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Assay Detail

CHEMBL896865

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Functional
Agonist activity at human androgen receptor by luciferase reporter gene assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators.
Martinborough E, Shen Y, Oeveren Av, Long YO, Lau TL, Marschke KB, Chang WY, López FJ, Vajda EG, Rix PJ, Viveros OH, Negro-Vilar A, Zhi L.
J Med Chem (2007) 50 : 5049 -5052
PubMed 17887661 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 8.18 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL436784 1 9.70
CHEMBL244896 1 8.59
CHEMBL27769 STANOLONE 2.0 1 8.29
CHEMBL467888 LGD-2941 1.0 1 8.15
CHEMBL2113293 1 8.08
CHEMBL395992 1 7.92
CHEMBL244895 1 7.89
CHEMBL243252 1 7.68
CHEMBL243251 1 7.32
CHEMBL446191 1 -
CHEMBL63560 (R)-BICALUTAMIDE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL436784 EC50 = 0.2 nM 9.70
CHEMBL244896 EC50 = 2.6 nM 8.59
CHEMBL27769 STANOLONE EC50 = 5.1 nM 8.29
CHEMBL467888 LGD-2941 EC50 = 7.1 nM 8.15
CHEMBL2113293 EC50 = 8.4 nM 8.08
CHEMBL395992 EC50 = 12.0 nM 7.92
CHEMBL244895 EC50 = 13.0 nM 7.89
CHEMBL243252 EC50 = 21.0 nM 7.68
CHEMBL243251 EC50 = 48.0 nM 7.32
CHEMBL446191 EC50 > 10000.0 nM -
CHEMBL63560 (R)-BICALUTAMIDE EC50 > 10000.0 nM -