Assay Detail
Binding
CHEMBL856737
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Inhibition of catalytic domain of human cloned CA12 by stopped-flow CO2 hydration method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Carbonic anhydrase inhibitors: clash with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.77 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL220491 | BRINZOLAMIDE | 4.0 | 1 | 8.52 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 8.47 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 8.46 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 8.24 |
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 7.66 |
| CHEMBL17 | DICHLORPHENAMIDE | 4.0 | 1 | 7.30 |
| CHEMBL283695 | — | — | 1 | 5.73 |
| CHEMBL220492 | TOPIRAMATE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL220491 | BRINZOLAMIDE | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL17 | DICHLORPHENAMIDE | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL283695 | — | Ki | = | 1875.0 | nM | 5.73 |
| CHEMBL220492 | TOPIRAMATE | Ki | = | 3.8 | nM | - |