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Assay Detail

CHEMBL913353

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Functional
Agonist activity at rat AR transfected in mouse C2C12 cells by luciferase reporter transactivation assay
12
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type C2C12
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Androgen receptor (CHEMBL3072)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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
EC50 12 7.37 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220359 2 8.82
CHEMBL425646 2 8.64
CHEMBL27769 STANOLONE 2.0 1 8.55
CHEMBL374781 1 8.36
CHEMBL218914 1 8.20
CHEMBL2096842 1 6.58
CHEMBL374121 1 6.57
CHEMBL219198 1 6.50
CHEMBL384533 1 6.42
CHEMBL218809 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220359 EC50 = 1.5 nM 8.82
CHEMBL425646 EC50 = 2.3 nM 8.64
CHEMBL27769 STANOLONE EC50 = 2.8 nM 8.55
CHEMBL374781 EC50 = 4.4 nM 8.36
CHEMBL218914 EC50 = 6.3 nM 8.20
CHEMBL2096842 EC50 = 265.0 nM 6.58
CHEMBL374121 EC50 = 270.0 nM 6.57
CHEMBL220359 EC50 = 281.0 nM 6.55
CHEMBL219198 EC50 = 320.0 nM 6.50
CHEMBL384533 EC50 = 385.0 nM 6.42
CHEMBL425646 EC50 = 1298.0 nM 5.89
CHEMBL218809 EC50 > 1000.0 nM -