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Assay Detail

CHEMBL4058430

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

Binding
Displacement of fluormone-AL Green from recombinant rat His-tagged/GST-fused androgen receptor LBD expressed in baculovirus expression system measured after 1.5 hrs by fluorescence polarization assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Androgen receptor (CHEMBL3072)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, synthesis and biological evaluation of novel 3-oxo-4-oxa-5α-androst-17β-amide derivatives as dual 5α-reductase inhibitors and androgen receptor antagonists.
Lao K, Sun J, Wang C, Wang Y, You Q, Xiao H, Xiang H.
Bioorg Med Chem Lett (2017) 27 : 4212 -4217
PubMed 28757062 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.61 4.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4076351 1 4.77
CHEMBL258918 MESTEROLONE 2.0 1 4.74
CHEMBL4061869 1 4.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4076351 IC50 = 16840.0 nM 4.77
CHEMBL258918 MESTEROLONE IC50 = 18280.0 nM 4.74
CHEMBL4061869 IC50 = 47610.0 nM 4.32