Assay Detail
Binding
CHEMBL5531697
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human URAT1 expressed in HEK293T cells using 14C- uric acid assessed as uric acid absorption by measuring intracellular liquid radiation value by liquid scintillation counting analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Novel Thienopyrimidine Compound as a Urate Transporter 1 and Glucose Transporter 9 Dual Inhibitor with Improved Efficacy and Favorable Druggability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.44 | 5.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5590320 | — | — | 1 | 5.70 |
| CHEMBL5542414 | — | — | 1 | 5.60 |
| CHEMBL5579679 | — | — | 1 | 5.56 |
| CHEMBL5570059 | — | — | 1 | 5.43 |
| CHEMBL5565332 | — | — | 1 | 5.40 |
| CHEMBL5555561 | — | — | 1 | 5.36 |
| CHEMBL5573620 | — | — | 1 | 5.33 |
| CHEMBL5571882 | — | — | 1 | 5.31 |
| CHEMBL2105720 | LESINURAD | 4.0 | 1 | 5.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5590320 | — | IC50 | = | 2010.0 | nM | 5.70 |
| CHEMBL5542414 | — | IC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL5579679 | — | IC50 | = | 2750.0 | nM | 5.56 |
| CHEMBL5570059 | — | IC50 | = | 3750.0 | nM | 5.43 |
| CHEMBL5565332 | — | IC50 | = | 3960.0 | nM | 5.40 |
| CHEMBL5555561 | — | IC50 | = | 4350.0 | nM | 5.36 |
| CHEMBL5573620 | — | IC50 | = | 4730.0 | nM | 5.33 |
| CHEMBL5571882 | — | IC50 | = | 4860.0 | nM | 5.31 |
| CHEMBL2105720 | LESINURAD | IC50 | = | 5540.0 | nM | 5.26 |