Assay Detail
Binding
CHEMBL1290840
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Inhibition of human recombinant CA12 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 | 8 — Homologous 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 | 7.20 | 9.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1288596 | — | — | 1 | 9.01 |
| CHEMBL1288595 | — | — | 1 | 9.00 |
| CHEMBL1288620 | — | — | 1 | 8.06 |
| CHEMBL1290111 | — | — | 1 | 7.65 |
| CHEMBL1288621 | — | — | 1 | 7.58 |
| CHEMBL1290219 | — | — | 1 | 7.50 |
| CHEMBL1288622 | — | — | 1 | 7.48 |
| CHEMBL1288623 | — | — | 1 | 7.42 |
| CHEMBL572366 | — | — | 1 | 7.31 |
| CHEMBL1288594 | — | — | 1 | 7.21 |
| CHEMBL1288557 | — | — | 1 | 7.21 |
| CHEMBL446518 | — | — | 1 | 7.21 |
| CHEMBL51628 | UMBELLIFERONE | — | 1 | 6.12 |
| CHEMBL1288558 | — | — | 1 | 5.18 |
| CHEMBL1290110 | — | — | 1 | 4.11 |
| CHEMBL6466 | COUMARIN | 4.0 | 1 | - |
| CHEMBL1288534 | — | — | 1 | - |
| CHEMBL1288535 | — | — | 1 | - |
| CHEMBL1288559 | — | — | 1 | - |
| CHEMBL1288560 | — | — | 1 | - |
| CHEMBL1288593 | — | — | 1 | - |
| CHEMBL1290010 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1288596 | — | Ki | = | 0.98 | nM | 9.01 |
| CHEMBL1288595 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1288620 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL1290111 | — | Ki | = | 22.4 | nM | 7.65 |
| CHEMBL1288621 | — | Ki | = | 26.3 | nM | 7.58 |
| CHEMBL1290219 | — | Ki | = | 31.5 | nM | 7.50 |
| CHEMBL1288622 | — | Ki | = | 33.2 | nM | 7.48 |
| CHEMBL1288623 | — | Ki | = | 38.4 | nM | 7.42 |
| CHEMBL572366 | — | Ki | = | 48.6 | nM | 7.31 |
| CHEMBL1288594 | — | Ki | = | 60.9 | nM | 7.21 |
| CHEMBL1288557 | — | Ki | = | 61.7 | nM | 7.21 |
| CHEMBL446518 | — | Ki | = | 61.9 | nM | 7.21 |
| CHEMBL51628 | UMBELLIFERONE | Ki | = | 754.0 | nM | 6.12 |
| CHEMBL1288558 | — | Ki | = | 6540.0 | nM | 5.18 |
| CHEMBL1290110 | — | Ki | = | 77700.0 | nM | 4.11 |
| CHEMBL6466 | COUMARIN | Ki | > | 100.0 | nM | - |
| CHEMBL1288534 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL1288535 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL1288559 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL1288560 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL1288593 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL1290010 | — | Ki | > | 100000.0 | nM | - |