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Assay Detail

CHEMBL911188

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

Functional
Antagonist activity against human androgen receptor in CV1 cells measured as inhibition of DHT-stimulated luciferase reporter gene activity by cotransfection assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Expert

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
van Oeveren A, Motamedi M, Mani NS, Marschke KB, López FJ, Schrader WT, Negro-Vilar A, Zhi L.
J Med Chem (2006) 49 : 6143 -6146
PubMed 17034117 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.58 7.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL217428 1 7.78
CHEMBL385509 1 7.58
CHEMBL405835 1 7.56
CHEMBL216949 1 7.53
CHEMBL217168 1 7.47
CHEMBL436784 1 -
CHEMBL267260 1 -
CHEMBL217769 1 -
CHEMBL217324 1 -
CHEMBL217402 1 -
CHEMBL442240 1 -
CHEMBL277378 1 -
CHEMBL27769 STANOLONE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL217428 IC50 = 16.5 nM 7.78
CHEMBL385509 IC50 = 26.0 nM 7.58
CHEMBL405835 IC50 = 27.5 nM 7.56
CHEMBL216949 IC50 = 29.5 nM 7.53
CHEMBL217168 IC50 = 34.0 nM 7.47
CHEMBL436784 IC50 > 10000.0 nM -
CHEMBL267260 IC50 > 10000.0 nM -
CHEMBL217769 IC50 > 10000.0 nM -
CHEMBL217324 IC50 > 10000.0 nM -
CHEMBL217402 IC50 > 10000.0 nM -
CHEMBL442240 IC50 > 10000.0 nM -
CHEMBL277378 IC50 > 10000.0 nM -
CHEMBL27769 STANOLONE IC50 > 10000.0 nM -