Assay Detail
Functional
CHEMBL871565
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity against human GLUR2 flop 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 | 6.10 | 6.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL214833 | — | — | 1 | 6.67 |
| CHEMBL214834 | — | — | 1 | 6.64 |
| CHEMBL213197 | — | — | 1 | 6.51 |
| CHEMBL385220 | — | — | 1 | 6.32 |
| CHEMBL384010 | — | — | 1 | 6.18 |
| CHEMBL217111 | — | — | 1 | 5.74 |
| CHEMBL435582 | — | — | 1 | 5.72 |
| CHEMBL387304 | — | — | 1 | 5.61 |
| CHEMBL218347 | — | — | 1 | 5.54 |
| CHEMBL378065 | — | — | 1 | - |
| CHEMBL212021 | — | — | 1 | - |
| CHEMBL213379 | — | — | 1 | - |
| CHEMBL538396 | — | — | 1 | - |
| CHEMBL215987 | — | — | 1 | - |
| CHEMBL216478 | — | — | 1 | - |
| CHEMBL377662 | — | — | 1 | - |
| CHEMBL334920 | — | — | 1 | - |
| CHEMBL384175 | — | — | 1 | - |
| CHEMBL61593 | CYCLOTHIAZIDE | 4.0 | 1 | - |
| CHEMBL385502 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL214833 | — | EC50 | = | 216.0 | nM | 6.67 |
| CHEMBL214834 | — | EC50 | = | 231.0 | nM | 6.64 |
| CHEMBL213197 | — | EC50 | = | 309.0 | nM | 6.51 |
| CHEMBL385220 | — | EC50 | = | 474.0 | nM | 6.32 |
| CHEMBL384010 | — | EC50 | = | 663.0 | nM | 6.18 |
| CHEMBL217111 | — | EC50 | = | 1808.0 | nM | 5.74 |
| CHEMBL435582 | — | EC50 | = | 1905.0 | nM | 5.72 |
| CHEMBL387304 | — | EC50 | = | 2433.0 | nM | 5.61 |
| CHEMBL218347 | — | EC50 | = | 2854.0 | nM | 5.54 |
| CHEMBL378065 | — | EC50 | - | — | - | |
| CHEMBL212021 | — | EC50 | - | — | - | |
| CHEMBL213379 | — | EC50 | - | — | - | |
| CHEMBL538396 | — | EC50 | - | — | - | |
| CHEMBL215987 | — | EC50 | - | — | - | |
| CHEMBL216478 | — | EC50 | - | — | - | |
| CHEMBL377662 | — | EC50 | - | — | - | |
| CHEMBL334920 | — | EC50 | - | — | - | |
| CHEMBL384175 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL61593 | CYCLOTHIAZIDE | EC50 | - | — | - | |
| CHEMBL385502 | — | EC50 | > | 3000.0 | nM | - |