Assay Detail
Binding
CHEMBL1787515
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Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 4.61 | 5.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1782072 | — | — | 1 | 5.14 |
| CHEMBL1783635 | — | — | 1 | 5.06 |
| CHEMBL333985 | — | — | 1 | 5.04 |
| CHEMBL1783638 | — | — | 1 | 4.82 |
| CHEMBL1783625 | — | — | 1 | 4.76 |
| CHEMBL1783634 | — | — | 1 | 4.73 |
| CHEMBL1783637 | — | — | 1 | 4.66 |
| CHEMBL1783627 | — | — | 1 | 4.64 |
| CHEMBL1783636 | — | — | 1 | 4.53 |
| CHEMBL1783631 | — | — | 1 | 4.49 |
| CHEMBL1783622 | — | — | 1 | 4.49 |
| CHEMBL1783624 | — | — | 1 | 4.45 |
| CHEMBL1783633 | — | — | 1 | 4.41 |
| CHEMBL1783629 | — | — | 1 | 4.38 |
| CHEMBL1783628 | — | — | 1 | 4.29 |
| CHEMBL1783626 | — | — | 1 | 4.28 |
| CHEMBL1783623 | — | — | 1 | 4.16 |
| CHEMBL1783632 | — | — | 1 | - |
| CHEMBL1783630 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1782072 | — | IC50 | = | 7210.0 | nM | 5.14 |
| CHEMBL1783635 | — | IC50 | = | 8620.0 | nM | 5.06 |
| CHEMBL333985 | — | IC50 | = | 9210.0 | nM | 5.04 |
| CHEMBL1783638 | — | IC50 | = | 15100.0 | nM | 4.82 |
| CHEMBL1783625 | — | IC50 | = | 17400.0 | nM | 4.76 |
| CHEMBL1783634 | — | IC50 | = | 18700.0 | nM | 4.73 |
| CHEMBL1783637 | — | IC50 | = | 22100.0 | nM | 4.66 |
| CHEMBL1783627 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL1783636 | — | IC50 | = | 29600.0 | nM | 4.53 |
| CHEMBL1783631 | — | IC50 | = | 32500.0 | nM | 4.49 |
| CHEMBL1783622 | — | IC50 | = | 32700.0 | nM | 4.49 |
| CHEMBL1783624 | — | IC50 | = | 35500.0 | nM | 4.45 |
| CHEMBL1783633 | — | IC50 | = | 39100.0 | nM | 4.41 |
| CHEMBL1783629 | — | IC50 | = | 41600.0 | nM | 4.38 |
| CHEMBL1783628 | — | IC50 | = | 51700.0 | nM | 4.29 |
| CHEMBL1783626 | — | IC50 | = | 52100.0 | nM | 4.28 |
| CHEMBL1783623 | — | IC50 | = | 69900.0 | nM | 4.16 |
| CHEMBL1783632 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1783630 | — | IC50 | > | 100000.0 | nM | - |