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Inhibition of S-COMT (unknown origin)
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of S-COMT (unknown origin) assessed as scopoletin formation by measuring fluorescence using 6,7-dihydroxycoumarin as substrate at 100 uM and measured for 60 mins by fluorescence based microplate reader assay
Assay data:6 Active, 11 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of S-COMT (unknown origin) assessed as scopoletin formation by measuring fluorescence using 6,7-dihydroxycoumarin as substrate at 10 uM and measured for 60 mins by fluorescence based microplate reader assay
Assay data:1 Active, 11 Tested
Inhibition of rat brain COMT using pyrocatechol as substrate by radiometric assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Fluorescence Polarization Assay from US Patent US9260413: "Inhibitors of catechol O-methyl transferase and their use in the treatment of psychotic disorders"
Assay data:5 Active, 5 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Radiochemical Assay from Article 10.1002/cbic.200400084: "Bisubstrate inhibitors of the enzyme catechol O-methyltransferase (COMT): efficient inhibition despite the lack of a nitro group."
Assay data:20 Active, 17 Activity ≤ 1 µM, 20 Tested
CATOMETHTRAN Cerep selectivity data (BI)
Assay data:1 Tested
SummaryRelated BioAssays by Target
Primary Screen for Target Class Profiling of Small Molecule Inhibitors of Methyltransferases
Assay data:968 Active, 24930 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Confirmatory Screen for Target Class Profiling of Small Molecule Inhibitors of Methyltransferases
Assay data:902 Active, 1111 Tested
Substrate activity at COMT (unknown origin) assessed as 3-methoxythyramine formation in presence of cofactor SAM incubated for 120 mins by HPLC analysis
Substrate activity at COMT (unknown origin) assessed as N-(4-Hydroxy-3-methoxyphenethyl)octanamide formation in presence of cofactor SAM at 180 mins by HPLC analysis
Substrate activity at COMT (unknown origin) assessed as N-(2-Fluoro-4,5-dimethoxyphenethyl)octanamide formation in presence of cofactor SAM at 180 mins by HPLC analysis
Binding affinity to human wild-type SUMO-tagged catechol O-methyltransferase assessed as dissociation constant by surface plasmon resonance analysis
Assay data:1 Active, 3 Tested
Inhibition of recombinant wild-type human COMT expressed in Escherichia coli BL21 using 4-nitrocatechol-Alexa488 as substrate in presence of cofactor SAM preincubated for 1 min followed by substrate addition and measured every 60 sec up to 180 times by fluorescence based microtiter plate reader analysis
Assay data:13 Active, 7 Activity ≤ 1 µM, 27 Tested
Inhibition of COMT (unknown origin)
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Inhibition of rat liver COMT using esculetin as substrate by fluorescence based spectrophotometry
Assay data:17 Active, 17 Activity ≤ 1 µM, 17 Tested
Potency index, ratio of IC50 of 1-(3,4-dihydroxy-5-nitro-phenyl)-3-(3-methoxyphenyl)prop-2-en-1-one to IC50 of compound for inhibition of rat liver COMT using esculetin as substrate by fluorescence based spectrophotometry
Binding affinity to COMT in SILAC labeled human H1299 cells incubated for 3 hrs followed by compound washout twice with PBS buffer to remove excess compound and further irradiated with UV-light at 365 nm for 20 mins by LC-MS/MS analysis
Assay data:1 Active, 1 Tested
Inhibition of MB-COMT in Wistar rat brain assessed as metanephrine formation preincubated for 20 mins followed by addition of adrenaline as substrate and SAM measured after 15 mins by chromatographic analysis
Assay data:14 Active, 2 Activity ≤ 1 nM, 14 Activity ≤ 1 µM, 16 Tested
Inhibition of S-COMT in Wistar rat liver assessed as metanephrine formation preincubated for 20 mins followed by addition of adrenaline as substrate and SAM measured after 5 mins by chromatographic analysis
Assay data:14 Active, 13 Activity ≤ 1 µM, 16 Tested
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