Assay Detail
Binding
CHEMBL4230385
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Inhibition of bovine xanthine oxidase assessed as reduction in uric acid formation using xanthine as substrate preincubated for 15 mins followed by substrate addition by spectrophotometric analysis
39
Total Activities
31
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and biological evaluation of 1-hydroxy-2-phenyl-4-pyridyl-1H-imidazole derivatives as xanthine oxidase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 30 | 6.19 | 8.00 |
| IC50 | 8 | 5.65 | 8.32 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1078685 | TOPIROXOSTAT | 2.0 | 1 | 8.32 |
| CHEMBL460160 | — | — | 1 | 8.00 |
| CHEMBL516626 | — | — | 1 | 8.00 |
| CHEMBL468706 | — | — | 1 | 7.77 |
| CHEMBL459952 | — | — | 1 | 7.70 |
| CHEMBL462284 | — | — | 1 | 7.68 |
| CHEMBL461228 | — | — | 1 | 7.62 |
| CHEMBL459319 | — | — | 1 | 7.62 |
| CHEMBL462283 | — | — | 1 | 7.59 |
| CHEMBL460158 | — | — | 1 | 7.51 |
| CHEMBL462497 | — | — | 1 | 7.40 |
| CHEMBL508591 | — | — | 1 | 7.37 |
| CHEMBL518362 | — | — | 1 | 7.22 |
| CHEMBL462498 | — | — | 1 | 7.19 |
| CHEMBL462496 | — | — | 1 | 6.96 |
| CHEMBL4240082 | — | — | 3 | 6.19 |
| CHEMBL4248090 | — | — | 2 | 5.36 |
| CHEMBL4251121 | — | — | 2 | 5.32 |
| CHEMBL513690 | — | — | 1 | 5.23 |
| CHEMBL4243871 | — | — | 2 | 5.17 |
| CHEMBL4237723 | — | — | 1 | 5.17 |
| CHEMBL4249720 | — | — | 1 | 5.09 |
| CHEMBL4238313 | — | — | 2 | 5.02 |
| CHEMBL4240097 | — | — | 2 | 4.99 |
| CHEMBL4240552 | — | — | 2 | 4.81 |
| CHEMBL4251498 | — | — | 1 | 4.79 |
| CHEMBL4239301 | — | — | 1 | 4.74 |
| CHEMBL4248086 | — | — | 1 | 4.68 |
| CHEMBL4243408 | — | — | 1 | 4.63 |
| CHEMBL4243524 | — | — | 1 | 4.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1078685 | TOPIROXOSTAT | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL460160 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL516626 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL468706 | — | EC50 | = | 16.98 | nM | 7.77 |
| CHEMBL459952 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL462284 | — | EC50 | = | 20.89 | nM | 7.68 |
| CHEMBL461228 | — | EC50 | = | 23.99 | nM | 7.62 |
| CHEMBL459319 | — | EC50 | = | 23.99 | nM | 7.62 |
| CHEMBL462283 | — | EC50 | = | 25.7 | nM | 7.59 |
| CHEMBL460158 | — | EC50 | = | 30.9 | nM | 7.51 |
| CHEMBL462497 | — | EC50 | = | 39.81 | nM | 7.40 |
| CHEMBL508591 | — | EC50 | = | 42.66 | nM | 7.37 |
| CHEMBL518362 | — | EC50 | = | 60.26 | nM | 7.22 |
| CHEMBL462498 | — | EC50 | = | 64.57 | nM | 7.19 |
| CHEMBL462496 | — | EC50 | = | 109.65 | nM | 6.96 |
| CHEMBL4240082 | — | EC50 | = | 645.65 | nM | 6.19 |
| CHEMBL4240082 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL4248090 | — | EC50 | = | 4365.16 | nM | 5.36 |
| CHEMBL4248090 | — | IC50 | = | 4350.0 | nM | 5.36 |
| CHEMBL4251121 | — | IC50 | = | 4750.0 | nM | 5.32 |
| CHEMBL4251121 | — | EC50 | = | 4786.3 | nM | 5.32 |
| CHEMBL513690 | — | EC50 | = | 5888.44 | nM | 5.23 |
| CHEMBL4237723 | — | EC50 | = | 6760.83 | nM | 5.17 |
| CHEMBL4243871 | — | IC50 | = | 6730.0 | nM | 5.17 |
| CHEMBL4243871 | — | EC50 | = | 6760.83 | nM | 5.17 |
| CHEMBL4249720 | — | EC50 | = | 8128.31 | nM | 5.09 |
| CHEMBL4238313 | — | EC50 | = | 9549.93 | nM | 5.02 |
| CHEMBL4238313 | — | IC50 | = | 9620.0 | nM | 5.02 |
| CHEMBL4240097 | — | IC50 | = | 10280.0 | nM | 4.99 |
| CHEMBL4240097 | — | EC50 | = | 10232.93 | nM | 4.99 |
| CHEMBL4240552 | — | EC50 | = | 15488.17 | nM | 4.81 |
| CHEMBL4240552 | — | IC50 | = | 15420.0 | nM | 4.81 |
| CHEMBL4251498 | — | EC50 | = | 16218.1 | nM | 4.79 |
| CHEMBL4239301 | — | EC50 | = | 18197.01 | nM | 4.74 |
| CHEMBL4248086 | — | EC50 | = | 20892.96 | nM | 4.68 |
| CHEMBL4243408 | — | EC50 | = | 23442.29 | nM | 4.63 |
| CHEMBL4243524 | — | EC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL4239183 | — | EC50 | = | 44668.36 | nM | 4.35 |
| CHEMBL4240082 | — | Inhibition | - | % | - |