Assay Detail
Binding
CHEMBL3404500
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Inhibition of Anopheles gambiae carbonic anhydrase pre-incubated for 15 mins by stopped-flow CO2 hydration assay
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Anopheles gambiae |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
The β-carbonic anhydrase from the malaria mosquito Anopheles gambiae is highly inhibited by sulfonamides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 40 | 6.48 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2324864 | — | — | 1 | 8.21 |
| CHEMBL268439 | — | — | 1 | 8.17 |
| CHEMBL73962 | BENZOLAMIDE | — | 1 | 8.01 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.56 |
| CHEMBL26 | SULPIRIDE | 3.0 | 1 | 7.53 |
| CHEMBL435 | HYDROCHLOROTHIAZIDE | 4.0 | 1 | 7.50 |
| CHEMBL220491 | BRINZOLAMIDE | 4.0 | 1 | 7.50 |
| CHEMBL7146 | — | — | 1 | 7.33 |
| CHEMBL266026 | — | — | 1 | 7.09 |
| CHEMBL269122 | — | — | 1 | 7.08 |
| CHEMBL310671 | SACCHARIN | 3.0 | 1 | 7.02 |
| CHEMBL865 | VALDECOXIB | 4.0 | 1 | 6.79 |
| CHEMBL118 | CELECOXIB | 4.0 | 1 | 6.76 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 6.74 |
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 6.73 |
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 6.65 |
| CHEMBL328560 | SULTHIAME | 3.0 | 1 | 6.58 |
| CHEMBL750 | ZONISAMIDE | 4.0 | 1 | 6.58 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 6.56 |
| CHEMBL17 | DICHLORPHENAMIDE | 4.0 | 1 | 6.20 |
| CHEMBL414 | CARZENIDE | 2.0 | 1 | 6.15 |
| CHEMBL265674 | — | — | 1 | 6.13 |
| CHEMBL266240 | — | — | 1 | 6.12 |
| CHEMBL7087 | — | — | 1 | 6.08 |
| CHEMBL2324868 | — | — | 1 | 6.07 |
| CHEMBL6724 | — | — | 1 | 6.07 |
| CHEMBL21 | SULFANILAMIDE | 4.0 | 1 | 6.06 |
| CHEMBL6852 | — | — | 1 | 6.05 |
| CHEMBL6853 | — | — | 1 | 6.04 |
| CHEMBL6753 | — | — | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2324864 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL268439 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL73962 | BENZOLAMIDE | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 27.3 | nM | 7.56 |
| CHEMBL26 | SULPIRIDE | Ki | = | 29.5 | nM | 7.53 |
| CHEMBL435 | HYDROCHLOROTHIAZIDE | Ki | = | 31.5 | nM | 7.50 |
| CHEMBL220491 | BRINZOLAMIDE | Ki | = | 31.4 | nM | 7.50 |
| CHEMBL7146 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL266026 | — | Ki | = | 81.9 | nM | 7.09 |
| CHEMBL269122 | — | Ki | = | 83.4 | nM | 7.08 |
| CHEMBL310671 | SACCHARIN | Ki | = | 95.3 | nM | 7.02 |
| CHEMBL865 | VALDECOXIB | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL118 | CELECOXIB | Ki | = | 173.0 | nM | 6.76 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 184.0 | nM | 6.74 |
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL77517 | INDISULAM | Ki | = | 226.0 | nM | 6.65 |
| CHEMBL328560 | SULTHIAME | Ki | = | 265.0 | nM | 6.58 |
| CHEMBL750 | ZONISAMIDE | Ki | = | 263.0 | nM | 6.58 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 275.0 | nM | 6.56 |
| CHEMBL17 | DICHLORPHENAMIDE | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL414 | CARZENIDE | Ki | = | 703.0 | nM | 6.15 |
| CHEMBL265674 | — | Ki | = | 737.0 | nM | 6.13 |
| CHEMBL266240 | — | Ki | = | 756.0 | nM | 6.12 |
| CHEMBL7087 | — | Ki | = | 835.0 | nM | 6.08 |
| CHEMBL2324868 | — | Ki | = | 843.0 | nM | 6.07 |
| CHEMBL6724 | — | Ki | = | 855.0 | nM | 6.07 |
| CHEMBL21 | SULFANILAMIDE | Ki | = | 862.0 | nM | 6.06 |
| CHEMBL6852 | — | Ki | = | 887.0 | nM | 6.05 |
| CHEMBL6853 | — | Ki | = | 902.0 | nM | 6.04 |
| CHEMBL6753 | — | Ki | = | 1685.0 | nM | 5.77 |
| CHEMBL418 | 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE | Ki | = | 4360.0 | nM | 5.36 |
| CHEMBL2324869 | — | Ki | = | 6480.0 | nM | 5.19 |
| CHEMBL6633 | — | Ki | = | 10600.0 | nM | 4.97 |
| CHEMBL7092 | — | Ki | = | 12430.0 | nM | 4.91 |
| CHEMBL574 | P-TOLUENESULFONAMIDE | Ki | = | 12400.0 | nM | 4.91 |
| CHEMBL419 | MAFENIDE | Ki | = | 13600.0 | nM | 4.87 |
| CHEMBL224292 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL6919 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL6784 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL220492 | TOPIRAMATE | Ki | > | 100000.0 | nM | - |