Assay Detail
Binding
CHEMBL701552
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Inhibition of [3H]kainate binding at rat forebrain ionotropic glutamate receptor kainate 2
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Glutamate receptor ionotropic, kainate 2 (CHEMBL3607) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis of a series of aryl kainic acid analogs and evaluation in cells stably expressing the kainate receptor humGluR6.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 7.95 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121741 | — | — | 1 | 8.80 |
| CHEMBL120785 | — | — | 1 | 8.72 |
| CHEMBL121113 | — | — | 1 | 8.68 |
| CHEMBL332818 | — | — | 1 | 8.66 |
| CHEMBL334119 | — | — | 1 | 8.64 |
| CHEMBL332334 | — | — | 1 | 8.59 |
| CHEMBL120003 | — | — | 1 | 8.57 |
| CHEMBL122507 | — | — | 1 | 8.55 |
| CHEMBL332168 | — | — | 1 | 8.46 |
| CHEMBL120288 | — | — | 1 | 8.44 |
| CHEMBL120753 | — | — | 1 | 8.44 |
| CHEMBL275040 | KAINIC ACID | 2.0 | 1 | 8.43 |
| CHEMBL333015 | — | — | 1 | 8.41 |
| CHEMBL431839 | — | — | 1 | 8.41 |
| CHEMBL120450 | — | — | 1 | 8.32 |
| CHEMBL332114 | — | — | 1 | 8.21 |
| CHEMBL332467 | — | — | 1 | 8.11 |
| CHEMBL118502 | — | — | 1 | 8.05 |
| CHEMBL333790 | — | — | 1 | 8.04 |
| CHEMBL121461 | — | — | 1 | 8.02 |
| CHEMBL368275 | — | — | 1 | 7.92 |
| CHEMBL334024 | — | — | 1 | 7.80 |
| CHEMBL331339 | — | — | 1 | 7.73 |
| CHEMBL431657 | — | — | 1 | 7.63 |
| CHEMBL177627 | — | — | 1 | 6.90 |
| CHEMBL330771 | — | — | 1 | 6.68 |
| CHEMBL121194 | — | — | 1 | 6.64 |
| CHEMBL121311 | — | — | 1 | 5.52 |
| CHEMBL332126 | — | — | 1 | 5.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121741 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL120785 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL121113 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL332818 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL334119 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL332334 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL120003 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL122507 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL332168 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL120288 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL120753 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL275040 | KAINIC ACID | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL333015 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL431839 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL120450 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL332114 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL332467 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL118502 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL333790 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL121461 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL368275 | — | Ki | = | 11.9 | nM | 7.92 |
| CHEMBL334024 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL331339 | — | Ki | = | 18.5 | nM | 7.73 |
| CHEMBL431657 | — | Ki | = | 23.3 | nM | 7.63 |
| CHEMBL177627 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL330771 | — | Ki | = | 210.3 | nM | 6.68 |
| CHEMBL121194 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL121311 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL332126 | — | Ki | = | 5400.0 | nM | 5.27 |