Assay Detail
Binding
CHEMBL4312563
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIF-2alpha (unknown origin) expressed in human 786-O cells measured after 24 hrs by one-glo luciferase reporter gene assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Endothelial PAS domain-containing protein 1 (CHEMBL1744522) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
3-[(1<i>S</i>,2<i>S</i>,3<i>R</i>)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 6.97 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4453227 | — | — | 1 | 8.40 |
| CHEMBL4585668 | BELZUTIFAN | 4.0 | 1 | 7.96 |
| CHEMBL4173075 | — | — | 1 | 7.57 |
| CHEMBL4169671 | — | — | 1 | 7.41 |
| CHEMBL4467490 | — | — | 1 | 6.34 |
| CHEMBL4170809 | — | — | 1 | 6.31 |
| CHEMBL4437382 | — | — | 1 | 6.03 |
| CHEMBL4516708 | — | — | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4453227 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4585668 | BELZUTIFAN | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4173075 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4169671 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4467490 | — | EC50 | = | 460.0 | nM | 6.34 |
| CHEMBL4170809 | — | EC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4437382 | — | EC50 | = | 930.0 | nM | 6.03 |
| CHEMBL4516708 | — | EC50 | = | 1900.0 | nM | 5.72 |