Assay Detail
Functional
CHEMBL1059448
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at rat recombinant GluR4 flip isomer expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay
6
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
The glutamate receptor GluR5 agonist (S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid and the 8-methyl analogue: synthesis, molecular pharmacology, and biostructural characterization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 4.67 | 5.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL28472 | — | — | 1 | 5.17 |
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 1 | 4.70 |
| CHEMBL553028 | — | — | 2 | 4.46 |
| CHEMBL275040 | KAINIC ACID | 2.0 | 1 | 4.33 |
| CHEMBL27130 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL28472 | — | EC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL575060 | GLUTAMIC ACID | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL553028 | — | EC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL275040 | KAINIC ACID | EC50 | = | 47000.0 | nM | 4.33 |
| CHEMBL27130 | — | EC50 | = | 150.0 | % | - |
| CHEMBL553028 | — | EC50 | = | 158489.32 | nM | - |