Assay Detail
Binding
CHEMBL935609
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human full length carbonic anhydrase 1 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 | 6.39 | 8.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL262628 | — | — | 1 | 8.12 |
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 7.30 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 6.60 |
| CHEMBL17 | DICHLORPHENAMIDE | 4.0 | 1 | 6.43 |
| CHEMBL220491 | BRINZOLAMIDE | 4.0 | 1 | 4.35 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 4.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL262628 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL17 | DICHLORPHENAMIDE | Ki | = | 374.0 | nM | 6.43 |
| CHEMBL220491 | BRINZOLAMIDE | Ki | = | 45000.0 | nM | 4.35 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 50000.0 | nM | 4.30 |