Assay Detail
Functional
CHEMBL856920
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at human recombinant iGluR2 flip expressed in HEK293 cells measured as change in intracellular calcium ion concentration in presence of glutamate by FLIPR assay
25
Total Activities
25
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 positive allosteric modulators of AMPA receptors: design, synthesis, and structure-activity relationships of 3-biphenyl-4-yl-4-cyano-5-ethyl-1-methyl-1H-pyrrole-2-carboxylic acid, LY2059346.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 25 | 6.69 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL384402 | — | — | 1 | 7.38 |
| CHEMBL215090 | — | — | 1 | 7.24 |
| CHEMBL384847 | — | — | 1 | 7.09 |
| CHEMBL384271 | — | — | 1 | 7.08 |
| CHEMBL213197 | — | — | 1 | 7.01 |
| CHEMBL385608 | — | — | 1 | 6.99 |
| CHEMBL215575 | — | — | 1 | 6.96 |
| CHEMBL385652 | — | — | 1 | 6.85 |
| CHEMBL385220 | — | — | 1 | 6.76 |
| CHEMBL217074 | — | — | 1 | 6.73 |
| CHEMBL214903 | — | — | 1 | 6.57 |
| CHEMBL215013 | — | — | 1 | 6.55 |
| CHEMBL215272 | — | — | 1 | 6.51 |
| CHEMBL214599 | — | — | 1 | 6.46 |
| CHEMBL215255 | — | — | 1 | 6.41 |
| CHEMBL214804 | — | — | 1 | 6.40 |
| CHEMBL214844 | — | — | 1 | 6.38 |
| CHEMBL215574 | — | — | 1 | 6.37 |
| CHEMBL385384 | — | — | 1 | 6.37 |
| CHEMBL384953 | — | — | 1 | 6.37 |
| CHEMBL215877 | — | — | 1 | 6.01 |
| CHEMBL385704 | — | — | 1 | - |
| CHEMBL387045 | — | — | 1 | - |
| CHEMBL262219 | — | — | 1 | - |
| CHEMBL214732 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL384402 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL215090 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL384847 | — | EC50 | = | 82.0 | nM | 7.09 |
| CHEMBL384271 | — | EC50 | = | 83.0 | nM | 7.08 |
| CHEMBL213197 | — | EC50 | = | 97.0 | nM | 7.01 |
| CHEMBL385608 | — | EC50 | = | 103.0 | nM | 6.99 |
| CHEMBL215575 | — | EC50 | = | 111.0 | nM | 6.96 |
| CHEMBL385652 | — | EC50 | = | 142.0 | nM | 6.85 |
| CHEMBL385220 | — | EC50 | = | 174.0 | nM | 6.76 |
| CHEMBL217074 | — | EC50 | = | 186.0 | nM | 6.73 |
| CHEMBL214903 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL215013 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL215272 | — | EC50 | = | 308.0 | nM | 6.51 |
| CHEMBL214599 | — | EC50 | = | 345.0 | nM | 6.46 |
| CHEMBL215255 | — | EC50 | = | 391.0 | nM | 6.41 |
| CHEMBL214804 | — | EC50 | = | 395.0 | nM | 6.40 |
| CHEMBL214844 | — | EC50 | = | 412.0 | nM | 6.38 |
| CHEMBL215574 | — | EC50 | = | 426.0 | nM | 6.37 |
| CHEMBL385384 | — | EC50 | = | 423.0 | nM | 6.37 |
| CHEMBL384953 | — | EC50 | = | 423.0 | nM | 6.37 |
| CHEMBL215877 | — | EC50 | = | 965.0 | nM | 6.01 |
| CHEMBL385704 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL387045 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL262219 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL214732 | — | EC50 | - | — | - |