Assay Detail
Binding
CHEMBL4605380
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 4-(2-((1E,3E)-5-((E)-3,3-Dimethyl-1-(6-oxo-6-((2-(4-(4-(1-(2-oxo-2-(11-oxo-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-5-yl)ethyl)piperidin-4-yl)butyl)piperazin-1-yl)ethyl)amino)hexyl)-5-sulfoindolin-2-ylidene)penta-1,3-dien-1-yl)-3,3-dimethyl-3H-indol-1-ium-1-yl)butane-1-sulfonate Bis(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
6
Total Activities
6
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 | 6 | 6.84 | 8.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3140030 | — | — | 1 | 8.93 |
| CHEMBL517712 | ATROPINE | 4.0 | 1 | 8.31 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 6.42 |
| CHEMBL7634 | OXOTREMORINE | — | 1 | 6.07 |
| CHEMBL266295 | — | — | 1 | 5.85 |
| CHEMBL4089376 | — | — | 1 | 5.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3140030 | — | Ki | = | 1.175 | nM | 8.93 |
| CHEMBL517712 | ATROPINE | Ki | = | 4.898 | nM | 8.31 |
| CHEMBL21536 | XANOMELINE | Ki | = | 380.19 | nM | 6.42 |
| CHEMBL7634 | OXOTREMORINE | Ki | = | 851.14 | nM | 6.07 |
| CHEMBL266295 | — | Ki | = | 1412.54 | nM | 5.85 |
| CHEMBL4089376 | — | Ki | = | 3548.13 | nM | 5.45 |