Assay Detail
Binding
CHEMBL4605382
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 4-(2-((1E,3E)-5-((E)-1-(6-((3,5-Bis((2-(3-(1-(4-(1-(2-oxo-2-(11-oxo-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-5-yl)ethyl)piperidin-4-yl)butyl)-1H-imidazol-4-yl)propanamido)ethyl)carbamoyl)benzyl)amino)-6-oxohexyl)-3,3-dimethyl-5-sulfoindolin-2-ylidene)penta-1,3-dien-1-yl)-3,3-dimethyl-3H-indol-1-ium-1-yl)butane-1-sulfonate Tris(hydrotrifluoroacetate) fluorescent tracer from human muscarinic M2 receptor expressed in CHO-K9 cells measured after 60 mins by Hoechst H33342 dye based confocal plate reader assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Red-Emitting Dibenzodiazepinone Derivatives as Fluorescent Dualsteric Probes for the Muscarinic Acetylcholine M<sub>2</sub> Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.15 | 9.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4116470 | — | — | 1 | 9.28 |
| CHEMBL3140030 | — | — | 1 | 9.23 |
| CHEMBL517712 | ATROPINE | 4.0 | 1 | 8.15 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 6.56 |
| CHEMBL266295 | — | — | 1 | 6.07 |
| CHEMBL7634 | OXOTREMORINE | — | 1 | 5.75 |
| CHEMBL4089376 | — | — | 1 | 5.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4116470 | — | Ki | = | 0.5248 | nM | 9.28 |
| CHEMBL3140030 | — | Ki | = | 0.5888 | nM | 9.23 |
| CHEMBL517712 | ATROPINE | Ki | = | 7.079 | nM | 8.15 |
| CHEMBL21536 | XANOMELINE | Ki | = | 275.42 | nM | 6.56 |
| CHEMBL266295 | — | Ki | = | 851.14 | nM | 6.07 |
| CHEMBL7634 | OXOTREMORINE | Ki | = | 1778.28 | nM | 5.75 |
| CHEMBL4089376 | — | Ki | = | 9332.54 | nM | 5.03 |