Assay Detail
Binding
CHEMBL2429048
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human cytosolic carbonic anhydrase 1 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 | 6.15 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 7.51 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 7.30 |
| CHEMBL750 | ZONISAMIDE | 4.0 | 1 | 7.25 |
| CHEMBL2424829 | — | — | 1 | 6.84 |
| CHEMBL2424832 | — | — | 1 | 6.73 |
| CHEMBL2424828 | — | — | 1 | 6.68 |
| CHEMBL2424831 | — | — | 1 | 6.60 |
| CHEMBL220492 | TOPIRAMATE | 4.0 | 1 | 6.60 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 6.60 |
| CHEMBL2424825 | — | — | 1 | 6.47 |
| CHEMBL2424830 | — | — | 1 | 6.37 |
| CHEMBL2424827 | — | — | 1 | 6.11 |
| CHEMBL26 | SULPIRIDE | 3.0 | 1 | 5.92 |
| CHEMBL1232755 | — | — | 1 | 5.89 |
| CHEMBL352535 | — | — | 1 | 5.40 |
| CHEMBL220491 | BRINZOLAMIDE | 4.0 | 1 | 4.35 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 4.30 |
| CHEMBL118 | CELECOXIB | 4.0 | 1 | 4.30 |
| CHEMBL865 | VALDECOXIB | 4.0 | 1 | 4.27 |
| CHEMBL2424826 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL77517 | INDISULAM | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL750 | ZONISAMIDE | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL2424829 | — | Ki | = | 143.0 | nM | 6.84 |
| CHEMBL2424832 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL2424828 | — | Ki | = | 208.0 | nM | 6.68 |
| CHEMBL2424831 | — | Ki | = | 251.0 | nM | 6.60 |
| CHEMBL220492 | TOPIRAMATE | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL2424825 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL2424830 | — | Ki | = | 432.0 | nM | 6.37 |
| CHEMBL2424827 | — | Ki | = | 770.0 | nM | 6.11 |
| CHEMBL26 | SULPIRIDE | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL1232755 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL352535 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL220491 | BRINZOLAMIDE | Ki | = | 45000.0 | nM | 4.35 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 50000.0 | nM | 4.30 |
| CHEMBL118 | CELECOXIB | Ki | = | 50000.0 | nM | 4.30 |
| CHEMBL865 | VALDECOXIB | Ki | = | 54000.0 | nM | 4.27 |
| CHEMBL2424826 | — | Ki | > | 10000.0 | nM | - |