Assay Detail
Binding
CHEMBL752316
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Ability to displace [3H]pirenzepine (pir) from muscarinic acetylcholine receptor M1 in rat cortical tissue.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M1 (CHEMBL276) ↗| Type | SINGLE PROTEIN |
| 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 | 5.81 | 7.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL88578 | — | — | 1 | 7.29 |
| CHEMBL7634 | OXOTREMORINE | — | 1 | 6.95 |
| CHEMBL37132 | — | — | 1 | 6.54 |
| CHEMBL316309 | — | — | 1 | 6.54 |
| CHEMBL313227 | — | — | 1 | 6.36 |
| CHEMBL327363 | — | — | 1 | 6.16 |
| CHEMBL315191 | — | — | 1 | 6.11 |
| CHEMBL550 | PILOCARPINE | 4.0 | 1 | 6.02 |
| CHEMBL92387 | — | — | 1 | 5.85 |
| CHEMBL7303 | ARECOLINE | -1.0 | 1 | 5.76 |
| CHEMBL92429 | — | — | 1 | 5.75 |
| CHEMBL91776 | — | — | 1 | 5.75 |
| CHEMBL327819 | METHAMILANE | — | 1 | 5.68 |
| CHEMBL90409 | — | — | 1 | 5.29 |
| CHEMBL12587 | MUSCARINE | — | 1 | 5.25 |
| CHEMBL313046 | PILOSININE | — | 1 | 5.00 |
| CHEMBL329000 | — | — | 1 | 5.00 |
| CHEMBL92257 | — | — | 1 | 5.00 |
| CHEMBL90532 | — | — | 1 | 4.99 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 4.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL88578 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL7634 | OXOTREMORINE | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL37132 | — | IC50 | = | 288.0 | nM | 6.54 |
| CHEMBL316309 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL313227 | — | IC50 | = | 435.0 | nM | 6.36 |
| CHEMBL327363 | — | IC50 | = | 695.0 | nM | 6.16 |
| CHEMBL315191 | — | IC50 | = | 775.0 | nM | 6.11 |
| CHEMBL550 | PILOCARPINE | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL92387 | — | IC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL7303 | ARECOLINE | IC50 | = | 1740.0 | nM | 5.76 |
| CHEMBL92429 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL91776 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL327819 | METHAMILANE | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL90409 | — | IC50 | = | 5150.0 | nM | 5.29 |
| CHEMBL12587 | MUSCARINE | IC50 | = | 5680.0 | nM | 5.25 |
| CHEMBL313046 | PILOSININE | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL329000 | — | IC50 | = | 9950.0 | nM | 5.00 |
| CHEMBL92257 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL90532 | — | IC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL14 | CARBACHOL | IC50 | = | 11850.0 | nM | 4.93 |