Assay Detail
Functional
CHEMBL5133865
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at OX1R (unknown origin)
30
Total Activities
30
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of orexin 2 receptor selective and dual orexin receptor agonists based on the tetralin structure: Switching of receptor selectivity by chirality on the tetralin ring.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 28 | 6.44 | 7.87 |
| Activity | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5203887 | — | — | 1 | 7.87 |
| CHEMBL438925 | — | — | 1 | 7.52 |
| CHEMBL5205313 | — | — | 1 | 7.51 |
| CHEMBL5204003 | — | — | 1 | 7.26 |
| CHEMBL5189784 | — | — | 1 | 7.06 |
| CHEMBL5198468 | — | — | 1 | 7.05 |
| CHEMBL5200587 | — | — | 1 | 7.04 |
| CHEMBL5180145 | — | — | 1 | 6.95 |
| CHEMBL5171076 | — | — | 1 | 6.92 |
| CHEMBL5186755 | — | — | 1 | 6.64 |
| CHEMBL5200472 | — | — | 1 | 6.54 |
| CHEMBL5201030 | — | — | 1 | 6.45 |
| CHEMBL5197252 | — | — | 1 | 6.43 |
| CHEMBL5194412 | — | — | 1 | 6.40 |
| CHEMBL5194511 | — | — | 1 | 6.15 |
| CHEMBL5199597 | — | — | 1 | 5.93 |
| CHEMBL5192814 | — | — | 1 | 5.91 |
| CHEMBL413434 | OREXIN B | — | 1 | 5.60 |
| CHEMBL5203080 | — | — | 1 | 5.49 |
| CHEMBL5175413 | — | — | 1 | 5.41 |
| CHEMBL5187462 | — | — | 1 | 5.38 |
| CHEMBL5186006 | — | — | 1 | 5.26 |
| CHEMBL5187194 | — | — | 1 | 5.24 |
| CHEMBL4650341 | DANAVOREXTON | 2.0 | 1 | - |
| CHEMBL5187376 | — | — | 1 | - |
| CHEMBL5179969 | — | — | 1 | - |
| CHEMBL5178928 | — | — | 1 | - |
| CHEMBL5186945 | — | — | 1 | - |
| CHEMBL5184945 | — | — | 1 | - |
| CHEMBL5192028 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5203887 | — | EC50 | = | 13.5 | nM | 7.87 |
| CHEMBL438925 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5205313 | — | EC50 | = | 30.7 | nM | 7.51 |
| CHEMBL5204003 | — | EC50 | = | 55.3 | nM | 7.26 |
| CHEMBL5189784 | — | EC50 | = | 86.3 | nM | 7.06 |
| CHEMBL5198468 | — | EC50 | = | 89.0 | nM | 7.05 |
| CHEMBL5200587 | — | EC50 | = | 92.2 | nM | 7.04 |
| CHEMBL5180145 | — | EC50 | = | 112.0 | nM | 6.95 |
| CHEMBL5171076 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5186755 | — | EC50 | = | 229.0 | nM | 6.64 |
| CHEMBL5200472 | — | EC50 | = | 287.0 | nM | 6.54 |
| CHEMBL5201030 | — | EC50 | = | 356.0 | nM | 6.45 |
| CHEMBL5197252 | — | EC50 | = | 372.0 | nM | 6.43 |
| CHEMBL5194412 | — | EC50 | = | 402.0 | nM | 6.40 |
| CHEMBL5194511 | — | EC50 | = | 713.0 | nM | 6.15 |
| CHEMBL5199597 | — | EC50 | = | 1182.0 | nM | 5.93 |
| CHEMBL5192814 | — | EC50 | = | 1244.0 | nM | 5.91 |
| CHEMBL413434 | OREXIN B | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5203080 | — | EC50 | = | 3252.0 | nM | 5.49 |
| CHEMBL5175413 | — | EC50 | = | 3917.0 | nM | 5.41 |
| CHEMBL5187462 | — | EC50 | = | 4180.0 | nM | 5.38 |
| CHEMBL5186006 | — | EC50 | = | 5485.0 | nM | 5.26 |
| CHEMBL5187194 | — | EC50 | = | 5782.0 | nM | 5.24 |
| CHEMBL4650341 | DANAVOREXTON | EC50 | > | 30000.0 | nM | - |
| CHEMBL5187376 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5179969 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5178928 | — | Activity | - | — | - | |
| CHEMBL5186945 | — | Activity | - | — | - | |
| CHEMBL5184945 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5192028 | — | EC50 | > | 10000.0 | nM | - |