Assay Detail
Binding
CHEMBL2329435
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Inhibition of human recombinant transmembrane CA12 catalytic domain after 6 hrs by stopped-flow CO2 hydration method
21
Total Activities
21
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
Sulfocoumarins (1,2-benzoxathiine-2,2-dioxides): a class of potent and isoform-selective inhibitors of tumor-associated carbonic anhydrases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.04 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 8.30 |
| CHEMBL2326518 | — | — | 1 | 8.15 |
| CHEMBL2326516 | — | — | 1 | 8.05 |
| CHEMBL2326514 | — | — | 1 | 7.92 |
| CHEMBL2326521 | — | — | 1 | 7.89 |
| CHEMBL2326515 | — | — | 1 | 7.89 |
| CHEMBL2326519 | — | — | 1 | 7.85 |
| CHEMBL2326517 | — | — | 1 | 7.80 |
| CHEMBL2326522 | — | — | 1 | 7.68 |
| CHEMBL2326511 | — | — | 1 | 7.64 |
| CHEMBL2326513 | — | — | 1 | 7.50 |
| CHEMBL2326520 | — | — | 1 | 7.41 |
| CHEMBL2326508 | — | — | 1 | 6.66 |
| CHEMBL2326506 | — | — | 1 | 6.63 |
| CHEMBL2326507 | — | — | 1 | 6.59 |
| CHEMBL2326509 | — | — | 1 | 6.14 |
| CHEMBL2326512 | — | — | 1 | 5.53 |
| CHEMBL2321923 | — | — | 1 | 5.50 |
| CHEMBL2326510 | — | — | 1 | 5.35 |
| CHEMBL572366 | — | — | 1 | 4.31 |
| CHEMBL6466 | COUMARIN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2326518 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2326516 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL2326514 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2326521 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL2326515 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL2326519 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL2326517 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2326522 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL2326511 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL2326513 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL2326520 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL2326508 | — | Ki | = | 219.0 | nM | 6.66 |
| CHEMBL2326506 | — | Ki | = | 234.0 | nM | 6.63 |
| CHEMBL2326507 | — | Ki | = | 254.0 | nM | 6.59 |
| CHEMBL2326509 | — | Ki | = | 717.0 | nM | 6.14 |
| CHEMBL2326512 | — | Ki | = | 2930.0 | nM | 5.53 |
| CHEMBL2321923 | — | Ki | = | 3160.0 | nM | 5.50 |
| CHEMBL2326510 | — | Ki | = | 4510.0 | nM | 5.35 |
| CHEMBL572366 | — | Ki | = | 48600.0 | nM | 4.31 |
| CHEMBL6466 | COUMARIN | Ki | > | 100000.0 | nM | - |