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Assay Detail

CHEMBL2415372

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

Binding
Inhibition of human 17beta-HSD5 expressed in human CWR22R cells using androstenedione as substrate assessed as testosterone synthesis after 4 hrs
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CWR22R
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Aldo-keto reductase family 1 member C3 (CHEMBL4681)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 2-methyl-1-{1-[(5-methyl-1H-indol-2-yl)carbonyl]piperidin-4-yl}propan-2-ol: a novel, potent and selective type 5 17β-hydroxysteroid dehydrogenase inhibitor.
Watanabe K, Kakefuda A, Yasuda M, Enjo K, Kikuchi A, Furutani T, Naritomi Y, Otsuka Y, Okada M, Ohta M.
Bioorg Med Chem (2013) 21 : 5261 -5270
PubMed 23845281 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.98 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2413849 1 8.72
CHEMBL2413863 1 7.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2413849 IC50 = 1.9 nM 8.72
CHEMBL2413863 IC50 = 58.0 nM 7.24