Assay Detail
Functional
CHEMBL703401
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonistic activity measured in isolated guinea pig left atrium (M2 receptor)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Cardiac atrium |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
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 |
|---|---|---|---|
| Kd | 5 | 8.62 | 9.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL265256 | TRIPITRAMINE | — | 1 | 9.75 |
| CHEMBL442014 | — | — | 1 | 9.14 |
| CHEMBL43383 | — | — | 1 | 8.50 |
| CHEMBL114885 | — | — | 1 | 7.90 |
| CHEMBL27673 | METHOCTRAMINE | — | 1 | 7.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL265256 | TRIPITRAMINE | Kd | = | 0.1778 | nM | 9.75 |
| CHEMBL442014 | — | Kd | = | 0.7244 | nM | 9.14 |
| CHEMBL43383 | — | Kd | = | 3.162 | nM | 8.50 |
| CHEMBL114885 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL27673 | METHOCTRAMINE | Kd | = | 15.14 | nM | 7.82 |