Assay Detail
Binding
CHEMBL993108
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Inhibition of human recombinant CA1 by stopped-flow CO2 hydrase assay
37
Total Activities
37
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: inhibition of the beta-class enzyme from the yeast Saccharomyces cerevisiae with sulfonamides and sulfamates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 37 | 5.67 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL268439 | — | — | 1 | 8.22 |
| CHEMBL73962 | BENZOLAMIDE | — | 1 | 7.82 |
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 7.51 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 7.30 |
| CHEMBL6919 | — | — | 1 | 7.26 |
| CHEMBL750 | ZONISAMIDE | 4.0 | 1 | 7.25 |
| CHEMBL6633 | — | — | 1 | 6.96 |
| CHEMBL266026 | — | — | 1 | 6.79 |
| CHEMBL7146 | — | — | 1 | 6.73 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 6.60 |
| CHEMBL220492 | TOPIRAMATE | 4.0 | 1 | 6.60 |
| CHEMBL328560 | SULTHIAME | 3.0 | 1 | 6.43 |
| CHEMBL360356 | — | — | 1 | 6.16 |
| CHEMBL17 | DICHLORPHENAMIDE | 4.0 | 1 | 5.92 |
| CHEMBL418 | 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE | — | 1 | 5.24 |
| CHEMBL268177 | — | — | 1 | 5.22 |
| CHEMBL6724 | — | — | 1 | 5.19 |
| CHEMBL451332 | — | — | 1 | 5.17 |
| CHEMBL266240 | — | — | 1 | 5.08 |
| CHEMBL6853 | — | — | 1 | 5.08 |
| CHEMBL265674 | — | — | 1 | 5.07 |
| CHEMBL6753 | — | — | 1 | 5.03 |
| CHEMBL7092 | — | — | 1 | 5.01 |
| CHEMBL26 | SULPIRIDE | 3.0 | 1 | 4.92 |
| CHEMBL310671 | SACCHARIN | 3.0 | 1 | 4.73 |
| CHEMBL6784 | — | — | 1 | 4.68 |
| CHEMBL7087 | — | — | 1 | 4.68 |
| CHEMBL414 | CARZENIDE | 2.0 | 1 | 4.64 |
| CHEMBL419 | MAFENIDE | 4.0 | 1 | 4.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL268439 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL73962 | BENZOLAMIDE | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL77517 | INDISULAM | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL6919 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL750 | ZONISAMIDE | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL6633 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL266026 | — | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL7146 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL220492 | TOPIRAMATE | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL328560 | SULTHIAME | Ki | = | 374.0 | nM | 6.43 |
| CHEMBL360356 | — | Ki | = | 690.0 | nM | 6.16 |
| CHEMBL17 | DICHLORPHENAMIDE | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL418 | 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE | Ki | = | 5800.0 | nM | 5.24 |
| CHEMBL268177 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL6724 | — | Ki | = | 6500.0 | nM | 5.19 |
| CHEMBL451332 | — | Ki | = | 6690.0 | nM | 5.17 |
| CHEMBL6853 | — | Ki | = | 8300.0 | nM | 5.08 |
| CHEMBL266240 | — | Ki | = | 8400.0 | nM | 5.08 |
| CHEMBL265674 | — | Ki | = | 8600.0 | nM | 5.07 |
| CHEMBL6753 | — | Ki | = | 9300.0 | nM | 5.03 |
| CHEMBL7092 | — | Ki | = | 9800.0 | nM | 5.01 |
| CHEMBL26 | SULPIRIDE | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL310671 | SACCHARIN | Ki | = | 18540.0 | nM | 4.73 |
| CHEMBL6784 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL7087 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL414 | CARZENIDE | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL419 | MAFENIDE | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL21 | SULFANILAMIDE | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL220491 | BRINZOLAMIDE | Ki | = | 45000.0 | nM | 4.35 |
| CHEMBL6705 | — | Ki | = | 45400.0 | nM | 4.34 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 50000.0 | nM | 4.30 |
| CHEMBL118 | CELECOXIB | Ki | = | 50000.0 | nM | 4.30 |
| CHEMBL865 | VALDECOXIB | Ki | = | 54000.0 | nM | 4.27 |
| CHEMBL574 | P-TOLUENESULFONAMIDE | Ki | = | 78500.0 | nM | 4.11 |