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HSD2 Activity from US Patent US20240209019: "COMPOUNDS AND METHODS FOR TREATING HYPERKALEMIA"
Assay data:38 Active, 29 Activity ≤ 1 µM, 47 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition of human 11beta-HSD2 incubated for 2 hrs by HPLC analysis
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of human 11beta-HSD2 incubated for 2 hrs
HSD2 Activity from US Patent US11858959: "Glycyrrhetinic acid derivatives for use in treating hyperkalemia"
Assay data:44 Active, 28 Activity ≤ 1 µM, 46 Tested
Inhibition of human 11beta-HSD2
Assay data:2 Tested
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
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 rat 11beta-HSD2 up to 20 uM
Inhibition of mouse 11beta-HSD2 up to 20 uM
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
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 full-length mouse 11beta-HSD2 expressed in HEK293 microsomal fraction using [3H]cortisone as substrate after 1 hr by scintillation proximity assay
Assay data:6 Tested
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