Assay Detail
Binding
CHEMBL747393
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Binding affinity for muscarinic acetylcholine receptor M1 by measuring displacement of [3H]QNB from guinea pig cerebral cortex
40
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cerebral cortex |
| 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 | 40 | 6.28 | 10.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12980 | QUINUCLIDINYL BENZILATE | — | 1 | 10.29 |
| CHEMBL109405 | — | — | 1 | 8.02 |
| CHEMBL9967 | PIRENZEPINE | 2.0 | 1 | 7.85 |
| CHEMBL144385 | — | — | 1 | 7.47 |
| CHEMBL359027 | — | — | 1 | 7.43 |
| CHEMBL144693 | — | — | 1 | 7.24 |
| CHEMBL343236 | — | — | 2 | 7.23 |
| CHEMBL344327 | — | — | 1 | 7.09 |
| CHEMBL144751 | — | — | 1 | 7.00 |
| CHEMBL342958 | — | — | 1 | 6.77 |
| CHEMBL357444 | — | — | 1 | 6.66 |
| CHEMBL125764 | — | — | 1 | 6.54 |
| CHEMBL341476 | — | — | 1 | 6.52 |
| CHEMBL144435 | — | — | 1 | 6.44 |
| CHEMBL144434 | — | — | 1 | 6.44 |
| CHEMBL144123 | — | — | 1 | 6.39 |
| CHEMBL144580 | — | — | 1 | 6.28 |
| CHEMBL14580 | — | — | 1 | 6.27 |
| CHEMBL356321 | — | — | 1 | 6.15 |
| CHEMBL145301 | — | — | 1 | 6.09 |
| CHEMBL145081 | — | — | 1 | 6.09 |
| CHEMBL357200 | — | — | 1 | 5.96 |
| CHEMBL343697 | — | — | 2 | 5.96 |
| CHEMBL144493 | — | — | 1 | 5.92 |
| CHEMBL358505 | — | — | 1 | 5.92 |
| CHEMBL145488 | — | — | 1 | 5.82 |
| CHEMBL145533 | — | — | 1 | 5.75 |
| CHEMBL343182 | — | — | 2 | 5.66 |
| CHEMBL64779 | — | — | 1 | 5.66 |
| CHEMBL358493 | — | — | 1 | 5.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12980 | QUINUCLIDINYL BENZILATE | Ki | = | 0.051 | nM | 10.29 |
| CHEMBL109405 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL9967 | PIRENZEPINE | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL144385 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL359027 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL144693 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL343236 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL344327 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL144751 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL342958 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL357444 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL125764 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL341476 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL144435 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL144434 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL144123 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL343236 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL144580 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL14580 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL356321 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL145301 | — | Ki | = | 810.0 | nM | 6.09 |
| CHEMBL145081 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL343697 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL357200 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL358505 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL144493 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL145488 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL343697 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL145533 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL343182 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL64779 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL358493 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL357404 | — | Ki | = | 7400.0 | nM | 5.13 |
| CHEMBL343182 | — | Ki | = | 8100.0 | nM | 5.09 |
| CHEMBL343242 | — | Ki | = | 9200.0 | nM | 5.04 |
| CHEMBL144247 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL145608 | — | Ki | = | 11600.0 | nM | 4.94 |
| CHEMBL423746 | — | Ki | = | 14900.0 | nM | 4.83 |
| CHEMBL344568 | — | Ki | = | 30000.0 | nM | 4.52 |
| CHEMBL144737 | — | Ki | > | 15000.0 | nM | - |