Assay Detail
Binding
CHEMBL749018
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding affinity for muscarinic M1 receptor by displacing [3H]pirenzepine 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 | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M1 (CHEMBL276) ↗| Type | SINGLE PROTEIN |
| 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 | 6.80 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL335308 | — | — | 1 | 8.20 |
| CHEMBL134063 | — | — | 1 | 8.11 |
| CHEMBL339438 | — | — | 1 | 7.89 |
| CHEMBL130693 | — | — | 1 | 7.82 |
| CHEMBL130689 | — | — | 1 | 7.68 |
| CHEMBL131095 | — | — | 1 | 7.62 |
| CHEMBL130842 | — | — | 1 | 7.58 |
| CHEMBL130111 | — | — | 1 | 7.57 |
| CHEMBL338122 | — | — | 1 | 7.52 |
| CHEMBL278422 | — | — | 1 | 7.50 |
| CHEMBL129886 | — | — | 1 | 7.46 |
| CHEMBL131428 | ALVAMELINE | 2.0 | 1 | 7.44 |
| CHEMBL130927 | — | — | 1 | 7.43 |
| CHEMBL334493 | — | — | 1 | 7.43 |
| CHEMBL130127 | — | — | 1 | 7.40 |
| CHEMBL130688 | — | — | 1 | 7.36 |
| CHEMBL132503 | — | — | 1 | 7.24 |
| CHEMBL339175 | — | — | 1 | 7.11 |
| CHEMBL132894 | — | — | 3 | 7.08 |
| CHEMBL132502 | — | — | 1 | 7.08 |
| CHEMBL129998 | — | — | 1 | 7.00 |
| CHEMBL131777 | — | — | 3 | 7.00 |
| CHEMBL134177 | — | — | 1 | 6.92 |
| CHEMBL133905 | — | — | 1 | 6.92 |
| CHEMBL336834 | — | — | 1 | 6.85 |
| CHEMBL130387 | — | — | 1 | 6.75 |
| CHEMBL337474 | — | — | 1 | 6.60 |
| CHEMBL134122 | — | — | 1 | 6.58 |
| CHEMBL341193 | — | — | 1 | 6.58 |
| CHEMBL133680 | — | — | 1 | 6.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL335308 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL134063 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL339438 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL130693 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL130689 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL131095 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL130842 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL130111 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL338122 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL278422 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL129886 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL131428 | ALVAMELINE | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL130927 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL334493 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL130127 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL130688 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL132503 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL339175 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL132894 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL132502 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL131777 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL129998 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL134177 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL133905 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL336834 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL132894 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL132894 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL131777 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL130387 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL131777 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL337474 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL341193 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL134122 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL133680 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL273308 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL133961 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL74300 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL14 | CARBACHOL | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL335920 | — | Ki | = | 770.0 | nM | 6.11 |
| CHEMBL129923 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL131753 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL337676 | — | Ki | = | 960.0 | nM | 6.02 |
| CHEMBL440903 | — | Ki | = | 960.0 | nM | 6.02 |
| CHEMBL130148 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL130625 | — | Ki | = | 1350.0 | nM | 5.87 |
| CHEMBL130342 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL133986 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL554487 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL131249 | — | Ki | = | 4800.0 | nM | 5.32 |
| CHEMBL133184 | — | Ki | = | 24000.0 | nM | 4.62 |