Assay Detail
Binding
CHEMBL747656
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity for muscarinic acetylcholine receptor M1 using [3H]oxotremorine-M (Oxo-M) radioligand in rat hippocampus membranes
36
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Hippocampus |
| Subcellular | Membrane |
| 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 | 36 | 7.82 | 9.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL340435 | — | — | 2 | 9.42 |
| CHEMBL129821 | — | — | 2 | 9.22 |
| CHEMBL126846 | — | — | 2 | 9.12 |
| CHEMBL125732 | — | — | 3 | 8.85 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 8.70 |
| CHEMBL433867 | — | — | 1 | 8.60 |
| CHEMBL2111844 | — | — | 2 | 8.55 |
| CHEMBL337925 | — | — | 1 | 8.54 |
| CHEMBL341516 | — | — | 1 | 8.28 |
| CHEMBL129575 | — | — | 1 | 8.19 |
| CHEMBL126237 | — | — | 1 | 8.12 |
| CHEMBL341242 | — | — | 1 | 7.97 |
| CHEMBL126332 | — | — | 1 | 7.93 |
| CHEMBL129764 | — | — | 1 | 7.90 |
| CHEMBL126193 | — | — | 1 | 7.90 |
| CHEMBL125518 | — | — | 1 | 7.76 |
| CHEMBL339081 | — | — | 1 | 7.70 |
| CHEMBL129152 | — | — | 1 | 7.44 |
| CHEMBL340402 | — | — | 1 | 7.42 |
| CHEMBL129781 | — | — | 1 | 7.38 |
| CHEMBL129611 | — | — | 1 | 7.23 |
| CHEMBL129410 | — | — | 1 | 7.18 |
| CHEMBL129558 | — | — | 1 | 7.17 |
| CHEMBL128950 | — | — | 1 | 7.01 |
| CHEMBL340021 | — | — | 1 | 6.98 |
| CHEMBL20835 | ACECLIDINE | 3.0 | 1 | 6.92 |
| CHEMBL129474 | — | — | 1 | 6.80 |
| CHEMBL409280 | — | — | 1 | 6.70 |
| CHEMBL340624 | — | — | 1 | 6.60 |
| CHEMBL126383 | — | — | 1 | 6.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL340435 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL129821 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL126846 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL125732 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL21536 | XANOMELINE | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL433867 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL2111844 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL337925 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL125732 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL341516 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL126846 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL129821 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL125732 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL129575 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL126237 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL341242 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL126332 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL126193 | — | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL129764 | — | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL2111844 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL125518 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL339081 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL129152 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL340402 | — | IC50 | = | 38.2 | nM | 7.42 |
| CHEMBL129781 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL129611 | — | IC50 | = | 58.7 | nM | 7.23 |
| CHEMBL129410 | — | IC50 | = | 66.5 | nM | 7.18 |
| CHEMBL129558 | — | IC50 | = | 67.5 | nM | 7.17 |
| CHEMBL128950 | — | IC50 | = | 98.5 | nM | 7.01 |
| CHEMBL340021 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL20835 | ACECLIDINE | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL129474 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL340435 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL409280 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL340624 | — | IC50 | = | 252.0 | nM | 6.60 |
| CHEMBL126383 | — | IC50 | = | 537.0 | nM | 6.27 |