Assay Detail
Binding
CHEMBL743825
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity for muscarinic acetylcholine receptor M3 by measuring displacement of [3H]QNB from guinea pig parotid gland
39
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Muscarinic acetylcholine receptor M3 (CHEMBL5498) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
3-Heteroaryl-substituted quinuclidin-3-ol and quinuclidin-2-ene derivatives as muscarinic antagonists. Synthesis and structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 39 | 5.69 | 9.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12980 | QUINUCLIDINYL BENZILATE | — | 1 | 9.62 |
| CHEMBL109405 | — | — | 1 | 7.23 |
| CHEMBL359027 | — | — | 1 | 6.96 |
| CHEMBL9967 | PIRENZEPINE | 2.0 | 1 | 6.96 |
| CHEMBL144385 | — | — | 1 | 6.80 |
| CHEMBL144693 | — | — | 1 | 6.62 |
| CHEMBL343236 | — | — | 2 | 6.47 |
| CHEMBL344327 | — | — | 1 | 6.38 |
| CHEMBL144751 | — | — | 1 | 6.14 |
| CHEMBL357444 | — | — | 1 | 6.13 |
| CHEMBL144123 | — | — | 1 | 5.96 |
| CHEMBL342958 | — | — | 1 | 5.96 |
| CHEMBL341476 | — | — | 1 | 5.96 |
| CHEMBL125764 | — | — | 1 | 5.92 |
| CHEMBL144435 | — | — | 1 | 5.89 |
| CHEMBL144434 | — | — | 1 | 5.85 |
| CHEMBL144580 | — | — | 1 | 5.66 |
| CHEMBL356321 | — | — | 1 | 5.58 |
| CHEMBL145081 | — | — | 1 | 5.57 |
| CHEMBL14580 | — | — | 1 | 5.51 |
| CHEMBL358505 | — | — | 1 | 5.42 |
| CHEMBL144493 | — | — | 1 | 5.40 |
| CHEMBL145301 | — | — | 1 | 5.36 |
| CHEMBL145488 | — | — | 1 | 5.31 |
| CHEMBL357200 | — | — | 1 | 5.27 |
| CHEMBL343697 | — | — | 2 | 5.24 |
| CHEMBL64779 | — | — | 1 | 5.23 |
| CHEMBL145533 | — | — | 1 | 5.08 |
| CHEMBL343182 | — | — | 2 | 4.89 |
| CHEMBL358493 | — | — | 1 | 4.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12980 | QUINUCLIDINYL BENZILATE | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL109405 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL9967 | PIRENZEPINE | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL359027 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL144385 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL144693 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL343236 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL344327 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL144751 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL357444 | — | Ki | = | 740.0 | nM | 6.13 |
| CHEMBL342958 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL341476 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL144123 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL125764 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL144435 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL144434 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL144580 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL343236 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL356321 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL145081 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL14580 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL358505 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL144493 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL145301 | — | Ki | = | 4400.0 | nM | 5.36 |
| CHEMBL145488 | — | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL357200 | — | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL343697 | — | Ki | = | 5700.0 | nM | 5.24 |
| CHEMBL64779 | — | Ki | = | 5900.0 | nM | 5.23 |
| CHEMBL343697 | — | Ki | = | 7500.0 | nM | 5.12 |
| CHEMBL145533 | — | Ki | = | 8400.0 | nM | 5.08 |
| CHEMBL343182 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL358493 | — | Ki | = | 16000.0 | nM | 4.80 |
| CHEMBL343182 | — | Ki | = | 24000.0 | nM | 4.62 |
| CHEMBL357404 | — | Ki | = | 29900.0 | nM | 4.52 |
| CHEMBL343242 | — | Ki | = | 37000.0 | nM | 4.43 |
| CHEMBL144247 | — | Ki | = | 38000.0 | nM | 4.42 |
| CHEMBL145608 | — | Ki | = | 48000.0 | nM | 4.32 |
| CHEMBL423746 | — | Ki | = | 67000.0 | nM | 4.17 |
| CHEMBL144737 | — | Ki | > | 53000.0 | nM | - |