Assay Detail
Binding
CHEMBL1013089
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Displacement of [3H]SYM2081 from rat recombinant iGluR7
23
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 3 (CHEMBL3744) ↗| 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 | 23 | 6.56 | 8.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL482097 | DOMORIC ACID | — | 2 | 8.42 |
| CHEMBL275040 | KAINIC ACID | 2.0 | 2 | 8.42 |
| CHEMBL288166 | 2S,4R-4-METHYLGLUTAMATE | — | 2 | 8.33 |
| CHEMBL500042 | — | — | 2 | 7.30 |
| CHEMBL279561 | DIHYDROKAINATE | — | 2 | 6.44 |
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 2 | 6.31 |
| CHEMBL482080 | — | — | 2 | 6.02 |
| CHEMBL279956 | QUISQUALATE | — | 2 | 5.86 |
| CHEMBL479804 | — | — | 2 | 5.59 |
| CHEMBL479805 | — | — | 2 | 5.49 |
| CHEMBL518313 | — | — | 2 | 4.67 |
| CHEMBL500448 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL482097 | DOMORIC ACID | Ki | = | 3.802 | nM | 8.42 |
| CHEMBL482097 | DOMORIC ACID | Ki | = | 3.84 | nM | 8.42 |
| CHEMBL275040 | KAINIC ACID | Ki | = | 3.802 | nM | 8.42 |
| CHEMBL288166 | 2S,4R-4-METHYLGLUTAMATE | Ki | = | 4.677 | nM | 8.33 |
| CHEMBL288166 | 2S,4R-4-METHYLGLUTAMATE | Ki | = | 5.69 | nM | 8.24 |
| CHEMBL275040 | KAINIC ACID | Ki | = | 32.8 | nM | 7.48 |
| CHEMBL500042 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL500042 | — | Ki | = | 57.3 | nM | 7.24 |
| CHEMBL279561 | DIHYDROKAINATE | Ki | = | 363.08 | nM | 6.44 |
| CHEMBL279561 | DIHYDROKAINATE | Ki | = | 376.0 | nM | 6.42 |
| CHEMBL575060 | GLUTAMIC ACID | Ki | = | 494.0 | nM | 6.31 |
| CHEMBL575060 | GLUTAMIC ACID | Ki | = | 489.78 | nM | 6.31 |
| CHEMBL482080 | — | Ki | = | 954.99 | nM | 6.02 |
| CHEMBL482080 | — | Ki | = | 1010.0 | nM | 6.00 |
| CHEMBL279956 | QUISQUALATE | Ki | = | 1380.38 | nM | 5.86 |
| CHEMBL279956 | QUISQUALATE | Ki | = | 1670.0 | nM | 5.78 |
| CHEMBL479804 | — | Ki | = | 2570.4 | nM | 5.59 |
| CHEMBL479804 | — | Ki | = | 2820.0 | nM | 5.55 |
| CHEMBL479805 | — | Ki | = | 3235.94 | nM | 5.49 |
| CHEMBL479805 | — | Ki | = | 3460.0 | nM | 5.46 |
| CHEMBL518313 | — | Ki | = | 21379.62 | nM | 4.67 |
| CHEMBL518313 | — | Ki | = | 21400.0 | nM | 4.67 |
| CHEMBL500448 | — | Ki | - | — | - |