Assay Detail
Binding
CHEMBL5157202
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Mixed-type inhibition of xanthine oxidase (unknown origin) assessed as inhibitory constant of enzyme-substrate complex using xanthine as substrate at varying concentrations preincubated for 15 mins followed by substrate addition by UV spectrophotometric analysis
5
Total Activities
5
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 |
Publication
Intramolecular hydrogen bond interruption and scaffold hopping of TMC-5 led to 2-(4-alkoxy-3-cyanophenyl)pyrimidine-4/5-carboxylic acids and 6-(4-alkoxy-3-cyanophenyl)-1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-ones as potent pyrimidine-based xanthine oxidase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 8.38 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1164729 | FEBUXOSTAT | 4.0 | 1 | 10.00 |
| CHEMBL5197177 | — | — | 1 | 8.43 |
| CHEMBL4445985 | — | — | 1 | 8.38 |
| CHEMBL5186383 | — | — | 1 | 7.61 |
| CHEMBL5189353 | — | — | 1 | 7.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1164729 | FEBUXOSTAT | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL5197177 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL4445985 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL5186383 | — | Ki | = | 24.3 | nM | 7.61 |
| CHEMBL5189353 | — | Ki | = | 32.5 | nM | 7.49 |