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Assay Detail

CHEMBL911185

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

Binding
Displacement of [3H]DHT from human androgen receptor expressed in MDA-MB-453 cells by whole cell receptor binding assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MDA-MB-453
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
Ki 13 7.89 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27769 STANOLONE 2.0 1 9.70
CHEMBL436784 1 8.82
CHEMBL277378 1 8.36
CHEMBL217324 1 8.20
CHEMBL267260 1 8.15
CHEMBL217769 1 8.15
CHEMBL217402 1 8.13
CHEMBL405835 1 7.27
CHEMBL217428 1 7.24
CHEMBL442240 1 7.19
CHEMBL217168 1 6.82
CHEMBL216949 1 6.65
CHEMBL385509 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27769 STANOLONE Ki = 0.2 nM 9.70
CHEMBL436784 Ki = 1.5 nM 8.82
CHEMBL277378 Ki = 4.4 nM 8.36
CHEMBL217324 Ki = 6.3 nM 8.20
CHEMBL267260 Ki = 7.1 nM 8.15
CHEMBL217769 Ki = 7.1 nM 8.15
CHEMBL217402 Ki = 7.4 nM 8.13
CHEMBL405835 Ki = 54.0 nM 7.27
CHEMBL217428 Ki = 58.0 nM 7.24
CHEMBL442240 Ki = 64.0 nM 7.19
CHEMBL217168 Ki = 153.0 nM 6.82
CHEMBL216949 Ki = 222.0 nM 6.65
CHEMBL385509 Ki > 10000.0 nM -