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UGT1A1 Inhibition Assay from US Patent US11938127: "Methods and compositions relating to steroid hormone receptor-dependent proliferative disorders"
Assay data:1 Active, 1 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Binding affinity to UGT2B7 (unknown origin) assessed as inhibition constant
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity to UGT1A6 (unknown origin) assessed as inhibition constant
Inhibition of human UGT1A1
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of UGT1A1 in human liver microsomes using beta-estradiol as substrate incubated for 40 mins by LC-MS/MS analysis
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Inhibition of human recombinant UGT1A1 using bilirubin as substrate incubated for 40 mins by LC-MS/MS analysis
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Metabolic stability in human liver microsomes S9 fraction assessed as UGT-mediated metabolism by measuring parent compound remaining measured after 60 mins in presence of NADPH
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Metabolic stability in human liver microsomes S9 fraction assessed as UGT-mediated metabolism by measuring parent compound remaining measured after 30 mins in presence of NADPH
Metabolic stability in human liver microsomes S9 fraction assessed as UGT-mediated metabolism by measuring parent compound remaining measured after 15 mins in presence of NADPH
Inhibition of UGT1A1(unknown origin)
Metabolic stability assessed as human UGT-mediated metabolism by measuring half life by phase II UGT conjugation assay
Assay data:1 Tested
Metabolic stability in human assessed as UGT-mediated metabolism by measuring half life
UDP-glucuronosyltransferase Activity Assay from Article 10.3109/14756366.2010.518965: "The inhibition study of human UDP-glucuronosyltransferases with cytochrome P450 selective substrates and inhibitors."
Assay data:2 Active, 20 Tested
Inhibition of UGT1A1 (unknown origin)
Metabolic stability assessed as human UGT-mediated metabolism by measuring half life
Metabolic stability of the compound in human liver microsomes S9 fraction assessed as UGT-mediated metabolism by measuring parent compound remaining at 5 uM measured after 60 mins in presence of UDPGA by UPLC-MS analysis
Metabolic stability of the compound in human liver microsomes S9 fraction assessed as UGT-mediated metabolism by measuring parent compound remaining at 5 uM measured after 30 mins in presence of UDPGA by UPLC-MS analysis
Metabolic stability of the compound in human liver microsomes S9 fraction assessed as UGT-mediated metabolism by measuring parent compound remaining at 5 uM measured after 15 mins in presence of UDPGA by UPLC-MS analysis
Inhibition of UGT2B15 (unknown origin)
Inhibition of UGT2B7 (unknown origin)
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