Assay Detail
Binding
CHEMBL1013087
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Displacement of [3H]SYM2081 from rat recombinant iGluR5
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 1 (CHEMBL2919) ↗| 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 | 7.36 | 9.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL288166 | 2S,4R-4-METHYLGLUTAMATE | — | 2 | 9.18 |
| CHEMBL482097 | DOMORIC ACID | — | 2 | 8.97 |
| CHEMBL500042 | — | — | 2 | 8.42 |
| CHEMBL479804 | — | — | 2 | 8.18 |
| CHEMBL482080 | — | — | 2 | 7.38 |
| CHEMBL275040 | KAINIC ACID | 2.0 | 2 | 7.15 |
| CHEMBL518313 | — | — | 2 | 6.86 |
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 2 | 6.86 |
| CHEMBL279956 | QUISQUALATE | — | 2 | 6.77 |
| CHEMBL479805 | — | — | 2 | 6.20 |
| CHEMBL279561 | DIHYDROKAINATE | — | 2 | 5.09 |
| CHEMBL500448 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL288166 | 2S,4R-4-METHYLGLUTAMATE | Ki | = | 0.663 | nM | 9.18 |
| CHEMBL288166 | 2S,4R-4-METHYLGLUTAMATE | Ki | = | 0.6607 | nM | 9.18 |
| CHEMBL482097 | DOMORIC ACID | Ki | = | 1.072 | nM | 8.97 |
| CHEMBL482097 | DOMORIC ACID | Ki | = | 1.11 | nM | 8.96 |
| CHEMBL500042 | — | Ki | = | 3.81 | nM | 8.42 |
| CHEMBL500042 | — | Ki | = | 3.802 | nM | 8.42 |
| CHEMBL479804 | — | Ki | = | 6.607 | nM | 8.18 |
| CHEMBL479804 | — | Ki | = | 7.45 | nM | 8.13 |
| CHEMBL482080 | — | Ki | = | 41.69 | nM | 7.38 |
| CHEMBL482080 | — | Ki | = | 42.8 | nM | 7.37 |
| CHEMBL275040 | KAINIC ACID | Ki | = | 70.79 | nM | 7.15 |
| CHEMBL275040 | KAINIC ACID | Ki | = | 75.9 | nM | 7.12 |
| CHEMBL518313 | — | Ki | = | 138.04 | nM | 6.86 |
| CHEMBL575060 | GLUTAMIC ACID | Ki | = | 138.04 | nM | 6.86 |
| CHEMBL518313 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL575060 | GLUTAMIC ACID | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL279956 | QUISQUALATE | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL279956 | QUISQUALATE | Ki | = | 169.82 | nM | 6.77 |
| CHEMBL479805 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL479805 | — | Ki | = | 641.0 | nM | 6.19 |
| CHEMBL279561 | DIHYDROKAINATE | Ki | = | 8180.0 | nM | 5.09 |
| CHEMBL279561 | DIHYDROKAINATE | Ki | = | 8128.31 | nM | 5.09 |
| CHEMBL500448 | — | Ki | - | — | - |