Assay Detail
Binding
CHEMBL1104007
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CGP39653 from NMDA receptor in Sprague-Dawley rat brain membranes
23
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| 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 | 23 | 5.17 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 1 | 6.70 |
| CHEMBL1098104 | 2-AMINO-5-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PENTANOIC ACID (STRUCTURAL MIX) | — | 6 | 5.75 |
| CHEMBL1098101 | 2-AMINO-4-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)BUTANOIC ACID (STRUCTURAL MIX) | — | 6 | 5.47 |
| CHEMBL291278 | N-METHYL-D-ASPARTIC ACID (NMDA) | 2.0 | 1 | 5.21 |
| CHEMBL1099097 | — | — | 2 | 5.20 |
| CHEMBL1094129 | 2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) | — | 5 | 4.90 |
| CHEMBL275040 | KAINIC ACID | 2.0 | 1 | - |
| CHEMBL13378 | (R,S)-AMPA | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL575060 | GLUTAMIC ACID | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL1098104 | 2-AMINO-5-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PENTANOIC ACID (STRUCTURAL MIX) | Ki | = | 1778.28 | nM | 5.75 |
| CHEMBL1098104 | 2-AMINO-5-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PENTANOIC ACID (STRUCTURAL MIX) | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL1098104 | 2-AMINO-5-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PENTANOIC ACID (STRUCTURAL MIX) | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL1098104 | 2-AMINO-5-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PENTANOIC ACID (STRUCTURAL MIX) | Ki | = | 2884.03 | nM | 5.54 |
| CHEMBL1098101 | 2-AMINO-4-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)BUTANOIC ACID (STRUCTURAL MIX) | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL1098101 | 2-AMINO-4-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)BUTANOIC ACID (STRUCTURAL MIX) | Ki | = | 3388.44 | nM | 5.47 |
| CHEMBL1098101 | 2-AMINO-4-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)BUTANOIC ACID (STRUCTURAL MIX) | Ki | = | 4897.79 | nM | 5.31 |
| CHEMBL1098101 | 2-AMINO-4-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)BUTANOIC ACID (STRUCTURAL MIX) | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL291278 | N-METHYL-D-ASPARTIC ACID (NMDA) | Ki | = | 6200.0 | nM | 5.21 |
| CHEMBL1099097 | — | Ki | = | 6309.57 | nM | 5.20 |
| CHEMBL1099097 | — | Ki | = | 6300.0 | nM | 5.20 |
| CHEMBL1094129 | 2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) | Ki | = | 12589.25 | nM | 4.90 |
| CHEMBL1094129 | 2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL1094129 | 2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) | Ki | = | 16000.0 | nM | 4.80 |
| CHEMBL1094129 | 2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) | Ki | = | 15848.93 | nM | 4.80 |
| CHEMBL1098104 | 2-AMINO-5-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PENTANOIC ACID (STRUCTURAL MIX) | Ki | = | 21877.62 | nM | 4.66 |
| CHEMBL1098104 | 2-AMINO-5-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PENTANOIC ACID (STRUCTURAL MIX) | Ki | = | 22000.0 | nM | 4.66 |
| CHEMBL1098101 | 2-AMINO-4-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)BUTANOIC ACID (STRUCTURAL MIX) | Ki | = | 73000.0 | nM | 4.14 |
| CHEMBL1098101 | 2-AMINO-4-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)BUTANOIC ACID (STRUCTURAL MIX) | Ki | = | 74131.02 | nM | 4.13 |
| CHEMBL1094129 | 2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) | Ki | > | 100000.0 | nM | - |
| CHEMBL275040 | KAINIC ACID | Ki | > | 100000.0 | nM | - |
| CHEMBL13378 | (R,S)-AMPA | Ki | > | 100000.0 | nM | - |