Assay Detail
Functional
CHEMBL895662
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Agonist activity at GluR1 expressed in HEK293 cells by Fluo-4/Ca2+ assay
12
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Functional characterization of Tet-AMPA [tetrazolyl-2-amino-3-(3-hydroxy-5-methyl- 4-isoxazolyl)propionic acid] analogues at ionotropic glutamate receptors GluR1-GluR4. The molecular basis for the functional selectivity profile of 2-Bn-Tet-AMPA.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 4.27 | 4.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL370941 | — | — | 2 | 4.38 |
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 2 | 4.15 |
| CHEMBL317790 | — | — | 2 | - |
| CHEMBL388746 | — | — | 2 | - |
| CHEMBL193087 | — | — | 2 | - |
| CHEMBL372643 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL370941 | — | EC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL575060 | GLUTAMIC ACID | EC50 | = | 71000.0 | nM | 4.15 |
| CHEMBL575060 | GLUTAMIC ACID | EC50 | = | 15848931924611.11 | nM | - |
| CHEMBL317790 | — | EC50 | > | 3000000.0 | nM | - |
| CHEMBL317790 | — | EC50 | < | 316227766016.84 | nM | - |
| CHEMBL388746 | — | EC50 | = | 3000000.0 | nM | - |
| CHEMBL388746 | — | EC50 | < | 316227766016.84 | nM | - |
| CHEMBL193087 | — | EC50 | = | 550000.0 | nM | - |
| CHEMBL193087 | — | EC50 | = | 1995262314968.88 | nM | - |
| CHEMBL372643 | — | EC50 | = | 480000.0 | nM | - |
| CHEMBL372643 | — | EC50 | = | 1995262314968.88 | nM | - |
| CHEMBL370941 | — | EC50 | = | 25118864315095.82 | nM | - |