Assay Detail
Binding
CHEMBL749925
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Binding affinity for muscarinic acetylcholine receptor M1 using [3H]pirenzepine (Pz) radioligand in rat hippocampus membranes.
34
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Hippocampus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M1 (CHEMBL276) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
1,2,5-Thiadiazole analogues of aceclidine as potent m1 muscarinic agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 7.48 | 9.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL340435 | — | — | 2 | 9.26 |
| CHEMBL125732 | — | — | 3 | 8.57 |
| CHEMBL126846 | — | — | 2 | 8.36 |
| CHEMBL433867 | — | — | 1 | 8.30 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 8.30 |
| CHEMBL341516 | — | — | 1 | 8.17 |
| CHEMBL2111844 | — | — | 2 | 8.15 |
| CHEMBL129575 | — | — | 1 | 7.70 |
| CHEMBL337925 | — | — | 1 | 7.68 |
| CHEMBL340402 | — | — | 1 | 7.65 |
| CHEMBL126237 | — | — | 1 | 7.55 |
| CHEMBL129152 | — | — | 1 | 7.39 |
| CHEMBL126332 | — | — | 1 | 7.38 |
| CHEMBL125518 | — | — | 1 | 7.37 |
| CHEMBL341242 | — | — | 1 | 7.37 |
| CHEMBL129781 | — | — | 1 | 7.36 |
| CHEMBL126193 | — | — | 1 | 7.35 |
| CHEMBL129764 | — | — | 1 | 7.32 |
| CHEMBL128950 | — | — | 1 | 7.20 |
| CHEMBL339081 | — | — | 1 | 7.18 |
| CHEMBL129611 | — | — | 1 | 7.18 |
| CHEMBL129558 | — | — | 1 | 7.16 |
| CHEMBL129410 | — | — | 1 | 7.10 |
| CHEMBL340624 | — | — | 1 | 7.04 |
| CHEMBL409280 | — | — | 1 | 6.81 |
| CHEMBL340021 | — | — | 1 | 6.46 |
| CHEMBL129474 | — | — | 1 | 6.44 |
| CHEMBL126383 | — | — | 1 | 6.08 |
| CHEMBL20835 | ACECLIDINE | 3.0 | 1 | 5.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL340435 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL125732 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL125732 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL126846 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL433867 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL21536 | XANOMELINE | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL341516 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL2111844 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL125732 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL129575 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2111844 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL337925 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL340402 | — | IC50 | = | 22.3 | nM | 7.65 |
| CHEMBL126237 | — | IC50 | = | 28.4 | nM | 7.55 |
| CHEMBL340435 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL129152 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL126332 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL341242 | — | IC50 | = | 42.3 | nM | 7.37 |
| CHEMBL125518 | — | IC50 | = | 42.5 | nM | 7.37 |
| CHEMBL129781 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL126193 | — | IC50 | = | 44.5 | nM | 7.35 |
| CHEMBL129764 | — | IC50 | = | 47.7 | nM | 7.32 |
| CHEMBL128950 | — | IC50 | = | 63.5 | nM | 7.20 |
| CHEMBL339081 | — | IC50 | = | 65.5 | nM | 7.18 |
| CHEMBL126846 | — | IC50 | = | 66.7 | nM | 7.18 |
| CHEMBL129611 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL129558 | — | IC50 | = | 68.5 | nM | 7.16 |
| CHEMBL129410 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL340624 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL409280 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL340021 | — | IC50 | = | 351.0 | nM | 6.46 |
| CHEMBL129474 | — | IC50 | = | 361.0 | nM | 6.44 |
| CHEMBL126383 | — | IC50 | = | 833.0 | nM | 6.08 |
| CHEMBL20835 | ACECLIDINE | IC50 | = | 2427.0 | nM | 5.62 |