Assay Detail
Binding
CHEMBL3296353
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 direct assay in presence of oxygen depleting system
5
Total Activities
5
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 | 5 | 5.57 | 6.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL973 | TERIFLUNOMIDE | 4.0 | 1 | 6.68 |
| CHEMBL3289672 | — | — | 1 | 5.68 |
| CHEMBL3289671 | — | — | 1 | 5.57 |
| CHEMBL3289670 | — | — | 1 | 4.35 |
| CHEMBL1738786 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL973 | TERIFLUNOMIDE | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3289672 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3289671 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3289670 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL1738786 | — | IC50 | > | 100000.0 | nM | - |