Assay Detail
Functional
CHEMBL1052812
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Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
19
Total Activities
19
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 | Intermediate |
Publication
Substituted 2-aminothiopen-derivatives: a potential new class of GluR6-antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.02 | 6.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL566136 | — | — | 1 | 6.12 |
| CHEMBL568515 | — | — | 1 | 5.62 |
| CHEMBL579009 | — | — | 1 | 5.46 |
| CHEMBL577069 | — | — | 1 | 5.44 |
| CHEMBL288166 | 2S,4R-4-METHYLGLUTAMATE | — | 1 | 5.40 |
| CHEMBL568300 | — | — | 1 | 5.39 |
| CHEMBL291935 | — | — | 1 | 5.35 |
| CHEMBL566530 | — | — | 1 | 5.24 |
| CHEMBL91 | MICONAZOLE | 4.0 | 1 | 5.19 |
| CHEMBL577248 | — | — | 1 | 5.07 |
| CHEMBL575059 | — | — | 1 | 5.00 |
| CHEMBL566318 | — | — | 1 | 4.97 |
| CHEMBL565503 | — | — | 1 | 4.92 |
| CHEMBL584345 | — | — | 1 | 4.68 |
| CHEMBL9790 | — | — | 1 | 4.64 |
| CHEMBL567862 | — | — | 1 | 4.42 |
| CHEMBL566754 | — | — | 1 | 4.27 |
| CHEMBL565502 | — | — | 1 | 4.15 |
| CHEMBL222519 | NBQX | — | 1 | 4.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL566136 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL568515 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL579009 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL577069 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL288166 | 2S,4R-4-METHYLGLUTAMATE | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL568300 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL291935 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL566530 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL91 | MICONAZOLE | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL577248 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL575059 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL566318 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL565503 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL584345 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL9790 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL567862 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL566754 | — | IC50 | = | 54000.0 | nM | 4.27 |
| CHEMBL565502 | — | IC50 | = | 71000.0 | nM | 4.15 |
| CHEMBL222519 | NBQX | IC50 | = | 74000.0 | nM | 4.13 |