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Assay Detail

CHEMBL4390975

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ADMET
Inhibition of human DHODH using DHO as substrate measured at 4 secs interval for 60 secs by DCIP reduction based indirect assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
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

Ligand-based design, synthesis and biochemical evaluation of potent and selective inhibitors of Schistosoma mansoni dihydroorotate dehydrogenase.
Calil FA, David JS, Chiappetta ERC, Fumagalli F, Mello RB, Leite FHA, Castilho MS, Emery FS, Nonato MC.
Eur J Med Chem (2019) 167 : 357 -366
PubMed 30776695 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 5.92 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38434 BREQUINAR 2.0 1 7.43
CHEMBL15193 LAPACHOL 1 7.00
CHEMBL4472078 1 6.97
CHEMBL4540838 1 6.91
CHEMBL973 TERIFLUNOMIDE 4.0 1 6.51
CHEMBL4566973 1 6.48
CHEMBL4560384 1 6.27
CHEMBL155771 1 6.15
CHEMBL4452960 1 6.09
CHEMBL4457147 1 6.04
CHEMBL4546952 1 5.98
CHEMBL4586212 1 5.75
CHEMBL2408377 1 5.58
CHEMBL1450 ATOVAQUONE 4.0 1 5.57
CHEMBL4524841 1 5.44
CHEMBL4474026 1 5.34
CHEMBL2041119 1 5.17
CHEMBL2023282 1 5.10
CHEMBL2408379 1 5.00
CHEMBL62718 1 5.00
CHEMBL8320 BENZOQUINONE 1 4.47
CHEMBL4527976 1 -
CHEMBL4464250 1 -
CHEMBL240963 LAWSONE 1 -
CHEMBL4436314 1 -
CHEMBL2408378 1 -
CHEMBL358225 Cresoquinone 1 -
CHEMBL2252966 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38434 BREQUINAR IC50 = 37.0 nM 7.43
CHEMBL15193 LAPACHOL IC50 = 100.0 nM 7.00
CHEMBL4472078 IC50 = 108.0 nM 6.97
CHEMBL4540838 IC50 = 123.0 nM 6.91
CHEMBL973 TERIFLUNOMIDE IC50 = 312.0 nM 6.51
CHEMBL4566973 IC50 = 330.0 nM 6.48
CHEMBL4560384 IC50 = 541.0 nM 6.27
CHEMBL155771 IC50 = 709.0 nM 6.15
CHEMBL4452960 IC50 = 808.0 nM 6.09
CHEMBL4457147 IC50 = 911.0 nM 6.04
CHEMBL4546952 IC50 = 1050.0 nM 5.98
CHEMBL4586212 IC50 = 1800.0 nM 5.75
CHEMBL2408377 IC50 = 2600.0 nM 5.58
CHEMBL1450 ATOVAQUONE IC50 = 2700.0 nM 5.57
CHEMBL4524841 IC50 = 3600.0 nM 5.44
CHEMBL4474026 IC50 = 4600.0 nM 5.34
CHEMBL2041119 IC50 = 6800.0 nM 5.17
CHEMBL2023282 IC50 = 7900.0 nM 5.10
CHEMBL2408379 IC50 = 10000.0 nM 5.00
CHEMBL62718 IC50 = 10000.0 nM 5.00
CHEMBL8320 BENZOQUINONE IC50 = 34000.0 nM 4.47
CHEMBL4527976 IC50 - -
CHEMBL4464250 IC50 - -
CHEMBL240963 LAWSONE IC50 - -
CHEMBL4436314 IC50 - -
CHEMBL2408378 IC50 - -
CHEMBL358225 Cresoquinone IC50 - -
CHEMBL2252966 IC50 - -