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Assay Detail

CHEMBL4149413

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

Binding
Inhibition of recombinant human HIF-PHD3 expressed in baculovirus-infected Sf9 cells using biotin labelled DLDLEMLAPYIPMDDDFQL as substrate preincubated for 60 mins followed by substrate addition measured after 60 mins by TR-FRET assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prolyl hydroxylase EGLN3 (CHEMBL5705)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
Joharapurkar AA, Pandya VB, Patel VJ, Desai RC, Jain MR.
J Med Chem (2018) 61 : 6964 -6982
PubMed 29712435 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.35 6.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3646118 MOLIDUSTAT 2.0 1 6.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3646118 MOLIDUSTAT IC50 = 450.0 nM 6.35