Assay Detail
Functional
CHEMBL872655
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro 100 nM cortex affinity to displace [3H]- -pirenzepine providing a measure of muscarinic m1 receptor antagonist affinity
30
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M1 (CHEMBL276) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Muscarinic agonist SAR of azaspirodioxolanes
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 5.81 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL352638 | — | — | 1 | 9.22 |
| CHEMBL2371594 | — | — | 1 | 6.70 |
| CHEMBL2021361 | — | — | 1 | 6.37 |
| CHEMBL168348 | — | — | 1 | 6.21 |
| CHEMBL433912 | — | — | 1 | 6.12 |
| CHEMBL167593 | — | — | 1 | 5.90 |
| CHEMBL144679 | — | — | 1 | 5.88 |
| CHEMBL291280 | — | — | 1 | 5.80 |
| CHEMBL170388 | — | — | 1 | 5.71 |
| CHEMBL105457 | — | — | 1 | 5.68 |
| CHEMBL166695 | — | — | 1 | 5.68 |
| CHEMBL424360 | — | — | 1 | 5.58 |
| CHEMBL168595 | — | — | 1 | 5.52 |
| CHEMBL168897 | — | — | 1 | 5.50 |
| CHEMBL353781 | — | — | 1 | 5.39 |
| CHEMBL168609 | — | — | 1 | 5.30 |
| CHEMBL166452 | — | — | 1 | 5.27 |
| CHEMBL12587 | MUSCARINE | — | 1 | 5.25 |
| CHEMBL288113 | — | — | 1 | 5.24 |
| CHEMBL170489 | — | — | 1 | 5.19 |
| CHEMBL2021360 | — | — | 1 | 5.17 |
| CHEMBL168755 | — | — | 1 | 5.11 |
| CHEMBL439621 | — | — | 1 | - |
| CHEMBL354854 | — | — | 1 | - |
| CHEMBL168685 | — | — | 1 | - |
| CHEMBL167501 | — | — | 2 | - |
| CHEMBL2021359 | — | — | 1 | - |
| CHEMBL166938 | — | — | 1 | - |
| CHEMBL134830 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL352638 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL2371594 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL2021361 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL168348 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL433912 | — | Ki | = | 765.0 | nM | 6.12 |
| CHEMBL167593 | — | Ki | = | 1250.0 | nM | 5.90 |
| CHEMBL144679 | — | Ki | = | 1325.0 | nM | 5.88 |
| CHEMBL291280 | — | Ki | = | 1575.0 | nM | 5.80 |
| CHEMBL170388 | — | Ki | = | 1950.0 | nM | 5.71 |
| CHEMBL166695 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL105457 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL424360 | — | Ki | = | 2650.0 | nM | 5.58 |
| CHEMBL168595 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL168897 | — | Ki | = | 3160.0 | nM | 5.50 |
| CHEMBL353781 | — | Ki | = | 4050.0 | nM | 5.39 |
| CHEMBL168609 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL166452 | — | Ki | = | 5325.0 | nM | 5.27 |
| CHEMBL12587 | MUSCARINE | Ki | = | 5680.0 | nM | 5.25 |
| CHEMBL288113 | — | Ki | = | 5825.0 | nM | 5.24 |
| CHEMBL170489 | — | Ki | = | 6400.0 | nM | 5.19 |
| CHEMBL2021360 | — | Ki | = | 6700.0 | nM | 5.17 |
| CHEMBL168755 | — | Ki | = | 7690.0 | nM | 5.11 |
| CHEMBL439621 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL168685 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL354854 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL167501 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2021359 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL167501 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL166938 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL134830 | — | Ki | > | 10000.0 | nM | - |