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Assay Detail

CHEMBL3772519

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

Binding
Displacement of FITC-HIF-1alpha (556 to 574 residues) from PHD2 (181 to 426 residues) (unknown origin) after 60 mins by fluorescence polarization assay
4
Total Activities
4
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

Affinity-Based Fluorescence Polarization Assay for High-Throughput Screening of Prolyl Hydroxylase 2 Inhibitors.
Lei Y, Hu T, Wu X, Wu Y, Bao Q, Zhang L, Xia H, Sun H, You Q, Zhang X.
ACS Med Chem Lett (2015) 6 : 1236 -1240
PubMed 26713111 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.18 6.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL426560 1 6.37
CHEMBL2338329 ROXADUSTAT 4.0 1 6.23
CHEMBL3646118 MOLIDUSTAT 2.0 1 6.06
CHEMBL3646215 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL426560 IC50 = 424.2 nM 6.37
CHEMBL2338329 ROXADUSTAT IC50 = 591.4 nM 6.23
CHEMBL3646118 MOLIDUSTAT IC50 = 876.3 nM 6.06
CHEMBL3646215 IC50 = 890.4 nM 6.05