Assay Detail
Binding
CHEMBL747013
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Binding affinity towards N-methyl-D-aspartate glutamate receptor 1 in rat cortical membranes using [3H]glycine as radioligand
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Glutamate receptor ionotropic, NMDA 1 (CHEMBL330) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
4,5-Dihydro-1,2,4-triazolo[1,5-a]quinoxalin-4-ones: excitatory amino acid antagonists with combined glycine/NMDA and AMPA receptor affinity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 5.44 | 6.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL311221 | — | — | 1 | 6.85 |
| CHEMBL83551 | — | — | 1 | 6.77 |
| CHEMBL82050 | — | — | 1 | 6.41 |
| CHEMBL84283 | — | — | 1 | 6.24 |
| CHEMBL420392 | — | — | 1 | 6.15 |
| CHEMBL81874 | — | — | 1 | 6.15 |
| CHEMBL310352 | — | — | 1 | 5.96 |
| CHEMBL309441 | — | — | 1 | 5.96 |
| CHEMBL79556 | — | — | 1 | 5.75 |
| CHEMBL310014 | — | — | 1 | 5.66 |
| CHEMBL81025 | — | — | 1 | 5.58 |
| CHEMBL83919 | — | — | 1 | 5.52 |
| CHEMBL79312 | — | — | 1 | 5.46 |
| CHEMBL83322 | — | — | 1 | 5.35 |
| CHEMBL309548 | — | — | 1 | 5.32 |
| CHEMBL81367 | — | — | 1 | 5.29 |
| CHEMBL83901 | — | — | 1 | 5.27 |
| CHEMBL82684 | — | — | 1 | 5.19 |
| CHEMBL82295 | — | — | 1 | 5.14 |
| CHEMBL309206 | — | — | 1 | 5.12 |
| CHEMBL313269 | — | — | 1 | 5.06 |
| CHEMBL84094 | — | — | 1 | 5.01 |
| CHEMBL86164 | — | — | 1 | 4.78 |
| CHEMBL83902 | — | — | 1 | 4.56 |
| CHEMBL311860 | — | — | 1 | 4.10 |
| CHEMBL315484 | — | — | 1 | 4.06 |
| CHEMBL83855 | — | — | 1 | 4.05 |
| CHEMBL310544 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL311221 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL83551 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL82050 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL84283 | — | Ki | = | 570.0 | nM | 6.24 |
| CHEMBL420392 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL81874 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL310352 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL309441 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL79556 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL310014 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL81025 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL83919 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL79312 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL83322 | — | Ki | = | 4500.0 | nM | 5.35 |
| CHEMBL309548 | — | Ki | = | 4800.0 | nM | 5.32 |
| CHEMBL81367 | — | Ki | = | 5100.0 | nM | 5.29 |
| CHEMBL83901 | — | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL82684 | — | Ki | = | 6500.0 | nM | 5.19 |
| CHEMBL82295 | — | Ki | = | 7200.0 | nM | 5.14 |
| CHEMBL309206 | — | Ki | = | 7500.0 | nM | 5.12 |
| CHEMBL313269 | — | Ki | = | 8800.0 | nM | 5.06 |
| CHEMBL84094 | — | Ki | = | 9700.0 | nM | 5.01 |
| CHEMBL86164 | — | Ki | = | 16700.0 | nM | 4.78 |
| CHEMBL83902 | — | Ki | = | 27700.0 | nM | 4.56 |
| CHEMBL311860 | — | Ki | = | 79400.0 | nM | 4.10 |
| CHEMBL315484 | — | Ki | = | 88000.0 | nM | 4.06 |
| CHEMBL83855 | — | Ki | = | 88200.0 | nM | 4.05 |
| CHEMBL310544 | — | Ki | > | 100000.0 | nM | - |