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Assay Detail

CHEMBL4012501

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Agonist activity at androgen receptor (unknown origin) expressed in African green monkey COS7 cells after 24 hrs by MMTV-promoter driven luciferase reporter gene assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs). Part II: Optimization of 4-(pyrrolidin-1-yl)benzonitrile derivatives.
Asano M, Hitaka T, Imada T, Yamada M, Morimoto M, Shinohara H, Hara T, Yamaoka M, Santou T, Nakayama M, Imai Y, Habuka N, Yano J, Wilson K, Fujita H, Hasuoka A.
Bioorg Med Chem Lett (2017) 27 : 1897 -1901
PubMed 28363748 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 9.61 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4090028 1 9.72
CHEMBL4060271 1 9.70
CHEMBL4092535 1 9.54
CHEMBL4068946 1 9.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4090028 IC50 = 0.19 nM 9.72
CHEMBL4060271 IC50 = 0.2 nM 9.70
CHEMBL4092535 IC50 = 0.29 nM 9.54
CHEMBL4068946 IC50 = 0.32 nM 9.49