DH376 [Ligand Id: 10244] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3895863
  • αβ-Hydrolase 6/Monoacylglycerol lipase ABHD6 in Human [ChEMBL: CHEMBL2189127] [GtoPdb: 2919] [UniProtKB: Q9BV23]
  • αβ-Hydrolase 6/Monoacylglycerol lipase ABHD6 in Mouse [ChEMBL: CHEMBL5010] [GtoPdb: 2919] [UniProtKB: Q8R2Y0]
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  • diacylglycerol lipase α/Sn1-specific diacylglycerol lipase alpha in Human [ChEMBL: CHEMBL5545] [GtoPdb: 1396] [UniProtKB: Q9Y4D2]
  • diacylglycerol lipase α/Sn1-specific diacylglycerol lipase alpha in Mouse [ChEMBL: CHEMBL5180] [GtoPdb: 1396] [UniProtKB: Q6WQJ1]
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  • diacylglycerol lipase β in Human [GtoPdb: 1397] [UniProtKB: Q8NCG7]
  • diacylglycerol lipase β/Sn1-specific diacylglycerol lipase beta in Mouse [ChEMBL: CHEMBL5656] [GtoPdb: 1397] [UniProtKB: Q91WC9]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
αβ-Hydrolase 6/Monoacylglycerol lipase ABHD6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189127] [GtoPdb: 2919] [UniProtKB: Q9BV23]
ChEMBL Inhibition of human ABHD6 using 2-AG as natural substrate by fluorescence based assay B 8.6 pIC50 2.51 nM IC50 J Med Chem (2017) 60: 428-440 [PMID:27992221]
αβ-Hydrolase 6/Monoacylglycerol lipase ABHD6 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5010] [GtoPdb: 2919] [UniProtKB: Q8R2Y0]
ChEMBL Inhibition of MB064 probe binding to ABHD6 in mouse brain membrane proteome preincubated for 30 mins followed by MB064 probe addition measured after 20 mins by gel-based competitive activity based protein profiling assay B 7.1 pIC50 79.43 nM IC50 J Med Chem (2017) 60: 428-440 [PMID:27992221]
diacylglycerol lipase α/Sn1-specific diacylglycerol lipase alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5545] [GtoPdb: 1396] [UniProtKB: Q9Y4D2]
GtoPdb - - 8.2 pIC50 - - - Proc Natl Acad Sci USA (2016) 113: 26-33 [PMID:26668358]
ChEMBL Inhibition of full length recombinant human DAGLalpha expressed in HEK293T cell membranes using PNP butyrate as substrate by colorimetric assay B 8.9 pIC50 1.26 nM IC50 J Med Chem (2017) 60: 428-440 [PMID:27992221]
ChEMBL Inhibition human DAGLalpha expressed in HEK293T cell membrane fractions using DAG as substrate preincubated for 30 mins followed by ABP HT01 probe addition measured after 30 mins in presence of probe by gel-based ABPP competition assay B 8.9 pIC50 1.26 nM IC50 Bioorg Med Chem Lett (2016) 26: 3831-3837 [PMID:27394666]
GtoPdb - - 8.9 pIC50 - - - J Med Chem (2017) 60: 428-440 [PMID:27992221]
diacylglycerol lipase α/Sn1-specific diacylglycerol lipase alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5180] [GtoPdb: 1396] [UniProtKB: Q6WQJ1]
ChEMBL Inhibition of mouse DAGL-alpha expressed in HEK293T cell membranes assessed as inhibition constant pre-incubated for 20 mins before PNP-butyrate substrate addition and measured after 30 mins by surrogate substrate assay B 9.57 pKi 0.27 nM Ki J Med Chem (2019) 62: 7910-7922 [PMID:31437392]
ChEMBL Inhibition of mouse DAGL-alpha expressed in HEK293T cell membranes pre-incubated for 20 mins before PNP-butyrate substrate addition and measured after 30 mins by surrogate substrate assay B 9 pIC50 <1 nM IC50 J Med Chem (2019) 62: 7910-7922 [PMID:31437392]
ChEMBL Inhibition of MB064 probe binding to DAGLalpha in mouse brain membrane proteome preincubated for 30 mins followed by MB064 probe addition measured after 20 mins by gel-based competitive activity based protein profiling assay B 9.2 pIC50 0.63 nM IC50 J Med Chem (2017) 60: 428-440 [PMID:27992221]
diacylglycerol lipase β in Human [GtoPdb: 1397] [UniProtKB: Q8NCG7]
GtoPdb - - 8.6 pIC50 - - - Proc Natl Acad Sci USA (2016) 113: 26-33 [PMID:26668358]
diacylglycerol lipase β/Sn1-specific diacylglycerol lipase beta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5656] [GtoPdb: 1397] [UniProtKB: Q91WC9]
ChEMBL Inhibition mouse DAGLbeta expressed in HEK293T cell membrane fractions using DAG as substrate preincubated for 30 mins followed by ABP HT01 probe addition measured after 30 mins in presence of probe by gel-based ABPP competition assay B 8.3 pIC50 5.01 nM IC50 Bioorg Med Chem Lett (2016) 26: 3831-3837 [PMID:27394666]

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]