Assay Detail
Binding
CHEMBL869404
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Inhibition of cloned human transmembrane, tumor-associated isozyme CA IX
15
Total Activities
15
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: inhibition of the human isozymes I, II, VA, and IX with a library of substituted difluoromethanesulfonamides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.17 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL122708 | EMATE | — | 1 | 7.52 |
| CHEMBL24259 | PHENYLSULFAMATE | — | 1 | 7.20 |
| CHEMBL198891 | — | — | 1 | 6.71 |
| CHEMBL1628081 | — | — | 1 | 6.68 |
| CHEMBL198913 | — | — | 1 | 6.62 |
| CHEMBL199464 | — | — | 1 | 6.60 |
| CHEMBL200673 | — | — | 1 | 5.83 |
| CHEMBL1628004 | — | — | 1 | 5.76 |
| CHEMBL370159 | — | — | 1 | 5.62 |
| CHEMBL370854 | — | — | 1 | 5.11 |
| CHEMBL371870 | PHENYLDIFLUOROMETHANESULFONAMIDE | — | 1 | 5.07 |
| CHEMBL369953 | PHENYLMETHANESULFONAMIDE | — | 1 | 5.03 |
| CHEMBL199493 | — | — | 1 | 5.03 |
| CHEMBL11185 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL122708 | EMATE | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL24259 | PHENYLSULFAMATE | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL198891 | — | Ki | = | 195.0 | nM | 6.71 |
| CHEMBL1628081 | — | Ki | = | 208.0 | nM | 6.68 |
| CHEMBL198913 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL199464 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL200673 | — | Ki | = | 1495.0 | nM | 5.83 |
| CHEMBL1628004 | — | Ki | = | 1725.0 | nM | 5.76 |
| CHEMBL370159 | — | Ki | = | 2420.0 | nM | 5.62 |
| CHEMBL370854 | — | Ki | = | 7730.0 | nM | 5.11 |
| CHEMBL371870 | PHENYLDIFLUOROMETHANESULFONAMIDE | Ki | = | 8500.0 | nM | 5.07 |
| CHEMBL369953 | PHENYLMETHANESULFONAMIDE | Ki | = | 9300.0 | nM | 5.03 |
| CHEMBL199493 | — | Ki | = | 9280.0 | nM | 5.03 |
| CHEMBL11185 | — | Ki | - | — | - |