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Assay Detail

CHEMBL2396181

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

Binding
Inhibition of human microsomal 11beta-HSD1 assessed as inhibition of conversion of radiolabeled cortisone to radiolabeled cortisol by cell-based assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Evaluation of selective inhibitors of 11β-HSD1 for the treatment of hypertension.
Bauman DR, Whitehead A, Contino LC, Cui J, Garcia-Calvo M, Gu X, Kevin N, Ma X, Pai LY, Shah K, Shen X, Stribling S, Zokian HJ, Metzger J, Shevell DE, Waddell ST.
Bioorg Med Chem Lett (2013) 23 : 3650 -3653
PubMed 23659858 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.51 5.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2391969 1 5.51
CHEMBL373257 1 -
CHEMBL1761313 1 -
CHEMBL1761321 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2391969 IC50 = 3100.0 nM 5.51
CHEMBL373257 IC50 = 2200.0 nM -
CHEMBL1761313 IC50 > 4000.0 nM -
CHEMBL1761321 IC50 > 4000.0 nM -