Assay Detail
Binding
CHEMBL935620
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Inhibition of human full length carbonic anhydrase 14 by stopped flow CO2 hydrase assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.24 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL220491 | BRINZOLAMIDE | 4.0 | 1 | 7.62 |
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 7.57 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.39 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 7.37 |
| CHEMBL262628 | — | — | 1 | 7.32 |
| CHEMBL17 | DICHLORPHENAMIDE | 4.0 | 1 | 5.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL220491 | BRINZOLAMIDE | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL262628 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL17 | DICHLORPHENAMIDE | Ki | = | 1540.0 | nM | 5.81 |