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Inhibition Assay from Article 10.1080/14756360109162353: "Inhibitors of human and rat testes microsomal 17beta-hydroxysteroid dehydrogenase (17beta-HSD) as potential agents for prostatic cancer."
Assay data:5 Active, 14 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of human 17-beta-HSD3 expressed in LNCaP cells assessed as reduction in oxidation of [14C]-4-androstene-3,17-dione to [14C]-testosterone at 3 uM incubated for 1 hr by thin layer chromatography
Assay data:7 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of human 17-beta-HSD3 expressed in LNCaP cells assessed as reduction in oxidation of [14C]-4-androstene-3,17-dione to [14C]-testosterone at 0.3 uM incubated for 1 hr by thin layer chromatography
Potency index, ratio of RM-532-105 IC50 to test compound IC50 for 17beta-HSD3 (unknown origin) expressed in human LNCAP cells
Assay data:5 Tested
Inhibition of 17beta-HSD3 in Sprague-Dawley rat testes microsomal fraction assessed as reduction in [14C]-testosterone formation from [14C]-4-androstene-3,17-dione measured after 2 hrs
Assay data:5 Active, 5 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of 17beta-HSD3 (unknown origin) expressed in human LNCAP cells assessed as reduction in [14C]-testosterone formation from [14C]-4-androstene-3,17-dione measured after 1 hr
Assay data:11 Active, 10 Activity ≤ 1 µM, 11 Tested
Inhibition of 17beta-HSD3 (unknown origin) expressed in human LNCAP cells assessed as reduction in [14C]-testosterone formation from [14C]-4-androstene-3,17-dione at 1 uM measured after 1 hr relative to control
Assay data:17 Tested
Inhibition of 17beta-HSD3 (unknown origin) expressed in human LNCAP cells assessed as reduction in [14C]-testosterone formation from [14C]-4-androstene-3,17-dione at 0.5 uM measured after 1 hr relative to control
Inhibition of 17beta-HSD3 (unknown origin) expressed in human LNCAP cells assessed as reduction in [14C]-testosterone formation from [14C]-4-androstene-3,17-dione at 0.1 uM measured after 1 hr relative to control
Inhibition of 17-beta-HSD3 (unknown origin) expressed in human LNCaP cells using [14C]-4-androstene-3,17-dione as substrate assessed as reduction of [14C]-testosterone level at 0.1 to 1 uM after 1 hr by TLC method
Assay data:3 Tested
Inhibition of 17-beta-HSD3 (unknown origin) expressed in human LNCaP cells using [14C]-4-androstene-3,17-dione as substrate assessed as reduction of [14C]-testosterone level after 1 hr by TLC method
Assay data:3 Active, 2 Activity ≤ 1 µM, 3 Tested
Inhibition of 17betaHSD3 (unknown origin) transfected in HEK293 cells
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of 17betaHSD3 (unknown origin) transfected in human LNCAP cells assessed as conversion of [14C]-4-androstene-3,17-dione into [14C]-testosterone after 3 hrs
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Inhibition of 17beta-HSD3 (unknown origin) expressed in human LNCaP cells using [14C]-4-androstene-3,17-dione as substrate at 0.5 uM after 3 hrs
Assay data:1 Tested
Inhibition of 17beta-HSD3 (unknown origin) expressed in human LNCaP cells using [14C]-4-androstene-3,17-dione as substrate at 1 uM after 3 hrs
Assay data:2 Tested
Ratio of delta4-dione IC50 to compound IC50 for 17beta-HSD3 in rat testes microsomes
Inhibition of 17beta-HSD3 in rat testes microsomes using [14C]-4-androstene-3,17-dione as substrate after 2 hrs
Inhibition of 17beta-HSD3 in rat testes microsomes using [14C]-4-androstene-3,17-dione as substrate measured based on 18% of initial enzyme transformation at 0.01 uM after 2 hrs
Inhibition of 17beta-HSD3 in rat testes microsomes using [14C]-4-androstene-3,17-dione as substrate measured based on 33% of initial enzyme transformation at 10 uM after 2 hrs
Assay data:13 Tested
Inhibition of 17beta-HSD3 in rat testes microsomes using [14C]-4-androstene-3,17-dione as substrate measured based on 33% of initial enzyme transformation at 1 uM after 2 hrs
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