Assay Detail
Binding
CHEMBL748288
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against M2 receptor in rat brainstem cells using radioligand [3H]quinuclidinyl benzilate ([3H]QNB)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M2 (CHEMBL309) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Chemical modification of ring c of himbacine: Discovery of a pharmacophoric element for M2-selectivity
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 7 | 6.86 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL277642 | HIMBACINE | — | 1 | 8.00 |
| CHEMBL160755 | — | — | 1 | 7.05 |
| CHEMBL159237 | — | — | 1 | 7.02 |
| CHEMBL159189 | — | — | 1 | 6.61 |
| CHEMBL346049 | — | — | 1 | 6.53 |
| CHEMBL160666 | — | — | 1 | 6.45 |
| CHEMBL158589 | — | — | 1 | 6.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL277642 | HIMBACINE | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL160755 | — | Kd | = | 89.0 | nM | 7.05 |
| CHEMBL159237 | — | Kd | = | 96.0 | nM | 7.02 |
| CHEMBL159189 | — | Kd | = | 248.5 | nM | 6.61 |
| CHEMBL346049 | — | Kd | = | 293.0 | nM | 6.53 |
| CHEMBL160666 | — | Kd | = | 353.0 | nM | 6.45 |
| CHEMBL158589 | — | Kd | = | 464.0 | nM | 6.33 |