Assay Detail
Binding
CHEMBL709393
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity constant measured against M2 muscarinic receptor in rat heart r
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Heart |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M2 (CHEMBL309) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and biological activity of some methoctramine-related tetraamines bearing a 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-one moiety as antimuscarinics: a second generation of highly selective M2 muscarinic receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 2 | 7.82 | 9.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL265256 | TRIPITRAMINE | — | 1 | 9.54 |
| CHEMBL9967 | PIRENZEPINE | 2.0 | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL265256 | TRIPITRAMINE | Ki | = | 0.2884 | nM | 9.54 |
| CHEMBL9967 | PIRENZEPINE | Ki | = | 794.33 | nM | 6.10 |