Assay Detail
Binding
CHEMBL1815531
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Inhibition of human recombinant cytosolic carbonic anhydrase 1 preincubated for 15 mins by CO2 hydration method
27
Total Activities
27
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
Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 6.32 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL78755 | — | — | 1 | 8.15 |
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL189526 | — | — | 1 | 7.48 |
| CHEMBL190024 | — | — | 1 | 7.46 |
| CHEMBL190733 | — | — | 1 | 7.41 |
| CHEMBL187274 | — | — | 1 | 7.12 |
| CHEMBL1813210 | — | — | 1 | 6.96 |
| CHEMBL366069 | — | — | 1 | 6.92 |
| CHEMBL187901 | — | — | 1 | 6.87 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 6.60 |
| CHEMBL1813207 | — | — | 1 | 6.30 |
| CHEMBL1813213 | — | — | 1 | 6.22 |
| CHEMBL1813208 | — | — | 1 | 6.17 |
| CHEMBL1738787 | — | — | 1 | 5.96 |
| CHEMBL17 | DICHLORPHENAMIDE | 4.0 | 1 | 5.92 |
| CHEMBL1813211 | — | — | 1 | 5.91 |
| CHEMBL1813209 | — | — | 1 | 5.88 |
| CHEMBL1813217 | — | — | 1 | 5.81 |
| CHEMBL1813214 | — | — | 1 | 5.78 |
| CHEMBL1813218 | — | — | 1 | 5.69 |
| CHEMBL1813215 | — | — | 1 | 5.63 |
| CHEMBL1813216 | — | — | 1 | 5.52 |
| CHEMBL191045 | — | — | 1 | 5.52 |
| CHEMBL1738792 | — | — | 1 | 5.51 |
| CHEMBL1813212 | — | — | 1 | 5.46 |
| CHEMBL1813219 | — | — | 1 | 5.43 |
| CHEMBL1813206 | — | — | 1 | 5.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL78755 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL189526 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL190024 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL190733 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL187274 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL1813210 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL366069 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL187901 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL1813207 | — | Ki | = | 502.0 | nM | 6.30 |
| CHEMBL1813213 | — | Ki | = | 607.0 | nM | 6.22 |
| CHEMBL1813208 | — | Ki | = | 673.0 | nM | 6.17 |
| CHEMBL1738787 | — | Ki | = | 1098.0 | nM | 5.96 |
| CHEMBL17 | DICHLORPHENAMIDE | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL1813211 | — | Ki | = | 1245.0 | nM | 5.91 |
| CHEMBL1813209 | — | Ki | = | 1324.0 | nM | 5.88 |
| CHEMBL1813217 | — | Ki | = | 1549.0 | nM | 5.81 |
| CHEMBL1813214 | — | Ki | = | 1659.0 | nM | 5.78 |
| CHEMBL1813218 | — | Ki | = | 2040.0 | nM | 5.69 |
| CHEMBL1813215 | — | Ki | = | 2360.0 | nM | 5.63 |
| CHEMBL1813216 | — | Ki | = | 3021.0 | nM | 5.52 |
| CHEMBL191045 | — | Ki | = | 3032.0 | nM | 5.52 |
| CHEMBL1738792 | — | Ki | = | 3075.0 | nM | 5.51 |
| CHEMBL1813212 | — | Ki | = | 3472.0 | nM | 5.46 |
| CHEMBL1813219 | — | Ki | = | 3704.0 | nM | 5.43 |
| CHEMBL1813206 | — | Ki | = | 4550.0 | nM | 5.34 |