Assay Detail
Binding
CHEMBL751550
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Binding activity to the muscarinic acetylcholine receptor in rat cortex, assayed using [3H]PZ as a radioligand.
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cortex |
| 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 | 5.80 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL310852 | — | — | 1 | 7.40 |
| CHEMBL108439 | — | — | 1 | 7.16 |
| CHEMBL107491 | — | — | 1 | 7.00 |
| CHEMBL2092935 | — | — | 1 | 6.85 |
| CHEMBL7634 | OXOTREMORINE | — | 1 | 6.85 |
| CHEMBL2092936 | — | — | 1 | 6.77 |
| CHEMBL2111700 | — | — | 1 | 6.72 |
| CHEMBL326905 | — | — | 1 | 6.38 |
| CHEMBL2111699 | — | — | 1 | 5.93 |
| CHEMBL110208 | — | — | 1 | 5.91 |
| CHEMBL111087 | — | — | 1 | 5.83 |
| CHEMBL2111696 | — | — | 1 | 5.80 |
| CHEMBL2111697 | — | — | 1 | 5.79 |
| CHEMBL1203011 | — | — | 1 | 5.69 |
| CHEMBL1203014 | — | — | 1 | 5.65 |
| CHEMBL1203010 | — | — | 1 | 5.51 |
| CHEMBL2092934 | — | — | 1 | 5.39 |
| CHEMBL2111698 | — | — | 1 | 5.28 |
| CHEMBL2111695 | — | — | 1 | 5.25 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 5.24 |
| CHEMBL1203012 | — | — | 1 | 5.22 |
| CHEMBL2092938 | — | — | 1 | 5.19 |
| CHEMBL107713 | — | — | 1 | 5.04 |
| CHEMBL1203013 | — | — | 1 | 4.88 |
| CHEMBL321684 | — | — | 1 | 4.86 |
| CHEMBL2092937 | — | — | 1 | 4.60 |
| CHEMBL108411 | — | — | 1 | 4.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL310852 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL108439 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL107491 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL2092935 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL7634 | OXOTREMORINE | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL2092936 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL2111700 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL326905 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL2111699 | — | Ki | = | 1180.0 | nM | 5.93 |
| CHEMBL110208 | — | Ki | = | 1230.0 | nM | 5.91 |
| CHEMBL111087 | — | Ki | = | 1480.0 | nM | 5.83 |
| CHEMBL2111696 | — | Ki | = | 1590.0 | nM | 5.80 |
| CHEMBL2111697 | — | Ki | = | 1630.0 | nM | 5.79 |
| CHEMBL1203011 | — | Ki | = | 2060.0 | nM | 5.69 |
| CHEMBL1203014 | — | Ki | = | 2220.0 | nM | 5.65 |
| CHEMBL1203010 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL2092934 | — | Ki | = | 4110.0 | nM | 5.39 |
| CHEMBL2111698 | — | Ki | = | 5250.0 | nM | 5.28 |
| CHEMBL2111695 | — | Ki | = | 5600.0 | nM | 5.25 |
| CHEMBL14 | CARBACHOL | Ki | = | 5800.0 | nM | 5.24 |
| CHEMBL1203012 | — | Ki | = | 6050.0 | nM | 5.22 |
| CHEMBL2092938 | — | Ki | = | 6500.0 | nM | 5.19 |
| CHEMBL107713 | — | Ki | = | 9040.0 | nM | 5.04 |
| CHEMBL1203013 | — | Ki | = | 13200.0 | nM | 4.88 |
| CHEMBL321684 | — | Ki | = | 13900.0 | nM | 4.86 |
| CHEMBL2092937 | — | Ki | = | 25200.0 | nM | 4.60 |
| CHEMBL108411 | — | Ki | = | 40000.0 | nM | 4.40 |