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Assay Detail

CHEMBL828424

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

Binding
Inhibition of [3H]mibolerone binding to human Androgen receptor of PC3/AR Cell Lysate
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Studies of targeting and intracellular trafficking of an anti-androgen doxorubicin-formaldehyde conjugate in PC-3 prostate cancer cells bearing androgen receptor-GFP chimera.
Cogan PS, Koch TH.
J Med Chem (2004) 47 : 5690 -5699
PubMed 15509168 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.19 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL146858 1 8.22
CHEMBL1274 NILUTAMIDE 4.0 1 8.05
CHEMBL2113036 1 7.31
CHEMBL386437 1 7.20
CHEMBL2113034 1 7.11
CHEMBL264131 1 7.05
CHEMBL806 FLUTAMIDE 4.0 1 6.81
CHEMBL2113032 1 6.48
CHEMBL347556 1 6.46
CHEMBL147457 1 -
CHEMBL27577 SALICYLAMIDE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL146858 IC50 = 6.0 nM 8.22
CHEMBL1274 NILUTAMIDE IC50 = 9.0 nM 8.05
CHEMBL2113036 IC50 = 49.0 nM 7.31
CHEMBL386437 IC50 = 63.0 nM 7.20
CHEMBL2113034 IC50 = 77.0 nM 7.11
CHEMBL264131 IC50 = 90.0 nM 7.05
CHEMBL806 FLUTAMIDE IC50 = 154.0 nM 6.81
CHEMBL2113032 IC50 = 332.0 nM 6.48
CHEMBL347556 IC50 = 346.0 nM 6.46
CHEMBL147457 IC50 > 1000.0 nM -
CHEMBL27577 SALICYLAMIDE IC50 >> 1000.0 nM -