Assay Detail
Binding
CHEMBL912682
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Inhibition of human cloned CA12 catalytic domain by CO2 hydration assay
25
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Carbonic anhydrase inhibitors. Inhibition of the cytosolic human isozymes I and II, and the transmembrane, tumor-associated isozymes IX and XII with substituted aromatic sulfonamides activatable in hypoxic tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 6.81 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 8.47 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 8.47 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 8.24 |
| CHEMBL386517 | — | — | 1 | 7.70 |
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 7.66 |
| CHEMBL215291 | — | — | 1 | 7.45 |
| CHEMBL17 | DICHLORPHENAMIDE | 4.0 | 1 | 7.30 |
| CHEMBL215990 | — | — | 1 | 7.28 |
| CHEMBL215917 | — | — | 1 | 6.97 |
| CHEMBL215916 | — | — | 2 | 6.93 |
| CHEMBL214993 | — | — | 1 | 6.72 |
| CHEMBL385451 | — | — | 1 | 6.00 |
| CHEMBL380158 | — | — | 1 | 5.96 |
| CHEMBL212811 | — | — | 1 | 5.87 |
| CHEMBL387480 | — | — | 1 | 5.86 |
| CHEMBL215776 | — | — | 1 | 5.71 |
| CHEMBL215355 | — | — | 1 | 5.62 |
| CHEMBL215276 | — | — | 1 | 5.62 |
| CHEMBL385073 | — | — | 1 | 5.52 |
| CHEMBL385195 | — | — | 1 | - |
| CHEMBL215454 | — | — | 1 | - |
| CHEMBL215548 | — | — | 1 | - |
| CHEMBL384791 | — | — | 1 | - |
| CHEMBL217638 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL77517 | INDISULAM | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL386517 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL215291 | — | Ki | = | 35.6 | nM | 7.45 |
| CHEMBL17 | DICHLORPHENAMIDE | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL215990 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL215917 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL215916 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL215916 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL214993 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL385451 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL380158 | — | Ki | = | 1103.0 | nM | 5.96 |
| CHEMBL212811 | — | Ki | = | 1348.0 | nM | 5.87 |
| CHEMBL387480 | — | Ki | = | 1390.0 | nM | 5.86 |
| CHEMBL215776 | — | Ki | = | 1970.0 | nM | 5.71 |
| CHEMBL215276 | — | Ki | = | 2417.0 | nM | 5.62 |
| CHEMBL215355 | — | Ki | = | 2404.0 | nM | 5.62 |
| CHEMBL385073 | — | Ki | = | 3045.0 | nM | 5.52 |
| CHEMBL385195 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL215454 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL215548 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL384791 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL217638 | — | Ki | > | 10000.0 | nM | - |