Assay Detail
Functional
CHEMBL747677
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist potency against carbachol induced inhibition of electrically stimulated guinea pig atria Muscarinic acetylcholine receptor
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships among methoctramine-related polymethylene tetraamines. Chain-length and substituent effects on M-2 muscarinic receptor blocking activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 16 | 7.10 | 7.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27673 | METHOCTRAMINE | — | 1 | 7.71 |
| CHEMBL168841 | — | — | 1 | 7.57 |
| CHEMBL352334 | — | — | 1 | 7.56 |
| CHEMBL167690 | — | — | 1 | 7.43 |
| CHEMBL168616 | — | — | 1 | 7.23 |
| CHEMBL165700 | — | — | 1 | 7.18 |
| CHEMBL166232 | — | — | 1 | 7.08 |
| CHEMBL166803 | — | — | 1 | 7.02 |
| CHEMBL168786 | — | — | 1 | 7.02 |
| CHEMBL166544 | — | — | 1 | 6.89 |
| CHEMBL167587 | — | — | 1 | 6.87 |
| CHEMBL170554 | — | — | 1 | 6.85 |
| CHEMBL354855 | — | — | 1 | 6.82 |
| CHEMBL168736 | — | — | 1 | 6.79 |
| CHEMBL168304 | — | — | 1 | 6.78 |
| CHEMBL170113 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27673 | METHOCTRAMINE | Kd | = | 19.5 | nM | 7.71 |
| CHEMBL168841 | — | Kd | = | 26.92 | nM | 7.57 |
| CHEMBL352334 | — | Kd | = | 27.54 | nM | 7.56 |
| CHEMBL167690 | — | Kd | = | 37.15 | nM | 7.43 |
| CHEMBL168616 | — | Kd | = | 58.88 | nM | 7.23 |
| CHEMBL165700 | — | Kd | = | 66.07 | nM | 7.18 |
| CHEMBL166232 | — | Kd | = | 83.18 | nM | 7.08 |
| CHEMBL166803 | — | Kd | = | 95.5 | nM | 7.02 |
| CHEMBL168786 | — | Kd | = | 95.5 | nM | 7.02 |
| CHEMBL166544 | — | Kd | = | 128.82 | nM | 6.89 |
| CHEMBL167587 | — | Kd | = | 134.9 | nM | 6.87 |
| CHEMBL170554 | — | Kd | = | 141.25 | nM | 6.85 |
| CHEMBL354855 | — | Kd | = | 151.36 | nM | 6.82 |
| CHEMBL168736 | — | Kd | = | 162.18 | nM | 6.79 |
| CHEMBL168304 | — | Kd | = | 165.96 | nM | 6.78 |
| CHEMBL170113 | — | Kd | = | 177.83 | nM | 6.75 |