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Assay Detail

CHEMBL4132704

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of 11beta-HSD1 in CD1 mouse liver microsomes using cortisone as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by LC-MS analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Liver
Subcellular microsomes
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

11-beta-hydroxysteroid dehydrogenase 1 (CHEMBL3910)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Design, synthesis and in vivo study of novel pyrrolidine-based 11β-HSD1 inhibitors for age-related cognitive dysfunction.
Leiva R, Griñan-Ferré C, Seira C, Valverde E, McBride A, Binnie M, Pérez B, Luque FJ, Pallàs M, Bidon-Chanal A, Webster SP, Vázquez S.
Eur J Med Chem (2017) 139 : 412 -428
PubMed 28818766 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.10 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4162610 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4162610 IC50 = 80.0 nM 7.10