Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2014777

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

Binding
Inhibition of human DHODH after 20 mins by 2,6-dichloroindophenol-reduction based assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Optimization of Potent Inhibitors of P. falciparum Dihydroorotate Dehydrogenase for the Treatment of Malaria.
Skerlj RT, Bastos CM, Booker ML, Kramer ML, Barker RH, Celatka CA, O'Shea TJ, Munoz B, Sidhu AB, Cortese JF, Wittlin S, Papastogiannidis P, Angulo-Barturen I, Jimenez-Diaz MB, Sybertz E.
ACS Med Chem Lett (2011) 2 : 708 -713
PubMed 24900364 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.05 5.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2012961 1 5.51
CHEMBL2012963 1 5.25
CHEMBL2012964 1 5.14
CHEMBL2012966 1 4.83
CHEMBL2012831 1 4.82
CHEMBL2012965 1 4.76
CHEMBL2012821 1 -
CHEMBL2012822 1 -
CHEMBL2012823 1 -
CHEMBL2012824 1 -
CHEMBL2012825 1 -
CHEMBL2012826 1 -
CHEMBL2012827 1 -
CHEMBL2012829 1 -
CHEMBL2012820 1 -
CHEMBL2012941 1 -
CHEMBL2012951 1 -
CHEMBL2012962 1 -
CHEMBL2012830 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2012961 IC50 = 3100.0 nM 5.51
CHEMBL2012963 IC50 = 5600.0 nM 5.25
CHEMBL2012964 IC50 = 7300.0 nM 5.14
CHEMBL2012966 IC50 = 14900.0 nM 4.83
CHEMBL2012831 IC50 = 15100.0 nM 4.82
CHEMBL2012965 IC50 = 17200.0 nM 4.76
CHEMBL2012821 IC50 > 30000.0 nM -
CHEMBL2012822 IC50 > 30000.0 nM -
CHEMBL2012823 IC50 > 30000.0 nM -
CHEMBL2012824 IC50 > 30000.0 nM -
CHEMBL2012825 IC50 > 30000.0 nM -
CHEMBL2012826 IC50 > 30000.0 nM -
CHEMBL2012827 IC50 > 30000.0 nM -
CHEMBL2012829 IC50 > 30000.0 nM -
CHEMBL2012820 IC50 > 30000.0 nM -
CHEMBL2012941 IC50 > 30000.0 nM -
CHEMBL2012951 IC50 > 30000.0 nM -
CHEMBL2012962 IC50 > 30000.0 nM -
CHEMBL2012830 IC50 > 30000.0 nM -