Assay Detail
Binding
CHEMBL5259066
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M2 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Hybridization into a Bitopic Ligand Increased Muscarinic Receptor Activation for Isopilocarpine but Not for Pilocarpine Derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 6.14 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5287159 | — | — | 1 | 6.60 |
| CHEMBL5285668 | — | — | 1 | 6.27 |
| CHEMBL550 | PILOCARPINE | 4.0 | 1 | 6.00 |
| CHEMBL5287096 | — | — | 1 | 5.97 |
| CHEMBL5272950 | — | — | 1 | 5.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5287159 | — | EC50 | = | 251.19 | nM | 6.60 |
| CHEMBL5285668 | — | EC50 | = | 537.03 | nM | 6.27 |
| CHEMBL550 | PILOCARPINE | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5287096 | — | EC50 | = | 1071.52 | nM | 5.97 |
| CHEMBL5272950 | — | EC50 | = | 1380.38 | nM | 5.86 |