Assay Detail
Binding
CHEMBL857564
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Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M3 (CHEMBL320) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 6.54 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL131865 | — | — | 1 | 8.52 |
| CHEMBL134692 | — | — | 1 | 7.15 |
| CHEMBL1202003 | — | — | 1 | 6.96 |
| CHEMBL1202004 | — | — | 1 | 6.94 |
| CHEMBL265256 | TRIPITRAMINE | — | 1 | 6.83 |
| CHEMBL335115 | — | — | 1 | 6.80 |
| CHEMBL112244 | — | — | 1 | 6.48 |
| CHEMBL1202000 | — | — | 1 | 6.40 |
| CHEMBL27673 | METHOCTRAMINE | — | 1 | 6.02 |
| CHEMBL1202002 | — | — | 1 | 5.60 |
| CHEMBL1202001 | — | — | 1 | 5.59 |
| CHEMBL407678 | — | — | 1 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL131865 | — | Ki | = | 3.02 | nM | 8.52 |
| CHEMBL134692 | — | Ki | = | 70.79 | nM | 7.15 |
| CHEMBL1202003 | — | Ki | = | 109.65 | nM | 6.96 |
| CHEMBL1202004 | — | Ki | = | 114.82 | nM | 6.94 |
| CHEMBL265256 | TRIPITRAMINE | Ki | = | 147.91 | nM | 6.83 |
| CHEMBL335115 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL112244 | — | Ki | = | 331.13 | nM | 6.48 |
| CHEMBL1202000 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL27673 | METHOCTRAMINE | Ki | = | 954.99 | nM | 6.02 |
| CHEMBL1202002 | — | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL1202001 | — | Ki | = | 2570.4 | nM | 5.59 |
| CHEMBL407678 | — | Ki | = | 5754.4 | nM | 5.24 |