Assay Detail
Binding
CHEMBL2429045
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human membrane bound carbonic anhydrase 9 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay
21
Total Activities
21
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: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.65 | 8.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL750 | ZONISAMIDE | 4.0 | 1 | 8.29 |
| CHEMBL2424828 | — | — | 1 | 8.07 |
| CHEMBL2424829 | — | — | 1 | 8.06 |
| CHEMBL2424830 | — | — | 1 | 8.04 |
| CHEMBL2424827 | — | — | 1 | 8.03 |
| CHEMBL2424831 | — | — | 1 | 7.91 |
| CHEMBL352535 | — | — | 1 | 7.85 |
| CHEMBL2424832 | — | — | 1 | 7.80 |
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 7.62 |
| CHEMBL2424825 | — | — | 1 | 7.62 |
| CHEMBL1232755 | — | — | 1 | 7.62 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 7.57 |
| CHEMBL865 | VALDECOXIB | 4.0 | 1 | 7.57 |
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 7.47 |
| CHEMBL220491 | BRINZOLAMIDE | 4.0 | 1 | 7.43 |
| CHEMBL26 | SULPIRIDE | 3.0 | 1 | 7.34 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 7.28 |
| CHEMBL220492 | TOPIRAMATE | 4.0 | 1 | 7.24 |
| CHEMBL2424826 | — | — | 1 | 6.63 |
| CHEMBL118 | CELECOXIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL750 | ZONISAMIDE | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL2424828 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL2424829 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL2424830 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL2424827 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL2424831 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL352535 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL2424832 | — | Ki | = | 15.9 | nM | 7.80 |
| CHEMBL77517 | INDISULAM | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL2424825 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL1232755 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL865 | VALDECOXIB | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL220491 | BRINZOLAMIDE | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL26 | SULPIRIDE | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL220492 | TOPIRAMATE | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL2424826 | — | Ki | = | 234.0 | nM | 6.63 |
| CHEMBL118 | CELECOXIB | Ki | = | 16.0 | nM | - |