Assay Detail
Binding
CHEMBL4331522
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Inhibition of Plasmodium falciparum recombinant N-terminal His6-tagged DHODH (159-569 residues) expressed in Escherichia coli BL21(DE3) using DHO as substrate measured every min for 5 mins by DCPI dye-based photometric analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Plasmodium falciparum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Dihydroorotate dehydrogenase (CHEMBL3486) ↗| Type | SINGLE PROTEIN |
| Organism | Plasmodium falciparum |
Publication
Hydroxyazole scaffold-based Plasmodium falciparum dihydroorotate dehydrogenase inhibitors: Synthesis, biological evaluation and X-ray structural studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.03 | 7.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL475813 | — | — | 1 | 7.19 |
| CHEMBL4458056 | — | — | 1 | 5.55 |
| CHEMBL4539458 | — | — | 1 | 5.28 |
| CHEMBL4517934 | — | — | 1 | 4.92 |
| CHEMBL4514989 | — | — | 1 | 4.80 |
| CHEMBL4457827 | — | — | 1 | 4.72 |
| CHEMBL4451149 | — | — | 1 | 4.64 |
| CHEMBL4514633 | — | — | 1 | 4.60 |
| CHEMBL4436588 | — | — | 1 | 4.46 |
| CHEMBL4464362 | — | — | 1 | 4.12 |
| CHEMBL4526067 | — | — | 1 | - |
| CHEMBL4437588 | — | — | 1 | - |
| CHEMBL4440085 | — | — | 1 | - |
| CHEMBL4544292 | — | — | 1 | - |
| CHEMBL4569109 | — | — | 1 | - |
| CHEMBL4568957 | — | — | 1 | - |
| CHEMBL4449622 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL475813 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4458056 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4539458 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4517934 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4514989 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL4457827 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4451149 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL4514633 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4436588 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL4464362 | — | IC50 | = | 75000.0 | nM | 4.12 |
| CHEMBL4526067 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL4437588 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL4440085 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL4544292 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL4569109 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL4568957 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL4449622 | — | IC50 | > | 250000.0 | nM | - |