Assay Detail
Binding
CHEMBL828796
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Inhibitory activity against human carbonic anhydrase IX expressed in Escherichia coli BL21
25
Total Activities
25
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: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating 1,2,4-triazine moieties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 7.55 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL363543 | — | — | 1 | 9.92 |
| CHEMBL366069 | — | — | 1 | 9.82 |
| CHEMBL183945 | — | — | 1 | 9.47 |
| CHEMBL184107 | — | — | 1 | 8.96 |
| CHEMBL186504 | — | — | 1 | 8.89 |
| CHEMBL366086 | — | — | 1 | 7.92 |
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 7.62 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 7.57 |
| CHEMBL7087 | — | — | 1 | 7.48 |
| 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 |
| CHEMBL419 | MAFENIDE | 4.0 | 1 | 6.99 |
| CHEMBL187901 | — | — | 1 | 6.91 |
| CHEMBL187274 | — | — | 1 | 6.86 |
| CHEMBL183153 | — | — | 1 | 6.85 |
| CHEMBL365860 | — | — | 1 | 6.82 |
| CHEMBL186716 | — | — | 1 | 6.82 |
| CHEMBL185549 | — | — | 1 | 6.81 |
| CHEMBL184923 | — | — | 1 | 6.79 |
| CHEMBL21 | SULFANILAMIDE | 4.0 | 1 | 6.53 |
| CHEMBL185473 | — | — | 1 | 6.44 |
| CHEMBL359997 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL363543 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL366069 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL183945 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL184107 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL186504 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL366086 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL77517 | INDISULAM | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL7087 | — | Ki | = | 33.0 | nM | 7.48 |
| 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 |
| CHEMBL419 | MAFENIDE | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL187901 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL187274 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL183153 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL365860 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL186716 | — | Ki | = | 153.0 | nM | 6.82 |
| CHEMBL185549 | — | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL184923 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL21 | SULFANILAMIDE | Ki | = | 294.0 | nM | 6.53 |
| CHEMBL185473 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL359997 | — | Ki | = | 549.0 | nM | 6.26 |