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Assay Detail

CHEMBL3137111

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

Binding
Binding affinity to recombinant human PHD3-Fe2+ complex expressed in Escherichia coli using HIF19 peptide as substrate by fluorescence emission spectroscopy
8
Total Activities
8
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

Azole derivatives as novel non-iron-chelating inhibitors of prolyl hydroxylase 3 for HIF-1 activation
Cao J, Ma X, Wang X, Wang X, Zhang Z, Geng Z, Wang Z
Medchemcomm (2013) 4 : 1222 -1230
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 8 10.40 10.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3133889 1 10.82
CHEMBL20724 1 10.26
CHEMBL3133888 1 10.11
CHEMBL3133892 1 -
CHEMBL3133891 1 -
CHEMBL84963 BENZOTRIAZOLE 1 -
CHEMBL306226 BENZIMIDAZOLE -1.0 1 -
CHEMBL3133890 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3133889 Kd = 0.0152 nM 10.82
CHEMBL20724 Kd = 0.0544 nM 10.26
CHEMBL3133888 Kd = 0.0784 nM 10.11
CHEMBL3133892 Kd = 0.00734 nM -
CHEMBL3133891 Kd = 0.00567 nM -
CHEMBL84963 BENZOTRIAZOLE Kd - -
CHEMBL306226 BENZIMIDAZOLE Kd - -
CHEMBL3133890 Kd = 0.00347 nM -