Assay Detail
Binding
CHEMBL2215474
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 after 22 hrs by liquid scintillation counting
7
Total Activities
7
Compounds Tested
1
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 |
|---|---|---|---|
| Ki | 7 | 7.33 | 10.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL376897 | METHSCOPOLAMINE | 4.0 | 1 | 10.02 |
| CHEMBL517712 | ATROPINE | 4.0 | 1 | 9.24 |
| CHEMBL845 | N-DESMETHYLCLOZAPINE | — | 1 | 7.22 |
| CHEMBL2206333 | — | — | 1 | 6.00 |
| CHEMBL2206334 | — | — | 1 | 5.76 |
| CHEMBL2206335 | — | — | 1 | 5.71 |
| CHEMBL1306565 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL376897 | METHSCOPOLAMINE | Ki | = | 0.0955 | nM | 10.02 |
| CHEMBL517712 | ATROPINE | Ki | = | 0.5754 | nM | 9.24 |
| CHEMBL845 | N-DESMETHYLCLOZAPINE | Ki | = | 60.26 | nM | 7.22 |
| CHEMBL2206333 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL2206334 | — | Ki | = | 1737.8 | nM | 5.76 |
| CHEMBL2206335 | — | Ki | = | 1949.84 | nM | 5.71 |
| CHEMBL1306565 | — | Ki | > | 1000000.0 | nM | - |