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Assay Detail

CHEMBL5624382

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

Binding
PROTAC activity at VHL/HiBit tagged AR in human LNCaP cells cells assessed as degradation of AR incubated for 18 hrs by Nano-Glo HiBiT assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type LNCaP
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

Structure-Guided Design and Optimization of Covalent VHL-Targeted Sulfonyl Fluoride PROTACs.
Shah RR, De Vita E, Sathyamurthi PS, Conole D, Zhang X, Fellows E, Dickinson ER, Fleites CM, Queisser MA, Harling JD, Tate EW.
J Med Chem (2024) 67 : 4641 -4654
PubMed 38478885 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.48 6.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5555109 1 6.67
CHEMBL5560053 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5555109 EC50 = 212.0 nM 6.67
CHEMBL5560053 EC50 = 527.0 nM 6.28