Assay Detail
Functional
CHEMBL869262
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity against human GLUR4 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
A novel class of AMPA receptor allosteric modulators. Part 1: design, synthesis, and SAR of 3-aryl-4-cyano-5-substituted-heteroaryl-2-carboxylic acid derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 6.17 | 6.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL214833 | — | — | 1 | 6.74 |
| CHEMBL213197 | — | — | 1 | 6.67 |
| CHEMBL214834 | — | — | 1 | 6.56 |
| CHEMBL385220 | — | — | 1 | 6.41 |
| CHEMBL435582 | — | — | 1 | 6.38 |
| CHEMBL215987 | — | — | 1 | 6.36 |
| CHEMBL218347 | — | — | 1 | 6.32 |
| CHEMBL378065 | — | — | 1 | 6.31 |
| CHEMBL384010 | — | — | 1 | 6.26 |
| CHEMBL217111 | — | — | 1 | 6.20 |
| CHEMBL334920 | — | — | 1 | 6.18 |
| CHEMBL377662 | — | — | 1 | 6.10 |
| CHEMBL387304 | — | — | 1 | 6.00 |
| CHEMBL213379 | — | — | 1 | 5.73 |
| CHEMBL216478 | — | — | 1 | 5.70 |
| CHEMBL538396 | — | — | 1 | 5.54 |
| CHEMBL61593 | CYCLOTHIAZIDE | 4.0 | 1 | 5.42 |
| CHEMBL384175 | — | — | 1 | - |
| CHEMBL212021 | — | — | 1 | - |
| CHEMBL385502 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL214833 | — | EC50 | = | 183.0 | nM | 6.74 |
| CHEMBL213197 | — | EC50 | = | 214.0 | nM | 6.67 |
| CHEMBL214834 | — | EC50 | = | 273.0 | nM | 6.56 |
| CHEMBL385220 | — | EC50 | = | 394.0 | nM | 6.41 |
| CHEMBL435582 | — | EC50 | = | 420.0 | nM | 6.38 |
| CHEMBL215987 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL218347 | — | EC50 | = | 474.0 | nM | 6.32 |
| CHEMBL378065 | — | EC50 | = | 489.0 | nM | 6.31 |
| CHEMBL384010 | — | EC50 | = | 554.0 | nM | 6.26 |
| CHEMBL217111 | — | EC50 | = | 629.0 | nM | 6.20 |
| CHEMBL334920 | — | EC50 | = | 660.0 | nM | 6.18 |
| CHEMBL377662 | — | EC50 | = | 795.0 | nM | 6.10 |
| CHEMBL387304 | — | EC50 | = | 1009.0 | nM | 6.00 |
| CHEMBL213379 | — | EC50 | = | 1873.0 | nM | 5.73 |
| CHEMBL216478 | — | EC50 | = | 1979.0 | nM | 5.70 |
| CHEMBL538396 | — | EC50 | = | 2892.0 | nM | 5.54 |
| CHEMBL61593 | CYCLOTHIAZIDE | EC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL384175 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL212021 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL385502 | — | EC50 | > | 3000.0 | nM | - |