Assay Detail
Binding
CHEMBL4194337
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Inhibition of recombinant human carbonic anhydrase 9 catalytic domain preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay
11
Total Activities
11
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
Exploring Heteroaryl-pyrazole Carboxylic Acids as Human Carbonic Anhydrase XII Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 5.93 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 7.57 |
| CHEMBL17 | DICHLORPHENAMIDE | 4.0 | 1 | 7.30 |
| CHEMBL4208348 | — | — | 1 | 6.33 |
| CHEMBL4203483 | — | — | 1 | 5.54 |
| CHEMBL4212188 | — | — | 1 | 5.52 |
| CHEMBL4215693 | — | — | 1 | 5.35 |
| CHEMBL4212738 | — | — | 1 | 5.13 |
| CHEMBL2070207 | — | — | 1 | 5.11 |
| CHEMBL4207837 | — | — | 1 | 5.10 |
| CHEMBL4204007 | — | — | 1 | 4.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL17 | DICHLORPHENAMIDE | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL4208348 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL4203483 | — | Ki | = | 2910.0 | nM | 5.54 |
| CHEMBL4212188 | — | Ki | = | 3020.0 | nM | 5.52 |
| CHEMBL4215693 | — | Ki | = | 4510.0 | nM | 5.35 |
| CHEMBL4212738 | — | Ki | = | 7360.0 | nM | 5.13 |
| CHEMBL2070207 | — | Ki | = | 7790.0 | nM | 5.11 |
| CHEMBL4207837 | — | Ki | = | 7900.0 | nM | 5.10 |
| CHEMBL4204007 | — | Ki | = | 18900.0 | nM | 4.72 |