Assay Detail
Binding
CHEMBL4015147
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Inhibition of human URAT1 expressed in HEK293T cells assessed as reduction in [14C]uric acid uptake measured after 5 mins by liquid scintillation counting method
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and evaluation of sulfonamide derivatives as potent Human Uric Acid Transporter 1 (hURAT1) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.22 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4087516 | — | — | 1 | 8.70 |
| CHEMBL4088988 | — | — | 1 | 8.00 |
| CHEMBL4100597 | — | — | 1 | 7.08 |
| CHEMBL388590 | BENZBROMARONE | 4.0 | 1 | 6.92 |
| CHEMBL4104410 | — | — | 1 | 6.90 |
| CHEMBL4103898 | — | — | 1 | 6.69 |
| CHEMBL4066146 | — | — | 1 | 6.67 |
| CHEMBL4079640 | — | — | 1 | 6.62 |
| CHEMBL4078667 | — | — | 1 | 6.58 |
| CHEMBL4074756 | — | — | 1 | 6.41 |
| CHEMBL4094280 | — | — | 1 | 6.22 |
| CHEMBL4067774 | — | — | 1 | 6.15 |
| CHEMBL4066753 | — | — | 1 | 5.96 |
| CHEMBL4085591 | — | — | 1 | 5.85 |
| CHEMBL4086514 | — | — | 1 | 5.70 |
| CHEMBL4096139 | — | — | 1 | 5.55 |
| CHEMBL4076833 | — | — | 1 | 5.44 |
| CHEMBL4095219 | — | — | 1 | 5.40 |
| CHEMBL4068847 | — | — | 1 | 5.39 |
| CHEMBL4060192 | — | — | 1 | 5.01 |
| CHEMBL4088415 | — | — | 1 | 4.92 |
| CHEMBL4064028 | — | — | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4087516 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4088988 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4100597 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL388590 | BENZBROMARONE | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4104410 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL4103898 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL4066146 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL4079640 | — | IC50 | = | 241.0 | nM | 6.62 |
| CHEMBL4078667 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL4074756 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4094280 | — | IC50 | = | 597.0 | nM | 6.22 |
| CHEMBL4067774 | — | IC50 | = | 713.0 | nM | 6.15 |
| CHEMBL4066753 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4085591 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4086514 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4096139 | — | IC50 | = | 2827.0 | nM | 5.55 |
| CHEMBL4076833 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4095219 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4068847 | — | IC50 | = | 4059.0 | nM | 5.39 |
| CHEMBL4060192 | — | IC50 | = | 9836.0 | nM | 5.01 |
| CHEMBL4088415 | — | IC50 | = | 11999.0 | nM | 4.92 |
| CHEMBL4064028 | — | IC50 | = | 20900.0 | nM | 4.68 |