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Assay Detail

CHEMBL4480649

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

Binding
Inhibition of N-terminal His6-tagged truncated PHD2 (181 to 426 residues) (unknown origin) expressed in Escherichia coli BL21 DE3 using H1F1-alpha NODD as substrate preincubated for 15 mins followed by substrate addition and measured after 15 mins by mass spectrometry
20
Total Activities
20
Compounds Tested
2
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

Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors.
Holt-Martyn JP, Tumber A, Rahman MZ, Lippl K, Figg W, Figg W, McDonough MA, Chowdhury R, Schofield CJ.
Medchemcomm (2019) 10 : 500 -504
PubMed 31057728 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.91 7.31
Inhibition 9 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4536280 1 7.31
CHEMBL4535543 1 7.26
CHEMBL4482885 1 7.20
CHEMBL4557378 1 7.16
CHEMBL4526672 1 7.03
CHEMBL2043005 1 6.90
CHEMBL2042999 1 6.37
CHEMBL4514222 1 6.04
CHEMBL4537110 1 -
CHEMBL4525775 1 -
CHEMBL4563706 1 -
CHEMBL4557919 1 -
CHEMBL4574692 1 -
CHEMBL4555144 1 -
CHEMBL4531046 1 -
CHEMBL4569324 1 -
CHEMBL4589011 1 -
CHEMBL4561626 1 -
CHEMBL4573683 1 -
CHEMBL4579945 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4536280 IC50 = 49.0 nM 7.31
CHEMBL4535543 IC50 = 55.0 nM 7.26
CHEMBL4482885 IC50 = 63.0 nM 7.20
CHEMBL4557378 IC50 = 70.0 nM 7.16
CHEMBL4526672 IC50 = 94.0 nM 7.03
CHEMBL2043005 IC50 = 127.0 nM 6.90
CHEMBL2042999 IC50 = 427.0 nM 6.37
CHEMBL4514222 IC50 = 905.0 nM 6.04
CHEMBL4537110 Inhibition - % -
CHEMBL4525775 Inhibition - % -
CHEMBL4563706 Inhibition - % -
CHEMBL4557919 Inhibition - % -
CHEMBL4574692 Inhibition - % -
CHEMBL4555144 Inhibition - % -
CHEMBL4531046 Inhibition - % -
CHEMBL4569324 Inhibition - % -
CHEMBL4589011 Inhibition - % -
CHEMBL4561626 IC50 > 25000.0 nM -
CHEMBL4573683 IC50 > 25000.0 nM -
CHEMBL4579945 IC50 > 25000.0 nM -