ChEMBL ligand: CHEMBL3895863
diacylglycerol lipase α/Diacylglycerol lipase-alpha in Human [ChEMBL: CHEMBL5545] [GtoPdb: 1396] [UniProtKB: Q9Y4D2] diacylglycerol lipase α/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/Diacylglycerol lipase-beta in Human [ChEMBL: CHEMBL5521] [GtoPdb: 1397] [UniProtKB: Q8NCG7] diacylglycerol lipase β/Diacylglycerol lipase-beta in Mouse [ChEMBL: CHEMBL5656] [GtoPdb: 1397] [UniProtKB: Q91WC9] There should be some charts here, you may need to enable JavaScript!
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] 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
diacylglycerol lipase α/Diacylglycerol lipase-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5545] [GtoPdb: 1396] [UniProtKB: Q9Y4D2]
ChEMBL	In Vitro Inhibition of DAGL: Briefly, membrane proteome (1 mg/ml, 20 μL) was prepared from HEK293T cells (transiently transfected with hDAGLα-FLAG or hDAGLα-S472A-FLAG, hDAGLβ-FLAG or hDAGLβ-S443A-FLAG) as described in Example 16. The proteome was incubated at room temperature with vehicle (DMSO) or compound in 0.5 μL DMSO for 30 min. The membrane proteome sample was subsequently treated for 30 min with HT-01 probe (1 μM) or FP-Rh probe (1 μM). The reactions were quenched with 10 μL 3× Laemmli sample buffer (final concentrations: 60 mM Tris-Cl pH 6.8, 2% (w/v) SDS, 10% (v/v) glycerol, 5% (v/v) (3-mercaptoethanol, 0.01% (v/v) bromophenol blue). The samples were directly loaded and resolved on SDS page gel (10% acrylamide). The gels were scanned using a ChemiDoc MP system (Cy3 settings, 605/50 filter).The resolved proteins were transferred from the gels to a polyvinyldifluoride membrane for Western Blotting using a Trans-Blot® Turbo (BioRad). FLAG-tagged enzymes were stained using rabbit anti-FLAG as primary antibody, and goat-anti-rabbit HRP as secondary antibody. The blot was developed in the dark using a 10 mL luminal solution, 100 μL ECL enhancer and 3 μL H2O2. Chemiluminescence was visualized using a ChemiDoc XRS (BioRad).The percentage of DAGL activity remaining in the assayed samples was determined by measuring the integrated optical intensity of the fluorescent protein bands of the Western Blot using image lab 4.1. The relative intensity was compared to the vehicle (DMSO) treated proteins, which were set to 100%. IC50 values were determined by plotting a log(inhibitor) vs. normalized response (Variable slope) dose-response curve generated using Prism software (GraphPad).	B	6.4	pIC50	<400	nM	IC50	US-10583137-B2. Triazole DAGLα inhibitors (2020)
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/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/Diacylglycerol lipase-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5521] [GtoPdb: 1397] [UniProtKB: Q8NCG7]
ChEMBL	In Vitro Inhibition of DAGL: Briefly, membrane proteome (1 mg/ml, 20 μL) was prepared from HEK293T cells (transiently transfected with hDAGLα-FLAG or hDAGLα-S472A-FLAG, hDAGLβ-FLAG or hDAGLβ-S443A-FLAG) as described in Example 16. The proteome was incubated at room temperature with vehicle (DMSO) or compound in 0.5 μL DMSO for 30 min. The membrane proteome sample was subsequently treated for 30 min with HT-01 probe (1 μM) or FP-Rh probe (1 μM). The reactions were quenched with 10 μL 3× Laemmli sample buffer (final concentrations: 60 mM Tris-Cl pH 6.8, 2% (w/v) SDS, 10% (v/v) glycerol, 5% (v/v) (3-mercaptoethanol, 0.01% (v/v) bromophenol blue). The samples were directly loaded and resolved on SDS page gel (10% acrylamide). The gels were scanned using a ChemiDoc MP system (Cy3 settings, 605/50 filter).The resolved proteins were transferred from the gels to a polyvinyldifluoride membrane for Western Blotting using a Trans-Blot® Turbo (BioRad). FLAG-tagged enzymes were stained using rabbit anti-FLAG as primary antibody, and goat-anti-rabbit HRP as secondary antibody. The blot was developed in the dark using a 10 mL luminal solution, 100 μL ECL enhancer and 3 μL H2O2. Chemiluminescence was visualized using a ChemiDoc XRS (BioRad).The percentage of DAGL activity remaining in the assayed samples was determined by measuring the integrated optical intensity of the fluorescent protein bands of the Western Blot using image lab 4.1. The relative intensity was compared to the vehicle (DMSO) treated proteins, which were set to 100%. IC50 values were determined by plotting a log(inhibitor) vs. normalized response (Variable slope) dose-response curve generated using Prism software (GraphPad).	B	6.4	pIC50	<400	nM	IC50	US-10583137-B2. Triazole DAGLα inhibitors (2020)
GtoPdb	-	-	8.6	pIC50	-	-	-	Proc Natl Acad Sci USA (2016) 113: 26-33 [PMID:26668358]
diacylglycerol lipase β/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]
αβ-Hydrolase 6/Monoacylglycerol lipase ABHD6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189127] [GtoPdb: 2919] [UniProtKB: Q9BV23]
ChEMBL	Inhibition of human recombinant ABHD6	B	8.55	pIC50	2.8	nM	IC50	Eur J Med Chem (2020) 198: 112353-112353 [PMID:32371333]
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 ABHD6 in mouse brain membrane using HT-01 probe as substrate incubated for 30 mins by gel based competitive ABPP assay	B	6.9	pIC50	126	nM	IC50	Eur J Med Chem (2020) 198: 112353-112353 [PMID:32371333]
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]

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]