Assay Detail
Binding
CHEMBL657968
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Inhibitory activity against human carbonic anhydrase IX
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with fluorine-containing sulfonamides. The first subnanomolar CA IX inhibitor discovered.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.93 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL76956 | — | — | 1 | 9.10 |
| CHEMBL77359 | — | — | 1 | 8.49 |
| CHEMBL307939 | — | — | 1 | 8.37 |
| CHEMBL75620 | — | — | 1 | 8.32 |
| CHEMBL306118 | — | — | 1 | 8.26 |
| CHEMBL305726 | — | — | 1 | 8.15 |
| CHEMBL77284 | — | — | 1 | 8.14 |
| CHEMBL76626 | — | — | 1 | 8.12 |
| CHEMBL265534 | — | — | 1 | 8.07 |
| CHEMBL75747 | — | — | 1 | 8.02 |
| CHEMBL308631 | — | — | 1 | 8.02 |
| CHEMBL76607 | — | — | 1 | 7.98 |
| CHEMBL75855 | — | — | 1 | 7.90 |
| CHEMBL76563 | — | — | 1 | 7.82 |
| CHEMBL309592 | — | — | 1 | 7.80 |
| CHEMBL74491 | — | — | 1 | 7.62 |
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 7.62 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 7.57 |
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 7.47 |
| CHEMBL220491 | BRINZOLAMIDE | 4.0 | 1 | 7.43 |
| CHEMBL17 | DICHLORPHENAMIDE | 4.0 | 1 | 7.30 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL76956 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL77359 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL307939 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL75620 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL306118 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL305726 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL77284 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL76626 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL265534 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL75747 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL308631 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL76607 | — | Ki | = | 10.5 | nM | 7.98 |
| CHEMBL75855 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL76563 | — | Ki | = | 15.2 | nM | 7.82 |
| CHEMBL309592 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL74491 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL77517 | INDISULAM | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL220491 | BRINZOLAMIDE | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL17 | DICHLORPHENAMIDE | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 52.0 | nM | 7.28 |