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Assay Detail

CHEMBL833436

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

Functional
Inhibition of androgen dependent human prostate cancer cell MDA-MB-PCa2b proliferation
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Cancer cell lines
Confidence 9 — Direct single protein target
Curated By Expert

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists.
Salvati ME, Balog A, Shan W, Wei DD, Pickering D, Attar RM, Geng J, Rizzo CA, Gottardis MM, Weinmann R, Krystek SR, Sack J, An Y, Kish K.
Bioorg Med Chem Lett (2005) 15 : 271 -276
PubMed 15603938 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.82 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL182412 1 9.40
CHEMBL182993 1 6.83
CHEMBL182593 1 6.75
CHEMBL183882 1 6.75
CHEMBL409 BICALUTAMIDE 4.0 1 6.14
CHEMBL183173 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL182412 IC50 = 0.4 nM 9.40
CHEMBL182993 IC50 = 148.0 nM 6.83
CHEMBL182593 IC50 = 180.0 nM 6.75
CHEMBL183882 IC50 = 179.0 nM 6.75
CHEMBL409 BICALUTAMIDE IC50 = 725.0 nM 6.14
CHEMBL183173 IC50 = 8460.0 nM 5.07