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Assay Detail

CHEMBL3587049

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

Binding
Inhibition of human human recombinant CP4H1 expressed in Escherichia coli Origami B(DE3) pre-incubated for 2 mins followed by alpha-ketoglutarate addition using dansylGlyProProGlyOEt substrate in Tris-HCl buffer at pH 7.8 at 30 degC by HPLC method
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

Prolyl 4-hydroxylase subunit alpha-1 (CHEMBL1250350)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective inhibition of prolyl 4-hydroxylases by bipyridinedicarboxylates.
Vasta JD, Raines RT.
Bioorg Med Chem (2015) 23 : 3081 -3090
PubMed 26022078 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.61 6.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL332005 1 6.08
CHEMBL3586252 1 5.92
CHEMBL88972 PYRIDINE-2,5-DICARBOXYLIC ACID 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL332005 IC50 = 840.0 nM 6.08
CHEMBL3586252 IC50 = 1200.0 nM 5.92
CHEMBL88972 PYRIDINE-2,5-DICARBOXYLIC ACID IC50 = 15000.0 nM 4.82