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Assay Detail

CHEMBL1960215

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

Binding
Inhibition of human recombinant DHODH transmembrane domain using 2,6-dichloroindophenol sodium, L-Dihydroorotic acid, and decylubiquinone as substrate mix after 30 mins by microplate reader
10
Total Activities
10
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

Discovery of 4-hydroxy-1,6-naphthyridine-3-carbonitrile derivatives as novel PDE10A inhibitors.
Bauer U, Giordanetto F, Bauer M, O'Mahony G, Johansson KE, Knecht W, Hartleib-Geschwindner J, Carlsson ET, Enroth C.
Bioorg Med Chem Lett (2012) 22 : 1944 -1948
PubMed 22321214 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.80 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1957366 1 6.70
CHEMBL1957462 1 5.96
CHEMBL1957460 1 5.89
CHEMBL1957380 1 5.24
CHEMBL1957370 1 5.20
CHEMBL1957379 1 -
CHEMBL1957381 1 -
CHEMBL1957372 1 -
CHEMBL1957371 1 -
CHEMBL1957461 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1957366 IC50 = 200.0 nM 6.70
CHEMBL1957462 IC50 = 1100.0 nM 5.96
CHEMBL1957460 IC50 = 1300.0 nM 5.89
CHEMBL1957380 IC50 = 5700.0 nM 5.24
CHEMBL1957370 IC50 = 6300.0 nM 5.20
CHEMBL1957379 IC50 > 9900.0 nM -
CHEMBL1957381 IC50 > 9900.0 nM -
CHEMBL1957372 IC50 > 9900.0 nM -
CHEMBL1957371 IC50 > 9900.0 nM -
CHEMBL1957461 IC50 > 9900.0 nM -