Assay Detail
Binding
CHEMBL653166
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Inhibition of human recombinant carbonic anhydrase I
31
Total Activities
31
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 cytosolic isozymes I and II and transmembrane, tumor-associated isozyme IX with sulfamates including EMATE also acting as steroid sulfatase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 7.16 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL24259 | PHENYLSULFAMATE | — | 1 | 8.68 |
| CHEMBL24261 | OCTYL SULFAMATE | — | 1 | 8.46 |
| CHEMBL24210 | — | — | 1 | 8.42 |
| CHEMBL23350 | — | — | 1 | 8.34 |
| CHEMBL221802 | — | — | 1 | 8.22 |
| CHEMBL283121 | — | — | 1 | 8.14 |
| CHEMBL24120 | — | — | 1 | 8.02 |
| CHEMBL220493 | — | — | 1 | 7.82 |
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL544763 | — | — | 1 | 7.55 |
| CHEMBL71371 | — | — | 1 | 7.51 |
| CHEMBL71872 | — | — | 1 | 7.48 |
| CHEMBL68590 | — | — | 1 | 7.43 |
| CHEMBL122708 | EMATE | — | 1 | 7.43 |
| CHEMBL23258 | — | — | 1 | 7.40 |
| CHEMBL69948 | — | — | 1 | 7.37 |
| CHEMBL67749 | — | — | 1 | 6.99 |
| CHEMBL68257 | — | — | 1 | 6.98 |
| CHEMBL417287 | — | — | 1 | 6.95 |
| CHEMBL69322 | — | — | 1 | 6.94 |
| CHEMBL220492 | TOPIRAMATE | 4.0 | 1 | 6.60 |
| CHEMBL302593 | — | — | 1 | 6.56 |
| CHEMBL71549 | — | — | 1 | 6.50 |
| CHEMBL303601 | — | — | 1 | 6.43 |
| CHEMBL68536 | PERFLUOROPHENYL SULFAMATE | — | 1 | 6.38 |
| CHEMBL71873 | SULFAMIC ACID PENTACHLOROPHENYL ESTER | — | 1 | 6.37 |
| CHEMBL303942 | — | — | 1 | 6.34 |
| CHEMBL24119 | — | — | 1 | 6.32 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 6.11 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL24259 | PHENYLSULFAMATE | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL24261 | OCTYL SULFAMATE | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL24210 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL23350 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL221802 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL283121 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL24120 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL220493 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL544763 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL71371 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL71872 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL68590 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL122708 | EMATE | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL23258 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL69948 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL67749 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL68257 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL417287 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL69322 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL220492 | TOPIRAMATE | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL302593 | — | Ki | = | 278.0 | nM | 6.56 |
| CHEMBL71549 | — | Ki | = | 315.0 | nM | 6.50 |
| CHEMBL303601 | — | Ki | = | 369.0 | nM | 6.43 |
| CHEMBL68536 | PERFLUOROPHENYL SULFAMATE | Ki | = | 415.0 | nM | 6.38 |
| CHEMBL71873 | SULFAMIC ACID PENTACHLOROPHENYL ESTER | Ki | = | 432.0 | nM | 6.37 |
| CHEMBL303942 | — | Ki | = | 454.0 | nM | 6.34 |
| CHEMBL24119 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL68253 | SULFAMATE | Ki | = | 21000.0 | nM | 4.68 |