Assay Detail
Binding
CHEMBL3587853
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human HIF1alpha-mediated transcription expressed in human U251 cells co-transfected with pGL2-TK-HRE incubated for 24 hrs by luciferase reporter gene assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U-251 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Tetracycline analogues with a selective inhibitory effect on HIF-1
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 5.63 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL84 | TOPOTECAN | 4.0 | 1 | 7.92 |
| CHEMBL3585463 | — | — | 1 | 5.85 |
| CHEMBL3585448 | — | — | 1 | 5.64 |
| CHEMBL3585467 | — | — | 1 | 5.39 |
| CHEMBL3585464 | — | — | 1 | 5.17 |
| CHEMBL3585447 | — | — | 1 | 5.17 |
| CHEMBL3585466 | — | — | 1 | 5.11 |
| CHEMBL3585465 | — | — | 1 | 4.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL84 | TOPOTECAN | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3585463 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3585448 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3585467 | — | EC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL3585464 | — | EC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL3585447 | — | EC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL3585466 | — | EC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL3585465 | — | EC50 | = | 15500.0 | nM | 4.81 |