Assay Detail
Binding
CHEMBL3116663
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Inhibition of human transmembrane carbonic anhydrase 12 by stopped-flow CO2 hydration assay
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
Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.38 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL220491 | BRINZOLAMIDE | 4.0 | 1 | 8.52 |
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 8.47 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 8.47 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 8.46 |
| CHEMBL26 | SULPIRIDE | 3.0 | 1 | 8.41 |
| CHEMBL1232755 | — | — | 1 | 8.30 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 8.24 |
| CHEMBL352535 | — | — | 1 | 8.15 |
| CHEMBL865 | VALDECOXIB | 4.0 | 1 | 7.89 |
| CHEMBL118 | CELECOXIB | 4.0 | 1 | 7.75 |
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 7.66 |
| CHEMBL2377773 | — | — | 1 | 7.05 |
| CHEMBL3113926 | — | — | 1 | 7.02 |
| CHEMBL2377772 | — | — | 1 | 6.92 |
| CHEMBL3113922 | — | — | 1 | 6.31 |
| CHEMBL3113927 | — | — | 1 | 6.21 |
| CHEMBL3113923 | — | — | 1 | 6.08 |
| CHEMBL3113925 | — | — | 1 | 5.43 |
| CHEMBL750 | ZONISAMIDE | 4.0 | 1 | 4.96 |
| CHEMBL220492 | TOPIRAMATE | 4.0 | 1 | - |
| CHEMBL3113924 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL220491 | BRINZOLAMIDE | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL77517 | INDISULAM | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL26 | SULPIRIDE | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL1232755 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL352535 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL865 | VALDECOXIB | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL118 | CELECOXIB | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2377773 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL3113926 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL2377772 | — | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL3113922 | — | Ki | = | 491.0 | nM | 6.31 |
| CHEMBL3113927 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL3113923 | — | Ki | = | 838.0 | nM | 6.08 |
| CHEMBL3113925 | — | Ki | = | 3746.0 | nM | 5.43 |
| CHEMBL750 | ZONISAMIDE | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL220492 | TOPIRAMATE | Ki | = | 3.8 | nM | - |
| CHEMBL3113924 | — | Ki | > | 10000.0 | nM | - |