Assay Detail
Binding
CHEMBL2415808
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration 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
Carbonic anhydrase inhibitors: Synthesis and inhibition of the cytosolic mammalian carbonic anhydrase isoforms I, II and VII with benzene sulfonamides incorporating 4,5,6,7-tetrachlorophthalimide moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.19 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 7.51 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 7.30 |
| CHEMBL750 | ZONISAMIDE | 4.0 | 1 | 7.25 |
| CHEMBL2414442 | — | — | 1 | 6.82 |
| CHEMBL220492 | TOPIRAMATE | 4.0 | 1 | 6.60 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 6.60 |
| CHEMBL2414443 | — | — | 1 | 6.55 |
| CHEMBL2414438 | — | — | 1 | 6.49 |
| CHEMBL2377770 | — | — | 1 | 6.48 |
| CHEMBL2414441 | — | — | 1 | 6.43 |
| CHEMBL2377796 | — | — | 1 | 6.37 |
| CHEMBL2414439 | — | — | 1 | 6.35 |
| CHEMBL26 | SULPIRIDE | 3.0 | 1 | 5.92 |
| CHEMBL220491 | BRINZOLAMIDE | 4.0 | 1 | 4.35 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 4.30 |
| CHEMBL118 | CELECOXIB | 4.0 | 1 | 4.30 |
| CHEMBL865 | VALDECOXIB | 4.0 | 1 | 4.27 |
| CHEMBL2414440 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL77517 | INDISULAM | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL750 | ZONISAMIDE | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL2414442 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL220492 | TOPIRAMATE | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL2414443 | — | Ki | = | 281.0 | nM | 6.55 |
| CHEMBL2414438 | — | Ki | = | 326.0 | nM | 6.49 |
| CHEMBL2377770 | — | Ki | = | 332.0 | nM | 6.48 |
| CHEMBL2414441 | — | Ki | = | 368.0 | nM | 6.43 |
| CHEMBL2377796 | — | Ki | = | 427.0 | nM | 6.37 |
| CHEMBL2414439 | — | Ki | = | 444.0 | nM | 6.35 |
| CHEMBL26 | SULPIRIDE | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL220491 | BRINZOLAMIDE | Ki | = | 45000.0 | nM | 4.35 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 50000.0 | nM | 4.30 |
| CHEMBL118 | CELECOXIB | Ki | = | 50000.0 | nM | 4.30 |
| CHEMBL865 | VALDECOXIB | Ki | = | 54000.0 | nM | 4.27 |
| CHEMBL2414440 | — | Ki | > | 10000.0 | nM | - |