Assay Detail
Binding
CHEMBL881708
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Inhibition of cloned human carbonic anhydrase II
10
Total Activities
10
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: stacking with Phe131 determines active site binding region of inhibitors as exemplified by the X-ray crystal structure of a membrane-impermeant antitumor sulfonamide complexed with isozyme II.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 8.10 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL309431 | — | — | 1 | 8.85 |
| CHEMBL196871 | — | — | 1 | 8.82 |
| CHEMBL51668 | — | — | 1 | 8.30 |
| CHEMBL220492 | TOPIRAMATE | 4.0 | 1 | 8.30 |
| CHEMBL122708 | EMATE | — | 1 | 8.00 |
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 7.82 |
| CHEMBL361827 | — | — | 1 | 7.72 |
| CHEMBL352535 | — | — | 1 | 7.68 |
| CHEMBL196677 | — | — | 1 | 7.40 |
| CHEMBL118 | CELECOXIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL309431 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL196871 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL51668 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL220492 | TOPIRAMATE | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL122708 | EMATE | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL77517 | INDISULAM | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL361827 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL352535 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL196677 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL118 | CELECOXIB | Ki | = | 21.0 | nM | - |