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Assay Detail

CHEMBL858790

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

Binding
Inhibition of human AR
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
Kinoyama I, Taniguchi N, Toyoshima A, Nozawa E, Kamikubo T, Imamura M, Matsuhisa A, Samizu K, Kawanimani E, Niimi T, Hamada N, Koutoku H, Furutani T, Kudoh M, Okada M, Ohta M, Tsukamoto S.
J Med Chem (2006) 49 : 716 -726
PubMed 16420057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.03 8.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL197595 1 8.34
CHEMBL409 BICALUTAMIDE 4.0 1 7.72
CHEMBL201488 1 -
CHEMBL201314 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL197595 Ki = 4.6 nM 8.34
CHEMBL409 BICALUTAMIDE Ki = 19.0 nM 7.72
CHEMBL201488 Ki - -
CHEMBL201314 Ki - -