Assay Detail
Binding
CHEMBL4158423
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at HIF-2alpha in human 786-O cells assessed as free plasma adjusted EC50 for reduction in VEGFA concentration after 24 hrs by ELISA
5
Total Activities
5
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
Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate ( S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 6.64 | 6.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4175320 | — | — | 1 | 6.84 |
| CHEMBL4173075 | — | — | 1 | 6.80 |
| CHEMBL4162398 | — | — | 1 | 6.74 |
| CHEMBL4165848 | — | — | 1 | 6.63 |
| CHEMBL4167415 | — | — | 1 | 6.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4175320 | — | EC50 | = | 145.0 | nM | 6.84 |
| CHEMBL4173075 | — | EC50 | = | 158.0 | nM | 6.80 |
| CHEMBL4162398 | — | EC50 | = | 182.0 | nM | 6.74 |
| CHEMBL4165848 | — | EC50 | = | 233.0 | nM | 6.63 |
| CHEMBL4167415 | — | EC50 | = | 617.0 | nM | 6.21 |