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Assay Detail

CHEMBL830413

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

Binding
Inhibition of rat prostate cytosolic androgen receptor
16
Total Activities
16
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

Synthesis and structure-activity investigation of iodinated arylhydantoins and arylthiohydantoins for development as androgen receptor radioligands.
Van Dort ME, Jung YW.
Bioorg Med Chem Lett (2004) 14 : 5285 -5288
PubMed 15454212 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.73 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL419767 1 9.15
CHEMBL425863 MIBOLERONE 2.0 1 9.12
CHEMBL187251 1 8.70
CHEMBL331820 1 8.65
CHEMBL362518 1 8.60
CHEMBL386630 TESTOSTERONE 4.0 1 8.31
CHEMBL184759 1 7.96
CHEMBL188175 1 7.70
CHEMBL9337 RU-58841 1 7.58
CHEMBL365030 1 7.43
CHEMBL365035 1 7.23
CHEMBL362745 1 7.11
CHEMBL186591 1 6.93
CHEMBL184833 1 6.66
CHEMBL366116 1 6.40
CHEMBL440563 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL419767 Ki = 0.71 nM 9.15
CHEMBL425863 MIBOLERONE Ki = 0.75 nM 9.12
CHEMBL187251 Ki = 2.0 nM 8.70
CHEMBL331820 Ki = 2.23 nM 8.65
CHEMBL362518 Ki = 2.5 nM 8.60
CHEMBL386630 TESTOSTERONE Ki = 4.9 nM 8.31
CHEMBL184759 Ki = 11.0 nM 7.96
CHEMBL188175 Ki = 20.0 nM 7.70
CHEMBL9337 RU-58841 Ki = 26.0 nM 7.58
CHEMBL365030 Ki = 37.0 nM 7.43
CHEMBL365035 Ki = 59.0 nM 7.23
CHEMBL362745 Ki = 77.0 nM 7.11
CHEMBL186591 Ki = 117.0 nM 6.93
CHEMBL184833 Ki = 219.0 nM 6.66
CHEMBL366116 Ki = 400.0 nM 6.40
CHEMBL440563 Ki = 639.0 nM 6.19