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HSD2 Activity from US Patent US11858959: "Glycyrrhetinic acid derivatives for use in treating hyperkalemia"
Assay data:44 Active, 28 Activity ≤ 1 µM, 46 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition of human 11beta-HSD2
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Homogenous Time-Resolved Fluorescence (HTRF) Assay from US Patent US9073906: "Sulfamide derivative having an adamantyl group and its pharmaceutically acceptable salt"
Assay data:21 Active, 5 Activity ≤ 1 nM, 19 Activity ≤ 1 µM, 23 Tested
11beta-HSD2 Homogeneous Time-Resolved Fluorescence (HTRF) Assay from Article 10.1016/j.bmcl.2009.02.123: "Discovery and structure-guided drug design of inhibitors of 11beta-hydroxysteroid-dehydrogenase type I based on a spiro-carboxamide scaffold."
Assay data:4 Tested
SummaryPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Human 11beta-HSD1 Scintillation Proximity Assay (SPA) from Article 10.1021/jm701551j: "2-Amino-1,3-thiazol-4(5H)-ones as Potent and Selective 11beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitors: Enzyme-Ligand Co-Crystal Structure and Demonstration of Pharmacodynamic Effects in C57Bl/6 Mice."
Assay data:24 Active, 24 Activity ≤ 1 µM, 24 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Human and Mouse 11beta-HSD1 SPA Assay from Article 10.1016/j.bmcl.2006.10.074: "Discovery of adamantane ethers as inhibitors of 11beta-HSD-1: Synthesis and biological evaluation."
Assay data:20 Active, 20 Activity ≤ 1 µM, 20 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of human 11beta-HSD2 expressed in microsomes
Assay data:1 Tested
Inhibition of human 11beta-HSD2 expressed in microsomes at 10 uM relative to control
Inhibition of human 11beta-HSD2 expressed in microsomes at 1 uM relative to control
Inhibition of recombinant human 11beta-HSD2 expressed in cells up to 30 uM using cortisone as substrate by LC-MS analysis
Inhibition of 11beta-HSD2 (unknown origin) expressed in HEK293 cells using cortisone as substrate measured after 2 hrs in presence of NAD+ by HTRF assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 20 Tested
RNAi screen for vemurafenib enhancer genes in BRAFV600 melanoma - Primary Screen
Assay data:790 Active, 18119 Tested
Summary
Inhibition of human full-length 11beta-HSD2 expressed in HEK293 cells using cortisol as substrate after 2 hrs by LC-MS analysis
Assay data:6 Active, 6 Activity ≤ 1 µM, 6 Tested
Inhibition of human full-length 11beta-HSD2 expressed in HEK293 cells at 10 uM using cortisol as substrate after 2 hrs by LC-MS analysis relative to control
Inhibition of full-length human 11beta-HSD2 expressed in HEK293 microsomal fraction using [3H]cortisone as substrate after 2 hr by scintillation proximity assay
Assay data:3 Active, 1 Activity ≤ 1 µM, 7 Tested
Inhibition of 11beta-HSD2 (unknown origin)
Inhibition of recombinant human 11beta-HSD2 expressed in HEK293 cells assessed as residual activity at 20 uM using cortisol as substrate after 10 mins in presence of radiolabeled tracer substrate by scintillation counting method relative to control
Assay data:11 Tested
Inhibition of human 11beta-HSD2 up to 30 uM
Inhibition of human 11beta-HSD2 expressed in HEK293 cell lysates at 200 uM using [1,2,6,7-3H]-cortisol as substrate preincubated for 10 mins followed by substrate addition in presence of NAD by scintillation counting relative to control
Inhibition of human 11beta-HSD2 expressed in HEK293 cell lysates at 10 uM using [1,2,6,7-3H]-cortisol as substrate preincubated for 10 mins followed by substrate addition in presence of NAD by scintillation counting relative to control
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