Assay Detail
Binding
CHEMBL932891
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](S)-N-(2-(1H-pyrrol-1-yl)phenyl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX2R 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 | 8.57 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL272715 | — | — | 1 | 10.05 |
| CHEMBL255763 | — | — | 1 | 10.00 |
| CHEMBL429848 | — | — | 1 | 9.70 |
| CHEMBL401653 | — | — | 1 | 9.70 |
| CHEMBL429130 | — | — | 1 | 9.52 |
| CHEMBL256789 | — | — | 1 | 9.22 |
| CHEMBL445161 | — | — | 1 | 9.10 |
| CHEMBL403259 | — | — | 1 | 9.00 |
| CHEMBL255780 | — | — | 1 | 8.70 |
| CHEMBL404734 | — | — | 1 | 8.70 |
| CHEMBL403667 | — | — | 1 | 8.70 |
| CHEMBL404053 | — | — | 1 | 8.52 |
| CHEMBL271438 | — | — | 1 | 8.52 |
| CHEMBL271232 | — | — | 1 | 8.22 |
| CHEMBL404343 | — | — | 1 | 8.10 |
| CHEMBL404153 | — | — | 1 | 7.96 |
| CHEMBL256788 | — | — | 1 | 7.96 |
| CHEMBL255845 | — | — | 1 | 6.88 |
| CHEMBL404397 | — | — | 1 | 6.55 |
| CHEMBL258298 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL272715 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL255763 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL429848 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL401653 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL429130 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL256789 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL445161 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL403259 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL255780 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL404734 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL403667 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL404053 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL271438 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL271232 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL404343 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL404153 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL256788 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL255845 | — | Ki | = | 131.0 | nM | 6.88 |
| CHEMBL404397 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL258298 | — | Ki | = | 560.0 | nM | 6.25 |