Assay Detail
Binding
CHEMBL746708
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro ability to inhibit the binding of [3H]glycine to glycine binding site of N-methyl-D-aspartate glutamate receptor in rat synaptic membranes
17
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Enantiomerically pure tetrahydroquinoline derivatives as in vivo potent antagonists of the glycine binding site associated to the NMDA receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 8.12 | 8.79 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL338753 | — | — | 3 | 8.79 |
| CHEMBL44793 | GAVESTINEL | 2.0 | 1 | 8.52 |
| CHEMBL339350 | — | — | 1 | 8.38 |
| CHEMBL124311 | — | — | 1 | 8.32 |
| CHEMBL446100 | — | — | 1 | 8.18 |
| CHEMBL126236 | — | — | 1 | 8.18 |
| CHEMBL126288 | — | — | 1 | 8.18 |
| CHEMBL340702 | — | — | 1 | 8.18 |
| CHEMBL129759 | — | — | 1 | 8.17 |
| CHEMBL126248 | — | — | 1 | 8.15 |
| CHEMBL339303 | — | — | 1 | 8.15 |
| CHEMBL124742 | — | — | 1 | 7.78 |
| CHEMBL129738 | — | — | 1 | 7.76 |
| CHEMBL339560 | — | — | 1 | 7.73 |
| CHEMBL341325 | — | — | 1 | 7.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL338753 | — | Ki | = | 1.622 | nM | 8.79 |
| CHEMBL338753 | — | Ki | = | 3.02 | nM | 8.52 |
| CHEMBL44793 | GAVESTINEL | Ki | = | 3.02 | nM | 8.52 |
| CHEMBL339350 | — | Ki | = | 4.169 | nM | 8.38 |
| CHEMBL124311 | — | Ki | = | 4.786 | nM | 8.32 |
| CHEMBL126288 | — | Ki | = | 6.607 | nM | 8.18 |
| CHEMBL340702 | — | Ki | = | 6.607 | nM | 8.18 |
| CHEMBL126236 | — | Ki | = | 6.607 | nM | 8.18 |
| CHEMBL446100 | — | Ki | = | 6.607 | nM | 8.18 |
| CHEMBL129759 | — | Ki | = | 6.761 | nM | 8.17 |
| CHEMBL339303 | — | Ki | = | 7.079 | nM | 8.15 |
| CHEMBL126248 | — | Ki | = | 7.079 | nM | 8.15 |
| CHEMBL124742 | — | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL129738 | — | Ki | = | 17.38 | nM | 7.76 |
| CHEMBL339560 | — | Ki | = | 18.62 | nM | 7.73 |
| CHEMBL341325 | — | Ki | = | 19.05 | nM | 7.72 |
| CHEMBL338753 | — | Ki | = | 50.12 | nM | 7.30 |