Assay Detail
Binding
CHEMBL701166
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Binding affinity against human ionotropic glutamate receptor ionotropic kainate 2 in HEK293 cells using [3H]kainate as radioligand
43
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Glutamate receptor ionotropic, kainate 2 (CHEMBL3683) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
4-Alkyl- and 4-cinnamylglutamic acid analogues are potent GluR5 kainate receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 43 | 5.53 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL288166 | 2S,4R-4-METHYLGLUTAMATE | — | 1 | 8.00 |
| CHEMBL275040 | KAINIC ACID | 2.0 | 1 | 7.50 |
| CHEMBL59284 | — | — | 2 | 7.32 |
| CHEMBL59551 | — | — | 1 | 6.80 |
| CHEMBL58808 | — | — | 1 | 6.47 |
| CHEMBL61697 | — | — | 1 | 6.30 |
| CHEMBL294683 | — | — | 1 | 6.25 |
| CHEMBL58718 | — | — | 1 | 6.08 |
| CHEMBL59792 | — | — | 1 | 6.00 |
| CHEMBL58054 | — | — | 1 | 5.95 |
| CHEMBL293548 | — | — | 1 | 5.85 |
| CHEMBL62086 | — | — | 1 | 5.84 |
| CHEMBL59297 | — | — | 1 | 5.80 |
| CHEMBL61997 | — | — | 1 | 5.61 |
| CHEMBL60406 | — | — | 1 | 5.54 |
| CHEMBL304434 | — | — | 1 | 5.53 |
| CHEMBL294139 | — | — | 1 | 5.49 |
| CHEMBL60168 | — | — | 1 | 5.42 |
| CHEMBL293118 | — | — | 1 | 5.40 |
| CHEMBL292745 | — | — | 1 | 5.36 |
| CHEMBL61751 | — | — | 1 | 5.36 |
| CHEMBL293829 | — | — | 1 | 5.35 |
| CHEMBL61307 | — | — | 1 | 5.27 |
| CHEMBL292896 | — | — | 1 | 5.25 |
| CHEMBL300368 | — | — | 1 | 5.22 |
| CHEMBL305346 | — | — | 1 | 5.20 |
| CHEMBL62053 | — | — | 1 | 5.14 |
| CHEMBL301915 | — | — | 1 | 5.14 |
| CHEMBL299449 | — | — | 1 | 5.08 |
| CHEMBL58541 | — | — | 1 | 4.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL288166 | 2S,4R-4-METHYLGLUTAMATE | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL275040 | KAINIC ACID | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL59284 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL59284 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL59551 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL58808 | — | Ki | = | 339.0 | nM | 6.47 |
| CHEMBL61697 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL294683 | — | Ki | = | 559.0 | nM | 6.25 |
| CHEMBL58718 | — | Ki | = | 823.0 | nM | 6.08 |
| CHEMBL59792 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL58054 | — | Ki | = | 1132.0 | nM | 5.95 |
| CHEMBL293548 | — | Ki | = | 1404.0 | nM | 5.85 |
| CHEMBL62086 | — | Ki | = | 1456.0 | nM | 5.84 |
| CHEMBL59297 | — | Ki | = | 1568.0 | nM | 5.80 |
| CHEMBL61997 | — | Ki | = | 2450.0 | nM | 5.61 |
| CHEMBL60406 | — | Ki | = | 2893.0 | nM | 5.54 |
| CHEMBL304434 | — | Ki | = | 2984.0 | nM | 5.53 |
| CHEMBL294139 | — | Ki | = | 3258.0 | nM | 5.49 |
| CHEMBL60168 | — | Ki | = | 3845.0 | nM | 5.42 |
| CHEMBL293118 | — | Ki | = | 3987.0 | nM | 5.40 |
| CHEMBL61751 | — | Ki | = | 4366.0 | nM | 5.36 |
| CHEMBL292745 | — | Ki | = | 4375.0 | nM | 5.36 |
| CHEMBL293829 | — | Ki | = | 4491.0 | nM | 5.35 |
| CHEMBL61307 | — | Ki | = | 5373.0 | nM | 5.27 |
| CHEMBL292896 | — | Ki | = | 5650.0 | nM | 5.25 |
| CHEMBL300368 | — | Ki | = | 6024.0 | nM | 5.22 |
| CHEMBL305346 | — | Ki | = | 6349.0 | nM | 5.20 |
| CHEMBL62053 | — | Ki | = | 7207.0 | nM | 5.14 |
| CHEMBL301915 | — | Ki | = | 7216.0 | nM | 5.14 |
| CHEMBL299449 | — | Ki | = | 8250.0 | nM | 5.08 |
| CHEMBL58541 | — | Ki | = | 10247.0 | nM | 4.99 |
| CHEMBL60114 | — | Ki | = | 11185.0 | nM | 4.95 |
| CHEMBL59948 | — | Ki | = | 13949.0 | nM | 4.86 |
| CHEMBL62055 | — | Ki | = | 13800.0 | nM | 4.86 |
| CHEMBL59299 | — | Ki | = | 22340.0 | nM | 4.65 |
| CHEMBL2111523 | — | Ki | = | 22529.0 | nM | 4.65 |
| CHEMBL61434 | — | Ki | = | 27280.0 | nM | 4.56 |
| CHEMBL302680 | — | Ki | = | 27532.0 | nM | 4.56 |
| CHEMBL58027 | — | Ki | = | 41152.0 | nM | 4.39 |
| CHEMBL59286 | — | Ki | = | 42809.0 | nM | 4.37 |
| CHEMBL291491 | — | Ki | = | 43929.0 | nM | 4.36 |
| CHEMBL302402 | — | Ki | = | 68547.0 | nM | 4.16 |
| CHEMBL305387 | — | Ki | > | 10000.0 | nM | - |