Assay Detail
Binding
CHEMBL3369302
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Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M2 receptor in heart
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M2 (CHEMBL309) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Novel quinuclidinyl heteroarylcarbamate derivatives as muscarinic receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 8.94 | 10.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3298595 | — | — | 1 | 10.57 |
| CHEMBL3298599 | — | — | 1 | 10.28 |
| CHEMBL3298596 | — | — | 1 | 9.92 |
| CHEMBL3545181 | TIOTROPIUM BROMIDE | 4.0 | 1 | 9.82 |
| CHEMBL3298600 | — | — | 1 | 9.68 |
| CHEMBL3298588 | — | — | 1 | 9.34 |
| CHEMBL3298763 | — | — | 1 | 9.19 |
| CHEMBL1908368 | — | — | 1 | 9.11 |
| CHEMBL3298591 | — | — | 1 | 9.10 |
| CHEMBL3298589 | — | — | 1 | 9.09 |
| CHEMBL3298597 | — | — | 1 | 8.92 |
| CHEMBL3298598 | — | — | 1 | 8.92 |
| CHEMBL3298333 | — | — | 1 | 8.85 |
| CHEMBL3298592 | — | — | 1 | 8.72 |
| CHEMBL3298334 | — | — | 1 | 8.44 |
| CHEMBL1779047 | — | — | 1 | 8.42 |
| CHEMBL3298590 | — | — | 1 | 7.89 |
| CHEMBL3298601 | — | — | 1 | 7.85 |
| CHEMBL3298593 | — | — | 1 | 7.41 |
| CHEMBL3298594 | — | — | 1 | 7.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3298595 | — | Ki | = | 0.027 | nM | 10.57 |
| CHEMBL3298599 | — | Ki | = | 0.053 | nM | 10.28 |
| CHEMBL3298596 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL3545181 | TIOTROPIUM BROMIDE | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL3298600 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL3298588 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL3298763 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL1908368 | — | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL3298591 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3298589 | — | Ki | = | 0.82 | nM | 9.09 |
| CHEMBL3298597 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3298598 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3298333 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3298592 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL3298334 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL1779047 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL3298590 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL3298601 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL3298593 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL3298594 | — | Ki | = | 59.0 | nM | 7.23 |