Assay Detail
Binding
CHEMBL745476
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In vitro receptor binding against Muscarinic acetylcholine receptor M2 in rat heart 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 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M2 (CHEMBL309) ↗| 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 | 8.18 | 9.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL293927 | — | — | 1 | 9.06 |
| CHEMBL553066 | — | — | 1 | 8.80 |
| CHEMBL517712 | ATROPINE | 4.0 | 1 | 8.57 |
| CHEMBL2146143 | ATROPINE METHYLBROMIDE | -1.0 | 1 | 8.57 |
| CHEMBL569713 | SCOPOLAMINE | 4.0 | 1 | 8.52 |
| CHEMBL544759 | — | — | 1 | 8.17 |
| CHEMBL553783 | — | — | 1 | 8.00 |
| CHEMBL544993 | — | — | 1 | 8.00 |
| CHEMBL553894 | — | — | 1 | 7.96 |
| CHEMBL553562 | — | — | 1 | 7.64 |
| CHEMBL21823 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL293927 | — | Kd | = | 0.87 | nM | 9.06 |
| CHEMBL553066 | — | Kd | = | 1.6 | nM | 8.80 |
| CHEMBL517712 | ATROPINE | Kd | = | 2.7 | nM | 8.57 |
| CHEMBL2146143 | ATROPINE METHYLBROMIDE | Kd | = | 2.7 | nM | 8.57 |
| CHEMBL569713 | SCOPOLAMINE | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL544759 | — | Kd | = | 6.7 | nM | 8.17 |
| CHEMBL553783 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL544993 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL553894 | — | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL553562 | — | Kd | = | 23.0 | nM | 7.64 |
| CHEMBL21823 | — | Kd | = | 220.0 | nM | 6.66 |