Assay Detail
Binding
CHEMBL3705095
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Radioligand Binding Assay: Radioligand binding assay described in Bergman et. al. Bioorg. Med. Chem. Lett. 2008, 18, 1425-1430.
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Orexin/Hypocretin receptor type 1 (CHEMBL1075232) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Pyridyl piperidine orexin receptor antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 7.80 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3655673 | — | — | 1 | 9.15 |
| CHEMBL3235249 | — | — | 1 | 9.00 |
| CHEMBL3655670 | — | — | 1 | 8.74 |
| CHEMBL2107822 | FILOREXANT | 2.0 | 1 | 8.54 |
| CHEMBL3655674 | — | — | 1 | 8.49 |
| CHEMBL3655664 | — | — | 1 | 8.48 |
| CHEMBL3655672 | — | — | 1 | 8.17 |
| CHEMBL3655676 | — | — | 1 | 8.15 |
| CHEMBL3655680 | — | — | 1 | 8.09 |
| CHEMBL3655675 | — | — | 1 | 8.00 |
| CHEMBL3655671 | — | — | 1 | 7.92 |
| CHEMBL3655667 | — | — | 1 | 7.85 |
| CHEMBL3655679 | — | — | 1 | 7.77 |
| CHEMBL3655665 | — | — | 1 | 7.66 |
| CHEMBL3655669 | — | — | 1 | 7.52 |
| CHEMBL3655677 | — | — | 1 | 7.44 |
| CHEMBL3655681 | — | — | 1 | 7.26 |
| CHEMBL3655683 | — | — | 1 | 7.19 |
| CHEMBL3655678 | — | — | 1 | 7.12 |
| CHEMBL3655668 | — | — | 1 | 7.08 |
| CHEMBL3655682 | — | — | 1 | 7.07 |
| CHEMBL3655663 | — | — | 1 | 7.02 |
| CHEMBL3655684 | — | — | 1 | 6.85 |
| CHEMBL3655666 | — | — | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3655673 | — | Ki | = | 0.71 | nM | 9.15 |
| CHEMBL3235249 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3655670 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL2107822 | FILOREXANT | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL3655674 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL3655664 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL3655672 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL3655676 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL3655680 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL3655675 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL3655671 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL3655667 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL3655679 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL3655665 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL3655669 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL3655677 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL3655681 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL3655683 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL3655678 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL3655668 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL3655682 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL3655663 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL3655684 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL3655666 | — | Ki | = | 260.0 | nM | 6.58 |