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Assay Detail

CHEMBL649839

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

Binding
Inhibitory constant against rat prostate cytosol androgen receptor using [3H]mibolerone
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Prostate gland
Confidence 9 — Direct single protein target
Curated By Expert

Target

Androgen receptor (CHEMBL3072)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, synthesis, and pharmacological characterization of 4-[4, 4-dimethyl-3-(4-hydroxybutyl)-5-oxo-2-thioxo-1-imidazolidinyl]- 2-iodobenzonitrile as a high-affinity nonsteroidal androgen receptor ligand.
Van Dort ME, Robins DM, Wayburn B.
J Med Chem (2000) 43 : 3344 -3347
PubMed 10966753 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.99 9.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27769 STANOLONE 2.0 1 9.16
CHEMBL419767 1 9.15
CHEMBL425863 MIBOLERONE 2.0 1 9.12
CHEMBL386630 TESTOSTERONE 4.0 1 8.85
CHEMBL331820 1 8.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27769 STANOLONE Ki = 0.69 nM 9.16
CHEMBL419767 Ki = 0.71 nM 9.15
CHEMBL425863 MIBOLERONE Ki = 0.75 nM 9.12
CHEMBL386630 TESTOSTERONE Ki = 1.4 nM 8.85
CHEMBL331820 Ki = 2.23 nM 8.65