Assay Detail
Binding
CHEMBL869740
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]MLA from alpha-7 nAChR in Sprague-Dawley rat brain homogenates
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL4980) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.99 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL378471 | — | — | 1 | 8.80 |
| CHEMBL378349 | — | — | 1 | 8.68 |
| CHEMBL268939 | — | — | 1 | 8.30 |
| CHEMBL210865 | — | — | 1 | 8.20 |
| CHEMBL208565 | — | — | 1 | 8.16 |
| CHEMBL214268 | PHA-543613 | 1.0 | 1 | 8.06 |
| CHEMBL379302 | — | — | 1 | 7.90 |
| CHEMBL378496 | — | — | 1 | 7.82 |
| CHEMBL177611 | PNU-282987 | — | 1 | 7.62 |
| CHEMBL214195 | — | — | 1 | 7.30 |
| CHEMBL211572 | — | — | 1 | 7.08 |
| CHEMBL377032 | — | — | 1 | - |
| CHEMBL214243 | — | — | 1 | - |
| CHEMBL375776 | — | — | 1 | - |
| CHEMBL377036 | — | — | 1 | - |
| CHEMBL212669 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL378471 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL378349 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL268939 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL210865 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL208565 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL214268 | PHA-543613 | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL379302 | — | Ki | = | 12.5 | nM | 7.90 |
| CHEMBL378496 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL177611 | PNU-282987 | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL214195 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL211572 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL377032 | — | Ki | - | — | - | |
| CHEMBL214243 | — | Ki | - | — | - | |
| CHEMBL375776 | — | Ki | - | — | - | |
| CHEMBL377036 | — | Ki | - | — | - | |
| CHEMBL212669 | — | Ki | - | — | - |