Assay Detail
Binding
CHEMBL2183728
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant full length CA2 pre-incubated for 15 mins by stopped-flow CO2 hydration method
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
Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.31 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2179308 | — | — | 1 | 7.80 |
| CHEMBL2179307 | — | — | 1 | 7.54 |
| CHEMBL865 | VALDECOXIB | 4.0 | 1 | 7.37 |
| CHEMBL2179304 | — | — | 1 | 7.31 |
| CHEMBL2179305 | — | — | 1 | 7.14 |
| CHEMBL2179306 | — | — | 1 | 6.68 |
| CHEMBL118 | CELECOXIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2179308 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2179307 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL865 | VALDECOXIB | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL2179304 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL2179305 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL2179306 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL118 | CELECOXIB | Ki | = | 21.0 | nM | - |