Assay Detail
Binding
CHEMBL5353064
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Inhibition of human URAT1 stably overexpressing in human HEK293 cells assessed as inhibition of 14C-uric acid uptake preincubated for 30 mins followed by substrate addition and measured after 15 mins using 14C-uric acid as substrate by liquid scintillation counting analysis
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of novel benzbromarone analogs with improved pharmacokinetics and benign toxicity profiles as antihyperuricemic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 5.70 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3707347 | VERINURAD | 2.0 | 1 | 6.89 |
| CHEMBL388590 | BENZBROMARONE | 4.0 | 1 | 6.28 |
| CHEMBL5439993 | — | — | 1 | 6.10 |
| CHEMBL5405072 | — | — | 1 | 5.81 |
| CHEMBL5400167 | — | — | 1 | 5.81 |
| CHEMBL5429502 | — | — | 1 | 5.80 |
| CHEMBL5396194 | — | — | 1 | 5.80 |
| CHEMBL5395589 | — | — | 1 | 5.76 |
| CHEMBL5417202 | — | — | 1 | 5.74 |
| CHEMBL5437905 | — | — | 1 | 5.70 |
| CHEMBL5412709 | — | — | 1 | 5.68 |
| CHEMBL5397658 | — | — | 1 | 5.65 |
| CHEMBL5405794 | — | — | 1 | 5.64 |
| CHEMBL5438015 | — | — | 1 | 5.63 |
| CHEMBL5436610 | — | — | 1 | 5.57 |
| CHEMBL5417306 | — | — | 1 | 5.57 |
| CHEMBL5435294 | — | — | 1 | 5.55 |
| CHEMBL5421730 | — | — | 1 | 5.53 |
| CHEMBL5437838 | — | — | 1 | 5.49 |
| CHEMBL5396907 | — | — | 1 | 5.42 |
| CHEMBL5394644 | — | — | 1 | 5.31 |
| CHEMBL5426916 | — | — | 1 | 5.23 |
| CHEMBL2105720 | LESINURAD | 4.0 | 1 | 5.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3707347 | VERINURAD | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL388590 | BENZBROMARONE | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL5439993 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL5405072 | — | IC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL5400167 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL5429502 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL5396194 | — | IC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL5395589 | — | IC50 | = | 1720.0 | nM | 5.76 |
| CHEMBL5417202 | — | IC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL5437905 | — | IC50 | = | 1980.0 | nM | 5.70 |
| CHEMBL5412709 | — | IC50 | = | 2080.0 | nM | 5.68 |
| CHEMBL5397658 | — | IC50 | = | 2260.0 | nM | 5.65 |
| CHEMBL5405794 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5438015 | — | IC50 | = | 2360.0 | nM | 5.63 |
| CHEMBL5436610 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL5417306 | — | IC50 | = | 2690.0 | nM | 5.57 |
| CHEMBL5435294 | — | IC50 | = | 2810.0 | nM | 5.55 |
| CHEMBL5421730 | — | IC50 | = | 2950.0 | nM | 5.53 |
| CHEMBL5437838 | — | IC50 | = | 3220.0 | nM | 5.49 |
| CHEMBL5396907 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL5394644 | — | IC50 | = | 4850.0 | nM | 5.31 |
| CHEMBL5426916 | — | IC50 | = | 5830.0 | nM | 5.23 |
| CHEMBL2105720 | LESINURAD | IC50 | = | 7560.0 | nM | 5.12 |