Assay Detail
Binding
CHEMBL2215472
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]NMS from EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as reduction of [3H]NMS dissociation rate after 22 hrs by liquid scintillation counting
8
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Fluorescent derivatives of AC-42 to probe bitopic orthosteric/allosteric binding mechanisms on muscarinic M1 receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| pEC50 | 5 | - | - |
| EC50 | 3 | 4.60 | 4.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2206333 | — | — | 1 | 4.60 |
| CHEMBL1306565 | — | — | 1 | - |
| CHEMBL845 | N-DESMETHYLCLOZAPINE | — | 1 | - |
| CHEMBL501756 | BRUCINE | -1.0 | 1 | - |
| CHEMBL360055 | GALLAMINE | 4.0 | 2 | - |
| CHEMBL2206335 | — | — | 1 | - |
| CHEMBL2206334 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2206333 | — | EC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL1306565 | — | pEC50 | - | — | - | |
| CHEMBL845 | N-DESMETHYLCLOZAPINE | pEC50 | - | — | - | |
| CHEMBL501756 | BRUCINE | pEC50 | - | — | - | |
| CHEMBL360055 | GALLAMINE | EC50 | = | 170000.0 | nM | - |
| CHEMBL360055 | GALLAMINE | EC50 | = | 173780.08 | nM | - |
| CHEMBL2206335 | — | pEC50 | - | — | - | |
| CHEMBL2206334 | — | pEC50 | - | — | - |