Assay Detail
Binding
CHEMBL699991
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Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2
36
Total Activities
36
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 (CHEMBL3683) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 36 | 6.72 | 7.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL420720 | DOMOATE | — | 1 | 7.74 |
| CHEMBL121741 | — | — | 1 | 7.53 |
| CHEMBL431839 | — | — | 1 | 7.50 |
| CHEMBL120003 | — | — | 1 | 7.42 |
| CHEMBL332334 | — | — | 1 | 7.39 |
| CHEMBL275040 | KAINIC ACID | 2.0 | 1 | 7.28 |
| CHEMBL120785 | — | — | 1 | 7.26 |
| CHEMBL333015 | — | — | 1 | 7.24 |
| CHEMBL332467 | — | — | 1 | 7.08 |
| CHEMBL121113 | — | — | 1 | 7.04 |
| CHEMBL332168 | — | — | 1 | 7.03 |
| CHEMBL334119 | — | — | 1 | 6.97 |
| CHEMBL332818 | — | — | 1 | 6.91 |
| CHEMBL332114 | — | — | 1 | 6.90 |
| CHEMBL121514 | — | — | 1 | 6.89 |
| CHEMBL120753 | — | — | 1 | 6.88 |
| CHEMBL333790 | — | — | 1 | 6.88 |
| CHEMBL120450 | — | — | 1 | 6.84 |
| CHEMBL122507 | — | — | 1 | 6.83 |
| CHEMBL120288 | — | — | 1 | 6.83 |
| CHEMBL121461 | — | — | 1 | 6.77 |
| CHEMBL368275 | — | — | 1 | 6.68 |
| CHEMBL331339 | — | — | 1 | 6.58 |
| CHEMBL431657 | — | — | 1 | 6.56 |
| CHEMBL118502 | — | — | 1 | 6.54 |
| CHEMBL123006 | — | — | 1 | 6.18 |
| CHEMBL334024 | — | — | 1 | 6.18 |
| CHEMBL122523 | — | — | 1 | 5.89 |
| CHEMBL177627 | — | — | 1 | 5.89 |
| CHEMBL332126 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL420720 | DOMOATE | Ki | = | 18.3 | nM | 7.74 |
| CHEMBL121741 | — | Ki | = | 29.8 | nM | 7.53 |
| CHEMBL431839 | — | Ki | = | 31.7 | nM | 7.50 |
| CHEMBL120003 | — | Ki | = | 38.4 | nM | 7.42 |
| CHEMBL332334 | — | Ki | = | 41.1 | nM | 7.39 |
| CHEMBL275040 | KAINIC ACID | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL120785 | — | Ki | = | 54.3 | nM | 7.26 |
| CHEMBL333015 | — | Ki | = | 57.4 | nM | 7.24 |
| CHEMBL332467 | — | Ki | = | 82.2 | nM | 7.08 |
| CHEMBL121113 | — | Ki | = | 90.6 | nM | 7.04 |
| CHEMBL332168 | — | Ki | = | 93.5 | nM | 7.03 |
| CHEMBL334119 | — | Ki | = | 107.8 | nM | 6.97 |
| CHEMBL332818 | — | Ki | = | 122.5 | nM | 6.91 |
| CHEMBL332114 | — | Ki | = | 126.2 | nM | 6.90 |
| CHEMBL121514 | — | Ki | = | 129.3 | nM | 6.89 |
| CHEMBL120753 | — | Ki | = | 131.5 | nM | 6.88 |
| CHEMBL333790 | — | Ki | = | 130.6 | nM | 6.88 |
| CHEMBL120450 | — | Ki | = | 145.6 | nM | 6.84 |
| CHEMBL122507 | — | Ki | = | 146.6 | nM | 6.83 |
| CHEMBL120288 | — | Ki | = | 146.8 | nM | 6.83 |
| CHEMBL121461 | — | Ki | = | 169.3 | nM | 6.77 |
| CHEMBL368275 | — | Ki | = | 209.6 | nM | 6.68 |
| CHEMBL331339 | — | Ki | = | 262.7 | nM | 6.58 |
| CHEMBL431657 | — | Ki | = | 275.3 | nM | 6.56 |
| CHEMBL118502 | — | Ki | = | 288.0 | nM | 6.54 |
| CHEMBL123006 | — | Ki | = | 663.3 | nM | 6.18 |
| CHEMBL334024 | — | Ki | = | 667.0 | nM | 6.18 |
| CHEMBL122523 | — | Ki | = | 1284.0 | nM | 5.89 |
| CHEMBL177627 | — | Ki | = | 1295.7 | nM | 5.89 |
| CHEMBL332126 | — | Ki | = | 2303.3 | nM | 5.64 |
| CHEMBL330771 | — | Ki | = | 2423.3 | nM | 5.62 |
| CHEMBL121510 | — | Ki | = | 3109.2 | nM | 5.51 |
| CHEMBL121194 | — | Ki | = | 6969.0 | nM | 5.16 |
| CHEMBL121311 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL420724 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL331477 | — | Ki | > | 10000.0 | nM | - |