Assay Detail
Binding
CHEMBL743966
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Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Submaxillary gland |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M3 (CHEMBL320) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Design, synthesis, and biological activity of methoctramine-related tetraamines bearing an 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4] benzodiazepin-6-one moiety: structural requirements for optimum occupancy of muscarinic receptor subtypes as revealed by symmetrical and unsymmetrical polyamines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 6.26 | 6.81 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1201998 | — | — | 1 | 6.81 |
| CHEMBL442014 | — | — | 1 | 6.76 |
| CHEMBL9967 | PIRENZEPINE | 2.0 | 1 | 6.76 |
| CHEMBL1201994 | — | — | 1 | 6.60 |
| CHEMBL43383 | — | — | 1 | 6.60 |
| CHEMBL112244 | — | — | 1 | 6.33 |
| CHEMBL265256 | TRIPITRAMINE | — | 1 | 6.19 |
| CHEMBL116172 | — | — | 1 | 6.10 |
| CHEMBL27673 | METHOCTRAMINE | — | 1 | 5.96 |
| CHEMBL1201997 | — | — | 1 | 5.60 |
| CHEMBL1201995 | — | — | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1201998 | — | Ki | = | 154.88 | nM | 6.81 |
| CHEMBL442014 | — | Ki | = | 173.78 | nM | 6.76 |
| CHEMBL9967 | PIRENZEPINE | Ki | = | 173.78 | nM | 6.76 |
| CHEMBL1201994 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL43383 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL112244 | — | Ki | = | 467.74 | nM | 6.33 |
| CHEMBL265256 | TRIPITRAMINE | Ki | = | 645.65 | nM | 6.19 |
| CHEMBL116172 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL27673 | METHOCTRAMINE | Ki | = | 1096.48 | nM | 5.96 |
| CHEMBL1201997 | — | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL1201995 | — | Ki | = | 6760.83 | nM | 5.17 |