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Assay Detail

CHEMBL5036171

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

Binding
Binding affinity to N-terminal His6-tagged VHL (54 to 213 residues) (unknown origin) expressed in Escherichia coli assessed as displacement of HIF-1alpha by fluorescence polarization assay
9
Total Activities
9
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

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

Publication

Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity.
Klein VG, Bond AG, Craigon C, Lokey RS, Ciulli A.
J Med Chem (2021) 64 : 18082 -18101
PubMed 34881891 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 6.82 6.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3344081 1 6.95
CHEMBL5087145 1 6.92
CHEMBL5082521 1 6.87
CHEMBL4793272 1 6.86
CHEMBL5081396 1 6.84
CHEMBL5087530 1 6.77
CHEMBL5094871 1 6.77
CHEMBL5086047 1 6.70
CHEMBL5086897 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3344081 Kd = 113.0 nM 6.95
CHEMBL5087145 Kd = 119.0 nM 6.92
CHEMBL5082521 Kd = 136.0 nM 6.87
CHEMBL4793272 Kd = 138.0 nM 6.86
CHEMBL5081396 Kd = 144.0 nM 6.84
CHEMBL5087530 Kd = 170.0 nM 6.77
CHEMBL5094871 Kd = 170.0 nM 6.77
CHEMBL5086047 Kd = 200.0 nM 6.70
CHEMBL5086897 Kd = 200.0 nM 6.70