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ChEMBL ligand: CHEMBL473967 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]