Assay Detail
Binding
CHEMBL5158147
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human URAT1 mediated 14C-uric acid uptake expressed in HEK293 cells using 14C-uric acid as substrate incubated for 30 mins by liquid scintillation counter
9
Total Activities
9
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 Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.49 | 5.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5199889 | — | — | 1 | 5.87 |
| CHEMBL5175070 | — | — | 1 | 5.60 |
| CHEMBL5175653 | — | — | 1 | 5.59 |
| CHEMBL5200839 | — | — | 1 | 5.51 |
| CHEMBL5200105 | — | — | 1 | 5.45 |
| CHEMBL5191410 | — | — | 1 | 5.43 |
| CHEMBL5196337 | — | — | 1 | 5.43 |
| CHEMBL5179331 | — | — | 1 | 5.31 |
| CHEMBL2105720 | LESINURAD | 4.0 | 1 | 5.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5199889 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL5175070 | — | IC50 | = | 2490.0 | nM | 5.60 |
| CHEMBL5175653 | — | IC50 | = | 2570.0 | nM | 5.59 |
| CHEMBL5200839 | — | IC50 | = | 3060.0 | nM | 5.51 |
| CHEMBL5200105 | — | IC50 | = | 3550.0 | nM | 5.45 |
| CHEMBL5191410 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL5196337 | — | IC50 | = | 3670.0 | nM | 5.43 |
| CHEMBL5179331 | — | IC50 | = | 4940.0 | nM | 5.31 |
| CHEMBL2105720 | LESINURAD | IC50 | = | 5540.0 | nM | 5.26 |