Assay Detail
Binding
CHEMBL5111970
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST-fusion tagged DHODH expressed in Escherichia coli BL21 (DE3) using dihydroorotate as substrate at 50 uM preincubated for 5 mins followed by substrate addition measured after 5 mins by DCIP assay
3
Total Activities
3
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
Targeting Acute Myelogenous Leukemia Using Potent Human Dihydroorotate Dehydrogenase Inhibitors Based on the 2-Hydroxypyrazolo[1,5-<i>a</i>]pyridine Scaffold: SAR of the Aryloxyaryl Moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.99 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4173846 | — | — | 1 | 8.92 |
| CHEMBL38434 | BREQUINAR | 2.0 | 1 | 8.74 |
| CHEMBL4167855 | — | — | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4173846 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL38434 | BREQUINAR | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4167855 | — | IC50 | = | 480.0 | nM | 6.32 |