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Assay Detail

CHEMBL863437

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Binding
Inhibitory activity against recombinant human DHODH
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Dihydroorotate dehydrogenase (quinone), mitochondrial (CHEMBL1966)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Biphenyl-4-ylcarbamoyl thiophene carboxylic acids as potent DHODH inhibitors.
Leban J, Kralik M, Mies J, Baumgartner R, Gassen M, Tasler S.
Bioorg Med Chem Lett (2006) 16 : 267 -270
PubMed 16246558 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.54 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL199361 1 9.00
CHEMBL200699 1 8.52
CHEMBL38434 BREQUINAR 2.0 1 8.10
CHEMBL345701 1 8.10
CHEMBL200856 1 8.05
CHEMBL199347 1 8.00
CHEMBL383165 1 8.00
CHEMBL200858 1 7.92
CHEMBL200895 1 7.80
CHEMBL371732 1 7.36
CHEMBL197194 VIDOFLUDIMUS 3.0 1 6.87
CHEMBL381043 1 6.52
CHEMBL370228 1 6.47
CHEMBL348270 1 6.39
CHEMBL199501 1 6.00
CHEMBL371482 1 -
CHEMBL426299 1 -
CHEMBL200894 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL199361 IC50 = 1.0 nM 9.00
CHEMBL200699 IC50 = 3.0 nM 8.52
CHEMBL38434 BREQUINAR IC50 = 8.0 nM 8.10
CHEMBL345701 IC50 = 8.0 nM 8.10
CHEMBL200856 IC50 = 9.0 nM 8.05
CHEMBL199347 IC50 = 10.0 nM 8.00
CHEMBL383165 IC50 = 10.0 nM 8.00
CHEMBL200858 IC50 = 12.0 nM 7.92
CHEMBL200895 IC50 = 16.0 nM 7.80
CHEMBL371732 IC50 = 44.0 nM 7.36
CHEMBL197194 VIDOFLUDIMUS IC50 = 134.0 nM 6.87
CHEMBL381043 IC50 = 303.0 nM 6.52
CHEMBL370228 IC50 = 340.0 nM 6.47
CHEMBL348270 IC50 = 410.0 nM 6.39
CHEMBL199501 IC50 = 1000.0 nM 6.00
CHEMBL371482 IC50 > 1000.0 nM -
CHEMBL426299 IC50 > 1000.0 nM -
CHEMBL200894 IC50 > 1000.0 nM -