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Assay Detail

CHEMBL879486

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

Binding
Inhibition of N-terminally truncated recombinant human dihydroorotate dehydrogenase using in vitro enzyme assay
23
Total Activities
23
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

SAR, species specificity, and cellular activity of cyclopentene dicarboxylic acid amides as DHODH inhibitors.
Leban J, Kralik M, Mies J, Gassen M, Tentschert K, Baumgartner R.
Bioorg Med Chem Lett (2005) 15 : 4854 -4857
PubMed 16143532 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.91 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL194955 1 8.40
CHEMBL154623 1 8.15
CHEMBL193365 1 7.96
CHEMBL195622 1 7.96
CHEMBL194075 1 7.82
CHEMBL157105 1 7.48
CHEMBL193371 1 7.39
CHEMBL194954 1 7.24
CHEMBL194776 1 6.98
CHEMBL196181 1 6.96
CHEMBL197553 1 6.90
CHEMBL194023 1 6.88
CHEMBL197194 VIDOFLUDIMUS 3.0 1 6.87
CHEMBL195246 1 6.76
CHEMBL195163 1 6.69
CHEMBL197455 1 6.44
CHEMBL348270 1 6.39
CHEMBL973 TERIFLUNOMIDE 4.0 1 6.38
CHEMBL372101 1 6.18
CHEMBL194395 1 6.17
CHEMBL196256 1 5.84
CHEMBL370008 1 5.70
CHEMBL196173 1 5.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL194955 IC50 = 4.0 nM 8.40
CHEMBL154623 IC50 = 7.0 nM 8.15
CHEMBL193365 IC50 = 11.0 nM 7.96
CHEMBL195622 IC50 = 11.0 nM 7.96
CHEMBL194075 IC50 = 15.0 nM 7.82
CHEMBL157105 IC50 = 33.0 nM 7.48
CHEMBL193371 IC50 = 41.0 nM 7.39
CHEMBL194954 IC50 = 58.0 nM 7.24
CHEMBL194776 IC50 = 105.0 nM 6.98
CHEMBL196181 IC50 = 110.0 nM 6.96
CHEMBL197553 IC50 = 127.0 nM 6.90
CHEMBL194023 IC50 = 131.0 nM 6.88
CHEMBL197194 VIDOFLUDIMUS IC50 = 134.0 nM 6.87
CHEMBL195246 IC50 = 173.0 nM 6.76
CHEMBL195163 IC50 = 205.0 nM 6.69
CHEMBL197455 IC50 = 360.0 nM 6.44
CHEMBL348270 IC50 = 410.0 nM 6.39
CHEMBL973 TERIFLUNOMIDE IC50 = 420.0 nM 6.38
CHEMBL372101 IC50 = 667.0 nM 6.18
CHEMBL194395 IC50 = 680.0 nM 6.17
CHEMBL196256 IC50 = 1460.0 nM 5.84
CHEMBL370008 IC50 = 2000.0 nM 5.70
CHEMBL196173 IC50 = 3800.0 nM 5.42