Assay Detail
Binding
CHEMBL4035751
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Inhibition of human carbonic anhydrase-2 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay
39
Total Activities
39
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
Sulfonamide inhibition profiles of the β-carbonic anhydrase from the pathogenic bacterium Francisella tularensis responsible of the febrile illness tularemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 39 | 7.38 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL224292 | — | — | 1 | 8.70 |
| CHEMBL220491 | BRINZOLAMIDE | 4.0 | 1 | 8.52 |
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 8.10 |
| CHEMBL328560 | SULTHIAME | 3.0 | 1 | 8.05 |
| CHEMBL73962 | BENZOLAMIDE | — | 1 | 8.05 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 8.05 |
| CHEMBL220492 | TOPIRAMATE | 4.0 | 1 | 8.00 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.92 |
| CHEMBL268439 | — | — | 1 | 7.92 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 7.85 |
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 7.82 |
| CHEMBL6753 | — | — | 1 | 7.72 |
| CHEMBL6633 | — | — | 1 | 7.52 |
| CHEMBL414 | CARZENIDE | 2.0 | 1 | 7.48 |
| CHEMBL750 | ZONISAMIDE | 4.0 | 1 | 7.46 |
| CHEMBL17 | DICHLORPHENAMIDE | 4.0 | 1 | 7.42 |
| CHEMBL26 | SULPIRIDE | 3.0 | 1 | 7.40 |
| CHEMBL6724 | — | — | 1 | 7.40 |
| CHEMBL865 | VALDECOXIB | 4.0 | 1 | 7.37 |
| CHEMBL6919 | — | — | 1 | 7.34 |
| CHEMBL6784 | — | — | 1 | 7.30 |
| CHEMBL6853 | — | — | 1 | 7.22 |
| CHEMBL265674 | — | — | 1 | 7.22 |
| CHEMBL418 | 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE | — | 1 | 7.20 |
| CHEMBL2324869 | — | — | 1 | 7.16 |
| CHEMBL266240 | — | — | 1 | 7.12 |
| CHEMBL2324864 | — | — | 1 | 7.10 |
| CHEMBL7092 | — | — | 1 | 6.96 |
| CHEMBL269122 | — | — | 1 | 6.90 |
| CHEMBL7146 | — | — | 1 | 6.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL224292 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL220491 | BRINZOLAMIDE | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL328560 | SULTHIAME | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL73962 | BENZOLAMIDE | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL220492 | TOPIRAMATE | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL268439 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL77517 | INDISULAM | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL6753 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL6633 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL414 | CARZENIDE | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL750 | ZONISAMIDE | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL17 | DICHLORPHENAMIDE | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL26 | SULPIRIDE | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL6724 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL865 | VALDECOXIB | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL6919 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL6784 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL6853 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL265674 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL418 | 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL2324869 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL266240 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL2324864 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL7092 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL7146 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL269122 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL266026 | — | Ki | = | 133.0 | nM | 6.88 |
| CHEMBL7087 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL419 | MAFENIDE | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL21 | SULFANILAMIDE | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL435 | HYDROCHLOROTHIAZIDE | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL6852 | — | Ki | = | 295.0 | nM | 6.53 |
| CHEMBL2324868 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL574 | P-TOLUENESULFONAMIDE | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL118 | CELECOXIB | Ki | = | 21.0 | nM | - |