Assay Detail
Functional
CHEMBL747116
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist affinity evaluated against Muscarinic acetylcholine receptor M2 in isolated guinea pig left atrium
19
Total Activities
19
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 | Expert |
Publication
Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 19 | 8.48 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1202003 | — | — | 1 | 9.70 |
| CHEMBL265256 | TRIPITRAMINE | — | 1 | 9.65 |
| CHEMBL134692 | — | — | 1 | 9.53 |
| CHEMBL131748 | — | — | 1 | 9.34 |
| CHEMBL133561 | — | — | 1 | 9.30 |
| CHEMBL131865 | — | — | 1 | 9.15 |
| CHEMBL134294 | — | — | 1 | 9.01 |
| CHEMBL1202004 | — | — | 1 | 8.82 |
| CHEMBL1202000 | — | — | 1 | 8.60 |
| CHEMBL132926 | — | — | 1 | 8.57 |
| CHEMBL407678 | — | — | 1 | 8.36 |
| CHEMBL1202001 | — | — | 1 | 8.28 |
| CHEMBL334690 | — | — | 1 | 8.04 |
| CHEMBL335115 | — | — | 1 | 8.01 |
| CHEMBL112244 | — | — | 1 | 7.95 |
| CHEMBL27673 | METHOCTRAMINE | — | 1 | 7.91 |
| CHEMBL1202002 | — | — | 1 | 7.87 |
| CHEMBL265592 | — | — | 1 | 7.75 |
| CHEMBL133993 | — | — | 1 | 5.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1202003 | — | Kd | = | 0.1995 | nM | 9.70 |
| CHEMBL265256 | TRIPITRAMINE | Kd | = | 0.2239 | nM | 9.65 |
| CHEMBL134692 | — | Kd | = | 0.2951 | nM | 9.53 |
| CHEMBL131748 | — | Kd | = | 0.4571 | nM | 9.34 |
| CHEMBL133561 | — | Kd | = | 0.5012 | nM | 9.30 |
| CHEMBL131865 | — | Kd | = | 0.7079 | nM | 9.15 |
| CHEMBL134294 | — | Kd | = | 0.9772 | nM | 9.01 |
| CHEMBL1202004 | — | Kd | = | 1.514 | nM | 8.82 |
| CHEMBL1202000 | — | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL132926 | — | Kd | = | 2.692 | nM | 8.57 |
| CHEMBL407678 | — | Kd | = | 4.365 | nM | 8.36 |
| CHEMBL1202001 | — | Kd | = | 5.248 | nM | 8.28 |
| CHEMBL334690 | — | Kd | = | 9.12 | nM | 8.04 |
| CHEMBL335115 | — | Kd | = | 9.772 | nM | 8.01 |
| CHEMBL112244 | — | Kd | = | 11.22 | nM | 7.95 |
| CHEMBL27673 | METHOCTRAMINE | Kd | = | 12.3 | nM | 7.91 |
| CHEMBL1202002 | — | Kd | = | 13.49 | nM | 7.87 |
| CHEMBL265592 | — | Kd | = | 17.78 | nM | 7.75 |
| CHEMBL133993 | — | Kd | = | 5623.41 | nM | 5.25 |