Assay Detail
Binding
CHEMBL877449
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Inhibitory activity against catalytic domain of human carbonic anhydrase XII
30
Total Activities
30
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: design of thioureido sulfonamides with potent isozyme II and XII inhibitory properties and intraocular pressure lowering activity in a rabbit model of glaucoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 8.10 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL181082 | — | — | 1 | 8.82 |
| CHEMBL538564 | — | — | 1 | 8.77 |
| CHEMBL180177 | THIOUREIDO SULFONAMIDE | — | 1 | 8.74 |
| CHEMBL179355 | — | — | 1 | 8.72 |
| CHEMBL178560 | — | — | 1 | 8.70 |
| CHEMBL181825 | — | — | 1 | 8.68 |
| CHEMBL182197 | — | — | 1 | 8.64 |
| CHEMBL180506 | — | — | 1 | 8.52 |
| CHEMBL361955 | — | — | 1 | 8.52 |
| CHEMBL220491 | BRINZOLAMIDE | 4.0 | 1 | 8.52 |
| CHEMBL181422 | — | — | 1 | 8.48 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 8.47 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 8.46 |
| CHEMBL180936 | — | — | 1 | 8.32 |
| CHEMBL178603 | — | — | 1 | 8.31 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 8.24 |
| CHEMBL182135 | — | — | 1 | 8.00 |
| CHEMBL179218 | — | — | 1 | 7.92 |
| CHEMBL362636 | — | — | 1 | 7.92 |
| CHEMBL360254 | — | — | 1 | 7.92 |
| CHEMBL178403 | — | — | 1 | 7.89 |
| CHEMBL361827 | — | — | 1 | 7.75 |
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 7.66 |
| CHEMBL413357 | — | — | 1 | 7.62 |
| CHEMBL181716 | — | — | 1 | 7.48 |
| CHEMBL21 | SULFANILAMIDE | 4.0 | 1 | 7.43 |
| CHEMBL17 | DICHLORPHENAMIDE | 4.0 | 1 | 7.30 |
| CHEMBL178664 | THIOUREIDO SULFONAMIDE | — | 1 | 7.30 |
| CHEMBL180675 | THIOUREIDO SULFONAMIDE | — | 1 | 7.19 |
| CHEMBL180195 | — | — | 1 | 6.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL181082 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL538564 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL180177 | THIOUREIDO SULFONAMIDE | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL179355 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL178560 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL181825 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL182197 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL180506 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL361955 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL220491 | BRINZOLAMIDE | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL181422 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL180936 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL178603 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL182135 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL179218 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL362636 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL360254 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL178403 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL361827 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL413357 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL181716 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL21 | SULFANILAMIDE | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL17 | DICHLORPHENAMIDE | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL178664 | THIOUREIDO SULFONAMIDE | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL180675 | THIOUREIDO SULFONAMIDE | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL180195 | — | Ki | = | 144.0 | nM | 6.84 |