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Assay Detail

CHEMBL4049533

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

Binding
Inhibition of Wistar rat liver cytosol HPPD using HPP as substrate assessed as reduction in O2 consumption
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Subcellular Cytosol
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

4-hydroxyphenylpyruvate dioxygenase (CHEMBL5863)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

4-Hydroxyphenylpyruvate Dioxygenase and Its Inhibition in Plants and Animals: Small Molecules as Herbicides and Agents for the Treatment of Human Inherited Diseases.
Santucci A, Bernardini G, Braconi D, Petricci E, Manetti F.
J Med Chem (2017) 60 : 4101 -4125
PubMed 28128559 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.62 7.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4092919 1 7.44
CHEMBL1873440 MESOTRIONE 1 7.43
CHEMBL1337 NITISINONE 4.0 1 7.40
CHEMBL1498742 1 4.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4092919 IC50 = 36.0 nM 7.44
CHEMBL1873440 MESOTRIONE IC50 = 37.0 nM 7.43
CHEMBL1337 NITISINONE IC50 = 40.0 nM 7.40
CHEMBL1498742 IC50 = 60000.0 nM 4.22