ChEMBL ligand: CHEMBL2144065
αβ-Hydrolase 6/Monoacylglycerol lipase ABHD6 in Human [ChEMBL: CHEMBL2189127] [GtoPdb: 2919] [UniProtKB: Q9BV23] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!

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	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 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]