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Assay Detail

CHEMBL5045110

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

Binding
Binding affinity to human AR LBD (663 to 920 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant in presence of DHT by biolayer interferometry assay
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

Discovery of <i>N</i>-(4-(Benzyloxy)-phenyl)-sulfonamide Derivatives as Novel Antagonists of the Human Androgen Receptor Targeting the Activation Function 2.
Chai X, Sun H, Zhou W, Chen C, Shan L, Yang Y, He J, Pang J, Yang L, Wang X, Cui S, Fu Y, Xu X, Xu L, Yao X, Li D, Hou T.
J Med Chem (2022) 65 : 2507 -2521
PubMed 35077161 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 4.12 4.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5085066 1 4.12
CHEMBL1082407 ENZALUTAMIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5085066 Kd = 75870.0 nM 4.12
CHEMBL1082407 ENZALUTAMIDE Kd = 295400.0 nM -