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Assay Detail

CHEMBL4710579

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

Binding
Inhibition of androgen receptor (unknown origin)
6
Total Activities
3
Compounds Tested
2
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

New drug approvals for 2019: Synthesis and clinical applications.
Yuan S,Yu B,Liu HM
Eur J Med Chem (2020) 205 : 112667 -112667
PubMed 32911308 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.35 7.96
IC50 3 6.98 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4297185 DAROLUTAMIDE 4.0 2 7.96
CHEMBL1082407 ENZALUTAMIDE 4.0 2 7.07
CHEMBL3183409 APALUTAMIDE 4.0 2 7.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4297185 DAROLUTAMIDE Ki = 11.0 nM 7.96
CHEMBL4297185 DAROLUTAMIDE IC50 = 26.0 nM 7.58
CHEMBL1082407 ENZALUTAMIDE Ki = 86.0 nM 7.07
CHEMBL3183409 APALUTAMIDE Ki = 93.0 nM 7.03
CHEMBL3183409 APALUTAMIDE IC50 = 200.0 nM 6.70
CHEMBL1082407 ENZALUTAMIDE IC50 = 219.0 nM 6.66