Assay Detail
Binding
CHEMBL747405
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Ability to displace [3H]cis--2-methyl-5-((dimethylamino)methyl)-1,3-di oxolane from muscarinic acetylcholine receptor in rat cortical tissue.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor (CHEMBL1907609) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Muscarinic activity of the thiolactone, lactam, lactol, and thiolactol analogues of pilocarpine and a hypothetical model for the binding of agonists to the m1 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.85 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7634 | OXOTREMORINE | — | 1 | 8.55 |
| CHEMBL92387 | — | — | 1 | 8.25 |
| CHEMBL327819 | METHAMILANE | — | 1 | 8.19 |
| CHEMBL12587 | MUSCARINE | — | 1 | 7.92 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 7.78 |
| CHEMBL7303 | ARECOLINE | -1.0 | 1 | 7.70 |
| CHEMBL88578 | — | — | 1 | 7.35 |
| CHEMBL313227 | — | — | 1 | 7.27 |
| CHEMBL550 | PILOCARPINE | 4.0 | 1 | 7.10 |
| CHEMBL37132 | — | — | 1 | 7.00 |
| CHEMBL315191 | — | — | 1 | 6.50 |
| CHEMBL316309 | — | — | 1 | 6.48 |
| CHEMBL91776 | — | — | 1 | 6.37 |
| CHEMBL92429 | — | — | 1 | 6.35 |
| CHEMBL327363 | — | — | 1 | 6.15 |
| CHEMBL329000 | — | — | 1 | 6.10 |
| CHEMBL90409 | — | — | 1 | 6.07 |
| CHEMBL313046 | PILOSININE | — | 1 | 5.54 |
| CHEMBL90532 | — | — | 1 | 5.34 |
| CHEMBL92257 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7634 | OXOTREMORINE | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL92387 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL327819 | METHAMILANE | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL12587 | MUSCARINE | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL14 | CARBACHOL | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL7303 | ARECOLINE | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL88578 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL313227 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL550 | PILOCARPINE | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL37132 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL315191 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL316309 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL91776 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL92429 | — | IC50 | = | 445.0 | nM | 6.35 |
| CHEMBL327363 | — | IC50 | = | 705.0 | nM | 6.15 |
| CHEMBL329000 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL90409 | — | IC50 | = | 845.0 | nM | 6.07 |
| CHEMBL313046 | PILOSININE | IC50 | = | 2890.0 | nM | 5.54 |
| CHEMBL90532 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL92257 | — | IC50 | = | 10000.0 | nM | 5.00 |