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Assay Detail

CHEMBL4021779

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

Binding
Displacement of [3H]-R1881 from AR in human LNCaP cells preincubated for 30 mins followed by [3H]-R1881 addition measured after 30 mins by microbeta scintillation counter method
2
Total Activities
2
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

Design, synthesis, and biological evaluation of deuterated apalutamide with improved pharmacokinetic profiles.
Pang X, Wang Y, Chen Y.
Bioorg Med Chem Lett (2017) 27 : 2803 -2806
PubMed 28478926 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.80 7.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4105484 1 7.81
CHEMBL3183409 APALUTAMIDE 4.0 1 7.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4105484 IC50 = 15.41 nM 7.81
CHEMBL3183409 APALUTAMIDE IC50 = 16.25 nM 7.79