Assay Detail
Binding
CHEMBL1046494
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant CA9 catalytic domain expressed in Sf9 cells by stopped flow CO2 hydration assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Carbonic anhydrase inhibitors. Diazenylbenzenesulfonamides are potent and selective inhibitors of the tumor-associated isozymes IX and XII over the cytosolic isoforms I and II.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.61 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL569804 | — | — | 1 | 8.46 |
| CHEMBL571371 | — | — | 1 | 8.31 |
| CHEMBL274704 | — | — | 1 | 8.27 |
| CHEMBL570615 | — | — | 1 | 8.23 |
| CHEMBL16909 | — | — | 1 | 8.22 |
| CHEMBL571385 | — | — | 1 | 8.21 |
| CHEMBL379206 | — | — | 1 | 8.19 |
| CHEMBL576908 | — | — | 1 | 8.19 |
| CHEMBL277836 | — | — | 1 | 8.18 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 7.28 |
| CHEMBL570257 | — | — | 1 | 7.24 |
| CHEMBL569350 | — | — | 1 | 7.20 |
| CHEMBL569351 | SODIUM PHENYLAMINOMETHANESULFONATE | — | 1 | 5.29 |
| CHEMBL571598 | SODIUM(METHYL(PHENYL)AMINO)METHANESULFONATE | — | 1 | 5.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL569804 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL571371 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL274704 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL570615 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL16909 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL571385 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL379206 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL576908 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL277836 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL570257 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL569350 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL569351 | SODIUM PHENYLAMINOMETHANESULFONATE | Ki | = | 5100.0 | nM | 5.29 |
| CHEMBL571598 | SODIUM(METHYL(PHENYL)AMINO)METHANESULFONATE | Ki | = | 5850.0 | nM | 5.23 |