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Assay Detail

CHEMBL896869

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Binding
Binding affinity to human AR
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 11 7.75 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27769 STANOLONE 2.0 1 9.70
CHEMBL467888 LGD-2941 1.0 1 8.82
CHEMBL436784 1 8.34
CHEMBL2113293 1 8.12
CHEMBL395992 1 8.00
CHEMBL244896 1 7.72
CHEMBL243251 1 7.37
CHEMBL63560 (R)-BICALUTAMIDE 1 7.16
CHEMBL243252 1 7.16
CHEMBL244895 1 7.14
CHEMBL446191 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27769 STANOLONE Ki = 0.2 nM 9.70
CHEMBL467888 LGD-2941 Ki = 1.5 nM 8.82
CHEMBL436784 Ki = 4.6 nM 8.34
CHEMBL2113293 Ki = 7.6 nM 8.12
CHEMBL395992 Ki = 10.0 nM 8.00
CHEMBL244896 Ki = 19.0 nM 7.72
CHEMBL243251 Ki = 43.0 nM 7.37
CHEMBL63560 (R)-BICALUTAMIDE Ki = 70.0 nM 7.16
CHEMBL243252 Ki = 70.0 nM 7.16
CHEMBL244895 Ki = 72.0 nM 7.14
CHEMBL446191 Ki = 1700.0 nM 5.77