Assay Detail
Binding
CHEMBL4708446
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human CA2 incubated for 15 mins by stopped- flow CO2 hydrase assay method
25
Total Activities
25
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
Discovery of first-in-class multi-target adenosine A receptor antagonists-carbonic anhydrase IX and XII inhibitors. 8-Amino-6-aryl-2-phenyl-1,2,4-triazolo [4,3-a]pyrazin-3-one derivatives as new potential antitumor agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 5.97 | 8.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4761976 | — | — | 1 | 8.07 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.92 |
| CHEMBL4797036 | — | — | 1 | 7.34 |
| CHEMBL4786281 | — | — | 1 | 6.74 |
| CHEMBL4777796 | — | — | 1 | 6.61 |
| CHEMBL4753875 | — | — | 1 | 6.47 |
| CHEMBL4764597 | — | — | 1 | 6.43 |
| CHEMBL4758605 | — | — | 1 | 6.33 |
| CHEMBL4793920 | — | — | 1 | 6.28 |
| CHEMBL4741273 | — | — | 1 | 6.15 |
| CHEMBL4764804 | — | — | 1 | 6.05 |
| CHEMBL4757832 | — | — | 1 | 6.03 |
| CHEMBL4797465 | — | — | 1 | 5.17 |
| CHEMBL4781077 | — | — | 1 | 4.72 |
| CHEMBL4745014 | — | — | 1 | 4.50 |
| CHEMBL4799118 | — | — | 1 | 4.33 |
| CHEMBL4755619 | — | — | 1 | 4.20 |
| CHEMBL4068548 | — | — | 1 | 4.03 |
| CHEMBL4759740 | — | — | 1 | - |
| CHEMBL4785861 | — | — | 1 | - |
| CHEMBL4791834 | — | — | 1 | - |
| CHEMBL4764878 | — | — | 1 | - |
| CHEMBL4784043 | — | — | 1 | - |
| CHEMBL4789455 | — | — | 1 | - |
| CHEMBL4081800 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4761976 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 12.1 | nM | 7.92 |
| CHEMBL4797036 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL4786281 | — | Ki | = | 183.4 | nM | 6.74 |
| CHEMBL4777796 | — | Ki | = | 246.3 | nM | 6.61 |
| CHEMBL4753875 | — | Ki | = | 341.0 | nM | 6.47 |
| CHEMBL4764597 | — | Ki | = | 367.0 | nM | 6.43 |
| CHEMBL4758605 | — | Ki | = | 464.0 | nM | 6.33 |
| CHEMBL4793920 | — | Ki | = | 526.5 | nM | 6.28 |
| CHEMBL4741273 | — | Ki | = | 703.0 | nM | 6.15 |
| CHEMBL4764804 | — | Ki | = | 896.8 | nM | 6.05 |
| CHEMBL4757832 | — | Ki | = | 933.8 | nM | 6.03 |
| CHEMBL4797465 | — | Ki | = | 6763.0 | nM | 5.17 |
| CHEMBL4781077 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL4745014 | — | Ki | = | 31700.0 | nM | 4.50 |
| CHEMBL4799118 | — | Ki | = | 47300.0 | nM | 4.33 |
| CHEMBL4755619 | — | Ki | = | 63020.0 | nM | 4.20 |
| CHEMBL4068548 | — | Ki | = | 93000.0 | nM | 4.03 |
| CHEMBL4759740 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4785861 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4791834 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4764878 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4784043 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4789455 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4081800 | — | Ki | > | 100000.0 | nM | - |