Assay Detail
Binding
CHEMBL1290839
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant CA9 catalytic domain by stopped-flow CO2 hydration method
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
7,8-disubstituted- but not 6,7-disubstituted coumarins selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic ones I and II in the low nanomolar/subnanomolar range.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 6.55 | 7.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1288621 | — | — | 1 | 7.42 |
| CHEMBL1288622 | — | — | 1 | 7.33 |
| CHEMBL1288623 | — | — | 1 | 7.30 |
| CHEMBL1288596 | — | — | 1 | 7.25 |
| CHEMBL1288557 | — | — | 1 | 7.24 |
| CHEMBL1288620 | — | — | 1 | 7.21 |
| CHEMBL1290219 | — | — | 1 | 7.19 |
| CHEMBL1288595 | — | — | 1 | 7.15 |
| CHEMBL1290111 | — | — | 1 | 7.14 |
| CHEMBL446518 | — | — | 1 | 7.14 |
| CHEMBL1288594 | — | — | 1 | 7.11 |
| CHEMBL51628 | UMBELLIFERONE | — | 1 | 6.32 |
| CHEMBL1288559 | — | — | 1 | 5.13 |
| CHEMBL1288560 | — | — | 1 | 5.12 |
| CHEMBL1288558 | — | — | 1 | 5.11 |
| CHEMBL1288535 | — | — | 1 | 5.10 |
| CHEMBL1288534 | — | — | 1 | 5.09 |
| CHEMBL572366 | — | — | 1 | - |
| CHEMBL6466 | COUMARIN | 4.0 | 1 | - |
| CHEMBL1288593 | — | — | 1 | - |
| CHEMBL1290010 | — | — | 1 | - |
| CHEMBL1290110 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1288621 | — | Ki | = | 37.8 | nM | 7.42 |
| CHEMBL1288622 | — | Ki | = | 46.7 | nM | 7.33 |
| CHEMBL1288623 | — | Ki | = | 50.2 | nM | 7.30 |
| CHEMBL1288596 | — | Ki | = | 56.7 | nM | 7.25 |
| CHEMBL1288557 | — | Ki | = | 58.2 | nM | 7.24 |
| CHEMBL1288620 | — | Ki | = | 61.2 | nM | 7.21 |
| CHEMBL1290219 | — | Ki | = | 63.9 | nM | 7.19 |
| CHEMBL1288595 | — | Ki | = | 70.8 | nM | 7.15 |
| CHEMBL1290111 | — | Ki | = | 72.3 | nM | 7.14 |
| CHEMBL446518 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL1288594 | — | Ki | = | 78.3 | nM | 7.11 |
| CHEMBL51628 | UMBELLIFERONE | Ki | = | 482.0 | nM | 6.32 |
| CHEMBL1288559 | — | Ki | = | 7400.0 | nM | 5.13 |
| CHEMBL1288560 | — | Ki | = | 7580.0 | nM | 5.12 |
| CHEMBL1288558 | — | Ki | = | 7800.0 | nM | 5.11 |
| CHEMBL1288535 | — | Ki | = | 8015.0 | nM | 5.10 |
| CHEMBL1288534 | — | Ki | = | 8030.0 | nM | 5.09 |
| CHEMBL572366 | — | Ki | = | 54.5 | nM | - |
| CHEMBL6466 | COUMARIN | Ki | > | 100.0 | nM | - |
| CHEMBL1288593 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL1290010 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL1290110 | — | Ki | > | 100000.0 | nM | - |