Assay Detail
Binding
CHEMBL5327874
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIF-2alpha transcriptional activity in human 786-0 cells transfected with HRE-luc2P assessed as decrease in luminescence incubated for 48 hrs by luciferase reporter assay
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | 786-0 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Endothelial PAS domain-containing protein 1 (CHEMBL1744522) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Cycloalkyl[<i>c</i>]thiophenes as Novel Scaffolds for Hypoxia-Inducible Factor-2α Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 5.83 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4173075 | — | — | 1 | 7.57 |
| CHEMBL5398227 | — | — | 1 | 6.47 |
| CHEMBL5440288 | — | — | 1 | 6.38 |
| CHEMBL5414407 | — | — | 1 | 6.25 |
| CHEMBL5427105 | — | — | 1 | 6.20 |
| CHEMBL4641092 | — | — | 1 | 6.16 |
| CHEMBL5417823 | — | — | 1 | 5.96 |
| CHEMBL5439202 | — | — | 1 | 5.96 |
| CHEMBL5397307 | — | — | 1 | 5.89 |
| CHEMBL5394054 | — | — | 1 | 5.80 |
| CHEMBL5433232 | — | — | 1 | 5.75 |
| CHEMBL5395791 | — | — | 1 | 5.66 |
| CHEMBL5420728 | — | — | 1 | 5.62 |
| CHEMBL5431351 | — | — | 1 | 5.58 |
| CHEMBL5439150 | — | — | 1 | 5.42 |
| CHEMBL5399126 | — | — | 1 | 5.41 |
| CHEMBL5404562 | — | — | 1 | 5.35 |
| CHEMBL4639113 | — | — | 1 | 5.17 |
| CHEMBL5417825 | — | — | 1 | 5.15 |
| CHEMBL5419628 | — | — | 1 | 4.80 |
| CHEMBL5422094 | — | — | 1 | - |
| CHEMBL5439050 | — | — | 1 | - |
| CHEMBL5394371 | — | — | 1 | - |
| CHEMBL5439117 | — | — | 1 | - |
| CHEMBL5437026 | — | — | 1 | - |
| CHEMBL5411078 | — | — | 1 | - |
| CHEMBL5393977 | — | — | 1 | - |
| CHEMBL5394506 | — | — | 1 | - |
| CHEMBL5404293 | — | — | 1 | - |
| CHEMBL5423909 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4173075 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5398227 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5440288 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL5414407 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL5427105 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL4641092 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL5417823 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5439202 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5397307 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5394054 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL5433232 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5395791 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5420728 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL5431351 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL5439150 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL5399126 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL5404562 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4639113 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL5417825 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL5419628 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL5412171 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5414724 | — | IC50 | = | 4720000.0 | nM | - |
| CHEMBL5412636 | — | IC50 | = | 158000.0 | nM | - |
| CHEMBL5415217 | — | IC50 | = | 545000.0 | nM | - |
| CHEMBL5433224 | — | IC50 | = | 155000.0 | nM | - |
| CHEMBL5419647 | — | IC50 | = | 1630000.0 | nM | - |
| CHEMBL5426880 | — | IC50 | = | 181000.0 | nM | - |
| CHEMBL5438465 | — | IC50 | = | 821000.0 | nM | - |
| CHEMBL5404788 | — | IC50 | = | 136000.0 | nM | - |
| CHEMBL5428447 | — | IC50 | = | 199000.0 | nM | - |
| CHEMBL5395720 | — | IC50 | = | 895000.0 | nM | - |
| CHEMBL5423909 | — | IC50 | = | 353000.0 | nM | - |
| CHEMBL5404293 | — | IC50 | = | 280000.0 | nM | - |
| CHEMBL5394506 | — | IC50 | = | 222000.0 | nM | - |
| CHEMBL5393977 | — | IC50 | = | 481000.0 | nM | - |
| CHEMBL5411078 | — | IC50 | = | 102000.0 | nM | - |
| CHEMBL5437026 | — | IC50 | = | 130000.0 | nM | - |
| CHEMBL5439117 | — | IC50 | = | 164000.0 | nM | - |
| CHEMBL5394371 | — | IC50 | = | 398000.0 | nM | - |
| CHEMBL5439050 | — | IC50 | = | 456000.0 | nM | - |
| CHEMBL5422094 | — | IC50 | = | 166000.0 | nM | - |