Assay Detail
Binding
CHEMBL749016
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Displacement of [3H]pirenzepine from muscarinic M1 receptor of rat cortex homogenates.
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M1 (CHEMBL276) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Design of dual acting anticonvulsant-antimuscarinic succinimide and hydantoin derivatives
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.64 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL558910 | — | — | 1 | 9.82 |
| CHEMBL9967 | PIRENZEPINE | 2.0 | 1 | 8.28 |
| CHEMBL176400 | — | — | 1 | 7.52 |
| CHEMBL360491 | — | — | 1 | 6.92 |
| CHEMBL176012 | — | — | 1 | 6.42 |
| CHEMBL362438 | — | — | 1 | 6.34 |
| CHEMBL368792 | — | — | 1 | 6.28 |
| CHEMBL368109 | — | — | 1 | 6.19 |
| CHEMBL368190 | — | — | 1 | 6.17 |
| CHEMBL368568 | — | — | 1 | 5.98 |
| CHEMBL177259 | — | — | 1 | 5.80 |
| CHEMBL178323 | — | — | 1 | 5.79 |
| CHEMBL176228 | — | — | 1 | 5.79 |
| CHEMBL367436 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL558910 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL9967 | PIRENZEPINE | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL176400 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL360491 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL176012 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL362438 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL368792 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL368109 | — | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL368190 | — | Ki | = | 680.0 | nM | 6.17 |
| CHEMBL368568 | — | Ki | = | 1050.0 | nM | 5.98 |
| CHEMBL177259 | — | Ki | = | 1590.0 | nM | 5.80 |
| CHEMBL178323 | — | Ki | = | 1620.0 | nM | 5.79 |
| CHEMBL176228 | — | Ki | = | 1630.0 | nM | 5.79 |
| CHEMBL367436 | — | Ki | = | 2300.0 | nM | 5.64 |