Assay Detail
Binding
CHEMBL5248749
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 counting analysis
33
Total Activities
33
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
Design, synthesis and activity evaluation of novel lesinurad analogues containing thienopyrimidinone or pyridine substructure as human urate transporter 1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 4.97 | 5.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5271398 | — | — | 1 | 5.49 |
| CHEMBL4756866 | — | — | 1 | 5.38 |
| CHEMBL5277301 | — | — | 1 | 5.14 |
| CHEMBL5287151 | — | — | 1 | 5.12 |
| CHEMBL5284974 | — | — | 1 | 5.12 |
| CHEMBL5289202 | — | — | 1 | 5.10 |
| CHEMBL2105720 | LESINURAD | 4.0 | 1 | 5.03 |
| CHEMBL5269373 | — | — | 1 | 5.03 |
| CHEMBL5289441 | — | — | 1 | 5.01 |
| CHEMBL5278085 | — | — | 1 | 5.01 |
| CHEMBL5273217 | — | — | 1 | 5.01 |
| CHEMBL5279672 | — | — | 1 | 5.01 |
| CHEMBL5277066 | — | — | 1 | 5.00 |
| CHEMBL5268478 | — | — | 1 | 5.00 |
| CHEMBL5290258 | — | — | 1 | 4.99 |
| CHEMBL5282615 | — | — | 1 | 4.96 |
| CHEMBL5267727 | — | — | 1 | 4.95 |
| CHEMBL5285786 | — | — | 1 | 4.95 |
| CHEMBL5267010 | — | — | 1 | 4.94 |
| CHEMBL5291373 | — | — | 1 | 4.94 |
| CHEMBL5285533 | — | — | 1 | 4.94 |
| CHEMBL5268476 | — | — | 1 | 4.93 |
| CHEMBL5282586 | — | — | 1 | 4.92 |
| CHEMBL5290341 | — | — | 1 | 4.92 |
| CHEMBL5266247 | — | — | 1 | 4.91 |
| CHEMBL5272958 | — | — | 1 | 4.87 |
| CHEMBL5278304 | — | — | 1 | 4.86 |
| CHEMBL5272326 | — | — | 1 | 4.81 |
| CHEMBL5282047 | — | — | 1 | 4.80 |
| CHEMBL5269609 | — | — | 1 | 4.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5271398 | — | IC50 | = | 3270.0 | nM | 5.49 |
| CHEMBL4756866 | — | IC50 | = | 4170.0 | nM | 5.38 |
| CHEMBL5277301 | — | IC50 | = | 7310.0 | nM | 5.14 |
| CHEMBL5287151 | — | IC50 | = | 7680.0 | nM | 5.12 |
| CHEMBL5284974 | — | IC50 | = | 7560.0 | nM | 5.12 |
| CHEMBL5289202 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL2105720 | LESINURAD | IC50 | = | 9380.0 | nM | 5.03 |
| CHEMBL5269373 | — | IC50 | = | 9250.0 | nM | 5.03 |
| CHEMBL5289441 | — | IC50 | = | 9820.0 | nM | 5.01 |
| CHEMBL5278085 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL5273217 | — | IC50 | = | 9790.0 | nM | 5.01 |
| CHEMBL5279672 | — | IC50 | = | 9720.0 | nM | 5.01 |
| CHEMBL5277066 | — | IC50 | = | 9920.0 | nM | 5.00 |
| CHEMBL5268478 | — | IC50 | = | 10090.0 | nM | 5.00 |
| CHEMBL5290258 | — | IC50 | = | 10310.0 | nM | 4.99 |
| CHEMBL5282615 | — | IC50 | = | 11030.0 | nM | 4.96 |
| CHEMBL5267727 | — | IC50 | = | 11120.0 | nM | 4.95 |
| CHEMBL5285786 | — | IC50 | = | 11130.0 | nM | 4.95 |
| CHEMBL5267010 | — | IC50 | = | 11380.0 | nM | 4.94 |
| CHEMBL5291373 | — | IC50 | = | 11400.0 | nM | 4.94 |
| CHEMBL5285533 | — | IC50 | = | 11540.0 | nM | 4.94 |
| CHEMBL5268476 | — | IC50 | = | 11650.0 | nM | 4.93 |
| CHEMBL5282586 | — | IC50 | = | 11930.0 | nM | 4.92 |
| CHEMBL5290341 | — | IC50 | = | 12070.0 | nM | 4.92 |
| CHEMBL5266247 | — | IC50 | = | 12190.0 | nM | 4.91 |
| CHEMBL5272958 | — | IC50 | = | 13460.0 | nM | 4.87 |
| CHEMBL5278304 | — | IC50 | = | 13670.0 | nM | 4.86 |
| CHEMBL5272326 | — | IC50 | = | 15350.0 | nM | 4.81 |
| CHEMBL5282047 | — | IC50 | = | 15790.0 | nM | 4.80 |
| CHEMBL5269609 | — | IC50 | = | 16250.0 | nM | 4.79 |
| CHEMBL5284756 | — | IC50 | = | 17240.0 | nM | 4.76 |
| CHEMBL5287955 | — | IC50 | = | 18740.0 | nM | 4.73 |
| CHEMBL5270485 | — | IC50 | = | 20320.0 | nM | 4.69 |