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Assay Detail

CHEMBL923796

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

Binding
Displacement of [3H]DHT from androgen receptor expressed in Sf9 cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Sf9
Confidence 8 — Homologous 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 7.28 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL399439 1 7.37
CHEMBL251552 1 7.24
CHEMBL399887 1 7.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL399439 IC50 = 43.0 nM 7.37
CHEMBL251552 IC50 = 58.0 nM 7.24
CHEMBL399887 IC50 = 60.0 nM 7.22