Assay Detail
Binding
CHEMBL743977
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Tested for affinity constant against M4 muscarinic receptor in NG 108-15 cell homogenates using [3H]NMS
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | NG 108-15 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 7.67 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL442014 | — | — | 1 | 8.52 |
| CHEMBL1201996 | — | — | 1 | 8.22 |
| CHEMBL265256 | TRIPITRAMINE | — | 1 | 7.93 |
| CHEMBL1201997 | — | — | 1 | 7.90 |
| CHEMBL43383 | — | — | 1 | 7.82 |
| CHEMBL1201994 | — | — | 1 | 7.80 |
| CHEMBL112244 | — | — | 1 | 7.74 |
| CHEMBL27673 | METHOCTRAMINE | — | 1 | 7.58 |
| CHEMBL9967 | PIRENZEPINE | 2.0 | 1 | 7.46 |
| CHEMBL116172 | — | — | 1 | 7.24 |
| CHEMBL1201998 | — | — | 1 | 7.05 |
| CHEMBL1201995 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL442014 | — | Ki | = | 3.02 | nM | 8.52 |
| CHEMBL1201996 | — | Ki | = | 6.026 | nM | 8.22 |
| CHEMBL265256 | TRIPITRAMINE | Ki | = | 11.75 | nM | 7.93 |
| CHEMBL1201997 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL43383 | — | Ki | = | 15.14 | nM | 7.82 |
| CHEMBL1201994 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL112244 | — | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL27673 | METHOCTRAMINE | Ki | = | 26.3 | nM | 7.58 |
| CHEMBL9967 | PIRENZEPINE | Ki | = | 34.67 | nM | 7.46 |
| CHEMBL116172 | — | Ki | = | 57.54 | nM | 7.24 |
| CHEMBL1201998 | — | Ki | = | 89.13 | nM | 7.05 |
| CHEMBL1201995 | — | Ki | = | 190.55 | nM | 6.72 |