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Inhibition of mouse 11beta-HSD1 in liver microsome incubated for 24 hrs by LC-MS analysis
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of mouse 11beta-HSD1 expressed in CHO-K1 cells incubated for 3 hrs by HTRF assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Inhibition of mouse 11beta-HSD1 expressed in 3T3-L1 cells incubated for 24 hrs by HTRF assay
Inhibition of mouse 11beta-HSD1 incubated for 24 hrs by HTRF assay
Inhibition of mouse 11beta-HSD1 expressed in CHO-K1 cells incubated for 24 hrs by HTRF assay
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of mouse 11beta-HSD1 using steroid as substrate incubated for 20 to 30 mins by microplate fluorimeter analysis
Inhibition of mouse 11beta-HSD1
Assay data:2 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Enzyme Assay from US Patent US8486964: "Fused pyrrolidino-cyclopropane derivatives as selective 11-beta-hydroxysteroid dehydrogenase type 1 inhibitors"
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Human 11beta-HSD1 SPA Assay from Article 10.1016/j.bmcl.2008.05.025: "Discovery and initial SAR of arylsulfonylpiperazine inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1)."
Assay data:44 Active, 46 Activity ≤ 1 µM, 46 Tested
11beta-HSD1 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:13 Active, 1 Activity ≤ 1 nM, 10 Activity ≤ 1 µM, 13 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Mouse and Rat 11beta-HSD1 SPA Assay 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."
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
Inhibition of mouse 11beta-HSD1 expressed in microsomes
Ex vivo inhibition of 11 beta-HSD1 in brain of iv dosed mouse by measuring cortisol amount after 1 hr by ELISA
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
In vivo inhibition of 11 beta-HSD1 in brain of mouse at 30 mg/kg, po relative to control
In vivo inhibition of 11 beta-HSD1 in brain of mouse at 20 mg/kg, po relative to control
Assay data:4 Tested
Inhibition of mouse 11beta-HSD1 expressed in CHOK1 cells using XL665-labeled cortisol as substrate measured after 24 hrs by HTRF assay
Assay data:12 Active, 3 Activity ≤ 1 nM, 10 Activity ≤ 1 µM, 12 Tested
Inhibition of mouse microsomal 11beta-HSD1 overexpressed in HEK293 cells using [3H]-cortisone as substrate assessed as formation of [3H]-cortisol at 10 uM using [3H]cortisone by scintillation proximity assay in presence of NADPH
Assay data:5 Tested
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