Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL923797

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

Functional
Antagonist activity at androgen receptor expressed in MDA-MB-453 cells assessed as inhibition of dihydrotestosterone-induced response in reporter gene assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MDA-MB-453
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

(1R,2S)-4-(2-cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile, a potent androgen receptor antagonist for stimulating hair growth and reducing sebum production.
Hu LY, Du D, Hoffman J, Smith Y, Fedij V, Kostlan C, Johnson TR, Huang Y, Kesten S, Harter W, Yue WS, Li JJ, Barvian N, Mitchell L, Lei HJ, Lefker B, Carroll M, Dettling D, Krieger-Burke T, Samas B, Yalamanchili R, Lapham K, Pocalyko D, Sliskovic D, Ciotti S, Stoller B, Hena MA, Ding Q, Maiti SN, Stier M, Welgus H.
Bioorg Med Chem Lett (2007) 17 : 5983 -5988
PubMed 17827000 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.51 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL399887 1 7.92
CHEMBL251552 1 7.89
CHEMBL399439 1 6.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL399887 IC50 = 12.0 nM 7.92
CHEMBL251552 IC50 = 13.0 nM 7.89
CHEMBL399439 IC50 = 196.0 nM 6.71