Assay Detail
Binding
CHEMBL4716046
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Binding affinity to human muscarinic M2 receptor expressed in CHO-K9 cells assessed as unspecific binding at Kd incubated in dark at 22 degree C for 2 hrs in presence of atropine by FACSCantoII flow cytometric saturation binding study relative to control
12
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Differently fluorescence-labelled dibenzodiazepinone-type muscarinic acetylcholine receptor ligands with high M2R affinity
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 12 | 8.64 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4748004 | — | — | 2 | 9.19 |
| CHEMBL4650998 | — | — | 2 | 8.85 |
| CHEMBL4754371 | — | — | 2 | 8.74 |
| CHEMBL4744233 | — | — | 2 | 8.70 |
| CHEMBL4789147 | — | — | 2 | 8.62 |
| CHEMBL4742721 | — | — | 2 | 8.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4748004 | — | Kd | = | 0.6457 | nM | 9.19 |
| CHEMBL4650998 | — | Kd | = | 1.4 | nM | 8.85 |
| CHEMBL4754371 | — | Kd | = | 1.82 | nM | 8.74 |
| CHEMBL4748004 | — | Kd | = | 1.9 | nM | 8.72 |
| CHEMBL4754371 | — | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL4744233 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL4650998 | — | Kd | = | 2.344 | nM | 8.63 |
| CHEMBL4789147 | — | Kd | = | 2.4 | nM | 8.62 |
| CHEMBL4744233 | — | Kd | = | 3.8 | nM | 8.42 |
| CHEMBL4742721 | — | Kd | = | 3.89 | nM | 8.41 |
| CHEMBL4789147 | — | Kd | = | 4.365 | nM | 8.36 |
| CHEMBL4742721 | — | Kd | = | 4.5 | nM | 8.35 |