Assay Detail
Binding
CHEMBL1013088
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Displacement of [3H]SYM2081 from rat recombinant iGluR6
22
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, kainate 2 (CHEMBL3607) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 6.43 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL482097 | DOMORIC ACID | — | 2 | 8.24 |
| CHEMBL275040 | KAINIC ACID | 2.0 | 2 | 7.91 |
| CHEMBL288166 | 2S,4R-4-METHYLGLUTAMATE | — | 2 | 7.83 |
| CHEMBL500042 | — | — | 2 | 6.92 |
| CHEMBL279956 | QUISQUALATE | — | 2 | 6.88 |
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 2 | 6.48 |
| CHEMBL482080 | — | — | 2 | 5.21 |
| CHEMBL479804 | — | — | 2 | 5.02 |
| CHEMBL479805 | — | — | 2 | 4.99 |
| CHEMBL279561 | DIHYDROKAINATE | — | 2 | 4.92 |
| CHEMBL500448 | — | — | 1 | - |
| CHEMBL518313 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL482097 | DOMORIC ACID | Ki | = | 5.754 | nM | 8.24 |
| CHEMBL482097 | DOMORIC ACID | Ki | = | 6.04 | nM | 8.22 |
| CHEMBL275040 | KAINIC ACID | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL275040 | KAINIC ACID | Ki | = | 12.7 | nM | 7.90 |
| CHEMBL288166 | 2S,4R-4-METHYLGLUTAMATE | Ki | = | 14.79 | nM | 7.83 |
| CHEMBL288166 | 2S,4R-4-METHYLGLUTAMATE | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL500042 | — | Ki | = | 120.23 | nM | 6.92 |
| CHEMBL500042 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL279956 | QUISQUALATE | Ki | = | 131.83 | nM | 6.88 |
| CHEMBL279956 | QUISQUALATE | Ki | = | 134.0 | nM | 6.87 |
| CHEMBL575060 | GLUTAMIC ACID | Ki | = | 331.0 | nM | 6.48 |
| CHEMBL575060 | GLUTAMIC ACID | Ki | = | 331.13 | nM | 6.48 |
| CHEMBL482080 | — | Ki | = | 6165.95 | nM | 5.21 |
| CHEMBL482080 | — | Ki | = | 6670.0 | nM | 5.18 |
| CHEMBL479804 | — | Ki | = | 9549.93 | nM | 5.02 |
| CHEMBL479804 | — | Ki | = | 9660.0 | nM | 5.01 |
| CHEMBL479805 | — | Ki | = | 10232.93 | nM | 4.99 |
| CHEMBL479805 | — | Ki | = | 10600.0 | nM | 4.97 |
| CHEMBL279561 | DIHYDROKAINATE | Ki | = | 12022.64 | nM | 4.92 |
| CHEMBL279561 | DIHYDROKAINATE | Ki | = | 12300.0 | nM | 4.91 |
| CHEMBL500448 | — | Ki | - | — | - | |
| CHEMBL518313 | — | Ki | > | 100000.0 | nM | - |