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Assay Detail

CHEMBL5368623

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

Binding
Inhibition of NanoLuc-fused VHL (unknown origin) transfected in live HEK293 cells using NanoGlo substrate incubated for 30 mins by tracer based NanoBRET assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

von Hippel-Lindau disease tumor suppressor (CHEMBL3108660)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Expanding the Structural Diversity at the Phenylene Core of Ligands for the von Hippel-Lindau E3 Ubiquitin Ligase: Development of Highly Potent Hypoxia-Inducible Factor-1α Stabilizers.
Vu LP, Diehl CJ, Casement R, Bond AG, Steinebach C, Strašek N, Bricelj A, Perdih A, Schnakenburg G, Sosič I, Ciulli A, Gütschow M.
J Med Chem (2023) 66 : 12776 -12811
PubMed 37708384 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.46 6.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5421220 1 6.79
CHEMBL5425778 1 6.50
CHEMBL5403921 1 6.44
CHEMBL4225537 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5421220 IC50 = 164.0 nM 6.79
CHEMBL5425778 IC50 = 320.0 nM 6.50
CHEMBL5403921 IC50 = 366.0 nM 6.44
CHEMBL4225537 IC50 = 750.0 nM 6.12