Assay Detail
Binding
CHEMBL4137384
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant N-terminal GST-tagged human DHODH (31 to 395 residues) expressed in Escherichia coli BL21(DE3) assessed as inhibition of DCIP reduction using dihydroorotate as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins
10
Total Activities
10
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 Myeloid Differentiation Using Potent 2-Hydroxypyrazolo[1,5- a]pyridine Scaffold-Based Human Dihydroorotate Dehydrogenase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.45 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4173846 | — | — | 1 | 8.92 |
| CHEMBL38434 | BREQUINAR | 2.0 | 1 | 8.74 |
| CHEMBL4165923 | — | — | 1 | 8.37 |
| CHEMBL4177202 | — | — | 1 | 7.46 |
| CHEMBL4165815 | — | — | 1 | 7.37 |
| CHEMBL4062046 | — | — | 1 | 7.35 |
| CHEMBL973 | TERIFLUNOMIDE | 4.0 | 1 | 6.41 |
| CHEMBL4167855 | — | — | 1 | 6.32 |
| CHEMBL4175712 | — | — | 1 | 6.12 |
| CHEMBL4169359 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4173846 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL38434 | BREQUINAR | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4165923 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4177202 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4165815 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4062046 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL973 | TERIFLUNOMIDE | IC50 | = | 388.0 | nM | 6.41 |
| CHEMBL4167855 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL4175712 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL4169359 | — | IC50 | > | 5000.0 | nM | - |