Assay Detail
Binding
CHEMBL2429044
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human membrane bound carbonic anhydrase 12 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 | 7.92 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL220491 | BRINZOLAMIDE | 4.0 | 1 | 8.52 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 8.47 |
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 8.47 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 8.46 |
| CHEMBL26 | SULPIRIDE | 3.0 | 1 | 8.41 |
| CHEMBL1232755 | — | — | 1 | 8.30 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 8.24 |
| CHEMBL2424828 | — | — | 1 | 8.23 |
| CHEMBL2424830 | — | — | 1 | 8.21 |
| CHEMBL2424829 | — | — | 1 | 8.19 |
| CHEMBL352535 | — | — | 1 | 8.15 |
| CHEMBL2424827 | — | — | 1 | 8.12 |
| CHEMBL2424832 | — | — | 1 | 7.99 |
| CHEMBL2424831 | — | — | 1 | 7.91 |
| CHEMBL865 | VALDECOXIB | 4.0 | 1 | 7.89 |
| CHEMBL118 | CELECOXIB | 4.0 | 1 | 7.75 |
| CHEMBL2424825 | — | — | 1 | 7.72 |
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 7.66 |
| CHEMBL2424826 | — | — | 1 | 6.71 |
| CHEMBL750 | ZONISAMIDE | 4.0 | 1 | 4.96 |
| CHEMBL220492 | TOPIRAMATE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL220491 | BRINZOLAMIDE | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL77517 | INDISULAM | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL26 | SULPIRIDE | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL1232755 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL2424828 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL2424830 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL2424829 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL352535 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2424827 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL2424832 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL2424831 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL865 | VALDECOXIB | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL118 | CELECOXIB | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL2424825 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2424826 | — | Ki | = | 197.0 | nM | 6.71 |
| CHEMBL750 | ZONISAMIDE | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL220492 | TOPIRAMATE | Ki | = | 3.8 | nM | - |