Assay Detail
Functional
CHEMBL881931
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Efficacy at muscarinic acetylcholine receptor M1 measured by the ability to inhibit the electrically stimulated twitch of the rabbit vas deferens
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Tissue | Vas deferens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Novel functional M1 selective muscarinic agonists. 2. Synthesis and structure-activity relationships of 3-pyrazinyl-1,2,5,6-tetrahydro-1-methylpyridines. Construction of a molecular model for the M1 pharmacophore.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.84 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL101054 | — | — | 1 | 8.52 |
| CHEMBL327289 | — | — | 1 | 8.05 |
| CHEMBL120399 | — | — | 1 | 6.65 |
| CHEMBL307645 | — | — | 1 | 6.27 |
| CHEMBL7303 | ARECOLINE | -1.0 | 1 | 6.26 |
| CHEMBL130807 | — | — | 1 | 5.29 |
| CHEMBL131819 | TAZOMELINE | 2.0 | 1 | - |
| CHEMBL130715 | — | — | 1 | - |
| CHEMBL327754 | — | — | 1 | - |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL101054 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL327289 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL120399 | — | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL307645 | — | IC50 | = | 537.0 | nM | 6.27 |
| CHEMBL7303 | ARECOLINE | IC50 | = | 545.0 | nM | 6.26 |
| CHEMBL130807 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL131819 | TAZOMELINE | IC50 | = | 0.001 | nM | - |
| CHEMBL130715 | — | IC50 | = | 0.002 | nM | - |
| CHEMBL327754 | — | IC50 | = | 0.004 | nM | - |
| CHEMBL21536 | XANOMELINE | IC50 | = | 0.008 | nM | - |