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Assay Detail

CHEMBL649836

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

Binding
Binding affinity against rat prostate cytosolic Androgen receptor using [3H]mibolerone as radioligand
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Androgen receptor (CHEMBL3072)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and structure-activity studies of side-chain derivatized arylhydantoins for investigation as androgen receptor radioligands.
Van Dort ME, Jung YW.
Bioorg Med Chem Lett (2001) 11 : 1045 -1047
PubMed 11327585 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.14 9.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL425863 MIBOLERONE 2.0 1 9.12
CHEMBL386630 TESTOSTERONE 4.0 1 8.31
CHEMBL9389 1 7.89
CHEMBL9337 RU-58841 1 7.58
CHEMBL428309 1 7.43
CHEMBL266786 1 7.19
CHEMBL432658 1 6.92
CHEMBL9146 1 6.91
CHEMBL274667 1 6.85
CHEMBL9447 1 6.82
CHEMBL9328 1 6.67
CHEMBL9140 1 6.49
CHEMBL268214 1 6.44
CHEMBL269372 1 6.38
CHEMBL9390 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL425863 MIBOLERONE Ki = 0.75 nM 9.12
CHEMBL386630 TESTOSTERONE Ki = 4.9 nM 8.31
CHEMBL9389 Ki = 13.0 nM 7.89
CHEMBL9337 RU-58841 Ki = 26.0 nM 7.58
CHEMBL428309 Ki = 37.0 nM 7.43
CHEMBL266786 Ki = 65.0 nM 7.19
CHEMBL432658 Ki = 120.0 nM 6.92
CHEMBL9146 Ki = 123.0 nM 6.91
CHEMBL274667 Ki = 141.0 nM 6.85
CHEMBL9447 Ki = 150.0 nM 6.82
CHEMBL9328 Ki = 213.0 nM 6.67
CHEMBL9140 Ki = 321.0 nM 6.49
CHEMBL268214 Ki = 360.0 nM 6.44
CHEMBL269372 Ki = 415.0 nM 6.38
CHEMBL9390 Ki = 809.0 nM 6.09