Assay Detail
Binding
CHEMBL900173
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Inhibition of [3H]NMS dissociation from porcine muscarinic M2 receptor
16
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 8.13 | 9.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1203986 | — | — | 2 | 9.07 |
| CHEMBL555247 | — | — | 2 | 9.00 |
| CHEMBL1203985 | — | — | 2 | 8.89 |
| CHEMBL1203984 | — | — | 2 | 8.86 |
| CHEMBL540132 | — | — | 2 | 8.82 |
| CHEMBL540131 | — | — | 2 | 8.31 |
| CHEMBL360055 | GALLAMINE | 4.0 | 2 | 6.89 |
| CHEMBL95 | TACRINE | 4.0 | 2 | 5.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1203986 | — | EC50 | = | 0.8511 | nM | 9.07 |
| CHEMBL1203986 | — | EC50 | = | 0.9 | nM | 9.05 |
| CHEMBL555247 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL555247 | — | EC50 | = | 1.023 | nM | 8.99 |
| CHEMBL1203985 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL1203985 | — | EC50 | = | 1.318 | nM | 8.88 |
| CHEMBL1203984 | — | EC50 | = | 1.38 | nM | 8.86 |
| CHEMBL1203984 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL540132 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL540132 | — | EC50 | = | 1.514 | nM | 8.82 |
| CHEMBL540131 | — | EC50 | = | 4.898 | nM | 8.31 |
| CHEMBL540131 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL360055 | GALLAMINE | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL360055 | GALLAMINE | EC50 | = | 131.83 | nM | 6.88 |
| CHEMBL95 | TACRINE | EC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL95 | TACRINE | EC50 | = | 6309.57 | nM | 5.20 |