Assay Detail
Binding
CHEMBL4312562
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-(3-Chlorophenyl-4,6-t2)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine binding to his-tagged HIF-2alpha PAS-B domain (unknown origin) measured after 1 hr by scintillation proximity assay
10
Total Activities
10
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 |
|---|---|---|---|
| IC50 | 10 | 6.92 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4585668 | BELZUTIFAN | 4.0 | 1 | 8.05 |
| CHEMBL4453227 | — | — | 1 | 8.05 |
| CHEMBL4173075 | — | — | 1 | 7.92 |
| CHEMBL4169671 | — | — | 1 | 7.39 |
| CHEMBL4437382 | — | — | 1 | 6.80 |
| CHEMBL4467490 | — | — | 1 | 6.68 |
| CHEMBL4170809 | — | — | 1 | 6.46 |
| CHEMBL4516708 | — | — | 1 | 5.72 |
| CHEMBL4441175 | — | — | 1 | 5.19 |
| CHEMBL4434904 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4585668 | BELZUTIFAN | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4453227 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4173075 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4169671 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4437382 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4467490 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4170809 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4516708 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4441175 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL4434904 | — | IC50 | > | 10000.0 | nM | - |