Assay Detail
Binding
CHEMBL744152
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Inhibition of [3H]NMS (N-[3H]methylscopolamine) binding to Muscarinic acetylcholine receptor (mAChR)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor (CHEMBL2094109) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
Pyridophens: binary pyridostigmine-aprophen prodrugs with differential inhibition of acetylcholinesterase, butyrylcholinesterase, and muscarinic receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 5.62 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL517712 | ATROPINE | 4.0 | 1 | 8.62 |
| CHEMBL26505 | APROFENE | 2.0 | 1 | 7.29 |
| CHEMBL171501 | — | — | 1 | 5.58 |
| CHEMBL443499 | — | — | 1 | 5.33 |
| CHEMBL422905 | — | — | 1 | 5.09 |
| CHEMBL352808 | — | — | 1 | 4.54 |
| CHEMBL173955 | — | — | 1 | 4.38 |
| CHEMBL172729 | — | — | 1 | 4.12 |
| CHEMBL1115 | PYRIDOSTIGMINE | 4.0 | 1 | - |
| CHEMBL173710 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL517712 | ATROPINE | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL26505 | APROFENE | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL171501 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL443499 | — | Ki | = | 4700.0 | nM | 5.33 |
| CHEMBL422905 | — | Ki | = | 8100.01 | nM | 5.09 |
| CHEMBL352808 | — | Ki | = | 29000.0 | nM | 4.54 |
| CHEMBL173955 | — | Ki | = | 42000.1 | nM | 4.38 |
| CHEMBL172729 | — | Ki | = | 75000.1 | nM | 4.12 |
| CHEMBL1115 | PYRIDOSTIGMINE | Ki | > | 100000.0 | nM | - |
| CHEMBL173710 | — | Ki | > | 100000.0 | nM | - |