KT-109 [Ligand Id: 10245] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2144065
  • diacylglycerol lipase α in Human [GtoPdb: 1396] [UniProtKB: Q9Y4D2]
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  • diacylglycerol lipase β in Human [GtoPdb: 1397] [UniProtKB: Q8NCG7]
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  • αβ-Hydrolase 6 in Human [GtoPdb: 2919] [UniProtKB: Q9BV23]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
diacylglycerol lipase α in Human [GtoPdb: 1396] [UniProtKB: Q9Y4D2]
GtoPdb Determined by competitive ABPP using the HT-01 probe for inhibition of recombinant human DAGL-α - 5.64 pIC50 2300 nM IC50 Nat Chem Biol (2012) 8: 999-1007 [PMID:23103940]
diacylglycerol lipase β in Human [GtoPdb: 1397] [UniProtKB: Q8NCG7]
GtoPdb As measured by LC-MS substrate assay. - 7.09 pIC50 82 nM IC50 Nat Chem Biol (2012) 8: 999-1007 [PMID:23103940]
GtoPdb Determined by competitive ABPP using the HT-01 probe for inhibition of recombinant human DAGL-β - 7.4 pIC50 40 nM IC50 Nat Chem Biol (2012) 8: 999-1007 [PMID:23103940]
αβ-Hydrolase 6 in Human [GtoPdb: 2919] [UniProtKB: Q9BV23]
GtoPdb - - 7.8 pIC50 16 nM IC50 Nat Chem Biol (2012) 8: 999-1007 [PMID:23103940]

ChEMBL data shown on this page come from version 36:

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]