Assay Detail
Functional
CHEMBL748259
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro 100 nM cortex affinity to displace [3H]- -CD providing a measure of muscarinic m1 receptor agonist 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 | 6.59 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL105457 | — | — | 1 | 8.19 |
| CHEMBL352638 | — | — | 1 | 8.09 |
| CHEMBL12587 | MUSCARINE | — | 1 | 7.92 |
| CHEMBL170388 | — | — | 1 | 7.52 |
| CHEMBL166452 | — | — | 1 | 7.07 |
| CHEMBL433912 | — | — | 1 | 7.06 |
| CHEMBL291280 | — | — | 1 | 7.05 |
| CHEMBL288113 | — | — | 1 | 7.00 |
| CHEMBL2021361 | — | — | 1 | 6.98 |
| CHEMBL439621 | — | — | 1 | 6.84 |
| CHEMBL353781 | — | — | 1 | 6.76 |
| CHEMBL170489 | — | — | 1 | 6.75 |
| CHEMBL424360 | — | — | 1 | 6.73 |
| CHEMBL168609 | — | — | 1 | 6.68 |
| CHEMBL168755 | — | — | 1 | 6.62 |
| CHEMBL168595 | — | — | 1 | 6.53 |
| CHEMBL167593 | — | — | 1 | 6.29 |
| CHEMBL166695 | — | — | 1 | 6.28 |
| CHEMBL167501 | — | — | 2 | 6.26 |
| CHEMBL2021360 | — | — | 1 | 6.23 |
| CHEMBL168897 | — | — | 1 | 6.14 |
| CHEMBL144679 | — | — | 1 | 6.13 |
| CHEMBL168685 | — | — | 1 | 6.06 |
| CHEMBL2371594 | — | — | 1 | 6.02 |
| CHEMBL354854 | — | — | 1 | 5.92 |
| CHEMBL134830 | — | — | 1 | 5.73 |
| CHEMBL168348 | — | — | 1 | 5.55 |
| CHEMBL2021359 | — | — | 1 | 5.04 |
| CHEMBL166938 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL105457 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL352638 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL12587 | MUSCARINE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL170388 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL166452 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL433912 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL291280 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL288113 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL2021361 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL439621 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL353781 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL170489 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL424360 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL168609 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL168755 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL168595 | — | Ki | = | 295.0 | nM | 6.53 |
| CHEMBL167593 | — | Ki | = | 515.0 | nM | 6.29 |
| CHEMBL166695 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL167501 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL2021360 | — | Ki | = | 585.0 | nM | 6.23 |
| CHEMBL168897 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL144679 | — | Ki | = | 745.0 | nM | 6.13 |
| CHEMBL168685 | — | Ki | = | 870.0 | nM | 6.06 |
| CHEMBL2371594 | — | Ki | = | 960.0 | nM | 6.02 |
| CHEMBL354854 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL167501 | — | Ki | = | 1750.0 | nM | 5.76 |
| CHEMBL134830 | — | Ki | = | 1850.0 | nM | 5.73 |
| CHEMBL168348 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL2021359 | — | Ki | = | 9150.0 | nM | 5.04 |
| CHEMBL166938 | — | Ki | > | 10000.0 | nM | - |