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Assay Detail

CHEMBL3607519

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

Binding
Inhibition of 17beta-HSD3 in rat testes microsomes using [14C]-4-androstene-3,17-dione as substrate after 2 hrs
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Testis
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

17-beta-hydroxysteroid dehydrogenase type 3 (CHEMBL1075158)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, chemical synthesis and biological evaluation of 3-spiromorpholinone/3-spirocarbamate androsterone derivatives as inhibitors of 17β-hydroxysteroid dehydrogenase type 3.
Djigoué GB, Kenmogne LC, Roy J, Maltais R, Poirier D.
Bioorg Med Chem (2015) 23 : 5433 -5451
PubMed 26277760 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.26 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1813731 1 7.89
CHEMBL3605211 1 7.55
CHEMBL3605212 1 7.06
CHEMBL87285 ANDROSTERONE 1 7.05
CHEMBL274826 ANDROSTENEDIONE -1.0 1 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1813731 IC50 = 13.0 nM 7.89
CHEMBL3605211 IC50 = 28.0 nM 7.55
CHEMBL3605212 IC50 = 88.0 nM 7.06
CHEMBL87285 ANDROSTERONE IC50 = 90.0 nM 7.05
CHEMBL274826 ANDROSTENEDIONE IC50 = 169.0 nM 6.77