Assay Detail
Binding
CHEMBL4001627
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Inhibition of Burkholderia pseudomallei Gamma-carbonic anhydrase assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Burkholderia pseudomallei |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Sulfonamide inhibition profile of the γ-carbonic anhydrase identified in the genome of the pathogenic bacterium Burkholderia pseudomallei the etiological agent responsible of melioidosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 40 | 5.56 | 6.83 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 6.83 |
| CHEMBL6852 | — | — | 1 | 6.24 |
| CHEMBL73962 | BENZOLAMIDE | — | 1 | 6.18 |
| CHEMBL220491 | BRINZOLAMIDE | 4.0 | 1 | 5.90 |
| CHEMBL2324864 | — | — | 1 | 5.88 |
| CHEMBL414 | CARZENIDE | 2.0 | 1 | 5.82 |
| CHEMBL310671 | SACCHARIN | 3.0 | 1 | 5.81 |
| CHEMBL2324868 | — | — | 1 | 5.81 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 5.80 |
| CHEMBL4097591 | — | — | 1 | 5.77 |
| CHEMBL21 | SULFANILAMIDE | 4.0 | 1 | 5.76 |
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 5.75 |
| CHEMBL268439 | — | — | 1 | 5.74 |
| CHEMBL23684 | — | — | 1 | 5.74 |
| CHEMBL6753 | — | — | 1 | 5.74 |
| CHEMBL6784 | — | — | 1 | 5.74 |
| CHEMBL6633 | — | — | 1 | 5.74 |
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 5.73 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 5.65 |
| CHEMBL220492 | TOPIRAMATE | 4.0 | 1 | 5.52 |
| CHEMBL26 | SULPIRIDE | 3.0 | 1 | 5.25 |
| CHEMBL328560 | SULTHIAME | 3.0 | 1 | 5.05 |
| CHEMBL224292 | — | — | 1 | 5.01 |
| CHEMBL6919 | — | — | 1 | 4.97 |
| CHEMBL7092 | — | — | 1 | 4.90 |
| CHEMBL418 | 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE | — | 1 | 4.85 |
| CHEMBL265674 | — | — | 1 | 4.74 |
| CHEMBL266240 | — | — | 1 | 4.63 |
| CHEMBL4070416 | — | — | 1 | 4.61 |
| CHEMBL435 | HYDROCHLOROTHIAZIDE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL6852 | — | Ki | = | 574.0 | nM | 6.24 |
| CHEMBL73962 | BENZOLAMIDE | Ki | = | 653.0 | nM | 6.18 |
| CHEMBL220491 | BRINZOLAMIDE | Ki | = | 1270.0 | nM | 5.90 |
| CHEMBL2324864 | — | Ki | = | 1335.0 | nM | 5.88 |
| CHEMBL414 | CARZENIDE | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL310671 | SACCHARIN | Ki | = | 1550.0 | nM | 5.81 |
| CHEMBL2324868 | — | Ki | = | 1550.0 | nM | 5.81 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 1595.0 | nM | 5.80 |
| CHEMBL4097591 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL21 | SULFANILAMIDE | Ki | = | 1720.0 | nM | 5.76 |
| CHEMBL77517 | INDISULAM | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL6633 | — | Ki | = | 1838.0 | nM | 5.74 |
| CHEMBL6784 | — | Ki | = | 1825.0 | nM | 5.74 |
| CHEMBL6753 | — | Ki | = | 1810.0 | nM | 5.74 |
| CHEMBL268439 | — | Ki | = | 1810.0 | nM | 5.74 |
| CHEMBL23684 | — | Ki | = | 1805.0 | nM | 5.74 |
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 1865.0 | nM | 5.73 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 2260.0 | nM | 5.65 |
| CHEMBL220492 | TOPIRAMATE | Ki | = | 3010.0 | nM | 5.52 |
| CHEMBL26 | SULPIRIDE | Ki | = | 5600.0 | nM | 5.25 |
| CHEMBL328560 | SULTHIAME | Ki | = | 8900.0 | nM | 5.05 |
| CHEMBL224292 | — | Ki | = | 9650.0 | nM | 5.01 |
| CHEMBL6919 | — | Ki | = | 10800.0 | nM | 4.97 |
| CHEMBL7092 | — | Ki | = | 12500.0 | nM | 4.90 |
| CHEMBL418 | 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL265674 | — | Ki | = | 18400.0 | nM | 4.74 |
| CHEMBL266240 | — | Ki | = | 23500.0 | nM | 4.63 |
| CHEMBL4070416 | — | Ki | = | 24500.0 | nM | 4.61 |
| CHEMBL118 | CELECOXIB | Ki | > | 50000.0 | nM | - |
| CHEMBL865 | VALDECOXIB | Ki | > | 50000.0 | nM | - |
| CHEMBL750 | ZONISAMIDE | Ki | > | 50000.0 | nM | - |
| CHEMBL574 | P-TOLUENESULFONAMIDE | Ki | > | 50000.0 | nM | - |
| CHEMBL419 | MAFENIDE | Ki | > | 50000.0 | nM | - |
| CHEMBL7087 | — | Ki | > | 50000.0 | nM | - |
| CHEMBL6853 | — | Ki | > | 50000.0 | nM | - |
| CHEMBL6724 | — | Ki | > | 50000.0 | nM | - |
| CHEMBL2324869 | — | Ki | > | 50000.0 | nM | - |
| CHEMBL17 | DICHLORPHENAMIDE | Ki | > | 50000.0 | nM | - |
| CHEMBL435 | HYDROCHLOROTHIAZIDE | Ki | > | 50000.0 | nM | - |