Assay Detail
Binding
CHEMBL1246741
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human cloned CA2 after 15 mins by stopped-flow CO2 hydration assay
19
Total Activities
19
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. Regioselective synthesis of novel 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamides and their inhibition of the human cytosolic isozymes I and II and transmembrane cancer-associated isozymes IX and XII.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.23 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 8.10 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.92 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 7.85 |
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 7.82 |
| CHEMBL17 | DICHLORPHENAMIDE | 4.0 | 1 | 7.42 |
| CHEMBL1242890 | — | — | 1 | 7.30 |
| CHEMBL1242891 | — | — | 1 | 7.25 |
| CHEMBL1240572 | — | — | 1 | 7.11 |
| CHEMBL1240573 | — | — | 1 | 7.10 |
| CHEMBL1240620 | — | — | 1 | 7.02 |
| CHEMBL1242889 | — | — | 1 | 7.01 |
| CHEMBL1242794 | — | — | 1 | 6.99 |
| CHEMBL1241532 | — | — | 1 | 6.99 |
| CHEMBL1242793 | — | — | 1 | 6.98 |
| CHEMBL1242705 | — | — | 1 | 6.97 |
| CHEMBL1242792 | — | — | 1 | 6.97 |
| CHEMBL1242704 | — | — | 1 | 6.95 |
| CHEMBL1242706 | — | — | 1 | 6.94 |
| CHEMBL1240574 | — | — | 1 | 6.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL77517 | INDISULAM | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL17 | DICHLORPHENAMIDE | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL1242890 | — | Ki | = | 50.5 | nM | 7.30 |
| CHEMBL1242891 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL1240572 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL1240573 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL1240620 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL1242889 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL1242794 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL1241532 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL1242793 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL1242705 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL1242792 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL1242704 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL1242706 | — | Ki | = | 114.0 | nM | 6.94 |
| CHEMBL1240574 | — | Ki | = | 172.0 | nM | 6.76 |