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Inhibition of human placental cytosolic fraction 17beta-HSD1 at 50 nM using [3H]-E1 as substrate in presence of NADH measured after 24 hrs by LC-MS/MS method
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of human placental cytosolic fraction 17beta-HSD1 at 50 nM using [3H]-E1 as substrate in presence of NADH measured after 6.5 hrs by LC-MS/MS method
Inhibition of human 17beta-HSD1 at 50 nM using [3H]-E1 as substrate measured after 13.5 hrs in presence of NADH by LC-MS/MS analysis
Inhibition of human placental cytosolic fraction 17beta-HSD1 using [3H]-E1 as substrate in presence of NADH measured after 10 mins by HPLC method
Assay data:19 Active, 17 Activity ≤ 1 µM, 19 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of 17beta-HSD1 in human T47D cells using [3H]E1S as substrate measured after 24 hrs by HPLC analysis
Inhibition of human placental cytosolic fraction 17beta-HSD1 at 1 uM using [3H]-E1 as substrate measured after 10 mins in presence of NADH by HPLC method
Assay data:20 Tested
Assay data:10 Active, 10 Activity ≤ 1 µM, 10 Tested
Inhibition of HSD17B1 (unknown origin) using estradiol as substrate incubated for 3 hrs and measured after 1 hr by NADH Glo luminescence assay
Assay data:33 Active, 96 Tested
SummaryCompounds, ActiveRelated BioAssays by Target
Radioactivity Assay from US Patent US8546392: "17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases"
Assay data:17 Active, 17 Activity ≤ 1 µM, 17 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Inhibition of 17beta-HSD1 from Article 10.1021/jm8006917: "Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1)."
Assay data:17 Active, 22 Activity ≤ 1 µM, 25 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Enzyme Inhibition on the Conversion of E2 to E1 by 17beta-HSD1 from Article 10.1096/fj.02-0026fje: "A concerted, rational design of type 1 17beta-hydroxysteroid dehydrogenase inhibitors: estradiol-adenosine hybrids with high affinity."
Assay data:1 Active, 1 Activity ≤ 1 µM, 2 Tested
Enzymatic Assay (Inhibition of Type 1 17beta-HSD) from Article 10.1096/fj.02-0026fje: "A concerted, rational design of type 1 17beta-hydroxysteroid dehydrogenase inhibitors: estradiol-adenosine hybrids with high affinity."
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Inhibition of human placental cytosolic fraction 17beta-HSD1 using [3H]-E1 as substrate in presence of NAD+ by radio-HPLC analysis
Assay data:16 Active, 4 Activity ≤ 1 nM, 16 Activity ≤ 1 µM, 16 Tested
Assay data:15 Active, 4 Activity ≤ 1 nM, 15 Activity ≤ 1 µM, 15 Tested
Inhibition of human placental cytosolic fraction 17beta-HSD1 at 10 nM using [3H]-E1 as substrate in presence of NAD+ by radio-HPLC analysis relative to control
Assay data:2 Tested
Assay data:22 Active, 1 Activity ≤ 1 nM, 22 Activity ≤ 1 µM, 22 Tested
RNAi screen for vemurafenib enhancer genes in BRAFV600 melanoma - Primary Screen
Assay data:790 Active, 18119 Tested
Summary
Irreversible inhibition of 17beta-HSD1 in human T47D cells at 50 nM preincubated for 2 hrs followed by compound washout and addition of [3H]-E1S/E1S as substrate measured after 24 hrs by HPLC based radio-detection method
Inhibition of human placental cytosolic 17beta-HSD1 at 1 uM using [3H]-E1/E1 substrate and NADH after 10 mins by HPLC based radio-detection method
Inhibition of 17beta-HSD1 in human T47D cells assessed as [3H]-E2 level at 200 nM after 48 hrs by HPLC based radio-detection method (Rvb = 95.2%)
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