Assay Detail
Functional
CHEMBL745659
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist affinity evaluated against Muscarinic acetylcholine receptor M3 in isolated guinea pig longitudinal Ileum.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Muscarinic acetylcholine receptor M3 (CHEMBL5498) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 19 | 6.88 | 8.73 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL131748 | — | — | 1 | 8.73 |
| CHEMBL131865 | — | — | 1 | 8.32 |
| CHEMBL134692 | — | — | 1 | 7.86 |
| CHEMBL132926 | — | — | 1 | 7.77 |
| CHEMBL334690 | — | — | 1 | 7.74 |
| CHEMBL134294 | — | — | 1 | 7.71 |
| CHEMBL1202003 | — | — | 1 | 7.35 |
| CHEMBL133561 | — | — | 1 | 7.14 |
| CHEMBL1202004 | — | — | 1 | 6.95 |
| CHEMBL112244 | — | — | 1 | 6.56 |
| CHEMBL265256 | TRIPITRAMINE | — | 1 | 6.55 |
| CHEMBL27673 | METHOCTRAMINE | — | 1 | 6.44 |
| CHEMBL335115 | — | — | 1 | 6.36 |
| CHEMBL1202001 | — | — | 1 | 6.27 |
| CHEMBL407678 | — | — | 1 | 6.26 |
| CHEMBL1202000 | — | — | 1 | 6.04 |
| CHEMBL1202002 | — | — | 1 | 5.79 |
| CHEMBL265592 | — | — | 1 | 5.67 |
| CHEMBL133993 | — | — | 1 | 5.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL131748 | — | Kd | = | 1.862 | nM | 8.73 |
| CHEMBL131865 | — | Kd | = | 4.786 | nM | 8.32 |
| CHEMBL134692 | — | Kd | = | 13.8 | nM | 7.86 |
| CHEMBL132926 | — | Kd | = | 16.98 | nM | 7.77 |
| CHEMBL334690 | — | Kd | = | 18.2 | nM | 7.74 |
| CHEMBL134294 | — | Kd | = | 19.5 | nM | 7.71 |
| CHEMBL1202003 | — | Kd | = | 44.67 | nM | 7.35 |
| CHEMBL133561 | — | Kd | = | 72.44 | nM | 7.14 |
| CHEMBL1202004 | — | Kd | = | 112.2 | nM | 6.95 |
| CHEMBL112244 | — | Kd | = | 275.42 | nM | 6.56 |
| CHEMBL265256 | TRIPITRAMINE | Kd | = | 281.84 | nM | 6.55 |
| CHEMBL27673 | METHOCTRAMINE | Kd | = | 363.08 | nM | 6.44 |
| CHEMBL335115 | — | Kd | = | 436.52 | nM | 6.36 |
| CHEMBL1202001 | — | Kd | = | 537.03 | nM | 6.27 |
| CHEMBL407678 | — | Kd | = | 549.54 | nM | 6.26 |
| CHEMBL1202000 | — | Kd | = | 912.01 | nM | 6.04 |
| CHEMBL1202002 | — | Kd | = | 1621.81 | nM | 5.79 |
| CHEMBL265592 | — | Kd | = | 2137.96 | nM | 5.67 |
| CHEMBL133993 | — | Kd | = | 7244.36 | nM | 5.14 |