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Assay Detail

CHEMBL3062604

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

Binding
Inhibition of Plasmodium falciparum HIs6-tagged DHODH expressed in Escherichia coli DH5alpha using L-dihydroorotate as substrate by DCIP-based spectrophotometric analysis
22
Total Activities
22
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

Molecular modeling studies, synthesis and biological evaluation of derivatives of N-phenylbenzamide as Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitors
Desai KR, Shaikh MS, Coutinho EC
Med Chem Res (2011) 20 : 321 -332
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.41 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2234185 1 7.00
CHEMBL2234186 1 7.00
CHEMBL2234188 1 7.00
CHEMBL2234182 1 7.00
CHEMBL2234183 1 6.82
CHEMBL217893 1 6.82
CHEMBL2234187 1 6.82
CHEMBL1331783 1 6.70
CHEMBL2234191 1 6.60
CHEMBL2234189 1 6.60
CHEMBL2234184 1 6.60
CHEMBL2234190 1 6.52
CHEMBL2234192 1 6.26
CHEMBL199572 1 4.37
CHEMBL372561 1 4.03
CHEMBL973 TERIFLUNOMIDE 4.0 1 -
CHEMBL370865 1 -
CHEMBL199574 1 -
CHEMBL141040 1 -
CHEMBL344556 1 -
CHEMBL141732 1 -
CHEMBL141195 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2234185 IC50 = 100.0 nM 7.00
CHEMBL2234186 IC50 = 100.0 nM 7.00
CHEMBL2234188 IC50 = 100.0 nM 7.00
CHEMBL2234182 IC50 = 100.0 nM 7.00
CHEMBL2234183 IC50 = 151.36 nM 6.82
CHEMBL217893 IC50 = 151.36 nM 6.82
CHEMBL2234187 IC50 = 151.36 nM 6.82
CHEMBL1331783 IC50 = 199.53 nM 6.70
CHEMBL2234191 IC50 = 251.19 nM 6.60
CHEMBL2234189 IC50 = 251.19 nM 6.60
CHEMBL2234184 IC50 = 251.19 nM 6.60
CHEMBL2234190 IC50 = 302.0 nM 6.52
CHEMBL2234192 IC50 = 549.54 nM 6.26
CHEMBL199572 IC50 = 42657.95 nM 4.37
CHEMBL372561 IC50 = 93325.43 nM 4.03
CHEMBL973 TERIFLUNOMIDE IC50 = 190546.07 nM -
CHEMBL370865 IC50 = 154881.66 nM -
CHEMBL199574 IC50 = 141253.75 nM -
CHEMBL141040 IC50 = 870963.59 nM -
CHEMBL344556 IC50 = 537031.8 nM -
CHEMBL141732 IC50 = 1071519.31 nM -
CHEMBL141195 IC50 = 707945.78 nM -