Assay Detail
Binding
CHEMBL751136
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Tested for the binding affinity at glycine recognition site of the NMDA receptor in rat cortical membranes using radiolabeled [3H]- L-689 560
7
Total Activities
7
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
Anticonvulsant activity of glycine-site NMDA antagonists. 2. trans 2-carboxy-4-substituted tetrahydroquinolines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.03 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL424158 | — | — | 1 | 8.05 |
| CHEMBL133163 | — | — | 1 | 7.72 |
| CHEMBL131520 | — | — | 1 | 7.50 |
| CHEMBL50267 | — | — | 1 | 7.19 |
| CHEMBL293523 | — | — | 1 | 7.13 |
| CHEMBL323335 | — | — | 1 | 6.77 |
| CHEMBL299155 | TRANSTORINE | 1.0 | 1 | 4.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL424158 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL133163 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL131520 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL50267 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL293523 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL323335 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL299155 | TRANSTORINE | IC50 | = | 13800.0 | nM | 4.86 |