Assay Detail
Binding
CHEMBL4731276
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Inhibition of URAT1 in human RPTEC assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric acid addition and incubated under shaking condition for 2 hrs by scintillation counter method
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | RPTEC |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Dotinurad (FYU-981), a New Phenol Derivative with Highly Potent Uric Acid Lowering Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 4.97 | 5.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4762461 | — | — | 1 | 5.60 |
| CHEMBL4748804 | — | — | 1 | 5.58 |
| CHEMBL4749075 | — | — | 1 | 5.50 |
| CHEMBL4792097 | — | — | 1 | 5.37 |
| CHEMBL4796932 | — | — | 1 | 5.28 |
| CHEMBL4760971 | — | — | 1 | 5.24 |
| CHEMBL388590 | BENZBROMARONE | 4.0 | 1 | 5.17 |
| CHEMBL4594446 | DOTINURAD | 3.0 | 1 | 5.17 |
| CHEMBL4756915 | — | — | 1 | 5.15 |
| CHEMBL4796568 | — | — | 1 | 5.06 |
| CHEMBL4781629 | — | — | 1 | 4.97 |
| CHEMBL4744184 | — | — | 1 | 4.88 |
| CHEMBL4744854 | — | — | 1 | 4.83 |
| CHEMBL4762003 | — | — | 1 | 4.75 |
| CHEMBL4740995 | — | — | 1 | 4.72 |
| CHEMBL4753182 | — | — | 1 | 4.50 |
| CHEMBL4778323 | — | — | 1 | 4.47 |
| CHEMBL4781818 | — | — | 1 | 4.08 |
| CHEMBL4757464 | — | — | 1 | 4.08 |
| CHEMBL4756625 | — | — | 1 | - |
| CHEMBL4785815 | — | — | 1 | - |
| CHEMBL4800504 | — | — | 1 | - |
| CHEMBL4790389 | — | — | 1 | - |
| CHEMBL4785752 | — | — | 1 | - |
| CHEMBL4782683 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4762461 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4748804 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4749075 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4792097 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL4796932 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4760971 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL388590 | BENZBROMARONE | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL4594446 | DOTINURAD | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL4756915 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL4796568 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL4781629 | — | IC50 | = | 10800.0 | nM | 4.97 |
| CHEMBL4744184 | — | IC50 | = | 13100.0 | nM | 4.88 |
| CHEMBL4744854 | — | IC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL4762003 | — | IC50 | = | 17800.0 | nM | 4.75 |
| CHEMBL4740995 | — | IC50 | = | 19200.0 | nM | 4.72 |
| CHEMBL4753182 | — | IC50 | = | 31600.0 | nM | 4.50 |
| CHEMBL4778323 | — | IC50 | = | 33900.0 | nM | 4.47 |
| CHEMBL4781818 | — | IC50 | = | 83300.0 | nM | 4.08 |
| CHEMBL4757464 | — | IC50 | = | 83900.0 | nM | 4.08 |
| CHEMBL4756625 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4785815 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4800504 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4790389 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4785752 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4782683 | — | IC50 | > | 100000.0 | nM | - |