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Assay Detail

CHEMBL1930744

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Binding
Inhibition of human dihydroorotate dehydrogenase
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 Autocuration

Target

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

Publication

Biaryl analogues of teriflunomide as potent DHODH inhibitors.
Erra M, Moreno I, Sanahuja J, Andrés M, Reinoso RF, Lozoya E, Pizcueta P, Godessart N, Castro-Palomino JC.
Bioorg Med Chem Lett (2011) 21 : 7268 -7272
PubMed 22078215 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.15 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1929450 1 7.58
CHEMBL1929439 1 7.57
CHEMBL1929453 1 7.51
CHEMBL1929441 1 7.51
CHEMBL1929437 1 7.51
CHEMBL1929452 1 7.47
CHEMBL1929442 1 7.40
CHEMBL1929438 1 7.35
CHEMBL1929443 1 7.31
CHEMBL1929436 1 7.28
CHEMBL1929448 1 7.23
CHEMBL1929447 1 7.18
CHEMBL1929451 1 7.18
CHEMBL1929434 1 7.14
CHEMBL1929449 1 7.12
CHEMBL1929433 1 7.03
CHEMBL1929445 1 7.01
CHEMBL1929435 1 6.96
CHEMBL1929446 1 6.86
CHEMBL1929444 1 6.82
CHEMBL1929432 1 6.82
CHEMBL1929440 1 6.70
CHEMBL973 TERIFLUNOMIDE 4.0 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1929450 IC50 = 26.0 nM 7.58
CHEMBL1929439 IC50 = 27.0 nM 7.57
CHEMBL1929453 IC50 = 31.0 nM 7.51
CHEMBL1929441 IC50 = 31.0 nM 7.51
CHEMBL1929437 IC50 = 31.0 nM 7.51
CHEMBL1929452 IC50 = 34.0 nM 7.47
CHEMBL1929442 IC50 = 40.0 nM 7.40
CHEMBL1929438 IC50 = 45.0 nM 7.35
CHEMBL1929443 IC50 = 49.0 nM 7.31
CHEMBL1929436 IC50 = 52.0 nM 7.28
CHEMBL1929448 IC50 = 59.0 nM 7.23
CHEMBL1929447 IC50 = 66.0 nM 7.18
CHEMBL1929451 IC50 = 66.0 nM 7.18
CHEMBL1929434 IC50 = 73.0 nM 7.14
CHEMBL1929449 IC50 = 76.0 nM 7.12
CHEMBL1929433 IC50 = 93.0 nM 7.03
CHEMBL1929445 IC50 = 97.0 nM 7.01
CHEMBL1929435 IC50 = 110.0 nM 6.96
CHEMBL1929446 IC50 = 137.0 nM 6.86
CHEMBL1929444 IC50 = 150.0 nM 6.82
CHEMBL1929432 IC50 = 150.0 nM 6.82
CHEMBL1929440 IC50 = 198.0 nM 6.70
CHEMBL973 TERIFLUNOMIDE IC50 = 1083.0 nM 5.96