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Assay Detail

CHEMBL996726

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Functional
Agonist activity at rat androgen receptor expressed in mouse skeletal muscle C2C12 cells assessed as transcriptional activation after 24 hrs by androgen-specific response element driven luciferase reporter gene assay
13
Total Activities
13
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 Autocuration

Target

Androgen receptor (CHEMBL3072)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.
Nirschl AA, Zou Y, Krystek SR, Sutton JC, Simpkins LM, Lupisella JA, Kuhns JE, Seethala R, Golla R, Sleph PG, Beehler BC, Grover GJ, Egan D, Fura A, Vyas VP, Li YX, Sack JS, Kish KF, An Y, Bryson JA, Gougoutas JZ, DiMarco J, Zahler R, Ostrowski J, Hamann LG.
J Med Chem (2009) 52 : 2794 -2798
PubMed 19351168 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 8.19 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL484726 1 9.70
CHEMBL521329 1 8.96
CHEMBL484728 1 8.85
CHEMBL229861 1 8.74
CHEMBL483745 1 8.43
CHEMBL484919 1 8.32
CHEMBL229860 1 8.27
CHEMBL229808 1 8.19
CHEMBL229264 1 8.11
CHEMBL520174 1 7.85
CHEMBL484727 1 7.72
CHEMBL519169 1 7.36
CHEMBL482549 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL484726 EC50 = 0.2 nM 9.70
CHEMBL521329 EC50 = 1.1 nM 8.96
CHEMBL484728 EC50 = 1.4 nM 8.85
CHEMBL229861 EC50 = 1.8 nM 8.74
CHEMBL483745 EC50 = 3.7 nM 8.43
CHEMBL484919 EC50 = 4.8 nM 8.32
CHEMBL229860 EC50 = 5.4 nM 8.27
CHEMBL229808 EC50 = 6.4 nM 8.19
CHEMBL229264 EC50 = 7.8 nM 8.11
CHEMBL520174 EC50 = 14.0 nM 7.85
CHEMBL484727 EC50 = 19.0 nM 7.72
CHEMBL519169 EC50 = 44.0 nM 7.36
CHEMBL482549 EC50 = 1109.0 nM 5.96