Assay Detail
Binding
CHEMBL1058690
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIF1 activation in human U251 cells stably transfected in pGL2-TK-HRE plasmid under hypoxic condition after 16 to 24 hrs by luciferase reporter gene assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U-251 |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Hypoxia inducible factors; HIF-1-alpha, HIF-2-alpha (CHEMBL2221345) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
Cytotoxic and HIF-1alpha inhibitory compounds from Crossosoma bigelovii.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 6.79 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL399336 | CONVALLATOXIN | — | 1 | 7.70 |
| CHEMBL538442 | — | — | 1 | 7.40 |
| CHEMBL53463 | DOXORUBICIN | 4.0 | 1 | 6.92 |
| CHEMBL553660 | — | — | 1 | 6.22 |
| CHEMBL111743 | STROPHANTHIDIN | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL399336 | CONVALLATOXIN | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL538442 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL53463 | DOXORUBICIN | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL553660 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL111743 | STROPHANTHIDIN | EC50 | = | 2000.0 | nM | 5.70 |