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Assay Detail

CHEMBL911186

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

Functional
Agonist activity at human androgen receptor in CV1 cells measured as stimulation of 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
EC50 13 8.12 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL436784 1 9.70
CHEMBL217769 1 9.40
CHEMBL442240 1 8.82
CHEMBL217324 1 8.72
CHEMBL277378 1 8.68
CHEMBL217402 1 8.66
CHEMBL267260 1 8.55
CHEMBL27769 STANOLONE 2.0 1 8.29
CHEMBL217428 1 6.97
CHEMBL216949 1 5.89
CHEMBL405835 1 5.69
CHEMBL217168 1 -
CHEMBL385509 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL436784 EC50 = 0.2 nM 9.70
CHEMBL217769 EC50 = 0.4 nM 9.40
CHEMBL442240 EC50 = 1.5 nM 8.82
CHEMBL217324 EC50 = 1.9 nM 8.72
CHEMBL277378 EC50 = 2.1 nM 8.68
CHEMBL217402 EC50 = 2.2 nM 8.66
CHEMBL267260 EC50 = 2.8 nM 8.55
CHEMBL27769 STANOLONE EC50 = 5.1 nM 8.29
CHEMBL217428 EC50 = 106.0 nM 6.97
CHEMBL216949 EC50 = 1283.0 nM 5.89
CHEMBL405835 EC50 = 2022.0 nM 5.69
CHEMBL217168 EC50 > 10000.0 nM -
CHEMBL385509 EC50 > 10000.0 nM -