Assay Detail
Binding
CHEMBL840218
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards human orexin receptor type 2 was determined using [125I]-Orexin A as radio ligand
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 6.81 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL359632 | — | — | 1 | 8.30 |
| CHEMBL185088 | — | — | 1 | 8.20 |
| CHEMBL185136 | — | — | 1 | 7.70 |
| CHEMBL364814 | — | — | 1 | 7.60 |
| CHEMBL185093 | — | — | 1 | 7.40 |
| CHEMBL185424 | — | — | 1 | 7.30 |
| CHEMBL182473 | — | — | 1 | 7.20 |
| CHEMBL361716 | — | — | 1 | 7.20 |
| CHEMBL185131 | — | — | 1 | 7.10 |
| CHEMBL184596 | — | — | 1 | 7.10 |
| CHEMBL185382 | — | — | 1 | 7.10 |
| CHEMBL185435 | — | — | 1 | 7.10 |
| CHEMBL363951 | — | — | 1 | 7.00 |
| CHEMBL363743 | — | — | 1 | 7.00 |
| CHEMBL183421 | — | — | 1 | 7.00 |
| CHEMBL183576 | — | — | 1 | 6.90 |
| CHEMBL183734 | — | — | 1 | 6.70 |
| CHEMBL185324 | — | — | 1 | 6.70 |
| CHEMBL184936 | — | — | 1 | 6.60 |
| CHEMBL182269 | — | — | 1 | 6.50 |
| CHEMBL184303 | — | — | 1 | 6.40 |
| CHEMBL361748 | — | — | 1 | 6.40 |
| CHEMBL360377 | — | — | 1 | 6.30 |
| CHEMBL185080 | — | — | 1 | 6.00 |
| CHEMBL185005 | — | — | 1 | 5.90 |
| CHEMBL362742 | — | — | 1 | 5.80 |
| CHEMBL363273 | — | — | 1 | 5.80 |
| CHEMBL183786 | — | — | 1 | 5.60 |
| CHEMBL184384 | — | — | 1 | 5.60 |
| CHEMBL185219 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL359632 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL185088 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL185136 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL364814 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL185093 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL185424 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL182473 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL361716 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL185131 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL184596 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL185382 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL185435 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL363951 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL363743 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL183421 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL183576 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL183734 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL185324 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL184936 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL182269 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL184303 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL361748 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL360377 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL185080 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL185005 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL362742 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL363273 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL183786 | — | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL184384 | — | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL185219 | — | Ki | < | 5011.87 | nM | - |