Assay Detail
Binding
CHEMBL4312537
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 assessed as reduction in VEGFA level incubated for 20 hrs prior to compound compound washout followed by supplementation of growth medium and subsequent compound addition and measured after 24 hrs by ELISA
6
Total Activities
2
Compounds Tested
3
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 | 2 | 7.56 | 7.77 |
| fEC50 | 2 | - | - |
| fEC85 | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4585668 | BELZUTIFAN | 4.0 | 3 | 7.77 |
| CHEMBL4173075 | — | — | 3 | 7.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4585668 | BELZUTIFAN | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4173075 | — | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4173075 | — | fEC50 | = | 95.0 | ng/ml | - |
| CHEMBL4585668 | BELZUTIFAN | fEC85 | = | 75.0 | ng/ml | - |
| CHEMBL4585668 | BELZUTIFAN | fEC50 | = | 13.0 | ng/ml | - |
| CHEMBL4173075 | — | fEC85 | = | 540.0 | ng/ml | - |