Assay Detail
Binding
CHEMBL867415
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Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydrase assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 6.91 | 8.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL427654 | — | — | 1 | 8.02 |
| CHEMBL373666 | — | — | 1 | 8.00 |
| CHEMBL377326 | — | — | 1 | 7.77 |
| CHEMBL212440 | — | — | 1 | 7.75 |
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 7.51 |
| CHEMBL436936 | — | — | 1 | 7.39 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 7.30 |
| CHEMBL750 | ZONISAMIDE | 4.0 | 1 | 7.25 |
| CHEMBL377107 | — | — | 1 | 7.22 |
| CHEMBL212944 | — | — | 1 | 7.16 |
| CHEMBL213777 | — | — | 1 | 7.15 |
| CHEMBL214201 | — | — | 1 | 7.13 |
| CHEMBL214745 | — | — | 1 | 7.07 |
| CHEMBL209732 | — | — | 1 | 7.01 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 6.60 |
| CHEMBL386049 | — | — | 1 | 6.56 |
| CHEMBL215810 | — | — | 1 | 6.56 |
| CHEMBL17 | DICHLORPHENAMIDE | 4.0 | 1 | 5.92 |
| CHEMBL26 | SULPIRIDE | 3.0 | 1 | 5.92 |
| CHEMBL353498 | — | — | 1 | 5.37 |
| CHEMBL418037 | — | — | 1 | 5.36 |
| CHEMBL215936 | — | — | 1 | 5.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL427654 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL373666 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL377326 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL212440 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL77517 | INDISULAM | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL436936 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL750 | ZONISAMIDE | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL377107 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL212944 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL213777 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL214201 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL214745 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL209732 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL386049 | — | Ki | = | 276.0 | nM | 6.56 |
| CHEMBL215810 | — | Ki | = | 275.0 | nM | 6.56 |
| CHEMBL17 | DICHLORPHENAMIDE | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL26 | SULPIRIDE | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL353498 | — | Ki | = | 4265.0 | nM | 5.37 |
| CHEMBL418037 | — | Ki | = | 4350.0 | nM | 5.36 |
| CHEMBL215936 | — | Ki | = | 5115.0 | nM | 5.29 |