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Assay Detail

CHEMBL807120

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

Functional
In vitro inhibition of DHT (dihydrotestosterone) on proliferation of androgen-sensitive cancer Schionogi (SC-3) cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Androgen receptor (CHEMBL3056)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis and in vitro activity of 17 beta-(N-alkyl/arylformamido)- and 17 beta-[(N-alkyl/aryl)alkyl/arylamido]-4-methyl-4-aza-3-oxo-5 alpha-androstan-3-ones as inhibitors of human 5 alpha-reductases and antagonists of the androgen receptor.
Li X, Singh SM, Labrie F.
J Med Chem (1995) 38 : 1158 -1173
PubMed 7707319 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.78 7.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17222 1 7.34
CHEMBL417627 1 7.30
CHEMBL491 HYDROXYFLUTAMIDE 2.0 1 7.28
CHEMBL17206 1 7.24
CHEMBL17506 1 7.05
CHEMBL16533 1 7.05
CHEMBL275153 1 7.02
CHEMBL16927 1 6.96
CHEMBL17268 1 6.79
CHEMBL277053 1 6.78
CHEMBL16863 1 6.77
CHEMBL2298601 1 6.33
CHEMBL16690 1 6.00
CHEMBL274276 1 6.00
CHEMBL17193 1 5.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17222 IC50 = 46.0 nM 7.34
CHEMBL417627 IC50 = 50.0 nM 7.30
CHEMBL491 HYDROXYFLUTAMIDE IC50 = 52.0 nM 7.28
CHEMBL17206 IC50 = 58.0 nM 7.24
CHEMBL17506 IC50 = 89.0 nM 7.05
CHEMBL16533 IC50 = 90.0 nM 7.05
CHEMBL275153 IC50 = 96.0 nM 7.02
CHEMBL16927 IC50 = 110.0 nM 6.96
CHEMBL17268 IC50 = 162.0 nM 6.79
CHEMBL277053 IC50 = 166.0 nM 6.78
CHEMBL16863 IC50 = 171.0 nM 6.77
CHEMBL2298601 IC50 = 463.0 nM 6.33
CHEMBL16690 IC50 = 994.0 nM 6.00
CHEMBL274276 IC50 = 989.0 nM 6.00
CHEMBL17193 IC50 = 1476.0 nM 5.83