Assay Detail
Functional
CHEMBL1817069
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at Non-desensitized homomeric rat GluK1(Q)1b mutant expressed in Xenopus oocytes by two-electrode voltage-clamp electrophysiology
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | Oocyte |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 7 | 5.44 | 6.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL288166 | 2S,4R-4-METHYLGLUTAMATE | — | 1 | 6.25 |
| CHEMBL492630 | — | — | 1 | 6.14 |
| CHEMBL492469 | — | — | 1 | 5.81 |
| CHEMBL1812598 | — | — | 1 | 5.45 |
| CHEMBL1812596 | — | — | 1 | 5.37 |
| CHEMBL337577 | — | — | 1 | 5.01 |
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 1 | 4.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL288166 | 2S,4R-4-METHYLGLUTAMATE | EC50 | = | 558.0 | nM | 6.25 |
| CHEMBL492630 | — | EC50 | = | 719.0 | nM | 6.14 |
| CHEMBL492469 | — | EC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL1812598 | — | EC50 | = | 3550.0 | nM | 5.45 |
| CHEMBL1812596 | — | EC50 | = | 4230.0 | nM | 5.37 |
| CHEMBL337577 | — | EC50 | = | 9870.0 | nM | 5.01 |
| CHEMBL575060 | GLUTAMIC ACID | EC50 | = | 83500.0 | nM | 4.08 |