Assay Detail
ADMET
CHEMBL4306811
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Agonist activity at human Muscarinic acetylcholine receptor M2 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Selective M4 Muscarinic Acetylcholine Receptor Agonists with Novel Carbamate Isosteres.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 5.97 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4455058 | — | — | 1 | 6.60 |
| CHEMBL4515088 | — | — | 1 | 6.38 |
| CHEMBL4461438 | — | — | 1 | 5.60 |
| CHEMBL4583597 | — | — | 1 | 5.29 |
| CHEMBL4446791 | — | — | 1 | - |
| CHEMBL4524686 | — | — | 1 | - |
| CHEMBL4543638 | — | — | 1 | - |
| CHEMBL4541697 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4455058 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4515088 | — | EC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4461438 | — | EC50 | = | 2520.0 | nM | 5.60 |
| CHEMBL4583597 | — | EC50 | = | 5160.0 | nM | 5.29 |
| CHEMBL4446791 | — | EC50 | - | — | - | |
| CHEMBL4524686 | — | EC50 | > | 8830.0 | nM | - |
| CHEMBL4543638 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4541697 | — | EC50 | > | 7350.0 | nM | - |