Assay Detail
Binding
CHEMBL1066456
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]LY278584 from mouse 5HT3 receptor expressed in HEK293 cells
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 38 | 6.40 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL608735 | — | — | 1 | 8.92 |
| CHEMBL597842 | — | — | 1 | 8.47 |
| CHEMBL598873 | — | — | 1 | 8.41 |
| CHEMBL611082 | — | — | 1 | 7.89 |
| CHEMBL605715 | — | — | 1 | 7.04 |
| CHEMBL597681 | — | — | 1 | 6.90 |
| CHEMBL601899 | — | — | 1 | 6.85 |
| CHEMBL598045 | — | — | 1 | 6.79 |
| CHEMBL603052 | — | — | 1 | 6.61 |
| CHEMBL604798 | — | — | 1 | 6.57 |
| CHEMBL597688 | — | — | 1 | 6.26 |
| CHEMBL597843 | — | — | 1 | 6.24 |
| CHEMBL611369 | — | — | 1 | 6.03 |
| CHEMBL599590 | — | — | 1 | 5.94 |
| CHEMBL597241 | — | — | 1 | 5.86 |
| CHEMBL606254 | — | — | 1 | 5.71 |
| CHEMBL606383 | — | — | 1 | 5.67 |
| CHEMBL608144 | — | — | 1 | 5.67 |
| CHEMBL608726 | — | — | 1 | 5.47 |
| CHEMBL597476 | — | — | 1 | 5.43 |
| CHEMBL563848 | — | — | 1 | 5.40 |
| CHEMBL597440 | — | — | 1 | 5.21 |
| CHEMBL610228 | — | — | 1 | 5.20 |
| CHEMBL605573 | — | — | 1 | 5.17 |
| CHEMBL605840 | — | — | 1 | - |
| CHEMBL597687 | — | — | 1 | - |
| CHEMBL605955 | — | — | 1 | - |
| CHEMBL610205 | — | — | 1 | - |
| CHEMBL597276 | — | — | 1 | - |
| CHEMBL597275 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL608735 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL597842 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL598873 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL611082 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL605715 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL597681 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL601899 | — | Ki | = | 141.0 | nM | 6.85 |
| CHEMBL598045 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL603052 | — | Ki | = | 244.0 | nM | 6.61 |
| CHEMBL604798 | — | Ki | = | 269.0 | nM | 6.57 |
| CHEMBL597688 | — | Ki | = | 547.0 | nM | 6.26 |
| CHEMBL597843 | — | Ki | = | 579.0 | nM | 6.24 |
| CHEMBL611369 | — | Ki | = | 926.0 | nM | 6.03 |
| CHEMBL599590 | — | Ki | = | 1140.0 | nM | 5.94 |
| CHEMBL597241 | — | Ki | = | 1370.0 | nM | 5.86 |
| CHEMBL606254 | — | Ki | = | 1960.0 | nM | 5.71 |
| CHEMBL606383 | — | Ki | = | 2117.0 | nM | 5.67 |
| CHEMBL608144 | — | Ki | = | 2120.0 | nM | 5.67 |
| CHEMBL608726 | — | Ki | = | 3390.0 | nM | 5.47 |
| CHEMBL597476 | — | Ki | = | 3673.0 | nM | 5.43 |
| CHEMBL563848 | — | Ki | = | 3993.0 | nM | 5.40 |
| CHEMBL597440 | — | Ki | = | 6200.0 | nM | 5.21 |
| CHEMBL610228 | — | Ki | = | 6340.0 | nM | 5.20 |
| CHEMBL605573 | — | Ki | = | 6830.0 | nM | 5.17 |
| CHEMBL597644 | — | Ki | < | 17.0 | nM | - |
| CHEMBL607857 | — | Ki | < | 17.0 | nM | - |
| CHEMBL597441 | — | Ki | > | 5260.0 | nM | - |
| CHEMBL597737 | — | Ki | > | 3770.0 | nM | - |
| CHEMBL597537 | — | Ki | > | 3580.0 | nM | - |
| CHEMBL610212 | — | Ki | > | 5290.0 | nM | - |
| CHEMBL609622 | — | Ki | > | 5290.0 | nM | - |
| CHEMBL598555 | — | Ki | > | 5260.0 | nM | - |
| CHEMBL597275 | — | Ki | - | — | - | |
| CHEMBL597276 | — | Ki | - | — | - | |
| CHEMBL610205 | — | Ki | > | 5290.0 | nM | - |
| CHEMBL605955 | — | Ki | > | 7140.0 | nM | - |
| CHEMBL597687 | — | Ki | > | 5350.0 | nM | - |
| CHEMBL605840 | — | Ki | > | 5260.0 | nM | - |