Assay Detail
Binding
CHEMBL5157201
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of xanthine oxidase (unknown origin) using xanthine as substrate preincubated for 15 mins followed by substrate addition by UV spectrophotometric analysis
37
Total Activities
37
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 |
|---|---|---|---|
| IC50 | 37 | 6.97 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1164729 | FEBUXOSTAT | 4.0 | 1 | 7.55 |
| CHEMBL4445985 | — | — | 1 | 7.54 |
| CHEMBL5178809 | — | — | 1 | 7.41 |
| CHEMBL5197177 | — | — | 1 | 7.41 |
| CHEMBL5196996 | — | — | 1 | 7.37 |
| CHEMBL5191517 | — | — | 1 | 7.36 |
| CHEMBL5179253 | — | — | 1 | 7.35 |
| CHEMBL5193655 | — | — | 1 | 7.31 |
| CHEMBL5180223 | — | — | 1 | 7.30 |
| CHEMBL5206769 | — | — | 1 | 7.29 |
| CHEMBL5196602 | — | — | 1 | 7.28 |
| CHEMBL5186383 | — | — | 1 | 7.27 |
| CHEMBL5183372 | — | — | 1 | 7.24 |
| CHEMBL5189353 | — | — | 1 | 7.21 |
| CHEMBL5187769 | — | — | 1 | 7.17 |
| CHEMBL5202331 | — | — | 1 | 7.17 |
| CHEMBL5191800 | — | — | 1 | 7.14 |
| CHEMBL5185700 | — | — | 1 | 7.10 |
| CHEMBL5203944 | — | — | 1 | 7.03 |
| CHEMBL5205761 | — | — | 1 | 7.02 |
| CHEMBL5175675 | — | — | 1 | 7.00 |
| CHEMBL5190253 | — | — | 1 | 6.97 |
| CHEMBL5172810 | — | — | 1 | 6.95 |
| CHEMBL5170165 | — | — | 1 | 6.92 |
| CHEMBL5187940 | — | — | 1 | 6.87 |
| CHEMBL5192199 | — | — | 1 | 6.86 |
| CHEMBL5173648 | — | — | 1 | 6.86 |
| CHEMBL5177547 | — | — | 1 | 6.83 |
| CHEMBL5199185 | — | — | 1 | 6.82 |
| CHEMBL5185716 | — | — | 1 | 6.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1164729 | FEBUXOSTAT | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4445985 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5197177 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5178809 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5196996 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5191517 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5179253 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5193655 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5180223 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5206769 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL5196602 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5186383 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5183372 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5189353 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL5202331 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL5187769 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL5191800 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL5185700 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5203944 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL5205761 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL5175675 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL5190253 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL5172810 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL5170165 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL5187940 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL5192199 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL5173648 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL5177547 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL5199185 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL5185716 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL5207426 | — | IC50 | = | 188.0 | nM | 6.73 |
| CHEMBL5174688 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL5189770 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL5197680 | — | IC50 | = | 365.0 | nM | 6.44 |
| CHEMBL5169480 | — | IC50 | = | 725.0 | nM | 6.14 |
| CHEMBL5188474 | — | IC50 | = | 1739.0 | nM | 5.76 |
| CHEMBL1467 | ALLOPURINOL | IC50 | = | 7590.0 | nM | 5.12 |