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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 DAGLbeta 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
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of mouse DAGLbeta expressed in HEK293T cell membranes using SAG as substrate preincubated for 30 mins followed by substrate addition by enzyme coupled natural substrate assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
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
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
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
Assay data:5 Active, 4 Activity ≤ 1 µM, 5 Tested
Inhibition of full length 3' FLAG-tagged mouse DAGLbeta 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 DAGLbeta catalytic domain expressed in HEK293F cell membranes using EnzChek as substrate preincubated for 5 mins followed by substrate addition by fluorogenic surrogate substrate assay
Inhibition of DH379 probe binding to full length recombinant human DAGLbeta expressed in HEK293T cell membranes at 0.1 to 10000 nM after 30 mins by gel-based competitive activity based protein profiling assay
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of recombinant mouse DAGLbeta expressed in HEK293T cell membranes using PNP butyrate as substrate by colorimetric assay
Assay data:3 Active, 3 Activity ≤ 1 µM, 5 Tested
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
Inhibition of DAGLbeta (unknown origin)
Assay data:6 Active, 6 Activity ≤ 1 µM, 6 Tested
Inhibition of Daglb in mouse Neuro2a cells at 3 nM after 4 hrs by ABPP-SILAC assay
Assay data:3 Tested
Inhibition of FP-rhodamine-labelled recombinant mouse DAGLbeta expressed in HEK293T cells at 1 uM preincubated for 30 mins followed by FP-rhodamine labelling measured after 30 mins by gel-based competitive ABPP assay
Assay data:9 Tested
Inhibition of FP-rhodamine-labelled recombinant mouse DAGLbeta expressed in HEK293T cells at 10 uM preincubated for 30 mins followed by FP-rhodamine labelling measured after 30 mins by gel-based competitive ABPP assay
Assay data:5 Tested
Inhibition of FP-rhodamine-labelled recombinant mouse DAGLbeta expressed in HEK293T cells at 100 nM preincubated for 30 mins followed by FP-rhodamine labelling measured after 30 mins by gel-based competitive ABPP assay
Inhibition of DAGLB binding to FP-biotin in [12C][14N]-lysine, arginine and [13C6][15N2]-lysine, arginine labeled HEK293T cells at 20 uM after 1 hr by isotopic activity-based protein profiling-MudPIT assay
Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): fluorescence-based biochemical gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition of DAGLb by enantiomers of KT116
Assay data:2 Active, 3 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by DepositorRelated BioAssays by Same ProjectRelated BioAssays by Target
Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): LCMS-based biochemical dose response assay
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Same ProjectRelated BioAssays by Target
Assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): LC/MS-based biochemical inhibition of overexpressed DAGLb substrate turnover in vitro
Assay data:33 Active, 91 Tested
Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): fluorescence-based biochemical gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition of serine hydrolases in vitro
Assay data:3 Active, 3 Tested
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