Assay Detail
Binding
CHEMBL748968
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Binding affinity (low) of [3H](R)-QNB binding to Muscarinic acetylcholine receptor M1 expressed in A9 L cell line in the absence of 300 uM GTP-gamma-S
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | A9L |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M1 (CHEMBL3733) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Synthesis and biological characterization of 1,4,5,6-tetrahydropyrimidine and 2-amino-3,4,5,6-tetrahydropyridine derivatives as selective m1 agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.20 | 9.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12378 | — | — | 1 | 9.23 |
| CHEMBL277014 | — | — | 1 | 8.64 |
| CHEMBL542065 | — | — | 1 | 8.54 |
| CHEMBL7303 | ARECOLINE | -1.0 | 1 | 8.48 |
| CHEMBL542064 | — | — | 1 | 8.04 |
| CHEMBL542559 | — | — | 1 | 7.81 |
| CHEMBL21284 | — | — | 1 | 7.76 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 7.70 |
| CHEMBL538467 | — | — | 1 | 7.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12378 | — | Ki | = | 0.589 | nM | 9.23 |
| CHEMBL277014 | — | Ki | = | 2.31 | nM | 8.64 |
| CHEMBL542065 | — | Ki | = | 2.88 | nM | 8.54 |
| CHEMBL7303 | ARECOLINE | Ki | = | 3.33 | nM | 8.48 |
| CHEMBL542064 | — | Ki | = | 9.01 | nM | 8.04 |
| CHEMBL542559 | — | Ki | = | 15.5 | nM | 7.81 |
| CHEMBL21284 | — | Ki | = | 17.4 | nM | 7.76 |
| CHEMBL14 | CARBACHOL | Ki | = | 19.9 | nM | 7.70 |
| CHEMBL538467 | — | Ki | = | 23.6 | nM | 7.63 |