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Assay Detail

CHEMBL1041857

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

Functional
Agonist activity at androgen receptor LBD T877A mutant in mouse NIH3T3 cells transiently transfected with beta-galactosidase reporter gene assessed as cellular transformation by R-SAT assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type NIH3T3
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators.
Schlienger N, Lund BW, Pawlas J, Badalassi F, Bertozzi F, Lewinsky R, Fejzic A, Thygesen MB, Tabatabaei A, Bradley SR, Gardell LR, Piu F, Olsson R.
J Med Chem (2009) 52 : 7186 -7191
PubMed 19856921 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 7.63 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3084681 1 9.40
CHEMBL27769 STANOLONE 2.0 1 8.90
CHEMBL3084692 1 8.10
CHEMBL3084685 1 7.90
CHEMBL3084686 1 7.40
CHEMBL491 HYDROXYFLUTAMIDE 2.0 1 7.00
CHEMBL806 FLUTAMIDE 4.0 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3084681 EC50 = 0.3981 nM 9.40
CHEMBL27769 STANOLONE EC50 = 1.259 nM 8.90
CHEMBL3084692 EC50 = 7.943 nM 8.10
CHEMBL3084685 EC50 = 12.59 nM 7.90
CHEMBL3084686 EC50 = 39.81 nM 7.40
CHEMBL491 HYDROXYFLUTAMIDE EC50 = 100.0 nM 7.00
CHEMBL806 FLUTAMIDE EC50 = 19952.62 nM 4.70