Assay Detail
Binding
CHEMBL752398
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Binding affinity for muscarinic acetylcholine receptor M2 by measuring displacement of [3H]QNB from guinea pig heart
39
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
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 | 6.08 | 10.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12980 | QUINUCLIDINYL BENZILATE | — | 1 | 10.35 |
| CHEMBL109405 | — | — | 1 | 7.51 |
| CHEMBL359027 | — | — | 1 | 7.02 |
| CHEMBL144385 | — | — | 1 | 7.00 |
| CHEMBL343236 | — | — | 2 | 6.80 |
| CHEMBL144693 | — | — | 1 | 6.70 |
| CHEMBL344327 | — | — | 1 | 6.57 |
| CHEMBL9967 | PIRENZEPINE | 2.0 | 1 | 6.57 |
| CHEMBL144434 | — | — | 1 | 6.48 |
| CHEMBL341476 | — | — | 1 | 6.41 |
| CHEMBL144751 | — | — | 1 | 6.40 |
| CHEMBL357444 | — | — | 1 | 6.39 |
| CHEMBL144435 | — | — | 1 | 6.34 |
| CHEMBL342958 | — | — | 1 | 6.22 |
| CHEMBL125764 | — | — | 1 | 6.21 |
| CHEMBL144123 | — | — | 1 | 6.00 |
| CHEMBL144580 | — | — | 1 | 5.96 |
| CHEMBL343697 | — | — | 2 | 5.89 |
| CHEMBL14580 | — | — | 1 | 5.82 |
| CHEMBL145488 | — | — | 1 | 5.77 |
| CHEMBL356321 | — | — | 1 | 5.77 |
| CHEMBL144493 | — | — | 1 | 5.72 |
| CHEMBL145081 | — | — | 1 | 5.66 |
| CHEMBL145301 | — | — | 1 | 5.57 |
| CHEMBL64779 | — | — | 1 | 5.55 |
| CHEMBL358505 | — | — | 1 | 5.52 |
| CHEMBL357200 | — | — | 1 | 5.38 |
| CHEMBL343182 | — | — | 2 | 5.30 |
| CHEMBL358493 | — | — | 1 | 5.26 |
| CHEMBL145533 | — | — | 1 | 5.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12980 | QUINUCLIDINYL BENZILATE | Ki | = | 0.045 | nM | 10.35 |
| CHEMBL109405 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL359027 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL144385 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL343236 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL144693 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL344327 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL9967 | PIRENZEPINE | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL144434 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL341476 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL144751 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL357444 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL144435 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL342958 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL125764 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL144123 | — | Ki | = | 990.0 | nM | 6.00 |
| CHEMBL144580 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL343697 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL343236 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL14580 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL145488 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL356321 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL144493 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL145081 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL343697 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL145301 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL64779 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL358505 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL357200 | — | Ki | = | 4200.0 | nM | 5.38 |
| CHEMBL343182 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL358493 | — | Ki | = | 5500.0 | nM | 5.26 |
| CHEMBL145533 | — | Ki | = | 9200.0 | nM | 5.04 |
| CHEMBL357404 | — | Ki | = | 15900.0 | nM | 4.80 |
| CHEMBL144247 | — | Ki | = | 20000.0 | nM | 4.70 |
| CHEMBL423746 | — | Ki | = | 27000.0 | nM | 4.57 |
| CHEMBL145608 | — | Ki | > | 18000.0 | nM | - |
| CHEMBL343242 | — | Ki | > | 18000.0 | nM | - |
| CHEMBL144737 | — | Ki | > | 53000.0 | nM | - |
| CHEMBL343182 | — | Ki | > | 20000.0 | nM | - |