Assay Detail
Binding
CHEMBL751552
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Binding activity to muscarinic acetylcholine receptor in rat heart, assayed using [3H]QNB as a radioligand in the presence of Gpp(NH)p.
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor (CHEMBL1907609) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Chemical and biochemical studies of 2-propynylpyrrolidine derivatives. Restricted-rotation analogues of N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide (BM-5).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 5.28 | 6.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7634 | OXOTREMORINE | — | 1 | 6.85 |
| CHEMBL310852 | — | — | 1 | 6.75 |
| CHEMBL108439 | — | — | 1 | 6.05 |
| CHEMBL326905 | — | — | 1 | 6.02 |
| CHEMBL107491 | — | — | 1 | 6.00 |
| CHEMBL2111700 | — | — | 1 | 5.98 |
| CHEMBL2092935 | — | — | 1 | 5.97 |
| CHEMBL2092936 | — | — | 1 | 5.79 |
| CHEMBL1203014 | — | — | 1 | 5.68 |
| CHEMBL2111699 | — | — | 1 | 5.51 |
| CHEMBL2111696 | — | — | 1 | 5.30 |
| CHEMBL2111697 | — | — | 1 | 5.26 |
| CHEMBL111087 | — | — | 1 | 5.24 |
| CHEMBL1203010 | — | — | 1 | 5.05 |
| CHEMBL2092934 | — | — | 1 | 4.87 |
| CHEMBL107713 | — | — | 1 | 4.85 |
| CHEMBL1203012 | — | — | 1 | 4.82 |
| CHEMBL1203013 | — | — | 1 | 4.72 |
| CHEMBL2111695 | — | — | 1 | 4.71 |
| CHEMBL2092938 | — | — | 1 | 4.71 |
| CHEMBL1203011 | — | — | 1 | 4.65 |
| CHEMBL2092937 | — | — | 1 | 4.53 |
| CHEMBL2111698 | — | — | 1 | 4.37 |
| CHEMBL321684 | — | — | 1 | 4.33 |
| CHEMBL110208 | — | — | 1 | 4.11 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | - |
| CHEMBL108411 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7634 | OXOTREMORINE | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL310852 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL108439 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL326905 | — | Ki | = | 960.0 | nM | 6.02 |
| CHEMBL107491 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL2111700 | — | Ki | = | 1040.0 | nM | 5.98 |
| CHEMBL2092935 | — | Ki | = | 1070.0 | nM | 5.97 |
| CHEMBL2092936 | — | Ki | = | 1630.0 | nM | 5.79 |
| CHEMBL1203014 | — | Ki | = | 2080.0 | nM | 5.68 |
| CHEMBL2111699 | — | Ki | = | 3120.0 | nM | 5.51 |
| CHEMBL2111696 | — | Ki | = | 5060.0 | nM | 5.30 |
| CHEMBL2111697 | — | Ki | = | 5470.0 | nM | 5.26 |
| CHEMBL111087 | — | Ki | = | 5750.0 | nM | 5.24 |
| CHEMBL1203010 | — | Ki | = | 8860.0 | nM | 5.05 |
| CHEMBL2092934 | — | Ki | = | 13400.0 | nM | 4.87 |
| CHEMBL107713 | — | Ki | = | 14100.0 | nM | 4.85 |
| CHEMBL1203012 | — | Ki | = | 15100.0 | nM | 4.82 |
| CHEMBL1203013 | — | Ki | = | 19100.0 | nM | 4.72 |
| CHEMBL2111695 | — | Ki | = | 19600.0 | nM | 4.71 |
| CHEMBL2092938 | — | Ki | = | 19600.0 | nM | 4.71 |
| CHEMBL1203011 | — | Ki | = | 22600.0 | nM | 4.65 |
| CHEMBL2092937 | — | Ki | = | 29300.0 | nM | 4.53 |
| CHEMBL2111698 | — | Ki | = | 42400.0 | nM | 4.37 |
| CHEMBL321684 | — | Ki | = | 47100.0 | nM | 4.33 |
| CHEMBL110208 | — | Ki | = | 77000.0 | nM | 4.11 |
| CHEMBL14 | CARBACHOL | Ki | = | 160000.0 | nM | - |
| CHEMBL108411 | — | Ki | = | 175000.0 | nM | - |