Assay Detail
Binding
CHEMBL932893
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](S)-1-[2-(1-methyl-1H-benzoimidazol-2-ylsulfanyl)-acetyl]-pyrrolidine-2-carboxylic acid biphenyl-2-ylamide from human OX1R expressed in CHO cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Proline bis-amides as potent dual orexin receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.37 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL272715 | — | — | 1 | 9.15 |
| CHEMBL255763 | — | — | 1 | 8.70 |
| CHEMBL429848 | — | — | 1 | 8.52 |
| CHEMBL401653 | — | — | 1 | 8.52 |
| CHEMBL429130 | — | — | 1 | 8.05 |
| CHEMBL256789 | — | — | 1 | 8.00 |
| CHEMBL445161 | — | — | 1 | 7.82 |
| CHEMBL404053 | — | — | 1 | 7.57 |
| CHEMBL403259 | — | — | 1 | 7.55 |
| CHEMBL403667 | — | — | 1 | 7.41 |
| CHEMBL271232 | — | — | 1 | 7.40 |
| CHEMBL404734 | — | — | 1 | 7.31 |
| CHEMBL271438 | — | — | 1 | 7.16 |
| CHEMBL255780 | — | — | 1 | 7.07 |
| CHEMBL404343 | — | — | 1 | 6.92 |
| CHEMBL404153 | — | — | 1 | 6.89 |
| CHEMBL404397 | — | — | 1 | 6.30 |
| CHEMBL258298 | — | — | 1 | 5.85 |
| CHEMBL256788 | — | — | 1 | 5.64 |
| CHEMBL255845 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL272715 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL255763 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL429848 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL401653 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL429130 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL256789 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL445161 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL404053 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL403259 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL403667 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL271232 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL404734 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL271438 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL255780 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL404343 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL404153 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL404397 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL258298 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL256788 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL255845 | — | Ki | = | 2500.0 | nM | 5.60 |