Assay Detail
Binding
CHEMBL1948717
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Inhibition of dihydroorotate dehydrogenase in Wistar rat liver mitochondrial/microsomal membranes measured for 5 mins by 2,6-dichlorophenolindophenol reduction-based spectrophotometry
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Dihydroorotate dehydrogenase (quinone), mitochondrial (CHEMBL2383) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
New inhibitors of dihydroorotate dehydrogenase (DHODH) based on the 4-hydroxy-1,2,5-oxadiazol-3-yl (hydroxyfurazanyl) scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.02 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL973 | TERIFLUNOMIDE | 4.0 | 1 | 7.70 |
| CHEMBL38434 | BREQUINAR | 2.0 | 1 | 7.48 |
| CHEMBL1946851 | — | — | 1 | 7.30 |
| CHEMBL1946659 | — | — | 1 | 7.18 |
| CHEMBL1946850 | — | — | 1 | 6.92 |
| CHEMBL1946849 | — | — | 1 | 6.31 |
| CHEMBL1946658 | — | — | 1 | 6.06 |
| CHEMBL1946660 | — | — | 1 | 6.06 |
| CHEMBL1946848 | — | — | 1 | 5.64 |
| CHEMBL1946653 | — | — | 1 | 5.37 |
| CHEMBL1946654 | — | — | 1 | 4.96 |
| CHEMBL1946657 | — | — | 1 | 4.60 |
| CHEMBL1946655 | — | — | 1 | 4.35 |
| CHEMBL1946656 | — | — | 1 | 4.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL973 | TERIFLUNOMIDE | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL38434 | BREQUINAR | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL1946851 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1946659 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL1946850 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1946849 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL1946658 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL1946660 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL1946848 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL1946653 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL1946654 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1946657 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL1946655 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL1946656 | — | IC50 | = | 49000.0 | nM | 4.31 |