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Assay Detail

CHEMBL5328742

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

Binding
PROTAC activity at VHL/full-length AR in human 22Rv1 cells assessed as induction of AR degradation by Immunoblot analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type 22Rv1
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

von Hippel-Lindau disease tumor suppressor/Androgen receptor (CHEMBL4523730)
Type PROTEIN-PROTEIN INTERACTION
Organism Homo sapiens

Publication

Discovery of <b>BWA-522</b>, a First-in-Class and Orally Bioavailable PROTAC Degrader of the Androgen Receptor Targeting N-Terminal Domain for the Treatment of Prostate Cancer.
Zhang B, Liu C, Yang Z, Zhang S, Hu X, Li B, Mao M, Wang X, Li Z, Ma S, Zhang S, Qin C.
J Med Chem (2023) 66 : 11158 -11186
PubMed 37556600 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 5.70 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4747580 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4747580 EC50 = 2000.0 nM 5.70