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Assay Detail

CHEMBL907887

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Binding
Inhibition of rat DHODH
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Dihydroorotate dehydrogenase (quinone), mitochondrial (CHEMBL2383)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Enzyme inhibition potency enhancement by active site metal chelating and hydrogen bonding induced conformation-restricted cyclopropanecarbonyl derivatives.
Kuo PY, Shie TL, Chen YS, Lai JT, Yang DY.
Bioorg Med Chem Lett (2006) 16 : 6024 -6027
PubMed 16979340 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.58 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL141732 1 7.68
CHEMBL141047 1 7.64
CHEMBL141086 1 6.60
CHEMBL337130 1 6.55
CHEMBL220927 1 6.53
CHEMBL143438 1 4.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL141732 IC50 = 21.0 nM 7.68
CHEMBL141047 IC50 = 23.0 nM 7.64
CHEMBL141086 IC50 = 251.0 nM 6.60
CHEMBL337130 IC50 = 282.0 nM 6.55
CHEMBL220927 IC50 = 295.0 nM 6.53
CHEMBL143438 IC50 = 31600.0 nM 4.50