Assay Detail
Functional
CHEMBL780741
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Compound was tested in vitro for its ability to enhance the K+-stimulated release of [3H]acetylcholine from rat hippocampal slices preloaded with [3H]-Choline.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Hippocampus |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
2-Fluoro-4-pyridinylmethyl analogues of linopirdine as orally active acetylcholine release-enhancing agents with good efficacy and duration of action.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 5.68 | 6.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL344430 | — | — | 1 | 6.39 |
| CHEMBL342375 | — | — | 1 | 6.35 |
| CHEMBL343822 | — | — | 1 | 6.08 |
| CHEMBL435230 | — | — | 1 | 5.97 |
| CHEMBL143262 | — | — | 1 | 5.80 |
| CHEMBL139618 | — | — | 1 | 5.38 |
| CHEMBL319111 | LINOPIRDINE | 2.0 | 1 | 5.35 |
| CHEMBL356763 | — | — | 1 | 5.00 |
| CHEMBL343507 | — | — | 1 | 4.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL344430 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL342375 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL343822 | — | EC50 | = | 830.0 | nM | 6.08 |
| CHEMBL435230 | — | EC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL143262 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL139618 | — | EC50 | = | 4120.0 | nM | 5.38 |
| CHEMBL319111 | LINOPIRDINE | EC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL356763 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL343507 | — | EC50 | = | 15200.0 | nM | 4.82 |