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Inhibition of human AKR1C1-mediated progesterone metabolism expressed in bovine aortic endothelial cells assessed as formation of 20alpha-hydroxyprogesterone pretreated for 2 hrs before progesterone challenge measured after 6 hrs by LC/MS analysis
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Ratio of kcat/km for human recombinant AKR1C1 Leu308Val mutant expressed in Escherichia coli JM109 after 15 mins
Assay data:3 Tested
SummaryPubMed CitationRelated BioAssays by Target
Ratio of Km for human recombinant AKR1C1 Leu308Val mutant to Km for human recombinant wild type AKR1C1
Activity at human recombinant AKR1C1 Leu308Ala mutant expressed in Escherichia coli JM109 after 15 mins
Assay data:1 Tested
Ratio of kcat/km for human recombinant AKR1C1 Leu308Ala mutant expressed in Escherichia coli JM109 after 15 mins
Ratio of Km for human recombinant AKR1C1 Leu308Ala mutant to Km for human recombinant wild type AKR1C1
Ratio of Kcat/Km for human recombinant AKR1C1 Leu308Val mutant to Kcat/Km for human recombinant wild type AKR1C1
Ratio of Kcat/Km for human recombinant AKR1C1 Leu308Ala mutant to Kcat/Km for human recombinant wild type AKR1C1
Inhibition of human wild type AKR1C1 dehydrogenase activity by fluorometric assay
Assay data:12 Active, 1 Activity ≤ 1 nM, 12 Activity ≤ 1 µM, 12 Tested
Inhibition of human AKR1C1 Leu308Val mutant dehydrogenase activity by fluorometric assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Inhibition of human AKR1C1 Leu308Ala mutant dehydrogenase activity by fluorometric assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Inhibition of human AKR1C1-mediated progesterone metabolism expressed in bovine aortic endothelial cells assessed as formation of 20alpha-hydroxyprogesterone at 2 uM pretreated for 2 hrs before progesterone challenge measured after 6 hrs by LC/MS analysis
Inhibition of human AKR1C1-mediated progesterone metabolism expressed in bovine aortic endothelial cells assessed as formation of 20alpha-hydroxyprogesterone at 0.01 uM pretreated for 2 hrs before progesterone challenge measured after 6 hrs by LC/MS analysis
Activity at human recombinant AKR1C1 Leu308Val mutant expressed in Escherichia coli JM109 after 15 mins
Competitive inhibition of human recombinant AKR1C1 Leu54Val mutant by fluorescence assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Competitive inhibition of human recombinant AKR1C1 Leu306Ala mutant by fluorescence assay
Binding affinity to human AKR1C1 after 4 hrs by crystallography
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Competitive inhibition of human recombinant AKR1C1 Leu308Val mutant by fluorescence assay
Competitive inhibition of human recombinant AKR1C1 Leu308Ala mutant by fluorescence assay
Competitive inhibition of human recombinant AKR1C1 Phe311Leu mutant by fluorescence assay
Assay data:2 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
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