Assay Detail
Binding
CHEMBL5736862
Review assay metadata, readout intent, target linkage, and publication context from the same page.
URAT1 activity assay: URAT1 (SLC22A12) activity was evaluated in a cellular uptake assay using a 96-well plate with stably transfected URAT-1/CHO cells. 3H-orotate was used as the test transport agent, which was measured in a liquid scintillation counter, using benzbromarone as a positive control, and DMSO and non-transfected CHO cells as negative controls (Solvo Biotechnology, Boston, Mass.). Generally determined over 7 concentrations (range, 0.01 to 150 μM), a semi-log plot (percent relative transport of oratate vs. time) was generated to determine the concentration at which 50% inhibition was observed (i.e., the IC50).
75
Total Activities
23
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Compounds and their use for reducing uric acid levels
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 5.14 | 5.97 |
| kon | 25 | - | - |
| k_off | 25 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5933429 | — | — | 3 | 5.97 |
| CHEMBL5819142 | — | — | 3 | 5.73 |
| CHEMBL5919922 | — | — | 3 | 5.64 |
| CHEMBL5802156 | — | — | 3 | 5.61 |
| CHEMBL5886087 | — | — | 3 | 5.31 |
| CHEMBL5765459 | — | — | 3 | 5.12 |
| CHEMBL6057356 | — | — | 3 | 4.99 |
| CHEMBL5753958 | — | — | 3 | 4.85 |
| CHEMBL5968055 | — | — | 3 | 4.73 |
| CHEMBL2105720 | LESINURAD | 4.0 | 6 | 4.73 |
| CHEMBL5795784 | — | — | 3 | 4.70 |
| CHEMBL5765233 | — | — | 3 | 4.70 |
| CHEMBL5814665 | — | — | 3 | - |
| CHEMBL6028932 | — | — | 3 | - |
| CHEMBL5803335 | — | — | 3 | - |
| CHEMBL1467 | ALLOPURINOL | 4.0 | 6 | - |
| CHEMBL5973769 | — | — | 3 | - |
| CHEMBL6059324 | — | — | 3 | - |
| CHEMBL5791300 | — | — | 3 | - |
| CHEMBL5904234 | — | — | 3 | - |
| CHEMBL5806577 | — | — | 3 | - |
| CHEMBL5970628 | — | — | 3 | - |
| CHEMBL5395750 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5933429 | — | IC50 | = | 1077.0 | nM | 5.97 |
| CHEMBL5819142 | — | IC50 | = | 1850.0 | nM | 5.73 |
| CHEMBL5919922 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5802156 | — | IC50 | = | 2430.0 | nM | 5.61 |
| CHEMBL5886087 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL5765459 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL6057356 | — | IC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL5753958 | — | IC50 | = | 14160.0 | nM | 4.85 |
| CHEMBL2105720 | LESINURAD | IC50 | = | 18610.0 | nM | 4.73 |
| CHEMBL2105720 | LESINURAD | IC50 | = | 18610.0 | nM | 4.73 |
| CHEMBL5968055 | — | IC50 | = | 18530.0 | nM | 4.73 |
| CHEMBL5765233 | — | IC50 | = | 19900.0 | nM | 4.70 |
| CHEMBL5795784 | — | IC50 | = | 19880.0 | nM | 4.70 |
| CHEMBL6028932 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL6057356 | — | kon | = | - | — | - |
| CHEMBL5919922 | — | kon | = | - | — | - |
| CHEMBL5765233 | — | kon | = | - | — | - |
| CHEMBL5803335 | — | k_off | = | - | s-1 | - |
| CHEMBL5803335 | — | kon | = | - | — | - |
| CHEMBL5803335 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5765459 | — | k_off | = | - | s-1 | - |
| CHEMBL5791300 | — | kon | = | - | — | - |
| CHEMBL5919922 | — | k_off | = | - | s-1 | - |
| CHEMBL5970628 | — | k_off | = | - | s-1 | - |
| CHEMBL5753958 | — | kon | = | - | — | - |
| CHEMBL5806577 | — | k_off | = | - | s-1 | - |
| CHEMBL5806577 | — | kon | = | - | — | - |
| CHEMBL5806577 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5802156 | — | k_off | = | - | s-1 | - |
| CHEMBL5802156 | — | kon | = | - | — | - |
| CHEMBL6057356 | — | k_off | = | - | s-1 | - |
| CHEMBL1467 | ALLOPURINOL | IC50 | > | 300000.0 | nM | - |
| CHEMBL2105720 | LESINURAD | k_off | = | - | s-1 | - |
| CHEMBL5973769 | — | k_off | = | - | s-1 | - |
| CHEMBL5765459 | — | kon | = | - | — | - |
| CHEMBL2105720 | LESINURAD | kon | = | - | — | - |
| CHEMBL5886087 | — | kon | = | - | — | - |
| CHEMBL1467 | ALLOPURINOL | k_off | = | - | s-1 | - |
| CHEMBL1467 | ALLOPURINOL | kon | = | - | — | - |
| CHEMBL5886087 | — | k_off | = | - | s-1 | - |
| CHEMBL5973769 | — | kon | = | - | — | - |
| CHEMBL6028932 | — | kon | = | - | — | - |
| CHEMBL5973769 | — | IC50 | > | 90000.0 | nM | - |
| CHEMBL5765233 | — | k_off | = | - | s-1 | - |
| CHEMBL2105720 | LESINURAD | k_off | = | - | s-1 | - |
| CHEMBL2105720 | LESINURAD | kon | = | - | — | - |
| CHEMBL1467 | ALLOPURINOL | k_off | = | - | s-1 | - |
| CHEMBL1467 | ALLOPURINOL | kon | = | - | — | - |
| CHEMBL1467 | ALLOPURINOL | IC50 | > | 300000.0 | nM | - |
| CHEMBL6028932 | — | k_off | = | - | s-1 | - |