Assay Detail
Binding
CHEMBL4373339
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Inhibition of human URAT1 expressed in HEK293 cells assessed as reduction in [8-14C]uric acid uptake
21
Total Activities
21
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
Synthesis, biological evaluation and 3D-QSAR studies of 1,2,4-triazole-5-substituted carboxylic acid bioisosteres as uric acid transporter 1 (URAT1) inhibitors for the treatment of hyperuricemia associated with gout.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 5.64 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4546569 | — | — | 1 | 7.50 |
| CHEMBL4453888 | — | — | 1 | 7.03 |
| CHEMBL4458898 | — | — | 1 | 6.55 |
| CHEMBL4468962 | — | — | 1 | 6.19 |
| CHEMBL4448964 | — | — | 1 | 5.81 |
| CHEMBL4445587 | — | — | 1 | 5.78 |
| CHEMBL4585746 | — | — | 1 | 5.71 |
| CHEMBL4554148 | — | — | 1 | 5.66 |
| CHEMBL4556590 | — | — | 1 | 5.55 |
| CHEMBL4560122 | — | — | 1 | 5.49 |
| CHEMBL4573946 | — | — | 1 | 5.39 |
| CHEMBL4467680 | — | — | 1 | 5.29 |
| CHEMBL4473863 | — | — | 1 | 5.27 |
| CHEMBL4516802 | — | — | 1 | 5.20 |
| CHEMBL2105720 | LESINURAD | 4.0 | 1 | 5.14 |
| CHEMBL4436938 | — | — | 1 | 4.99 |
| CHEMBL4551589 | — | — | 1 | 4.98 |
| CHEMBL4568207 | — | — | 1 | 4.84 |
| CHEMBL4517057 | — | — | 1 | 4.80 |
| CHEMBL4459618 | — | — | 1 | - |
| CHEMBL4594032 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4546569 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4453888 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4458898 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4468962 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL4448964 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL4445587 | — | IC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL4585746 | — | IC50 | = | 1940.0 | nM | 5.71 |
| CHEMBL4554148 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4556590 | — | IC50 | = | 2790.0 | nM | 5.55 |
| CHEMBL4560122 | — | IC50 | = | 3240.0 | nM | 5.49 |
| CHEMBL4573946 | — | IC50 | = | 4050.0 | nM | 5.39 |
| CHEMBL4467680 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL4473863 | — | IC50 | = | 5410.0 | nM | 5.27 |
| CHEMBL4516802 | — | IC50 | = | 6380.0 | nM | 5.20 |
| CHEMBL2105720 | LESINURAD | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL4436938 | — | IC50 | = | 10210.0 | nM | 4.99 |
| CHEMBL4551589 | — | IC50 | = | 10570.0 | nM | 4.98 |
| CHEMBL4568207 | — | IC50 | = | 14380.0 | nM | 4.84 |
| CHEMBL4517057 | — | IC50 | = | 15780.0 | nM | 4.80 |
| CHEMBL4459618 | — | IC50 | = | 365000.0 | nM | - |
| CHEMBL4594032 | — | IC50 | = | 119000.0 | nM | - |