Assay Detail
Binding
CHEMBL5327875
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Inhibition of HIF-2alpha transcriptional activity in human 786-0 cells assessed as decrease in VEGF production incubated for 48 hrs by ELISA
40
Total Activities
40
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 | 40 | 5.88 | 7.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4173075 | — | — | 1 | 7.41 |
| CHEMBL5417823 | — | — | 1 | 6.40 |
| CHEMBL5440288 | — | — | 1 | 6.27 |
| CHEMBL5414407 | — | — | 1 | 6.26 |
| CHEMBL5427105 | — | — | 1 | 6.24 |
| CHEMBL5398227 | — | — | 1 | 6.15 |
| CHEMBL5394054 | — | — | 1 | 6.04 |
| CHEMBL5439202 | — | — | 1 | 5.85 |
| CHEMBL4641092 | — | — | 1 | 5.80 |
| CHEMBL4639113 | — | — | 1 | 5.64 |
| CHEMBL5404562 | — | — | 1 | 5.62 |
| CHEMBL5397307 | — | — | 1 | 5.57 |
| CHEMBL5433232 | — | — | 1 | 5.41 |
| CHEMBL5417825 | — | — | 1 | 5.35 |
| CHEMBL5431351 | — | — | 1 | 5.06 |
| CHEMBL5439150 | — | — | 1 | 5.01 |
| CHEMBL5394506 | — | — | 1 | - |
| CHEMBL5428447 | — | — | 1 | - |
| CHEMBL5404293 | — | — | 1 | - |
| CHEMBL5423909 | — | — | 1 | - |
| CHEMBL5395720 | — | — | 1 | - |
| CHEMBL5422094 | — | — | 1 | - |
| CHEMBL5393977 | — | — | 1 | - |
| CHEMBL5411078 | — | — | 1 | - |
| CHEMBL5437026 | — | — | 1 | - |
| CHEMBL5439117 | — | — | 1 | - |
| CHEMBL5394371 | — | — | 1 | - |
| CHEMBL5439050 | — | — | 1 | - |
| CHEMBL5404788 | — | — | 1 | - |
| CHEMBL5438465 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4173075 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5417823 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL5440288 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL5414407 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5427105 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL5398227 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL5394054 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL5439202 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4641092 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4639113 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5404562 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL5397307 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL5433232 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL5417825 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL5431351 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL5439150 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL5412171 | — | IC50 | - | — | - | |
| CHEMBL5420728 | — | IC50 | - | — | - | |
| CHEMBL5399126 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5395791 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5414724 | — | IC50 | = | 12200000.0 | nM | - |
| CHEMBL5412636 | — | IC50 | = | 414000.0 | nM | - |
| CHEMBL5415217 | — | IC50 | = | 1390000.0 | nM | - |
| CHEMBL5433224 | — | IC50 | = | 179000.0 | nM | - |
| CHEMBL5419647 | — | IC50 | = | 1110000.0 | nM | - |
| CHEMBL5426880 | — | IC50 | = | 367000.0 | nM | - |
| CHEMBL5438465 | — | IC50 | = | 598000.0 | nM | - |
| CHEMBL5404788 | — | IC50 | = | 273000.0 | nM | - |
| CHEMBL5439050 | — | IC50 | = | 558000.0 | nM | - |
| CHEMBL5394371 | — | IC50 | = | 634000.0 | nM | - |
| CHEMBL5439117 | — | IC50 | = | 305000.0 | nM | - |
| CHEMBL5437026 | — | IC50 | = | 271000.0 | nM | - |
| CHEMBL5411078 | — | IC50 | = | 129000.0 | nM | - |
| CHEMBL5393977 | — | IC50 | = | 626000.0 | nM | - |
| CHEMBL5422094 | — | IC50 | = | 299000.0 | nM | - |
| CHEMBL5395720 | — | IC50 | = | 1550000.0 | nM | - |
| CHEMBL5423909 | — | IC50 | = | 616000.0 | nM | - |
| CHEMBL5404293 | — | IC50 | = | 243000.0 | nM | - |
| CHEMBL5428447 | — | IC50 | = | 150000.0 | nM | - |
| CHEMBL5394506 | — | IC50 | = | 252000.0 | nM | - |