Assay Detail
Binding
CHEMBL4331760
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Inhibition of recombinant full length human carbonic anhydrase-1 assessed as reduction in CO2 hydration after 15 mins by phenol red dye based stopped flow assay
19
Total Activities
19
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 structural properties of potent human carbonic anhydrase inhibitors bearing a 4-(cycloalkylamino-1-carbonyl)benzenesulfonamide moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.73 | 9.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4453778 | — | — | 1 | 9.16 |
| CHEMBL4437968 | — | — | 1 | 8.77 |
| CHEMBL4462670 | — | — | 1 | 8.36 |
| CHEMBL4554983 | — | — | 1 | 8.20 |
| CHEMBL4465705 | — | — | 1 | 8.19 |
| CHEMBL4442611 | — | — | 1 | 8.18 |
| CHEMBL4450272 | — | — | 1 | 8.17 |
| CHEMBL4532154 | — | — | 1 | 8.11 |
| CHEMBL4590736 | — | — | 1 | 8.11 |
| CHEMBL4553372 | — | — | 1 | 8.04 |
| CHEMBL4547604 | — | — | 1 | 8.03 |
| CHEMBL4441940 | — | — | 1 | 7.30 |
| CHEMBL4593188 | — | — | 1 | 7.12 |
| CHEMBL3613783 | — | — | 1 | 7.11 |
| CHEMBL4533094 | — | — | 1 | 7.07 |
| CHEMBL4469954 | — | — | 1 | 7.04 |
| CHEMBL4590763 | — | — | 1 | 6.73 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 6.60 |
| CHEMBL220492 | TOPIRAMATE | 4.0 | 1 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4453778 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL4437968 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL4462670 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL4554983 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL4465705 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL4442611 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL4450272 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL4532154 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL4590736 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL4553372 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL4547604 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL4441940 | — | Ki | = | 50.1 | nM | 7.30 |
| CHEMBL4593188 | — | Ki | = | 75.5 | nM | 7.12 |
| CHEMBL3613783 | — | Ki | = | 78.6 | nM | 7.11 |
| CHEMBL4533094 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL4469954 | — | Ki | = | 91.1 | nM | 7.04 |
| CHEMBL4590763 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL220492 | TOPIRAMATE | Ki | = | 250.0 | nM | 6.60 |