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Assay Detail

CHEMBL2187568

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

Binding
Inhibition of Plasmodium falciparum DHODH expressed in Escherichia coli BL21 (DE3) using L-dihydroorotate as substrate after 10 mins by DCIP dye reduction assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Dihydroorotate dehydrogenase (CHEMBL3486)
Type SINGLE PROTEIN
Organism Plasmodium falciparum

Publication

Discovery of diverse human dihydroorotate dehydrogenase inhibitors as immunosuppressive agents by structure-based virtual screening.
Diao Y, Lu W, Jin H, Zhu J, Han L, Xu M, Gao R, Shen X, Zhao Z, Liu X, Xu Y, Huang J, Li H.
J Med Chem (2012) 55 : 8341 -8349
PubMed 22984987 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.42 6.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2178108 1 6.12
CHEMBL2178105 1 5.71
CHEMBL2178109 1 5.33
CHEMBL222556 1 5.02
CHEMBL973 TERIFLUNOMIDE 4.0 1 4.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2178108 IC50 = 760.0 nM 6.12
CHEMBL2178105 IC50 = 1930.0 nM 5.71
CHEMBL2178109 IC50 = 4670.0 nM 5.33
CHEMBL222556 IC50 = 9480.0 nM 5.02
CHEMBL973 TERIFLUNOMIDE IC50 = 11390.0 nM 4.94