhibition of rat microsomal DGAT1 by liquid scintillography B 7.72 pIC50 19 nM IC50 J Med Chem (2009) 52: 1558-1568 [PMID:19256504]
diacylglycerol O-acyltransferase 2/Diacylglycerol O-acyltransferase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5853] [GtoPdb: 3211] [UniProtKB: Q96PD7]
ChEMBL Inhibition of human DGAT-2 B 5 pIC50 >10000 nM IC50 ACS Med Chem Lett (2011) 2: 407-412 [PMID:24900321]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG by patch clamp assay B 5 pIC50 >10000 nM IC50 J Med Chem (2014) 57: 3464-3483 [PMID:24670009]

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]