Assay Detail
Binding
CHEMBL3385319
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-Orexin A from human OX1R expressed in CHO cells after 30 mins by topcount analysis
24
Total Activities
23
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
Design, synthesis, and structure-activity relationships of a series of novel N-aryl-2-phenylcyclopropanecarboxamide that are potent and orally active orexin receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 6.16 | 8.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3343242 | — | — | 1 | 8.14 |
| CHEMBL3343258 | — | — | 1 | 6.99 |
| CHEMBL3343260 | — | — | 2 | 6.97 |
| CHEMBL3343257 | — | — | 1 | 6.97 |
| CHEMBL3343259 | — | — | 1 | 6.91 |
| CHEMBL3343252 | — | — | 1 | 6.69 |
| CHEMBL3343254 | — | — | 1 | 6.54 |
| CHEMBL3343256 | — | — | 1 | 6.30 |
| CHEMBL3343250 | — | — | 1 | 6.13 |
| CHEMBL3343251 | — | — | 1 | 6.11 |
| CHEMBL3343255 | — | — | 1 | 6.08 |
| CHEMBL3343246 | — | — | 1 | 5.97 |
| CHEMBL3343253 | — | — | 1 | 5.85 |
| CHEMBL3343243 | — | — | 1 | 5.52 |
| CHEMBL3343241 | — | — | 1 | 5.38 |
| CHEMBL3341773 | — | — | 1 | 5.26 |
| CHEMBL3343247 | — | — | 1 | 5.17 |
| CHEMBL3343244 | — | — | 1 | 5.12 |
| CHEMBL3343245 | — | — | 1 | 5.00 |
| CHEMBL3343249 | — | — | 1 | - |
| CHEMBL3343239 | — | — | 1 | - |
| CHEMBL3343248 | — | — | 1 | - |
| CHEMBL3343240 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3343242 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL3343258 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL3343260 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL3343257 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL3343259 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL3343252 | — | Ki | = | 206.0 | nM | 6.69 |
| CHEMBL3343254 | — | Ki | = | 291.0 | nM | 6.54 |
| CHEMBL3343256 | — | Ki | = | 505.0 | nM | 6.30 |
| CHEMBL3343250 | — | Ki | = | 747.0 | nM | 6.13 |
| CHEMBL3343251 | — | Ki | = | 772.0 | nM | 6.11 |
| CHEMBL3343255 | — | Ki | = | 832.0 | nM | 6.08 |
| CHEMBL3343246 | — | Ki | = | 1068.0 | nM | 5.97 |
| CHEMBL3343253 | — | Ki | = | 1425.0 | nM | 5.85 |
| CHEMBL3343243 | — | Ki | = | 2994.0 | nM | 5.52 |
| CHEMBL3343241 | — | Ki | = | 4161.0 | nM | 5.38 |
| CHEMBL3341773 | — | Ki | = | 5538.0 | nM | 5.26 |
| CHEMBL3343247 | — | Ki | = | 6841.0 | nM | 5.17 |
| CHEMBL3343244 | — | Ki | = | 7535.0 | nM | 5.12 |
| CHEMBL3343245 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL3343248 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3343249 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3343239 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3343260 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL3343240 | — | Ki | > | 10000.0 | nM | - |