Assay Detail
Binding
CHEMBL3588583
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human OX1R by radioligand displacement binding assay
27
Total Activities
27
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
Discovery of (1R,2S)-2-{[(2,4-Dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide (E2006): A Potent and Efficacious Oral Orexin Receptor Antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 7.09 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3585957 | — | — | 1 | 8.70 |
| CHEMBL3585952 | — | — | 1 | 8.52 |
| CHEMBL3545367 | LEMBOREXANT | 4.0 | 1 | 8.22 |
| CHEMBL3585951 | — | — | 1 | 8.22 |
| CHEMBL3585955 | — | — | 1 | 8.15 |
| CHEMBL3585956 | — | — | 1 | 7.85 |
| CHEMBL3585948 | — | — | 1 | 7.41 |
| CHEMBL3585954 | — | — | 1 | 7.41 |
| CHEMBL3585942 | — | — | 1 | 7.37 |
| CHEMBL3585941 | — | — | 1 | 7.14 |
| CHEMBL3585953 | — | — | 1 | 7.09 |
| CHEMBL3343259 | — | — | 1 | 6.97 |
| CHEMBL3585940 | — | — | 1 | 6.92 |
| CHEMBL3585949 | — | — | 1 | 6.91 |
| CHEMBL3585947 | — | — | 1 | 6.86 |
| CHEMBL3585946 | — | — | 1 | 6.86 |
| CHEMBL3585938 | — | — | 1 | 6.77 |
| CHEMBL3585950 | — | — | 1 | 6.65 |
| CHEMBL3585936 | — | — | 1 | 6.41 |
| CHEMBL3585944 | — | — | 1 | 6.41 |
| CHEMBL3585933 | — | — | 1 | 6.03 |
| CHEMBL3585943 | — | — | 1 | 5.99 |
| CHEMBL3585945 | — | — | 1 | 5.80 |
| CHEMBL3585939 | — | — | 1 | 5.60 |
| CHEMBL3585934 | — | — | 1 | - |
| CHEMBL3585935 | — | — | 1 | - |
| CHEMBL3585937 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3585957 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3585952 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3545367 | LEMBOREXANT | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL3585951 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL3585955 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL3585956 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL3585948 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL3585954 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL3585942 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL3585941 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL3585953 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL3343259 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL3585940 | — | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL3585949 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL3585947 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL3585946 | — | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL3585938 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL3585950 | — | Ki | = | 224.0 | nM | 6.65 |
| CHEMBL3585936 | — | Ki | = | 391.0 | nM | 6.41 |
| CHEMBL3585944 | — | Ki | = | 391.0 | nM | 6.41 |
| CHEMBL3585933 | — | Ki | = | 938.0 | nM | 6.03 |
| CHEMBL3585943 | — | Ki | = | 1016.0 | nM | 5.99 |
| CHEMBL3585945 | — | Ki | = | 1581.0 | nM | 5.80 |
| CHEMBL3585939 | — | Ki | = | 2491.0 | nM | 5.60 |
| CHEMBL3585934 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL3585935 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL3585937 | — | Ki | > | 2000.0 | nM | - |