Assay Detail
Binding
CHEMBL5552437
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human CA9 assessed as inhibition constant preincubated for 15 mins by phenol red dye based stopped-flow CO2 hydration assay
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 | 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 | 24 | 7.06 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5591900 | — | — | 1 | 8.57 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 8.04 |
| CHEMBL2382401 | — | — | 1 | 8.01 |
| CHEMBL5574983 | — | — | 1 | 7.92 |
| CHEMBL5594056 | — | — | 1 | 7.82 |
| CHEMBL5575167 | — | — | 1 | 7.70 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL2382400 | — | — | 1 | 7.42 |
| CHEMBL1615281 | SLC-0111 | 1.0 | 1 | 7.35 |
| CHEMBL5573411 | — | — | 1 | 7.32 |
| CHEMBL5566364 | — | — | 1 | 7.28 |
| CHEMBL5565594 | — | — | 1 | 7.12 |
| CHEMBL5574036 | — | — | 1 | 7.06 |
| CHEMBL5569578 | — | — | 1 | 7.02 |
| CHEMBL5590657 | — | — | 1 | 6.92 |
| CHEMBL5570199 | — | — | 1 | 6.79 |
| CHEMBL5565094 | — | — | 1 | 6.59 |
| CHEMBL5571304 | — | — | 1 | 6.52 |
| CHEMBL2382337 | — | — | 1 | 6.37 |
| CHEMBL5569259 | — | — | 1 | 6.26 |
| CHEMBL5570589 | — | — | 1 | 6.17 |
| CHEMBL5573856 | — | — | 1 | 6.02 |
| CHEMBL5590806 | — | — | 1 | 5.85 |
| CHEMBL5594314 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5591900 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL477772 | PAZOPANIB | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL2382401 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL5574983 | — | Ki | = | 11.9 | nM | 7.92 |
| CHEMBL5594056 | — | Ki | = | 15.3 | nM | 7.82 |
| CHEMBL5575167 | — | Ki | = | 20.2 | nM | 7.70 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL2382400 | — | Ki | = | 37.6 | nM | 7.42 |
| CHEMBL1615281 | SLC-0111 | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL5573411 | — | Ki | = | 47.6 | nM | 7.32 |
| CHEMBL5566364 | — | Ki | = | 52.1 | nM | 7.28 |
| CHEMBL5565594 | — | Ki | = | 75.2 | nM | 7.12 |
| CHEMBL5574036 | — | Ki | = | 86.4 | nM | 7.06 |
| CHEMBL5569578 | — | Ki | = | 96.2 | nM | 7.02 |
| CHEMBL5590657 | — | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL5570199 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL5565094 | — | Ki | = | 259.2 | nM | 6.59 |
| CHEMBL5571304 | — | Ki | = | 303.9 | nM | 6.52 |
| CHEMBL2382337 | — | Ki | = | 427.2 | nM | 6.37 |
| CHEMBL5569259 | — | Ki | = | 551.2 | nM | 6.26 |
| CHEMBL5570589 | — | Ki | = | 672.1 | nM | 6.17 |
| CHEMBL5573856 | — | Ki | = | 945.7 | nM | 6.02 |
| CHEMBL5590806 | — | Ki | = | 1398.0 | nM | 5.85 |
| CHEMBL5594314 | — | Ki | = | 2307.0 | nM | 5.64 |