Assay Detail
Binding
CHEMBL3296347
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C-terminal His6-tagged human DHODH (amino acid residues 30 to 396) expressed in Escherichia coli BL21 cells assessed as orotic acid production using dihydroorotate as substrate by DCIP dye-based assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BL21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Dihydroorotate dehydrogenase (quinone), mitochondrial (CHEMBL1966) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Fluorine modulates species selectivity in the triazolopyrimidine class of Plasmodium falciparum dihydroorotate dehydrogenase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.65 | 6.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL973 | TERIFLUNOMIDE | 4.0 | 1 | 6.36 |
| CHEMBL3289672 | — | — | 1 | 5.80 |
| CHEMBL3289671 | — | — | 1 | 5.68 |
| CHEMBL3289670 | — | — | 1 | 4.77 |
| CHEMBL1738786 | — | — | 1 | - |
| CHEMBL1956290 | — | — | 1 | - |
| CHEMBL492529 | — | — | 1 | - |
| CHEMBL1784577 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL973 | TERIFLUNOMIDE | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL3289672 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3289671 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3289670 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL1738786 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1956290 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL492529 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1784577 | — | IC50 | > | 100000.0 | nM | - |