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Inhibition of human recombinant DAGLalpha expressed in African green monkey COS7 cells by beta counter analysis
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
In Vitro Inhibition of DAGL from US Patent US10583137: "Triazole DAGLα inhibitors"
Assay data:56 Active, 34 Activity ≤ 1 µM, 56 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition of mouse brain membrane DAGLalpha assessed as enzyme remaining activity at 10 uM preincubated for 30 mins followed by MB064 or FP-TAMRA addition and measured after 15 mins by SDS-PAGE based ABPP analysis relative to control
Inhibition of DAGLalpha (unknown origin) by natural substrate assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of human DAGLalpha using DAG as substrate assessed as accumulation of 2-AG
Inhibition of DAGLalpha in mouse brain proteome pre-incubated for 30 mins followed by ABP MB064 probe addition for 15 mins by ABPP assay
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Inhibition of human DAGLalpha expressed in HEK293T cell membrane fractions using PNP butyrate as substrate preincubated for 20 mins followed by substrate addition by colorimetric surrogate substrate assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
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
Assay data:5 Active, 1 Activity ≤ 1 nM, 4 Activity ≤ 1 µM, 5 Tested
Inhibition of full length V5 tagged human DAGLalpha expressed in African green monkey COS7 cells using sn-1-stearoyl-[14C]-arachidonoyl-glycerol as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by radiometric natural substrate assay
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
Inhibition of human C-terminal HA-tagged DAGLalpha expressed in HEK293F cell membrane fractions using DiFMU-octanoate as substrate by fluorogenic surrogate substrate assay
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 2 Tested
Inhibition of human C-terminal HA-tagged DAGLalpha expressed in HEK293F cell membrane fractions using PNP butyrate as substrate by colorimetric surrogate substrate assay
Assay data:2 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 2 Tested
Inhibition of recombinant human DAGLalpha expressed in COS7 cells at 100 uM using [14C]-oleoyl-2-arachidonoyl-glycerol as substrate measured after 20 mins by beta-counting method relative to control
Assay data:3 Tested
Inhibition of recombinant human DAGLalpha expressed in COS7 cells at 50 uM using [14C]-oleoyl-2-arachidonoyl-glycerol as substrate measured after 20 mins by beta-counting method relative to control
Assay data:8 Tested
Inhibition of recombinant human DAGLalpha expressed in COS7 cells using [14C]-oleoyl-2-arachidonoyl-glycerol as substrate measured after 20 mins by beta-counting method
Assay data:11 Tested
Inhibition of mouse DAGL-alpha expressed in HEK293T cell membranes assessed as inactivation constant pre-incubated for 20 mins before PNP-butyrate substrate addition and measured after 30 mins by surrogate substrate assay
Assay data:7 Tested
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
Assay data:5 Active, 3 Activity ≤ 1 nM, 5 Activity ≤ 1 µM, 8 Tested
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
Assay data:7 Active, 2 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 8 Tested
Inhibition of DGLalpha in rat brain homogenates using diheptadecanoyl-glycerol as substrate measured after 30 mins in presence of [2H5]-2AG by LC-MS/MS analysis
Inhibition of MB064 labelling of DAGLalpha in mouse brain homogenates at 10 uM pretreated for 30 mins followed by MB064 addition and measured after 20 mins by activity based protein profiling assay relative to control
Assay data:22 Tested
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