Assay Detail
Functional
CHEMBL3420196
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Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
14
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| EC50 | 13 | 6.92 | 8.69 |
| pEC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3121473 | — | — | 1 | 8.69 |
| CHEMBL3414842 | — | — | 1 | 7.81 |
| CHEMBL3414840 | — | — | 1 | 7.49 |
| CHEMBL3414838 | — | — | 1 | 7.24 |
| CHEMBL3414844 | — | — | 1 | 7.23 |
| CHEMBL3414847 | — | — | 1 | 7.22 |
| CHEMBL3414839 | — | — | 1 | 7.20 |
| CHEMBL3414841 | — | — | 1 | 6.75 |
| CHEMBL3414843 | — | — | 1 | 6.52 |
| CHEMBL667 | ACETYLCHOLINE | 4.0 | 1 | 6.43 |
| CHEMBL3414845 | — | — | 1 | 6.27 |
| CHEMBL550 | PILOCARPINE | 4.0 | 1 | 6.08 |
| CHEMBL608112 | — | — | 1 | 5.08 |
| CHEMBL3414846 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3121473 | — | EC50 | = | 2.042 | nM | 8.69 |
| CHEMBL3414842 | — | EC50 | = | 15.49 | nM | 7.81 |
| CHEMBL3414840 | — | EC50 | = | 32.36 | nM | 7.49 |
| CHEMBL3414838 | — | EC50 | = | 57.54 | nM | 7.24 |
| CHEMBL3414844 | — | EC50 | = | 58.88 | nM | 7.23 |
| CHEMBL3414847 | — | EC50 | = | 60.26 | nM | 7.22 |
| CHEMBL3414839 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL3414841 | — | EC50 | = | 177.83 | nM | 6.75 |
| CHEMBL3414843 | — | EC50 | = | 302.0 | nM | 6.52 |
| CHEMBL667 | ACETYLCHOLINE | EC50 | = | 371.54 | nM | 6.43 |
| CHEMBL3414845 | — | EC50 | = | 537.03 | nM | 6.27 |
| CHEMBL550 | PILOCARPINE | EC50 | = | 831.76 | nM | 6.08 |
| CHEMBL608112 | — | EC50 | = | 8317.64 | nM | 5.08 |
| CHEMBL3414846 | — | pEC50 | - | — | - |