Assay Detail
Binding
CHEMBL875203
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Affinity for rat Muscarinic acetylcholine receptor M2
21
Total Activities
17
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
Design, synthesis and activity of novel derivatives of oxybutynin and tolterodine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 6.95 | 8.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1382 | TOLTERODINE | 4.0 | 1 | 8.16 |
| CHEMBL1231 | OXYBUTYNIN | 4.0 | 1 | 8.16 |
| CHEMBL192485 | — | — | 4 | 7.66 |
| CHEMBL192065 | — | — | 1 | 7.51 |
| CHEMBL192061 | — | — | 2 | 7.47 |
| CHEMBL192337 | — | — | 1 | 7.40 |
| CHEMBL192537 | — | — | 1 | 7.14 |
| CHEMBL190815 | — | — | 1 | 6.98 |
| CHEMBL192885 | — | — | 1 | 6.66 |
| CHEMBL195169 | — | — | 1 | 6.19 |
| CHEMBL194870 | — | — | 1 | 6.13 |
| CHEMBL190459 | — | — | 1 | 5.71 |
| CHEMBL424832 | — | — | 1 | 5.45 |
| CHEMBL372462 | — | — | 1 | - |
| CHEMBL370757 | — | — | 1 | - |
| CHEMBL363865 | — | — | 1 | - |
| CHEMBL192083 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1382 | TOLTERODINE | Ki | = | 6.91 | nM | 8.16 |
| CHEMBL1231 | OXYBUTYNIN | Ki | = | 6.97 | nM | 8.16 |
| CHEMBL192485 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL192065 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL192061 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL192337 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL192061 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL192485 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL192537 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL190815 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL192885 | — | Ki | = | 221.0 | nM | 6.66 |
| CHEMBL192485 | — | Ki | = | 224.0 | nM | 6.65 |
| CHEMBL192485 | — | Ki | = | 425.0 | nM | 6.37 |
| CHEMBL195169 | — | Ki | = | 639.0 | nM | 6.19 |
| CHEMBL194870 | — | Ki | = | 736.0 | nM | 6.13 |
| CHEMBL190459 | — | Ki | = | 1926.0 | nM | 5.71 |
| CHEMBL424832 | — | Ki | = | 3582.0 | nM | 5.45 |
| CHEMBL363865 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL370757 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL372462 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL192083 | — | Ki | > | 10000.0 | nM | - |