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Assay Detail

CHEMBL5215684

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

Binding
Inhibition of FIH (unknown origin) by solid-phase extraction coupled to MS based assay
3
Total Activities
3
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

Hypoxia-inducible factor 1-alpha inhibitor (CHEMBL5909)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibition of the Oxygen-Sensing Asparaginyl Hydroxylase Factor Inhibiting Hypoxia-Inducible Factor: A Potential Hypoxia Response Modulating Strategy.
Wu Y, Li Z, McDonough MA, Schofield CJ, Zhang X.
J Med Chem (2021) 64 : 7189 -7209
PubMed 34029087 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.47 4.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3544988 DAPRODUSTAT 4.0 1 4.68
CHEMBL3646221 VADADUSTAT 4.0 1 4.54
CHEMBL3646118 MOLIDUSTAT 2.0 1 4.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3544988 DAPRODUSTAT IC50 = 21000.0 nM 4.68
CHEMBL3646221 VADADUSTAT IC50 = 29000.0 nM 4.54
CHEMBL3646118 MOLIDUSTAT IC50 = 66000.0 nM 4.18