Assay Detail
Binding
CHEMBL746582
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro receptor binding against Muscarinic acetylcholine receptor M1 in rat cerebral cortex was determined using [3H]pirenzepine
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M1 (CHEMBL276) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and biological evaluation of new antimuscarinic compounds with amidine basic centers. A useful bioisosteric replacement of classical cationic heads.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 11 | 8.45 | 9.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL569713 | SCOPOLAMINE | 4.0 | 1 | 9.12 |
| CHEMBL293927 | — | — | 1 | 8.96 |
| CHEMBL553066 | — | — | 1 | 8.96 |
| CHEMBL517712 | ATROPINE | 4.0 | 1 | 8.89 |
| CHEMBL553783 | — | — | 1 | 8.70 |
| CHEMBL2146143 | ATROPINE METHYLBROMIDE | -1.0 | 1 | 8.60 |
| CHEMBL544759 | — | — | 1 | 8.47 |
| CHEMBL544993 | — | — | 1 | 8.44 |
| CHEMBL553894 | — | — | 1 | 8.15 |
| CHEMBL553562 | — | — | 1 | 8.12 |
| CHEMBL21823 | — | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL569713 | SCOPOLAMINE | Kd | = | 0.75 | nM | 9.12 |
| CHEMBL293927 | — | Kd | = | 1.1 | nM | 8.96 |
| CHEMBL553066 | — | Kd | = | 1.1 | nM | 8.96 |
| CHEMBL517712 | ATROPINE | Kd | = | 1.3 | nM | 8.89 |
| CHEMBL553783 | — | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL2146143 | ATROPINE METHYLBROMIDE | Kd | = | 2.5 | nM | 8.60 |
| CHEMBL544759 | — | Kd | = | 3.4 | nM | 8.47 |
| CHEMBL544993 | — | Kd | = | 3.6 | nM | 8.44 |
| CHEMBL553894 | — | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL553562 | — | Kd | = | 7.5 | nM | 8.12 |
| CHEMBL21823 | — | Kd | = | 300.0 | nM | 6.52 |