Assay Detail
Binding
CHEMBL3420198
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Displacement of [3H]NMS from human muscarinic M1 acetylcholine receptor expressed in CHO cell membranes by radioligand binding assay
16
Total Activities
16
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Rational design of partial agonists for the muscarinic m1 acetylcholine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 12 | 6.18 | 7.14 |
| Imax | 2 | - | - |
| pKd | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3414840 | — | — | 1 | 7.14 |
| CHEMBL3414842 | — | — | 1 | 7.13 |
| CHEMBL3414839 | — | — | 1 | 6.85 |
| CHEMBL3414838 | — | — | 1 | 6.82 |
| CHEMBL3414844 | — | — | 1 | 6.82 |
| CHEMBL3414847 | — | — | 1 | 6.78 |
| CHEMBL3414841 | — | — | 1 | 6.31 |
| CHEMBL3414843 | — | — | 1 | 6.07 |
| CHEMBL3121473 | — | — | 1 | 5.67 |
| CHEMBL550 | PILOCARPINE | 4.0 | 1 | 5.57 |
| CHEMBL667 | ACETYLCHOLINE | 4.0 | 1 | 4.76 |
| CHEMBL608112 | — | — | 1 | 4.26 |
| CHEMBL3414854 | — | — | 1 | - |
| CHEMBL3414851 | — | — | 1 | - |
| CHEMBL3414845 | — | — | 1 | - |
| CHEMBL3414846 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3414840 | — | Kd | = | 72.44 | nM | 7.14 |
| CHEMBL3414842 | — | Kd | = | 74.13 | nM | 7.13 |
| CHEMBL3414839 | — | Kd | = | 141.25 | nM | 6.85 |
| CHEMBL3414838 | — | Kd | = | 151.36 | nM | 6.82 |
| CHEMBL3414844 | — | Kd | = | 151.36 | nM | 6.82 |
| CHEMBL3414847 | — | Kd | = | 165.96 | nM | 6.78 |
| CHEMBL3414841 | — | Kd | = | 489.78 | nM | 6.31 |
| CHEMBL3414843 | — | Kd | = | 851.14 | nM | 6.07 |
| CHEMBL3121473 | — | Kd | = | 2137.96 | nM | 5.67 |
| CHEMBL550 | PILOCARPINE | Kd | = | 2691.53 | nM | 5.57 |
| CHEMBL667 | ACETYLCHOLINE | Kd | = | 17378.01 | nM | 4.76 |
| CHEMBL608112 | — | Kd | = | 54954.09 | nM | 4.26 |
| CHEMBL3414854 | — | Imax | = | 10.0 | uM | - |
| CHEMBL3414851 | — | Imax | = | 3.0 | uM | - |
| CHEMBL3414845 | — | pKd | - | — | - | |
| CHEMBL3414846 | — | pKd | - | — | - |