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Drug metabolism assessed as human UGT1A8-mediated T-5224 hydroxyl O-glucuronide formation after 10 to 60 mins in presence of UDP-glucuronic acid by HPLC method
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Drug metabolism assessed as human recombinant UGT1A8-mediated (2S,3S,4S,5R,6S)-6-(2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid formation at 10 uM after 30 mins by LC-MS/MS analysis
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Activity of human recombinant UGT1A8 expressed in baculovirus-infected Sf9 cells assessed as glucuronidation activity per mg of protein at 100 to 200 uM after 60 mins in presence of 3 mM UDP-GlcUA
Assay data:2 Tested
Substrate inhibition of human recombinant UGT1A8 assessed as IRI-O-4'-monoglucuronide formation incubated for 5 mins prior to UDPGA addition measured after 90 mins by Eadie-Hoftsee plot analysis
Activity of human recombinant UGT1A8 assessed as intrinsic clearance incubated for 5 mins prior to UDPGA addition measured after 90 mins
Activity of human recombinant UGT1A8 assessed as IRI-O-5-monoglucuronide formation incubated for 5 mins prior to UDPGA addition measured after 90 mins by Eadie-Hoftsee plot analysis
Substrate inhibition of human recombinant UGT1A8 assessed as IRI-O-5-monoglucuronide formation incubated for 5 mins prior to UDPGA addition measured after 90 mins by Eadie-Hoftsee plot analysis
Activity of human recombinant UGT1A8 assessed as IRI-O-4'-monoglucuronide formation incubated for 5 mins prior to UDPGA addition measured after 90 mins by Eadie-Hoftsee plot analysis
Drug metabolism assessed as human recombinant UGT1A8-mediated irilone-O-5-monoglucuronide formation at 25 uM incubated for 5 mins prior to UDPGA addition measured after 90 mins by HPLC-DAD analysis
Drug metabolism assessed as human recombinant UGT1A8-mediated irilone-O-4'-monoglucuronide formation at 25 uM incubated for 5 mins prior to UDPGA addition measured after 90 mins by HPLC-DAD analysis
Drug level assessed as human recombinant UGT1A8-mediated glucuronidation treated with 25 uM irilone incubated for 5 mins prior to UDPGA addition measured after 90 mins by HPLC-DAD analysis
Drug metabolism assessed as human UGT1A8-mediated T-5224 hydroxyl O-glucuronide formation per mg protein after 10 to 60 mins in presence of UDP-glucuronic acid by HPLC method
Drug metabolism assessed as human recombinant UGT1A8-mediated compound formation treated with AMG 853 at 10 uM after 30 mins by LC-MS/MS analysis
Substrate inhibition of human UGT1A8-mediated T-5224 hydroxyl O-glucuronide formation after 10 to 60 mins in presence of UDP-glucuronic acid by HPLC method
Drug metabolism assessed as Vmax/Km ratio for human UGT1A8-mediated T-5224 hydroxyl O-glucuronide formation per mg protein after 10 to 60 mins in presence of UDP-glucuronic acid by HPLC method
Drug metabolism assessed as human UGT1A8-mediated T-5224 hydroxyl O-glucuronide formation rate after 10 to 60 mins in presence of UDP-glucuronic acid by HPLC method
Drug metabolism assessed as Kcat to Km ratio for human UGT1A8-mediated T-5224 hydroxyl O-glucuronide formation per mg protein after 10 to 60 mins in presence of UDP-glucuronic acid by HPLC method
Drug metabolism assessed as human UGT1A8-mediated T-5224 hydroxyl O-glucuronide formation at 5 to 50 uM after 60 mins in presence of UDP-glucuronic acid by HPLC method
Drug level assessed as human UGT1A8-mediated compound formation from 5 to 50 uM T-5224 after 60 mins in presence of UDP-glucuronic acid by HPLC method
Drug level assessed as human UGT1A8-mediated compound formation from 5 to 50 uM T-5224 after 10 to 60 mins in presence of UDP-glucuronic acid by HPLC method
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