Assay Detail
Binding
CHEMBL747483
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity against 3[H]TCP binding to N-methyl-D-aspartate glutamate receptor in rat brain membranes
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Novel benzo[b]quinolizinium cations as uncompetitive N-methyl-D-aspartic acid (NMDA) antagonists: the relationship between log D and agonist independent (closed) NMDA channel block.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 7.38 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1202362 | — | — | 1 | 8.92 |
| CHEMBL1202359 | — | — | 1 | 8.74 |
| CHEMBL299087 | — | — | 1 | 8.70 |
| CHEMBL1202358 | — | — | 1 | 8.68 |
| CHEMBL4524083 | — | — | 1 | 8.57 |
| CHEMBL1202357 | — | — | 1 | 8.44 |
| CHEMBL1202361 | — | — | 1 | 8.22 |
| CHEMBL329612 | — | — | 1 | 8.09 |
| CHEMBL1202353 | — | — | 1 | 8.00 |
| CHEMBL1202364 | — | — | 1 | 7.92 |
| CHEMBL1202350 | — | — | 1 | 7.72 |
| CHEMBL1202351 | — | — | 1 | 7.72 |
| CHEMBL332545 | — | — | 1 | 7.62 |
| CHEMBL1202356 | — | — | 1 | 7.54 |
| CHEMBL1202349 | — | — | 1 | 7.41 |
| CHEMBL120537 | — | — | 1 | 7.19 |
| CHEMBL1202355 | — | — | 1 | 6.90 |
| CHEMBL1202367 | — | — | 1 | 6.80 |
| CHEMBL1202354 | — | — | 1 | 6.53 |
| CHEMBL1202360 | — | — | 1 | 6.46 |
| CHEMBL330878 | — | — | 1 | 6.20 |
| CHEMBL1202363 | — | — | 1 | 5.82 |
| CHEMBL1202352 | — | — | 1 | 5.47 |
| CHEMBL1202365 | — | — | 1 | 5.42 |
| CHEMBL120184 | — | — | 1 | 5.42 |
| CHEMBL120752 | — | — | 1 | - |
| CHEMBL330816 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1202362 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL1202359 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL299087 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1202358 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL4524083 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL1202357 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL1202361 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL329612 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL1202353 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1202364 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1202350 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL1202351 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL332545 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL1202356 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL1202349 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL120537 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL1202355 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL1202367 | — | Ki | = | 159.0 | nM | 6.80 |
| CHEMBL1202354 | — | Ki | = | 294.0 | nM | 6.53 |
| CHEMBL1202360 | — | Ki | = | 345.0 | nM | 6.46 |
| CHEMBL330878 | — | Ki | = | 633.0 | nM | 6.20 |
| CHEMBL1202363 | — | Ki | = | 1530.0 | nM | 5.82 |
| CHEMBL1202352 | — | Ki | = | 3377.0 | nM | 5.47 |
| CHEMBL1202365 | — | Ki | = | 3793.0 | nM | 5.42 |
| CHEMBL120184 | — | Ki | = | 3785.0 | nM | 5.42 |
| CHEMBL120752 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL330816 | — | Ki | > | 10000.0 | nM | - |