Assay Detail
Functional
CHEMBL680873
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Potentiation of responses mediated by 100 uM L-glutamate in transfected HEK293 cells expressing human homomeric iGluR4 flip receptors.
20
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design and synthesis of a novel series of 1,2-disubstituted cyclopentanes as small, potent potentiators of 2-amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propanoic acid (AMPA) receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 6.70 | 7.65 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL63355 | — | — | 2 | 7.65 |
| CHEMBL294506 | — | — | 2 | 7.48 |
| CHEMBL63417 | — | — | 2 | 7.17 |
| CHEMBL304375 | — | — | 2 | 7.09 |
| CHEMBL67021 | — | — | 2 | 6.93 |
| CHEMBL63514 | — | — | 1 | 6.72 |
| CHEMBL63816 | — | — | 1 | 6.61 |
| CHEMBL435582 | — | — | 1 | 6.54 |
| CHEMBL304468 | — | — | 1 | 6.39 |
| CHEMBL67936 | — | — | 1 | 6.36 |
| CHEMBL68282 | — | — | 1 | 6.28 |
| CHEMBL304865 | — | — | 1 | 6.26 |
| CHEMBL307094 | — | — | 1 | 6.21 |
| CHEMBL67318 | — | — | 1 | 5.96 |
| CHEMBL67523 | — | — | 1 | 5.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL63355 | — | EC50 | = | 22.6 | nM | 7.65 |
| CHEMBL294506 | — | EC50 | = | 32.8 | nM | 7.48 |
| CHEMBL63355 | — | EC50 | = | 45.8 | nM | 7.34 |
| CHEMBL63417 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL304375 | — | EC50 | = | 82.1 | nM | 7.09 |
| CHEMBL294506 | — | EC50 | = | 93.1 | nM | 7.03 |
| CHEMBL67021 | — | EC50 | = | 118.0 | nM | 6.93 |
| CHEMBL304375 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL63417 | — | EC50 | = | 147.0 | nM | 6.83 |
| CHEMBL63514 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL63816 | — | EC50 | = | 247.0 | nM | 6.61 |
| CHEMBL67021 | — | EC50 | = | 281.0 | nM | 6.55 |
| CHEMBL435582 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL304468 | — | EC50 | = | 403.0 | nM | 6.39 |
| CHEMBL67936 | — | EC50 | = | 434.0 | nM | 6.36 |
| CHEMBL68282 | — | EC50 | = | 520.0 | nM | 6.28 |
| CHEMBL304865 | — | EC50 | = | 551.0 | nM | 6.26 |
| CHEMBL307094 | — | EC50 | = | 621.0 | nM | 6.21 |
| CHEMBL67318 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL67523 | — | EC50 | = | 1740.0 | nM | 5.76 |