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Assay Detail

CHEMBL853223

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

Binding
Inhibition of human recombinant 11-beta-HSD1 transfected in intact HEK293 cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

11-beta-hydroxysteroid dehydrogenase 1 (CHEMBL4235)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of new 11beta-hydroxysteroid dehydrogenase type 1 inhibitors by common feature pharmacophore modeling and virtual screening.
Schuster D, Maurer EM, Laggner C, Nashev LG, Wilckens T, Langer T, Odermatt A.
J Med Chem (2006) 49 : 3454 -3466
PubMed 16759088 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.57 6.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL211039 1 6.39
CHEMBL425772 1 5.99
CHEMBL207413 ACETOXOLONE -1.0 1 5.46
CHEMBL382614 1 5.42
CHEMBL210465 1 5.28
CHEMBL380677 1 4.90
CHEMBL206908 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL211039 IC50 = 410.0 nM 6.39
CHEMBL425772 IC50 = 1020.0 nM 5.99
CHEMBL207413 ACETOXOLONE IC50 = 3450.0 nM 5.46
CHEMBL382614 IC50 = 3840.0 nM 5.42
CHEMBL210465 IC50 = 5210.0 nM 5.28
CHEMBL380677 IC50 = 12600.0 nM 4.90
CHEMBL206908 IC50 > 50000.0 nM -