Assay Detail
Binding
CHEMBL748211
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding affinity for muscarinic receptor by displacing [3H]oxotremorine-M binding on rat brain homogenate.
50
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor (CHEMBL1907609) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 50 | 7.64 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL133961 | — | — | 1 | 9.47 |
| CHEMBL129886 | — | — | 1 | 9.11 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 8.89 |
| CHEMBL134063 | — | — | 1 | 8.80 |
| CHEMBL131095 | — | — | 1 | 8.77 |
| CHEMBL339438 | — | — | 1 | 8.60 |
| CHEMBL132894 | — | — | 3 | 8.60 |
| CHEMBL130693 | — | — | 1 | 8.59 |
| CHEMBL132503 | — | — | 1 | 8.55 |
| CHEMBL133905 | — | — | 1 | 8.43 |
| CHEMBL130625 | — | — | 1 | 8.35 |
| CHEMBL130688 | — | — | 1 | 8.35 |
| CHEMBL335308 | — | — | 1 | 8.33 |
| CHEMBL129998 | — | — | 1 | 8.31 |
| CHEMBL334493 | — | — | 1 | 8.30 |
| CHEMBL339175 | — | — | 1 | 8.21 |
| CHEMBL337474 | — | — | 1 | 8.21 |
| CHEMBL131428 | ALVAMELINE | 2.0 | 1 | 8.04 |
| CHEMBL341193 | — | — | 1 | 7.96 |
| CHEMBL130689 | — | — | 1 | 7.89 |
| CHEMBL273308 | — | — | 1 | 7.85 |
| CHEMBL130842 | — | — | 1 | 7.80 |
| CHEMBL74300 | — | — | 1 | 7.75 |
| CHEMBL337676 | — | — | 1 | 7.64 |
| CHEMBL131777 | — | — | 3 | 7.60 |
| CHEMBL338122 | — | — | 1 | 7.51 |
| CHEMBL134122 | — | — | 1 | 7.51 |
| CHEMBL130127 | — | — | 1 | 7.48 |
| CHEMBL554487 | — | — | 1 | 7.48 |
| CHEMBL278422 | — | — | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL133961 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL129886 | — | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL14 | CARBACHOL | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL134063 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL131095 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL132894 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL339438 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL130693 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL132503 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL133905 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL130625 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL130688 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL335308 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL129998 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL334493 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL132894 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL339175 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL337474 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL132894 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL131428 | ALVAMELINE | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL341193 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL130689 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL273308 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL130842 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL74300 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL337676 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL131777 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL338122 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL134122 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL130127 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL554487 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL131777 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL131777 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL278422 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL130387 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL130111 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL336834 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL132502 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL134177 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL130927 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL131753 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL130148 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL133680 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL133986 | — | Ki | = | 318.0 | nM | 6.50 |
| CHEMBL130342 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL129923 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL440903 | — | Ki | = | 570.0 | nM | 6.24 |
| CHEMBL335920 | — | Ki | = | 990.0 | nM | 6.00 |
| CHEMBL131249 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL133184 | — | Ki | = | 5400.0 | nM | 5.27 |