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Assay Detail

CHEMBL3707755

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

Binding
Enzyme Assay: The EGLN-1 (or EGLN-3) enzyme activity is determined using mass spectrometry (matrix-assisted laser desorption ionization, time-of-flight MS, MALDI-TOF MS—for assay details, see reference (Greis et al., 2006).
9
Total Activities
9
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 hydroxylase EGLN3 (CHEMBL5705)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Prolyl hydroxylase inhibitors and methods of use
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.80 7.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3646220 1 7.08
CHEMBL3646215 1 6.75
CHEMBL3646222 1 6.41
CHEMBL3646221 VADADUSTAT 4.0 1 6.41
CHEMBL3646219 1 6.25
CHEMBL3646227 1 5.89
CHEMBL3646212 1 4.67
CHEMBL3646218 1 4.43
CHEMBL3646217 1 4.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3646220 IC50 = 83.0 nM 7.08
CHEMBL3646215 IC50 = 180.0 nM 6.75
CHEMBL3646222 IC50 = 390.0 nM 6.41
CHEMBL3646221 VADADUSTAT IC50 = 390.0 nM 6.41
CHEMBL3646219 IC50 = 560.0 nM 6.25
CHEMBL3646227 IC50 = 1300.0 nM 5.89
CHEMBL3646212 IC50 = 21400.0 nM 4.67
CHEMBL3646218 IC50 = 37500.0 nM 4.43
CHEMBL3646217 IC50 = 52300.0 nM 4.28