Assay Detail
Binding
CHEMBL1799182
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Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Hep 3B2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
HIF-1α inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.45 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1795446 | — | — | 1 | 9.00 |
| CHEMBL1795435 | — | — | 1 | 8.38 |
| CHEMBL1795432 | — | — | 1 | 8.17 |
| CHEMBL205924 | MORACIN O | — | 1 | 8.17 |
| CHEMBL1795439 | — | — | 1 | 8.15 |
| CHEMBL1795433 | — | — | 1 | 8.00 |
| CHEMBL561971 | MORACIN P | — | 1 | 7.97 |
| CHEMBL1795434 | — | — | 1 | 7.34 |
| CHEMBL1795441 | — | — | 1 | 7.27 |
| CHEMBL1795436 | — | — | 1 | 7.27 |
| CHEMBL1795440 | — | — | 1 | 6.96 |
| CHEMBL1795442 | — | — | 1 | 6.51 |
| CHEMBL1795443 | — | — | 1 | 6.44 |
| CHEMBL1795437 | — | — | 1 | 6.31 |
| CHEMBL1795438 | — | — | 1 | 6.24 |
| CHEMBL1795444 | — | — | 1 | 5.96 |
| CHEMBL1795456 | — | — | 1 | 5.58 |
| CHEMBL1795431 | — | — | 1 | 5.28 |
| CHEMBL1795455 | — | — | 1 | 5.14 |
| CHEMBL380456 | (+/-)-MORACIN P | — | 1 | 4.97 |
| CHEMBL1795457 | — | — | 1 | 4.89 |
| CHEMBL1795454 | — | — | 1 | 4.78 |
| CHEMBL1795453 | — | — | 1 | 4.76 |
| CHEMBL1795452 | — | — | 1 | 4.76 |
| CHEMBL1795451 | — | — | 1 | 4.75 |
| CHEMBL1795448 | — | — | 1 | 4.58 |
| CHEMBL1795445 | — | — | 1 | - |
| CHEMBL1795447 | — | — | 1 | - |
| CHEMBL1795449 | — | — | 1 | - |
| CHEMBL1795450 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1795446 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1795435 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL1795432 | — | IC50 | = | 6.76 | nM | 8.17 |
| CHEMBL205924 | MORACIN O | IC50 | = | 6.76 | nM | 8.17 |
| CHEMBL1795439 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1795433 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL561971 | MORACIN P | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL1795434 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL1795441 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1795436 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1795440 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1795442 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL1795443 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL1795437 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL1795438 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL1795444 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1795456 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1795431 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL1795455 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL380456 | (+/-)-MORACIN P | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL1795457 | — | IC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL1795454 | — | IC50 | = | 16800.0 | nM | 4.78 |
| CHEMBL1795453 | — | IC50 | = | 17200.0 | nM | 4.76 |
| CHEMBL1795452 | — | IC50 | = | 17500.0 | nM | 4.76 |
| CHEMBL1795451 | — | IC50 | = | 17600.0 | nM | 4.75 |
| CHEMBL1795448 | — | IC50 | = | 26200.0 | nM | 4.58 |
| CHEMBL1795430 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1795429 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1795428 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1795427 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1795426 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1795450 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1795449 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1795447 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1795445 | — | IC50 | > | 30.0 | nM | - |