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Gel-based ABPP (CES1) from Article 10.1021/acschembio.6b00266: "Discovery of a Selective Covalent Inhibitor of Lysophospholipase-like 1 (LYPLAL1) as a Tool to Evaluate the Role of this Serine Hydrolase in Metabolism."
Assay data:7 Active, 6 Activity ≤ 1 µM, 12 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Fluorescent ACAT Assay from Article 10.1111/cbdd.12419: "Synthesis, biological evaluation, and molecular docking studies of xanthone sulfonamides as ACAT inhibitors."
Assay data:4 Active, 12 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Enzyme Inhibition Assay from Article 10.1016/s1074-5521(03)00071-1: "Crystal structure of human carboxylesterase 1 complexed with the Alzheimer's drug tacrine: from binding promiscuity to selective inhibition."
Assay data:1 Active, 3 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Enzyme Inhibition Assay from Article 10.1021/jm0706867: "Planarity and constraint of the carbonyl groups in 1,2-diones are determinants for selective inhibition of human carboxylesterase 1."
Assay data:17 Active, 11 Activity ≤ 1 µM, 18 Tested
Enzyme Inhibition Assay from Article 10.1021/jm061471k: "Selective inhibition of carboxylesterases by isatins, indole-2,3-diones."
Assay data:40 Active, 23 Activity ≤ 1 µM, 65 Tested
Enzyme Inhibition Assay from Article 10.1021/jm049011j: "Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases."
Assay data:36 Active, 30 Activity ≤ 1 µM, 60 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of human recombinant CES1 expressed in baculovirus infected BTI insect cells using 4-NPA as substrate by spectrophotometric analysis
Assay data:13 Active, 13 Activity ≤ 1 µM, 13 Tested
Inhibition of hCES1A in human liver microsome assessed as reduction in D-Iuciferin methyl ester hydrolysis preincubated for 10 mins followed by substrate addition measured after 10 mins by luminescence analysis
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of CES1A1 in human liver microsomes using D-luciferin methyl ester as substrate preincubated for 10 mins followed by substrate addition and measured after 10 mins by fluorescence assay
Assay data:9 Active, 9 Activity ≤ 1 µM, 9 Tested
Substrate activity at human carboxylesterase 1 expressed in baculovirus infected Sf9 insect cells assessed as enzyme-catalysed compound cleavage incubated for 2 hrs by HPLC analysis
Assay data:7 Tested
Inhibition of human CE1 using D-luciferin methyl ester as substrate preincubated for 10 mins followed by substrate addition and measured after 10 mins by luminescence assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 14 Tested
Stability assessed as recombinant human carboxyesterase-1 mediated compound hydrolysis by measuring half life at 50 ug/ml at 37 degC at pH 7.4
SummaryRelated BioAssays by Target
inhibition of FP-labeling of CE-1 (unknown origin) preincubated with mouse heart proteomes for 10 min followed by addition of FP-rhodamine
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Prodrug conversion assessed as CES1 (unknown origin) mediated aztreonam and beta-lactam ring-opened prodrug intermediate release in 2.5% acetonitrile in 0.05M citrate buffer at 0.5 mg/ml at pH 4.7 at 37degC in presence of CES1 at lower concentration by HPLC analysis
Assay data:3 Tested
Prodrug conversion assessed as CES1 (unknown origin) mediated aztreonam release in 2.5% acetonitrile in 0.05M citrate buffer at 0.5 mg/ml at pH 4.7 at 37degC measured immediately in presence of 150 units/ml of CES1 enzyme by HPLC analysis
Prodrug conversion assessed as CES1 (unknown origin) mediated aztreonam release in 2.5% acetonitrile in 0.05M citrate buffer at 0.5 mg/ml at pH 4.7 at 37degC after 30 mins in presence of 150 units/ml of CES1 enzyme by HPLC analysis
Prodrug conversion assessed as CES1 (unknown origin) mediated aztreonam release in 2.5% acetonitrile in 0.05M citrate buffer at 0.5 mg/ml at pH 4.7 at 37degC after 20 mins in presence of 150 units/ml of CES1 enzyme by HPLC analysis
Prodrug conversion assessed as CES1 (unknown origin) mediated aztreonam release in 2.5% acetonitrile in 0.05M citrate buffer at 0.5 mg/ml at pH 4.7 at 37degC after 10 mins in presence of 150 units/ml of CES1 enzyme by HPLC analysis
Prodrug conversion assessed as CES1 (unknown origin) mediated aztreonam release in 2.5% acetonitrile in 0.05M citrate buffer at 0.5 mg/ml at pH 4.7 at 37degC after 5 mins in presence of 150 units/ml of CES1 enzyme by HPLC analysis
Prodrug conversion assessed as CES1 (unknown origin) mediated aztreonam release in 2.5% acetonitrile in 0.05M citrate buffer at 0.5 mg/ml at pH 4.7 at 37degC after 2 mins in presence of 150 units/ml of CES1 enzyme by HPLC analysis
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