Assay Detail
Binding
CHEMBL748359
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Tested for affinity constant against M2 muscarinic receptor rat heart using [3H]-NMS
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 M2 (CHEMBL309) ↗| 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 | 12 | 8.19 | 9.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL265256 | TRIPITRAMINE | — | 1 | 9.54 |
| CHEMBL1201996 | — | — | 1 | 8.80 |
| CHEMBL116172 | — | — | 1 | 8.77 |
| CHEMBL442014 | — | — | 1 | 8.62 |
| CHEMBL43383 | — | — | 1 | 8.49 |
| CHEMBL1201994 | — | — | 1 | 8.43 |
| CHEMBL112244 | — | — | 1 | 8.37 |
| CHEMBL1201995 | — | — | 1 | 7.89 |
| CHEMBL27673 | METHOCTRAMINE | — | 1 | 7.84 |
| CHEMBL1201997 | — | — | 1 | 7.73 |
| CHEMBL1201998 | — | — | 1 | 7.66 |
| CHEMBL9967 | PIRENZEPINE | 2.0 | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL265256 | TRIPITRAMINE | Ki | = | 0.2884 | nM | 9.54 |
| CHEMBL1201996 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL116172 | — | Ki | = | 1.698 | nM | 8.77 |
| CHEMBL442014 | — | Ki | = | 2.399 | nM | 8.62 |
| CHEMBL43383 | — | Ki | = | 3.236 | nM | 8.49 |
| CHEMBL1201994 | — | Ki | = | 3.715 | nM | 8.43 |
| CHEMBL112244 | — | Ki | = | 4.266 | nM | 8.37 |
| CHEMBL1201995 | — | Ki | = | 12.88 | nM | 7.89 |
| CHEMBL27673 | METHOCTRAMINE | Ki | = | 14.45 | nM | 7.84 |
| CHEMBL1201997 | — | Ki | = | 18.62 | nM | 7.73 |
| CHEMBL1201998 | — | Ki | = | 21.88 | nM | 7.66 |
| CHEMBL9967 | PIRENZEPINE | Ki | = | 794.33 | nM | 6.10 |