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Assay Detail

CHEMBL913352

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Binding
Displacement of [3H]DHT from human AR in MDA453 cells
12
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MDA453
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold.
Sun C, Robl JA, Wang TC, Huang Y, Kuhns JE, Lupisella JA, Beehler BC, Golla R, Sleph PG, Seethala R, Fura A, Krystek SR, An Y, Malley MF, Sack JS, Salvati ME, Grover GJ, Ostrowski J, Hamann LG.
J Med Chem (2006) 49 : 7596 -7599
PubMed 17181141 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 8.59 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27769 STANOLONE 2.0 1 9.52
CHEMBL384533 1 9.00
CHEMBL220359 2 8.82
CHEMBL219198 1 8.82
CHEMBL374121 1 8.77
CHEMBL425646 2 8.49
CHEMBL374781 1 8.46
CHEMBL2096842 1 8.37
CHEMBL218914 1 8.26
CHEMBL218809 1 7.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27769 STANOLONE Ki = 0.3 nM 9.52
CHEMBL384533 Ki = 1.0 nM 9.00
CHEMBL220359 Ki = 1.5 nM 8.82
CHEMBL219198 Ki = 1.5 nM 8.82
CHEMBL374121 Ki = 1.7 nM 8.77
CHEMBL220359 Ki = 2.1 nM 8.68
CHEMBL425646 Ki = 3.2 nM 8.49
CHEMBL374781 Ki = 3.5 nM 8.46
CHEMBL2096842 Ki = 4.3 nM 8.37
CHEMBL425646 Ki = 5.3 nM 8.28
CHEMBL218914 Ki = 5.5 nM 8.26
CHEMBL218809 Ki = 24.0 nM 7.62