Assay Detail
Binding
CHEMBL4021392
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Inhibition of recombinant human carbonic anhydrase-9 assessed as reduction in CO2 hydration preincubated for 10 mins measured for 5 to 10 secs by stopped flow assay
15
Total Activities
15
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
N-Substituted and ring opened saccharin derivatives selectively inhibit transmembrane, tumor-associated carbonic anhydrases IX and XII.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.72 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL4090838 | — | — | 1 | 7.12 |
| CHEMBL443760 | — | — | 1 | 7.05 |
| CHEMBL310671 | SACCHARIN | 3.0 | 1 | 6.99 |
| CHEMBL421511 | — | — | 1 | 6.99 |
| CHEMBL79624 | — | — | 1 | 6.79 |
| CHEMBL4072571 | — | — | 1 | 6.68 |
| CHEMBL4091686 | — | — | 1 | 6.63 |
| CHEMBL4091692 | — | — | 1 | 6.60 |
| CHEMBL4068824 | — | — | 1 | 6.56 |
| CHEMBL4089916 | — | — | 1 | 6.47 |
| CHEMBL4070820 | — | — | 1 | 6.41 |
| CHEMBL4099433 | — | — | 1 | 6.36 |
| CHEMBL4081415 | — | — | 1 | 6.32 |
| CHEMBL4062903 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL4090838 | — | Ki | = | 76.1 | nM | 7.12 |
| CHEMBL443760 | — | Ki | = | 89.2 | nM | 7.05 |
| CHEMBL310671 | SACCHARIN | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL421511 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL79624 | — | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL4072571 | — | Ki | = | 209.0 | nM | 6.68 |
| CHEMBL4091686 | — | Ki | = | 236.0 | nM | 6.63 |
| CHEMBL4091692 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL4068824 | — | Ki | = | 277.0 | nM | 6.56 |
| CHEMBL4089916 | — | Ki | = | 342.0 | nM | 6.47 |
| CHEMBL4070820 | — | Ki | = | 392.0 | nM | 6.41 |
| CHEMBL4099433 | — | Ki | = | 436.0 | nM | 6.36 |
| CHEMBL4081415 | — | Ki | = | 481.0 | nM | 6.32 |
| CHEMBL4062903 | — | Ki | = | 563.0 | nM | 6.25 |