Assay Detail
Binding
CHEMBL3296346
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His6-tagged recombinant Plasmodium falciparum DHODH (amino acid residues 158 to 569) expressed in Escherichia coli BL21 cells assessed as orotic acid production using dihydroorotate as substrate by DCIP dye-based assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Plasmodium falciparum |
| Cell Type | BL21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Dihydroorotate dehydrogenase (CHEMBL3486) ↗| Type | SINGLE PROTEIN |
| Organism | Plasmodium falciparum |
Publication
Fluorine modulates species selectivity in the triazolopyrimidine class of Plasmodium falciparum dihydroorotate dehydrogenase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.09 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3289671 | — | — | 1 | 7.70 |
| CHEMBL3289672 | — | — | 1 | 7.66 |
| CHEMBL1956290 | — | — | 1 | 7.46 |
| CHEMBL3289670 | — | — | 1 | 7.46 |
| CHEMBL1738786 | — | — | 1 | 7.34 |
| CHEMBL492529 | — | — | 1 | 6.57 |
| CHEMBL973 | TERIFLUNOMIDE | 4.0 | 1 | 5.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3289671 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3289672 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1956290 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3289670 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1738786 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL492529 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL973 | TERIFLUNOMIDE | IC50 | = | 3900.0 | nM | 5.41 |