Assay Detail
Binding
CHEMBL5111971
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal GST-fusion tagged DHODH (31 to 395 residues) expressed in Escherichia coli BL21-GOLD (DE3) using dihydroorotate as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by DCIP assay
18
Total Activities
18
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 | 18 | 6.27 | 8.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5192490 | — | — | 1 | 8.14 |
| CHEMBL5196292 | — | — | 1 | 7.75 |
| CHEMBL4165815 | — | — | 1 | 7.30 |
| CHEMBL5183718 | — | — | 1 | 7.16 |
| CHEMBL5209405 | — | — | 1 | 6.94 |
| CHEMBL5182435 | — | — | 1 | 6.40 |
| CHEMBL5190641 | — | — | 1 | 5.66 |
| CHEMBL5181901 | — | — | 1 | 5.66 |
| CHEMBL5172821 | — | — | 1 | 5.55 |
| CHEMBL5178813 | — | — | 1 | 5.41 |
| CHEMBL5173387 | — | — | 1 | 5.28 |
| CHEMBL5193995 | — | — | 1 | 5.16 |
| CHEMBL5188838 | — | — | 1 | 5.14 |
| CHEMBL5180390 | — | — | 1 | - |
| CHEMBL5181455 | — | — | 1 | - |
| CHEMBL5185261 | — | — | 1 | - |
| CHEMBL5203155 | — | — | 1 | - |
| CHEMBL5169905 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5192490 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL5196292 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4165815 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5183718 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5209405 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL5182435 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL5190641 | — | IC50 | = | 2209.0 | nM | 5.66 |
| CHEMBL5181901 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5172821 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL5178813 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL5173387 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL5193995 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL5188838 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL5180390 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5181455 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5185261 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5203155 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5169905 | — | IC50 | > | 10000.0 | nM | - |