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Assay Detail

CHEMBL4669779

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

Binding
Inhibition of FITC-HIF1alpha (556 to 574 residues) binding to PHD2 (181 to 426 residues) (unknown origin) by fluorescence polarization assay
33
Total Activities
33
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

Discovery of Clinical Candidate (5-(3-(4-Chlorophenoxy)prop-1-yn-1-yl)-3-hydroxypicolinoyl)glycine, an Orally Bioavailable Prolyl Hydroxylase Inhibitor for the Treatment of Anemia.
Zhang X,Lei Y,Hu T,Wu Y,Li Z,Jiang Z,Yang C,Zhang L,You Q
J Med Chem (2020) 63 : 10045 -10060
PubMed 32787144 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.40 7.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4162752 DDO-3055 1.0 1 7.19
CHEMBL4795349 1 7.15
CHEMBL4776330 1 7.07
CHEMBL4754277 1 6.96
CHEMBL4756482 1 6.90
CHEMBL4755522 1 6.77
CHEMBL4760023 1 6.76
CHEMBL4747660 1 6.73
CHEMBL4763404 1 6.73
CHEMBL4760527 1 6.66
CHEMBL4760608 1 6.59
CHEMBL4746856 1 6.58
CHEMBL4756775 1 6.49
CHEMBL4789825 1 6.46
CHEMBL4749938 1 6.42
CHEMBL4742972 1 6.39
CHEMBL4753537 1 6.37
CHEMBL4748127 1 6.35
CHEMBL4763948 1 6.35
CHEMBL4757255 1 6.34
CHEMBL4781270 1 6.29
CHEMBL4779610 1 6.28
CHEMBL4788975 1 6.23
CHEMBL2338329 ROXADUSTAT 4.0 1 6.23
CHEMBL4745628 1 6.19
CHEMBL4746310 1 6.09
CHEMBL4796091 1 6.08
CHEMBL4745866 1 6.08
CHEMBL4781276 1 6.06
CHEMBL4743029 1 5.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4162752 DDO-3055 IC50 = 64.2 nM 7.19
CHEMBL4795349 IC50 = 70.4 nM 7.15
CHEMBL4776330 IC50 = 84.3 nM 7.07
CHEMBL4754277 IC50 = 110.0 nM 6.96
CHEMBL4756482 IC50 = 125.0 nM 6.90
CHEMBL4755522 IC50 = 169.0 nM 6.77
CHEMBL4760023 IC50 = 175.0 nM 6.76
CHEMBL4747660 IC50 = 186.0 nM 6.73
CHEMBL4763404 IC50 = 186.0 nM 6.73
CHEMBL4760527 IC50 = 218.0 nM 6.66
CHEMBL4760608 IC50 = 256.0 nM 6.59
CHEMBL4746856 IC50 = 263.0 nM 6.58
CHEMBL4756775 IC50 = 326.0 nM 6.49
CHEMBL4789825 IC50 = 346.0 nM 6.46
CHEMBL4749938 IC50 = 378.0 nM 6.42
CHEMBL4742972 IC50 = 408.0 nM 6.39
CHEMBL4753537 IC50 = 428.0 nM 6.37
CHEMBL4748127 IC50 = 444.0 nM 6.35
CHEMBL4763948 IC50 = 450.0 nM 6.35
CHEMBL4757255 IC50 = 454.0 nM 6.34
CHEMBL4781270 IC50 = 514.0 nM 6.29
CHEMBL4779610 IC50 = 527.0 nM 6.28
CHEMBL4788975 IC50 = 587.0 nM 6.23
CHEMBL2338329 ROXADUSTAT IC50 = 591.0 nM 6.23
CHEMBL4745628 IC50 = 651.0 nM 6.19
CHEMBL4746310 IC50 = 820.0 nM 6.09
CHEMBL4796091 IC50 = 825.0 nM 6.08
CHEMBL4745866 IC50 = 835.0 nM 6.08
CHEMBL4781276 IC50 = 877.0 nM 6.06
CHEMBL4743029 IC50 = 1073.0 nM 5.97
CHEMBL4789028 IC50 = 1200.0 nM 5.92
CHEMBL4127286 IC50 = 2900.0 nM 5.54
CHEMBL4759967 IC50 = 8103.0 nM 5.09