BMS-963272 [Ligand Id: 12738] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3912712
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  • Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase in Human [ChEMBL: CHEMBL2321630] [UniProtKB: Q10469]
  • Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase in Mouse [ChEMBL: CHEMBL2375203] [UniProtKB: Q921V5]
  • Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase in Rat [ChEMBL: CHEMBL4879456] [UniProtKB: Q09326]
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  • Beta-1,4-mannosyl-glycoprotein 4-beta-N-acetylglucosaminyltransferase in Human [ChEMBL: CHEMBL2375206] [UniProtKB: Q09327]
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  • diacylglycerol O-acyltransferase 1/Diacylglycerol O-acyltransferase 1 in Human [ChEMBL: CHEMBL6009] [GtoPdb: 2821] [UniProtKB: O75907]
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  • monoacylglycerol O-acyltransferase 2 in Human [GtoPdb: 2881] [UniProtKB: Q3SYC2]
  • monoacylglycerol O-acyltransferase 2 in Mouse [GtoPdb: 2881] [UniProtKB: Q80W94]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acyl-CoA wax alcohol acyltransferase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2375204] [UniProtKB: Q6E213]
ChEMBL Inhibition of human AWAT2 B 4.48 pIC50 >33000 nM IC50 J Med Chem (2021) 64: 14773-14792 [PMID:34613725]
Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321630] [UniProtKB: Q10469]
ChEMBL Inhibition of human recombinant MGAT2 expressed in Sf9 cell membrane using 2-monooleglycerol and [H3]-oleoyl-CoA as substrates incubated for 20 mins by scintillation proximity assay B 8.15 pIC50 7.1 nM IC50 J Med Chem (2021) 64: 14773-14792 [PMID:34613725]
Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2375203] [UniProtKB: Q921V5]
ChEMBL Inhibition of mouse recombinant MGAT2 expressed in Sf9 cell membrane using 2-oleoylglycerol and oleoyl-CoA as substrates incubated for 10 mins by LCMS assay B 7.74 pIC50 18 nM IC50 J Med Chem (2021) 64: 14773-14792 [PMID:34613725]
Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4879456] [UniProtKB: Q09326]
ChEMBL Inhibition of rat recombinant MGAT2 expressed in Sf9 cell membrane using 2-oleoylglycerol and oleoyl-CoA as substrates incubated for 10 mins by LCMS assay B 8 pIC50 10 nM IC50 J Med Chem (2021) 64: 14773-14792 [PMID:34613725]
Beta-1,4-mannosyl-glycoprotein 4-beta-N-acetylglucosaminyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2375206] [UniProtKB: Q09327]
ChEMBL Inhibition of human MGAT3 B 6.09 pIC50 >820 nM IC50 J Med Chem (2021) 64: 14773-14792 [PMID:34613725]
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 B 4.48 pIC50 >33000 nM IC50 J Med Chem (2021) 64: 14773-14792 [PMID:34613725]
Stanniocalcin-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4879441] [UniProtKB: P52823]
ChEMBL Inhibition of human STC1 in cell based assay B 7.48 pIC50 33 nM IC50 J Med Chem (2021) 64: 14773-14792 [PMID:34613725]
Stanniocalcin-1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4879418] [UniProtKB: O55183]
ChEMBL Inhibition of mouse STC1 in cell based assay B 7.06 pIC50 88 nM IC50 J Med Chem (2021) 64: 14773-14792 [PMID:34613725]
monoacylglycerol O-acyltransferase 2 in Human [GtoPdb: 2881] [UniProtKB: Q3SYC2]
GtoPdb - - 8.15 pIC50 7.1 nM IC50 J Med Chem (2021) 64: 14773-14792 [PMID:34613725]
monoacylglycerol O-acyltransferase 2 in Mouse [GtoPdb: 2881] [UniProtKB: Q80W94]
GtoPdb - - 7.74 pIC50 18 nM IC50 J Med Chem (2021) 64: 14773-14792 [PMID:34613725]

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]