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Assay Detail

CHEMBL2446445

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

Binding
Antagonist activity at androgen receptor H874Y mutant (unknown origin) expressed in human 22Rv1 cells assessed as inhibition of DHT-induced cell growth after 3 days by WST-8 assay
4
Total Activities
4
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

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and Synthesis of 4-(4-Benzoylaminophenoxy)phenol Derivatives As Androgen Receptor Antagonists.
Yamada A, Fujii S, Mori S, Kagechika H.
ACS Med Chem Lett (2013) 4 : 937 -941
PubMed 24900588 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.90 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2441094 1 6.66
CHEMBL2441092 1 5.89
CHEMBL2441107 1 5.72
CHEMBL409 BICALUTAMIDE 4.0 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2441094 IC50 = 220.0 nM 6.66
CHEMBL2441092 IC50 = 1300.0 nM 5.89
CHEMBL2441107 IC50 = 1900.0 nM 5.72
CHEMBL409 BICALUTAMIDE IC50 = 4600.0 nM 5.34