Assay Detail
Functional
CHEMBL745485
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonistic activity against M3 muscarinic receptor in guinea pig left ileum derived by plotting log(DR - 1) vs log[antagonist]
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Muscarinic acetylcholine receptor M3 (CHEMBL5498) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
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 |
|---|---|---|---|
| Kd | 16 | 6.17 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL43383 | — | — | 1 | 7.00 |
| CHEMBL442014 | — | — | 1 | 6.90 |
| CHEMBL265256 | TRIPITRAMINE | — | 1 | 6.55 |
| CHEMBL1201996 | — | — | 1 | 6.38 |
| CHEMBL1201997 | — | — | 1 | 6.35 |
| CHEMBL27673 | METHOCTRAMINE | — | 1 | 6.32 |
| CHEMBL116172 | — | — | 1 | 6.24 |
| CHEMBL114885 | — | — | 1 | 6.22 |
| CHEMBL112244 | — | — | 1 | 6.18 |
| CHEMBL1201998 | — | — | 1 | 6.12 |
| CHEMBL114681 | — | — | 1 | 6.08 |
| CHEMBL112208 | — | — | 1 | 5.90 |
| CHEMBL1201995 | — | — | 1 | 5.81 |
| CHEMBL114738 | — | — | 1 | 5.81 |
| CHEMBL1201994 | — | — | 1 | 5.69 |
| CHEMBL115878 | — | — | 1 | 5.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL43383 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL442014 | — | Kd | = | 125.89 | nM | 6.90 |
| CHEMBL265256 | TRIPITRAMINE | Kd | = | 281.84 | nM | 6.55 |
| CHEMBL1201996 | — | Kd | = | 416.87 | nM | 6.38 |
| CHEMBL1201997 | — | Kd | = | 446.68 | nM | 6.35 |
| CHEMBL27673 | METHOCTRAMINE | Kd | = | 478.63 | nM | 6.32 |
| CHEMBL116172 | — | Kd | = | 575.44 | nM | 6.24 |
| CHEMBL114885 | — | Kd | = | 602.56 | nM | 6.22 |
| CHEMBL112244 | — | Kd | = | 660.69 | nM | 6.18 |
| CHEMBL1201998 | — | Kd | = | 758.58 | nM | 6.12 |
| CHEMBL114681 | — | Kd | = | 831.76 | nM | 6.08 |
| CHEMBL112208 | — | Kd | = | 1258.93 | nM | 5.90 |
| CHEMBL1201995 | — | Kd | = | 1548.82 | nM | 5.81 |
| CHEMBL114738 | — | Kd | = | 1548.82 | nM | 5.81 |
| CHEMBL1201994 | — | Kd | = | 2041.74 | nM | 5.69 |
| CHEMBL115878 | — | Kd | = | 7585.78 | nM | 5.12 |