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ChEMBL ligand: CHEMBL2144065 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | 7.4 | pIC50 | 39.81 | nM | IC50 | J Med Chem (2017) 60: 428-440 [PMID:27992221] |
GtoPdb | - | - | 7.8 | pIC50 | 16 | nM | IC50 | Nat Chem Biol (2012) 8: 999-1007 [PMID:23103940] |
diacylglycerol lipase α/Sn1-specific diacylglycerol lipase alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5545] [GtoPdb: 1396] [UniProtKB: Q9Y4D2] | ||||||||
ChEMBL | Inhibition of HT-01 probe binding to recombinant human DAGLalpha expressed in HEK293T cell membrane proteomes preincubated for 30 mins followed by HT-01 probe addition measured after 30 mins by gel-based competitive activity based protein profiling assay | B | 5.6 | pIC50 | 2511.89 | 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 | 5.6 | pIC50 | 2511.89 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3831-3837 [PMID:27394666] |
ChEMBL | Inhibition of HT-01 probe binding to recombinant human DAGLalpha expressed in HEK293T cell membrane proteomes preincubated for 30 mins followed by HT-01 probe addition measured after 30 mins by gel-based competitive activity based protein profiling assay | B | 5.64 | pIC50 | 2300 | nM | IC50 | J Med Chem (2017) 60: 428-440 [PMID:27992221] |
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] |
ChEMBL | Inhibition of recombinant human DAGLalpha expressed in HEK293T cell membranes overexpressing MAGL using natural substrate 1-stearoyl-2-arachidonoly-sn-glycerol by fluorescence based assay | B | 6.9 | pIC50 | 125.89 | nM | IC50 | J Med Chem (2017) 60: 428-440 [PMID:27992221] |
ChEMBL | Inhibition of human GST-tagged DAGLalpha expressed in HEK293F cell membranes using 1-stearoyl-2-arachidonoyl-sn-glycerol as substrate preincubated for 20 mins followed by substrate addition by enzyme coupled natural substrate assay | B | 7.6 | pIC50 | 25.12 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3831-3837 [PMID:27394666] |
ChEMBL | Inhibition of full length recombinant human DAGLalpha expressed in HEK293T cell membranes using PNP butyrate as substrate by colorimetric assay | B | 8.2 | pIC50 | 6.31 | nM | IC50 | 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 | 9.46 | pKi | 0.35 | 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] |
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] |
diacylglycerol lipase β/Sn1-specific diacylglycerol lipase beta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5656] [GtoPdb: 1397] [UniProtKB: Q91WC9] | ||||||||
ChEMBL | Inhibition of recombinant mouse DAGLbeta expressed in HEK293T cell membranes using PNP butyrate as substrate by colorimetric assay | B | 7.1 | pIC50 | 79.43 | nM | IC50 | J Med Chem (2017) 60: 428-440 [PMID:27992221] |
ChEMBL | Inhibition of V-tagged mouse DAGLbeta expressed in HEK2934T cell membrane fractions using SAG as substrate assessed as accumulation of 2-AG preincubated for 30 mins followed by probe addition measured after 30 mins by LC-MS natural substrate assay | B | 7.1 | pIC50 | 79.43 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3831-3837 [PMID:27394666] |
ChEMBL | Inhibition of HT-01 probe binding to recombinant mouse DAGLbeta expressed in HEK293T cell membrane proteomes preincubated for 30 mins followed by HT-01 probe addition measured after 30 mins by gel-based competitive activity based protein profiling assay | B | 7.4 | pIC50 | 39.81 | nM | IC50 | J Med Chem (2017) 60: 428-440 [PMID:27992221] |
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 | 7.4 | pIC50 | 39.81 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3831-3837 [PMID:27394666] |
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]