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Assay Detail

CHEMBL2339069

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

Binding
Inhibition of wild type Androgen receptor (unknown origin) expressed in Freestyle293F cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of 3-aryl-3-hydroxy-1-phenylpyrrolidine derivatives as novel androgen receptor antagonists.
Yamamoto S, Kobayashi H, Kaku T, Aikawa K, Hara T, Yamaoka M, Kanzaki N, Hasuoka A, Baba A, Ito M.
Bioorg Med Chem (2013) 21 : 70 -83
PubMed 23199477 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.94 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27769 STANOLONE 2.0 1 8.68
CHEMBL2337509 1 8.10
CHEMBL2337516 1 7.89
CHEMBL2337510 1 7.57
CHEMBL2337511 1 7.50
CHEMBL2337513 1 7.36
CHEMBL409 BICALUTAMIDE 4.0 1 7.27
CHEMBL2337512 1 7.17
CHEMBL2337506 1 6.92
CHEMBL2337517 1 6.92
CHEMBL2337508 1 6.75
CHEMBL2337507 1 6.43
CHEMBL2337505 1 6.38
CHEMBL2337519 1 6.08
CHEMBL2337514 1 5.96
CHEMBL2337515 1 5.80
CHEMBL2337518 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27769 STANOLONE IC50 = 2.1 nM 8.68
CHEMBL2337509 IC50 = 8.0 nM 8.10
CHEMBL2337516 IC50 = 13.0 nM 7.89
CHEMBL2337510 IC50 = 27.0 nM 7.57
CHEMBL2337511 IC50 = 32.0 nM 7.50
CHEMBL2337513 IC50 = 44.0 nM 7.36
CHEMBL409 BICALUTAMIDE IC50 = 54.0 nM 7.27
CHEMBL2337512 IC50 = 68.0 nM 7.17
CHEMBL2337506 IC50 = 120.0 nM 6.92
CHEMBL2337517 IC50 = 120.0 nM 6.92
CHEMBL2337508 IC50 = 180.0 nM 6.75
CHEMBL2337507 IC50 = 370.0 nM 6.43
CHEMBL2337505 IC50 = 420.0 nM 6.38
CHEMBL2337519 IC50 = 830.0 nM 6.08
CHEMBL2337514 IC50 = 1100.0 nM 5.96
CHEMBL2337515 IC50 = 1600.0 nM 5.80
CHEMBL2337518 IC50 = 7600.0 nM 5.12