Assay Detail
Binding
CHEMBL1104010
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]SYM2081 from rat iGluR5 receptor expressed in Sf9 cells baculovirus system after 1 to 2 hrs by liquid scintillation counting
10
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, kainate 1 (CHEMBL2919) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological characterization at ionotropic glutamate receptors of compounds related to glutamate and its homologues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 4.90 | 6.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 2 | 6.86 |
| CHEMBL1094129 | 2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) | — | 4 | 5.09 |
| CHEMBL1098101 | 2-AMINO-4-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)BUTANOIC ACID (STRUCTURAL MIX) | — | 2 | 4.28 |
| CHEMBL1098104 | 2-AMINO-5-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PENTANOIC ACID (STRUCTURAL MIX) | — | 2 | 4.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL575060 | GLUTAMIC ACID | Ki | = | 138.04 | nM | 6.86 |
| CHEMBL575060 | GLUTAMIC ACID | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL1094129 | 2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) | Ki | = | 8100.0 | nM | 5.09 |
| CHEMBL1094129 | 2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) | Ki | = | 8128.31 | nM | 5.09 |
| CHEMBL1098101 | 2-AMINO-4-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)BUTANOIC ACID (STRUCTURAL MIX) | Ki | = | 53000.0 | nM | 4.28 |
| CHEMBL1098101 | 2-AMINO-4-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)BUTANOIC ACID (STRUCTURAL MIX) | Ki | = | 53703.18 | nM | 4.27 |
| CHEMBL1098104 | 2-AMINO-5-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PENTANOIC ACID (STRUCTURAL MIX) | Ki | = | 66069.34 | nM | 4.18 |
| CHEMBL1098104 | 2-AMINO-5-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PENTANOIC ACID (STRUCTURAL MIX) | Ki | = | 67000.0 | nM | 4.17 |
| CHEMBL1094129 | 2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) | Ki | = | 77000.0 | nM | 4.11 |
| CHEMBL1094129 | 2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) | Ki | = | 77624.71 | nM | 4.11 |