Assay Detail
Binding
CHEMBL5615906
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Inhibition of human URAT1 transfected in HEK293 cells by measuring 14C-uric acid uptake preincubated for 30 mins followed by 14--uric acid addition and measured after 15 mins by liquid scintillation counter analysis
26
Total Activities
26
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 bioactivity evaluation of isobavachin derivatives as hURAT1 inhibitors for hyperuricemia agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 5.91 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5618375 | — | — | 1 | 6.80 |
| CHEMBL5620069 | — | — | 1 | 6.72 |
| CHEMBL5618313 | — | — | 1 | 6.64 |
| CHEMBL5618175 | — | — | 1 | 6.62 |
| CHEMBL5618500 | — | — | 1 | 6.44 |
| CHEMBL5620318 | — | — | 1 | 6.19 |
| CHEMBL5620253 | — | — | 1 | 6.19 |
| CHEMBL5618811 | — | — | 1 | 6.14 |
| CHEMBL5619569 | — | — | 1 | 6.08 |
| CHEMBL5618194 | — | — | 1 | 6.07 |
| CHEMBL5619241 | — | — | 1 | 6.02 |
| CHEMBL5619047 | — | — | 1 | 6.01 |
| CHEMBL5620313 | — | — | 1 | 5.79 |
| CHEMBL5619255 | — | — | 1 | 5.72 |
| CHEMBL5620074 | — | — | 1 | 5.68 |
| CHEMBL5618197 | — | — | 1 | 5.66 |
| CHEMBL5620142 | — | — | 1 | 5.66 |
| CHEMBL5619092 | — | — | 1 | 5.62 |
| CHEMBL5620285 | — | — | 1 | 5.60 |
| CHEMBL5618751 | — | — | 1 | 5.57 |
| CHEMBL5619622 | — | — | 1 | 5.54 |
| CHEMBL5618630 | — | — | 1 | 5.52 |
| CHEMBL5618105 | — | — | 1 | 5.45 |
| CHEMBL5619161 | — | — | 1 | 5.37 |
| CHEMBL5619991 | — | — | 1 | 5.35 |
| CHEMBL2105720 | LESINURAD | 4.0 | 1 | 5.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5618375 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5620069 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5618313 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL5618175 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5618500 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5620318 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL5620253 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL5618811 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL5619569 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL5618194 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL5619241 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL5619047 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL5620313 | — | IC50 | = | 1640.0 | nM | 5.79 |
| CHEMBL5619255 | — | IC50 | = | 1890.0 | nM | 5.72 |
| CHEMBL5620074 | — | IC50 | = | 2110.0 | nM | 5.68 |
| CHEMBL5618197 | — | IC50 | = | 2180.0 | nM | 5.66 |
| CHEMBL5620142 | — | IC50 | = | 2180.0 | nM | 5.66 |
| CHEMBL5619092 | — | IC50 | = | 2410.0 | nM | 5.62 |
| CHEMBL5620285 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5618751 | — | IC50 | = | 2680.0 | nM | 5.57 |
| CHEMBL5619622 | — | IC50 | = | 2860.0 | nM | 5.54 |
| CHEMBL5618630 | — | IC50 | = | 3020.0 | nM | 5.52 |
| CHEMBL5618105 | — | IC50 | = | 3590.0 | nM | 5.45 |
| CHEMBL5619161 | — | IC50 | = | 4240.0 | nM | 5.37 |
| CHEMBL5619991 | — | IC50 | = | 4430.0 | nM | 5.35 |
| CHEMBL2105720 | LESINURAD | IC50 | = | 7180.0 | nM | 5.14 |