Assay Detail
Binding
CHEMBL3822209
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminally truncated human DHODH (Met30 to Arg396 residues) expressed in Escherichia coli BL21 (DE3) using dihydroorotate as substrate preincubated for 5 mins followed by substrate addition measured every 30 secs for 6 mins by DCIP-based spectrophotometric assay
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
Biological evaluation of quinoline derivatives as inhibitors of human dihydroorotate dehydrogenase
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.53 | 8.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38434 | BREQUINAR | 2.0 | 1 | 8.13 |
| CHEMBL3818031 | — | — | 1 | 8.01 |
| CHEMBL3818640 | — | — | 1 | 7.24 |
| CHEMBL3818257 | — | — | 1 | 6.87 |
| CHEMBL3818502 | — | — | 1 | 6.36 |
| CHEMBL3819188 | — | — | 1 | 6.18 |
| CHEMBL3817894 | — | — | 1 | 5.88 |
| CHEMBL2335126 | — | — | 1 | 5.80 |
| CHEMBL3818174 | — | — | 1 | 5.49 |
| CHEMBL1571058 | — | — | 1 | 5.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38434 | BREQUINAR | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL3818031 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL3818640 | — | IC50 | = | 57.1 | nM | 7.24 |
| CHEMBL3818257 | — | IC50 | = | 136.2 | nM | 6.87 |
| CHEMBL3818502 | — | IC50 | = | 436.7 | nM | 6.36 |
| CHEMBL3819188 | — | IC50 | = | 666.2 | nM | 6.18 |
| CHEMBL3817894 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL2335126 | — | IC50 | = | 1566.1 | nM | 5.80 |
| CHEMBL3818174 | — | IC50 | = | 3249.8 | nM | 5.49 |
| CHEMBL1571058 | — | IC50 | = | 5176.8 | nM | 5.29 |