Assay Detail
Binding
CHEMBL5552435
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Inhibition of human CA1 assessed as inhibition constant preincubated for 15 mins by phenol red dye based stopped-flow CO2 hydration assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A new framework for novel analogues of pazopanib as potent and selective human carbonic anhydrase inhibitors: Design, repurposing rational, synthesis, crystallographic, in vivo and in vitro biological assessments.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 5.62 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 7.92 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 6.60 |
| CHEMBL5574036 | — | — | 1 | 6.53 |
| CHEMBL5565594 | — | — | 1 | 6.36 |
| CHEMBL2382400 | — | — | 1 | 6.23 |
| CHEMBL5566364 | — | — | 1 | 6.18 |
| CHEMBL5573411 | — | — | 1 | 6.14 |
| CHEMBL2382337 | — | — | 1 | 6.00 |
| CHEMBL5594056 | — | — | 1 | 5.37 |
| CHEMBL5565094 | — | — | 1 | 5.22 |
| CHEMBL5569259 | — | — | 1 | 5.08 |
| CHEMBL5571304 | — | — | 1 | 5.02 |
| CHEMBL5573856 | — | — | 1 | 4.54 |
| CHEMBL5574983 | — | — | 1 | 4.50 |
| CHEMBL5590806 | — | — | 1 | 4.18 |
| CHEMBL5570589 | — | — | 1 | 4.02 |
| CHEMBL5590657 | — | — | 1 | - |
| CHEMBL5591900 | — | — | 1 | - |
| CHEMBL5594314 | — | — | 1 | - |
| CHEMBL5575167 | — | — | 1 | - |
| CHEMBL5570199 | — | — | 1 | - |
| CHEMBL5569578 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL477772 | PAZOPANIB | Ki | = | 12.1 | nM | 7.92 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL5574036 | — | Ki | = | 295.5 | nM | 6.53 |
| CHEMBL5565594 | — | Ki | = | 441.9 | nM | 6.36 |
| CHEMBL2382400 | — | Ki | = | 594.1 | nM | 6.23 |
| CHEMBL5566364 | — | Ki | = | 661.0 | nM | 6.18 |
| CHEMBL5573411 | — | Ki | = | 731.4 | nM | 6.14 |
| CHEMBL2382337 | — | Ki | = | 989.0 | nM | 6.00 |
| CHEMBL5594056 | — | Ki | = | 4320.0 | nM | 5.37 |
| CHEMBL5565094 | — | Ki | = | 6063.0 | nM | 5.22 |
| CHEMBL5569259 | — | Ki | = | 8406.0 | nM | 5.08 |
| CHEMBL5571304 | — | Ki | = | 9619.0 | nM | 5.02 |
| CHEMBL5573856 | — | Ki | = | 28697.0 | nM | 4.54 |
| CHEMBL5574983 | — | Ki | = | 31429.0 | nM | 4.50 |
| CHEMBL5590806 | — | Ki | = | 66075.0 | nM | 4.18 |
| CHEMBL5570589 | — | Ki | = | 95861.0 | nM | 4.02 |
| CHEMBL5590657 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5591900 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5594314 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5575167 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5570199 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5569578 | — | Ki | > | 100000.0 | nM | - |