Assay Detail
Binding
CHEMBL748854
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Displacement of [3H]pirenzepine binding to muscarinic M1 receptor in brain cortex of rat.
9
Total Activities
9
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 M1 (CHEMBL276) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Quinolizidinyl derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one as ligands for muscarinic receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.39 | 8.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL9967 | PIRENZEPINE | 2.0 | 1 | 8.42 |
| CHEMBL322378 | — | — | 1 | 8.10 |
| CHEMBL318316 | — | — | 1 | 8.00 |
| CHEMBL103189 | — | — | 1 | 8.00 |
| CHEMBL103785 | — | — | 1 | 7.55 |
| CHEMBL2111621 | — | — | 1 | 7.40 |
| CHEMBL2112418 | — | — | 1 | 6.96 |
| CHEMBL103529 | — | — | 1 | 6.19 |
| CHEMBL2112432 | — | — | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL9967 | PIRENZEPINE | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL322378 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL318316 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL103189 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL103785 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2111621 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2112418 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL103529 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL2112432 | — | IC50 | = | 1200.0 | nM | 5.92 |