Assay Detail
Binding
CHEMBL1053952
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human carbonic anhydrase 2 by stopped flow CO2 hydration assay
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 7.94 | 8.39 |
| IC50 | 2 | 6.86 | 7.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 8.39 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.92 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.52 |
| CHEMBL560175 | — | — | 1 | 7.23 |
| CHEMBL549757 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL255863 | NILOTINIB | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL941 | IMATINIB | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL560175 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL549757 | — | IC50 | = | 331.0 | nM | 6.48 |