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Assay Detail

CHEMBL855663

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

Binding
Inhibition of human EGLN1
14
Total Activities
14
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

Design and synthesis of a series of novel pyrazolopyridines as HIF-1alpha prolyl hydroxylase inhibitors.
Warshakoon NC, Wu S, Boyer A, Kawamoto R, Renock S, Xu K, Pokross M, Evdokimov AG, Zhou S, Winter C, Walter R, Mekel M.
Bioorg Med Chem Lett (2006) 16 : 5687 -5690
PubMed 16908145 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.75 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL222115 1 6.72
CHEMBL221012 1 6.24
CHEMBL426560 1 5.85
CHEMBL218070 1 5.80
CHEMBL269093 1 5.80
CHEMBL221241 1 5.77
CHEMBL221013 1 5.77
CHEMBL218424 1 5.68
CHEMBL222114 1 5.62
CHEMBL375008 1 5.62
CHEMBL221189 1 5.57
CHEMBL374147 1 5.55
CHEMBL386421 1 5.54
CHEMBL220743 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL222115 IC50 = 190.0 nM 6.72
CHEMBL221012 IC50 = 580.0 nM 6.24
CHEMBL426560 IC50 = 1400.0 nM 5.85
CHEMBL218070 IC50 = 1600.0 nM 5.80
CHEMBL269093 IC50 = 1600.0 nM 5.80
CHEMBL221241 IC50 = 1700.0 nM 5.77
CHEMBL221013 IC50 = 1700.0 nM 5.77
CHEMBL218424 IC50 = 2100.0 nM 5.68
CHEMBL222114 IC50 = 2400.0 nM 5.62
CHEMBL375008 IC50 = 2400.0 nM 5.62
CHEMBL221189 IC50 = 2700.0 nM 5.57
CHEMBL374147 IC50 = 2800.0 nM 5.55
CHEMBL386421 IC50 = 2900.0 nM 5.54
CHEMBL220743 IC50 = 12000.0 nM 4.92