Assay Detail
Binding
CHEMBL1246742
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Inhibition of human cloned catalytic domain of CA9 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 | 7.72 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1242890 | — | — | 1 | 8.28 |
| CHEMBL1242889 | — | — | 1 | 8.24 |
| CHEMBL1242891 | — | — | 1 | 8.16 |
| CHEMBL1240572 | — | — | 1 | 8.15 |
| CHEMBL1240573 | — | — | 1 | 8.11 |
| CHEMBL1242706 | — | — | 1 | 8.07 |
| CHEMBL1242705 | — | — | 1 | 8.01 |
| CHEMBL1242792 | — | — | 1 | 8.00 |
| CHEMBL1242704 | — | — | 1 | 7.93 |
| CHEMBL1242793 | — | — | 1 | 7.92 |
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 7.62 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 7.57 |
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 7.47 |
| CHEMBL17 | DICHLORPHENAMIDE | 4.0 | 1 | 7.30 |
| CHEMBL1240574 | — | — | 1 | 7.19 |
| CHEMBL1240620 | — | — | 1 | 7.17 |
| CHEMBL1241532 | — | — | 1 | 7.02 |
| CHEMBL1242794 | — | — | 1 | 6.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1242890 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL1242889 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL1242891 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL1240572 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL1240573 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL1242706 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL1242705 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL1242792 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL1242704 | — | Ki | = | 11.8 | nM | 7.93 |
| CHEMBL1242793 | — | Ki | = | 11.9 | nM | 7.92 |
| CHEMBL77517 | INDISULAM | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL17 | DICHLORPHENAMIDE | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL1240574 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL1240620 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL1241532 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL1242794 | — | Ki | = | 118.0 | nM | 6.93 |