Assay Detail
Binding
CHEMBL3100581
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-neurotensin from sortilin (unknown origin) incubated 30 mins prior to [3H]-neurotensin addition measured after 6 hrs by scintillation proximity assay
20
Total Activities
20
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 |
Publication
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.81 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3098768 | — | — | 1 | 7.00 |
| CHEMBL3098767 | — | — | 1 | 6.77 |
| CHEMBL3098745 | — | — | 1 | 6.48 |
| CHEMBL3098765 | — | — | 1 | 6.31 |
| CHEMBL3098741 | — | — | 1 | 6.15 |
| CHEMBL3098752 | — | — | 1 | 6.08 |
| CHEMBL3098744 | — | — | 1 | 5.96 |
| CHEMBL3098766 | — | — | 1 | 5.89 |
| CHEMBL3098742 | — | — | 1 | 5.85 |
| CHEMBL3098760 | — | — | 1 | 5.80 |
| CHEMBL3098746 | — | — | 1 | 5.77 |
| CHEMBL3098764 | — | — | 1 | 5.75 |
| CHEMBL3098761 | — | — | 1 | 5.62 |
| CHEMBL3098753 | — | — | 1 | 5.47 |
| CHEMBL3098759 | — | — | 1 | 5.44 |
| CHEMBL3098769 | — | — | 1 | 5.40 |
| CHEMBL3098758 | — | — | 1 | 5.28 |
| CHEMBL3098743 | — | — | 1 | 5.19 |
| CHEMBL3098751 | — | — | 1 | 5.04 |
| CHEMBL3098748 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3098768 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3098767 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3098745 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3098765 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL3098741 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL3098752 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL3098744 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3098766 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3098742 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3098760 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3098746 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3098764 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3098761 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3098753 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3098759 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL3098769 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3098758 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL3098743 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL3098751 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL3098748 | — | IC50 | = | 12000.0 | nM | 4.92 |