Assay Detail
Functional
CHEMBL748234
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Central presynaptic activity as effect on electrically evoked acetylcholine release from rat hippocampal slices (M2 model)
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Hippocampus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M2 (CHEMBL309) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Muscarinic activity of the thiolactone, lactam, lactol, and thiolactol analogues of pilocarpine and a hypothetical model for the binding of agonists to the m1 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 9 | 5.63 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL316282 | — | — | 1 | 6.40 |
| CHEMBL88578 | — | — | 1 | 6.20 |
| CHEMBL316309 | — | — | 1 | 5.60 |
| CHEMBL313227 | — | — | 1 | 5.50 |
| CHEMBL327363 | — | — | 1 | 5.40 |
| CHEMBL315191 | — | — | 1 | 5.30 |
| CHEMBL550 | PILOCARPINE | 4.0 | 1 | 5.00 |
| CHEMBL90409 | — | — | 1 | - |
| CHEMBL329000 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL316282 | — | Kd | = | 398.11 | nM | 6.40 |
| CHEMBL88578 | — | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL316309 | — | Kd | = | 2511.89 | nM | 5.60 |
| CHEMBL313227 | — | Kd | = | 3162.28 | nM | 5.50 |
| CHEMBL327363 | — | Kd | = | 3981.07 | nM | 5.40 |
| CHEMBL315191 | — | Kd | = | 5011.87 | nM | 5.30 |
| CHEMBL550 | PILOCARPINE | Kd | = | 10000.0 | nM | 5.00 |
| CHEMBL90409 | — | Kd | > | 100000.0 | nM | - |
| CHEMBL329000 | — | Kd | > | 100000.0 | nM | - |