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Assay Detail

CHEMBL1663403

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

Binding
Inhibition of DHODH in Wistar rat liver homogenates by DCIP reduction assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

1,2,5-Oxadiazole analogues of leflunomide and related compounds.
Giorgis M, Lolli ML, Rolando B, Rao A, Tosco P, Chaurasia S, Marabello D, Fruttero R, Gasco A.
Eur J Med Chem (2011) 46 : 383 -392
PubMed 21109332 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.20 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL973 TERIFLUNOMIDE 4.0 1 7.70
CHEMBL960 LEFLUNOMIDE 4.0 1 5.80
CHEMBL1651801 1 4.77
CHEMBL1651809 1 4.58
CHEMBL1651789 1 4.22
CHEMBL1651807 1 4.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL973 TERIFLUNOMIDE IC50 = 20.0 nM 7.70
CHEMBL960 LEFLUNOMIDE IC50 = 1600.0 nM 5.80
CHEMBL1651801 IC50 = 17000.0 nM 4.77
CHEMBL1651809 IC50 = 26000.0 nM 4.58
CHEMBL1651789 IC50 = 60000.0 nM 4.22
CHEMBL1651807 IC50 = 74000.0 nM 4.13