Assay Detail
Functional
CHEMBL4198696
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Antagonist activity at human M1 mAChR expressed in CHO cells assessed as inhibition of oxotremorine M-stimulated calcium influx preincubated for 10 mins followed by oxotremorine M addition by Fluo-4 NW dye based fluorescence assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 5.52 | 6.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4214668 | — | — | 1 | 6.34 |
| CHEMBL4205374 | — | — | 1 | 6.18 |
| CHEMBL4216601 | — | — | 1 | 5.97 |
| CHEMBL4204913 | — | — | 1 | 5.86 |
| CHEMBL4206484 | — | — | 1 | 5.83 |
| CHEMBL4202784 | — | — | 1 | 5.83 |
| CHEMBL4209755 | — | — | 1 | 5.80 |
| CHEMBL4204901 | — | — | 1 | 5.69 |
| CHEMBL4214900 | — | — | 1 | 5.67 |
| CHEMBL4217126 | — | — | 1 | 5.61 |
| CHEMBL4217346 | — | — | 1 | 5.56 |
| CHEMBL4217660 | — | — | 1 | 5.49 |
| CHEMBL4212151 | — | — | 1 | 5.43 |
| CHEMBL1256415 | — | — | 1 | 5.43 |
| CHEMBL4210729 | — | — | 1 | 5.40 |
| CHEMBL4215154 | — | — | 1 | 5.39 |
| CHEMBL4215217 | — | — | 1 | 5.37 |
| CHEMBL4213591 | — | — | 1 | 5.27 |
| CHEMBL292314 | — | — | 1 | 5.21 |
| CHEMBL4210274 | — | — | 1 | 5.11 |
| CHEMBL4205910 | — | — | 1 | 5.07 |
| CHEMBL4203672 | — | — | 1 | 5.03 |
| CHEMBL4217617 | — | — | 1 | 4.94 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 4.89 |
| CHEMBL608112 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4214668 | — | IC50 | = | 455.0 | nM | 6.34 |
| CHEMBL4205374 | — | IC50 | = | 658.0 | nM | 6.18 |
| CHEMBL4216601 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL4204913 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL4206484 | — | IC50 | = | 1490.0 | nM | 5.83 |
| CHEMBL4202784 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL4209755 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL4204901 | — | IC50 | = | 2050.0 | nM | 5.69 |
| CHEMBL4214900 | — | IC50 | = | 2140.0 | nM | 5.67 |
| CHEMBL4217126 | — | IC50 | = | 2480.0 | nM | 5.61 |
| CHEMBL4217346 | — | IC50 | = | 2780.0 | nM | 5.56 |
| CHEMBL4217660 | — | IC50 | = | 3270.0 | nM | 5.49 |
| CHEMBL4212151 | — | IC50 | = | 3710.0 | nM | 5.43 |
| CHEMBL1256415 | — | IC50 | = | 3710.0 | nM | 5.43 |
| CHEMBL4210729 | — | IC50 | = | 4010.0 | nM | 5.40 |
| CHEMBL4215154 | — | IC50 | = | 4110.0 | nM | 5.39 |
| CHEMBL4215217 | — | IC50 | = | 4230.0 | nM | 5.37 |
| CHEMBL4213591 | — | IC50 | = | 5350.0 | nM | 5.27 |
| CHEMBL292314 | — | IC50 | = | 6090.0 | nM | 5.21 |
| CHEMBL4210274 | — | IC50 | = | 7860.0 | nM | 5.11 |
| CHEMBL4205910 | — | IC50 | = | 8610.0 | nM | 5.07 |
| CHEMBL4203672 | — | IC50 | = | 9450.0 | nM | 5.03 |
| CHEMBL4217617 | — | IC50 | = | 11400.0 | nM | 4.94 |
| CHEMBL95 | TACRINE | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL608112 | — | IC50 | - | — | - |