Assay Detail
Binding
CHEMBL1246740
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human cloned CA1 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 | 5.83 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 7.51 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 6.51 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 6.11 |
| CHEMBL1242793 | — | — | 1 | 5.96 |
| CHEMBL1242792 | — | — | 1 | 5.96 |
| CHEMBL1242704 | — | — | 1 | 5.95 |
| CHEMBL1242705 | — | — | 1 | 5.93 |
| CHEMBL1242706 | — | — | 1 | 5.93 |
| CHEMBL17 | DICHLORPHENAMIDE | 4.0 | 1 | 5.92 |
| CHEMBL1240620 | — | — | 1 | 5.74 |
| CHEMBL1240572 | — | — | 1 | 5.46 |
| CHEMBL1240573 | — | — | 1 | 5.38 |
| CHEMBL1242891 | — | — | 1 | 5.38 |
| CHEMBL1240574 | — | — | 1 | 5.23 |
| CHEMBL1242889 | — | — | 1 | 5.21 |
| CHEMBL1242890 | — | — | 1 | 5.15 |
| CHEMBL1241532 | — | — | 1 | 4.92 |
| CHEMBL1242794 | — | — | 1 | 4.85 |
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 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL1242793 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL1242792 | — | Ki | = | 1090.0 | nM | 5.96 |
| CHEMBL1242704 | — | Ki | = | 1130.0 | nM | 5.95 |
| CHEMBL1242705 | — | Ki | = | 1170.0 | nM | 5.93 |
| CHEMBL1242706 | — | Ki | = | 1180.0 | nM | 5.93 |
| CHEMBL17 | DICHLORPHENAMIDE | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL1240620 | — | Ki | = | 1830.0 | nM | 5.74 |
| CHEMBL1240572 | — | Ki | = | 3440.0 | nM | 5.46 |
| CHEMBL1240573 | — | Ki | = | 4120.0 | nM | 5.38 |
| CHEMBL1242891 | — | Ki | = | 4160.0 | nM | 5.38 |
| CHEMBL1240574 | — | Ki | = | 5880.0 | nM | 5.23 |
| CHEMBL1242889 | — | Ki | = | 6100.0 | nM | 5.21 |
| CHEMBL1242890 | — | Ki | = | 7130.0 | nM | 5.15 |
| CHEMBL1241532 | — | Ki | = | 12100.0 | nM | 4.92 |
| CHEMBL1242794 | — | Ki | = | 14200.0 | nM | 4.85 |