Assay Detail
Binding
CHEMBL708982
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Affinity constant measured against M4 muscarinic receptor rat NG108-15 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | NG108-15 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M4 (CHEMBL317) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and biological activity of some methoctramine-related tetraamines bearing a 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-one moiety as antimuscarinics: a second generation of highly selective M2 muscarinic receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 7.74 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL43383 | — | — | 1 | 8.00 |
| CHEMBL265256 | TRIPITRAMINE | — | 1 | 7.93 |
| CHEMBL27673 | METHOCTRAMINE | — | 1 | 7.58 |
| CHEMBL9967 | PIRENZEPINE | 2.0 | 1 | 7.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL43383 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL265256 | TRIPITRAMINE | Ki | = | 11.75 | nM | 7.93 |
| CHEMBL27673 | METHOCTRAMINE | Ki | = | 26.3 | nM | 7.58 |
| CHEMBL9967 | PIRENZEPINE | Ki | = | 34.67 | nM | 7.46 |