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Assay Detail

CHEMBL5215683

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

Binding
Inhibition of N-terminal His tagged PHD2 (181 to 426 residues) (unknown origin) measured by MALDI-TOF MS analysis
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

Egl nine homolog 1 (CHEMBL5697)
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 7.62 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3646118 MOLIDUSTAT 2.0 1 8.15
CHEMBL3646221 VADADUSTAT 4.0 1 7.54
CHEMBL3544988 DAPRODUSTAT 4.0 1 7.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3646118 MOLIDUSTAT IC50 = 7.0 nM 8.15
CHEMBL3646221 VADADUSTAT IC50 = 29.0 nM 7.54
CHEMBL3544988 DAPRODUSTAT IC50 = 67.0 nM 7.17