Assay Detail
Binding
CHEMBL1048396
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Inhibition of human recombinant CA13 by stopped flow CO2 hydrase assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
The coumarin-binding site in carbonic anhydrase accommodates structurally diverse inhibitors: the antiepileptic lacosamide as an example and lead molecule for novel classes of carbonic anhydrase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 6.67 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.77 |
| CHEMBL21 | SULFANILAMIDE | 4.0 | 1 | 7.50 |
| CHEMBL220492 | TOPIRAMATE | 4.0 | 1 | 7.33 |
| CHEMBL750 | ZONISAMIDE | 4.0 | 1 | 6.37 |
| CHEMBL58323 | LACOSAMIDE | 4.0 | 1 | 5.92 |
| CHEMBL572366 | — | — | 1 | 5.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL21 | SULFANILAMIDE | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL220492 | TOPIRAMATE | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL750 | ZONISAMIDE | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL58323 | LACOSAMIDE | Ki | = | 1210.0 | nM | 5.92 |
| CHEMBL572366 | — | Ki | = | 7860.0 | nM | 5.11 |