Assay Detail
Binding
CHEMBL5732037
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Known Inhibitors of Carbonic Anhydrase: Compounds which are CAIs are well known in the art, see for example, Pastorekova et al, Journal of Enzyme Inhibition and Medicinal Chemistry, 19(3), 199-229, 2004. Methods for determining the carbonic anhydrase inhibitory activity of a compound, i.e. whether a compound can be classified as a CAI, are known in the art and may usefully identify further compounds which may be suitable for use in the present invention. Exemplary methods and levels of activity required for consideration as CAIs are described in US 20020022245 and the references cited therein, the contents of which are incorporated herein by reference, in particular Supuran et al, European Journal of Medicinal Chemistry, 1998, 33, 577-594 and Scozzafava et al, Journal of Medicinal Chemistry, 1999, 42 25, 3690-3700).
33
Total Activities
11
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Insulin sensitisers and methods of treatment
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.34 | 8.10 |
| kon | 11 | - | - |
| k_off | 11 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 3 | 8.10 |
| CHEMBL269001 | — | — | 3 | 8.05 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 3 | 7.92 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 3 | 7.85 |
| CHEMBL750 | ZONISAMIDE | 4.0 | 3 | 7.46 |
| CHEMBL17 | DICHLORPHENAMIDE | 4.0 | 3 | 7.42 |
| CHEMBL26 | SULPIRIDE | 3.0 | 3 | 7.40 |
| CHEMBL35 | FUROSEMIDE | 4.0 | 3 | 7.10 |
| CHEMBL1055 | CHLORTHALIDONE | 4.0 | 3 | 6.58 |
| CHEMBL6705 | — | — | 3 | 6.53 |
| CHEMBL842 | CHLOROTHIAZIDE | 4.0 | 3 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18 | ETHOXZOLAMIDE | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL269001 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL20 | ACETAZOLAMIDE | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL19 | METHAZOLAMIDE | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL750 | ZONISAMIDE | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL17 | DICHLORPHENAMIDE | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL26 | SULPIRIDE | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL35 | FUROSEMIDE | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1055 | CHLORTHALIDONE | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL6705 | — | IC50 | = | 295.0 | nM | 6.53 |
| CHEMBL842 | CHLOROTHIAZIDE | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL35 | FUROSEMIDE | k_off | = | - | s-1 | - |
| CHEMBL6705 | — | k_off | = | - | s-1 | - |
| CHEMBL6705 | — | kon | = | - | — | - |
| CHEMBL19 | METHAZOLAMIDE | k_off | = | - | s-1 | - |
| CHEMBL19 | METHAZOLAMIDE | kon | = | - | — | - |
| CHEMBL26 | SULPIRIDE | k_off | = | - | s-1 | - |
| CHEMBL26 | SULPIRIDE | kon | = | - | — | - |
| CHEMBL750 | ZONISAMIDE | k_off | = | - | s-1 | - |
| CHEMBL750 | ZONISAMIDE | kon | = | - | — | - |
| CHEMBL17 | DICHLORPHENAMIDE | k_off | = | - | s-1 | - |
| CHEMBL17 | DICHLORPHENAMIDE | kon | = | - | — | - |
| CHEMBL842 | CHLOROTHIAZIDE | kon | = | - | — | - |
| CHEMBL842 | CHLOROTHIAZIDE | k_off | = | - | s-1 | - |
| CHEMBL20 | ACETAZOLAMIDE | k_off | = | - | s-1 | - |
| CHEMBL20 | ACETAZOLAMIDE | kon | = | - | — | - |
| CHEMBL269001 | — | k_off | = | - | s-1 | - |
| CHEMBL269001 | — | kon | = | - | — | - |
| CHEMBL35 | FUROSEMIDE | kon | = | - | — | - |
| CHEMBL18 | ETHOXZOLAMIDE | kon | = | - | — | - |
| CHEMBL1055 | CHLORTHALIDONE | k_off | = | - | s-1 | - |
| CHEMBL1055 | CHLORTHALIDONE | kon | = | - | — | - |
| CHEMBL18 | ETHOXZOLAMIDE | k_off | = | - | s-1 | - |