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Assay Detail

CHEMBL940963

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

Binding
Displacement of [3H]dihydrotestosterone from human androgen receptor expressed in Sf9 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of amino-pyridines as androgen receptor antagonists for stimulating hair growth and reducing sebum production.
Hu LY, Lei HJ, Du D, Johnson TR, Fedij V, Kostlan C, Yue WS, Lovdahl M, Li JJ, Carroll M, Dettling D, Asbill J, Fan C, Wade K, Pocalyko D, Lapham K, Yalamanchili R, Samas B, Vrieze D, Ciotti S, Krieger-Burke T, Sliskovic D, Welgus H.
Bioorg Med Chem Lett (2007) 17 : 5693 -5697
PubMed 17766112 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.24 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL398431 1 9.10
CHEMBL249071 1 8.42
CHEMBL249070 1 8.15
CHEMBL9337 RU-58841 1 7.80
CHEMBL248690 1 7.70
CHEMBL249072 1 7.14
CHEMBL248868 1 7.11
CHEMBL399876 1 6.91
CHEMBL248841 1 6.77
CHEMBL398432 1 6.68
CHEMBL400098 1 5.77
CHEMBL248878 1 5.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL398431 IC50 = 0.8 nM 9.10
CHEMBL249071 IC50 = 3.8 nM 8.42
CHEMBL249070 IC50 = 7.0 nM 8.15
CHEMBL9337 RU-58841 IC50 = 15.9 nM 7.80
CHEMBL248690 IC50 = 20.0 nM 7.70
CHEMBL249072 IC50 = 73.0 nM 7.14
CHEMBL248868 IC50 = 78.0 nM 7.11
CHEMBL399876 IC50 = 123.0 nM 6.91
CHEMBL248841 IC50 = 169.0 nM 6.77
CHEMBL398432 IC50 = 209.0 nM 6.68
CHEMBL400098 IC50 = 1700.0 nM 5.77
CHEMBL248878 IC50 = 4926.0 nM 5.31