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Assay Detail

CHEMBL899496

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

Functional
Antagonist activity at human AR in MDA-MB453-MMTV-luci cells by functional assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Preparation of 4-aryl-2-trifluoromethylbenzonitrile derivatives as androgen receptor antagonists for topical suppression of sebum production.
Van Camp JA, Hu LY, Kostlan C, Lefker B, Li J, Mitchell L, Wang Z, Yue WS, Carroll M, Dettling D, Du D, Pocalyko D, Wade K.
Bioorg Med Chem Lett (2007) 17 : 5529 -5532
PubMed 17764935 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.82 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL391548 1 10.70
CHEMBL235159 1 9.10
CHEMBL235378 1 7.92
CHEMBL238366 1 7.70
CHEMBL443579 1 6.85
CHEMBL427678 1 6.40
CHEMBL392827 1 6.07
CHEMBL394392 1 -
CHEMBL235784 1 -
CHEMBL445409 1 -
CHEMBL266491 1 -
CHEMBL238338 1 -
CHEMBL238340 1 -
CHEMBL235601 1 -
CHEMBL238365 1 -
CHEMBL391549 1 -
CHEMBL396656 1 -
CHEMBL235379 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL391548 IC50 = 0.02 nM 10.70
CHEMBL235159 IC50 = 0.8 nM 9.10
CHEMBL235378 IC50 = 11.9 nM 7.92
CHEMBL238366 IC50 = 20.1 nM 7.70
CHEMBL443579 IC50 = 140.0 nM 6.85
CHEMBL427678 IC50 = 399.0 nM 6.40
CHEMBL392827 IC50 = 843.0 nM 6.07
CHEMBL394392 IC50 - -
CHEMBL235784 IC50 - -
CHEMBL445409 IC50 - -
CHEMBL266491 IC50 - -
CHEMBL238338 IC50 - -
CHEMBL238340 IC50 - -
CHEMBL235601 IC50 - -
CHEMBL238365 IC50 - -
CHEMBL391549 IC50 - -
CHEMBL396656 IC50 > 1.0 nM -
CHEMBL235379 IC50 > 1000.0 nM -