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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 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]