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Assay Detail

CHEMBL844877

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

Binding
Inhibition of prolyl 4-hydroxylase by chromatographic determination of [14C]-succinic acid on ion-exchange minicolumna
9
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Transmembrane prolyl 4-hydroxylase (CHEMBL3047)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel inhibitors of prolyl 4-hydroxylase. 5. The intriguing structure-activity relationships seen with 2,2'-bipyridine and its 5,5'-dicarboxylic acid derivatives.
Hales NJ, Beattie JF.
J Med Chem (1993) 36 : 3853 -3858
PubMed 8254616 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.55 6.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL332005 2 6.73
CHEMBL124527 1 6.50
CHEMBL332012 1 5.30
CHEMBL88972 PYRIDINE-2,5-DICARBOXYLIC ACID 1 5.29
CHEMBL125345 1 4.88
CHEMBL420149 1 4.47
CHEMBL39879 DIPYRIDYL 1 4.47
CHEMBL72628 2-PICOLINIC ACID 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL332005 IC50 = 185.0 nM 6.73
CHEMBL332005 IC50 = 190.0 nM 6.72
CHEMBL124527 IC50 = 320.0 nM 6.50
CHEMBL332012 IC50 = 5040.0 nM 5.30
CHEMBL88972 PYRIDINE-2,5-DICARBOXYLIC ACID IC50 = 5180.0 nM 5.29
CHEMBL125345 IC50 = 13200.0 nM 4.88
CHEMBL420149 IC50 = 33800.0 nM 4.47
CHEMBL39879 DIPYRIDYL IC50 = 34200.0 nM 4.47
CHEMBL72628 2-PICOLINIC ACID IC50 = 111500.0 nM -