Assay Detail
Binding
CHEMBL856733
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human cloned CA5A 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 |
Target
Carbonic anhydrase 5A, mitochondrial (CHEMBL4789) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 7.20 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL283695 | — | — | 1 | 7.50 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 7.38 |
| CHEMBL220491 | BRINZOLAMIDE | 4.0 | 1 | 7.30 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.20 |
| CHEMBL220492 | TOPIRAMATE | 4.0 | 1 | 7.20 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 7.19 |
| CHEMBL17 | DICHLORPHENAMIDE | 4.0 | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL283695 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL220491 | BRINZOLAMIDE | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL220492 | TOPIRAMATE | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL17 | DICHLORPHENAMIDE | Ki | = | 630.0 | nM | 6.20 |