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Assay Detail

CHEMBL615567

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

Binding
Inhibition of 4-hydroxyphenylpyruvate dioxygenase of purified pig liver by enol-borate method
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Expert

Target

4-hydroxyphenylpyruvate dioxygenase (CHEMBL3203)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

SAR studies of 2-o-substituted-benzoyl- and 2-alkanoyl-cyclohexane-1,3-diones as inhibitors of 4-hydroxyphenylpyruvate dioxygenase.
Lin YL, Wu CS, Lin SW, Yang DY.
Bioorg Med Chem Lett (2000) 10 : 843 -845
PubMed 10853644 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.73 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1337 NITISINONE 4.0 1 7.40
CHEMBL169696 1 6.80
CHEMBL166893 1 6.60
CHEMBL166951 1 6.30
CHEMBL168906 1 6.25
CHEMBL165937 1 6.12
CHEMBL355470 1 5.43
CHEMBL355709 1 5.22
CHEMBL167675 1 4.95
CHEMBL167062 1 4.93
CHEMBL166694 1 4.75
CHEMBL167585 1 4.03
CHEMBL168189 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1337 NITISINONE IC50 = 40.0 nM 7.40
CHEMBL169696 IC50 = 160.0 nM 6.80
CHEMBL166893 IC50 = 250.0 nM 6.60
CHEMBL166951 IC50 = 500.0 nM 6.30
CHEMBL168906 IC50 = 560.0 nM 6.25
CHEMBL165937 IC50 = 760.0 nM 6.12
CHEMBL355470 IC50 = 3750.0 nM 5.43
CHEMBL355709 IC50 = 6000.0 nM 5.22
CHEMBL167675 IC50 = 11200.0 nM 4.95
CHEMBL167062 IC50 = 11700.0 nM 4.93
CHEMBL166694 IC50 = 17800.0 nM 4.75
CHEMBL167585 IC50 = 93300.0 nM 4.03
CHEMBL168189 IC50 = 364500.0 nM -