Assay Detail
Binding
CHEMBL828779
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity against human carbonic anhydrase I expressed in Escherichia coli BL21
24
Total Activities
24
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 | 24 | 6.60 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 7.51 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 7.30 |
| CHEMBL187274 | — | — | 1 | 7.12 |
| CHEMBL363543 | — | — | 1 | 7.11 |
| CHEMBL366086 | — | — | 1 | 7.09 |
| CHEMBL186716 | — | — | 1 | 7.08 |
| CHEMBL365860 | — | — | 1 | 7.07 |
| CHEMBL184107 | — | — | 1 | 7.06 |
| CHEMBL186504 | — | — | 1 | 7.05 |
| CHEMBL185473 | — | — | 1 | 7.03 |
| CHEMBL359997 | — | — | 1 | 7.02 |
| CHEMBL183153 | — | — | 1 | 6.99 |
| CHEMBL184923 | — | — | 1 | 6.98 |
| CHEMBL183945 | — | — | 1 | 6.96 |
| CHEMBL185549 | — | — | 1 | 6.94 |
| CHEMBL366069 | — | — | 1 | 6.92 |
| CHEMBL187901 | — | — | 1 | 6.87 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 6.60 |
| CHEMBL17 | DICHLORPHENAMIDE | 4.0 | 1 | 5.92 |
| CHEMBL7087 | — | — | 1 | 4.68 |
| CHEMBL419 | MAFENIDE | 4.0 | 1 | 4.60 |
| CHEMBL21 | SULFANILAMIDE | 4.0 | 1 | 4.55 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 4.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL77517 | INDISULAM | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL187274 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL363543 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL366086 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL186716 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL365860 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL184107 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL186504 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL185473 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL359997 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL183153 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL184923 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL183945 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL185549 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL366069 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL187901 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL17 | DICHLORPHENAMIDE | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL7087 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL419 | MAFENIDE | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL21 | SULFANILAMIDE | Ki | = | 28000.0 | nM | 4.55 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 50000.0 | nM | 4.30 |