Assay Detail
Binding
CHEMBL748107
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to displace [3H]CPP from NMDA receptor in rat brain membrane
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Generation of N-methyl-D-aspartate agonist and competitive antagonist pharmacophore models. Design and synthesis of phosphonoalkyl-substituted tetrahydroisoquinolines as novel antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 53 | 5.61 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL26475 | — | — | 1 | 7.85 |
| CHEMBL29811 | CGP-37849 | — | 1 | 7.46 |
| CHEMBL283032 | — | — | 1 | 7.41 |
| CHEMBL39664 | SELFOTEL | 2.0 | 1 | 7.27 |
| CHEMBL284445 | — | — | 1 | 7.11 |
| CHEMBL28523 | — | — | 1 | 7.10 |
| CHEMBL22304 | — | — | 1 | 7.09 |
| CHEMBL29698 | — | — | 1 | 6.85 |
| CHEMBL29877 | — | — | 1 | 6.57 |
| CHEMBL29244 | — | — | 1 | 6.50 |
| CHEMBL30163 | — | — | 1 | 6.35 |
| CHEMBL435945 | — | — | 1 | 6.18 |
| CHEMBL282983 | — | — | 1 | 6.10 |
| CHEMBL28501 | — | — | 1 | 6.09 |
| CHEMBL280814 | — | — | 1 | 6.07 |
| CHEMBL22168 | — | — | 1 | 6.00 |
| CHEMBL28838 | — | — | 1 | 5.80 |
| CHEMBL29072 | — | — | 1 | 5.71 |
| CHEMBL28609 | — | — | 1 | 5.66 |
| CHEMBL28713 | — | — | 1 | 5.57 |
| CHEMBL418204 | — | — | 1 | 5.55 |
| CHEMBL280850 | — | — | 1 | 5.39 |
| CHEMBL2114361 | — | — | 1 | 5.24 |
| CHEMBL280846 | — | — | 1 | 5.23 |
| CHEMBL29634 | — | — | 1 | 5.08 |
| CHEMBL28900 | — | — | 1 | 5.04 |
| CHEMBL30021 | — | — | 1 | 5.03 |
| CHEMBL436148 | — | — | 1 | 5.01 |
| CHEMBL280828 | — | — | 1 | 5.00 |
| CHEMBL284895 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL26475 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL29811 | CGP-37849 | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL283032 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL39664 | SELFOTEL | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL284445 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL28523 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL22304 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL29698 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL29877 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL29244 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL30163 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL435945 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL282983 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL28501 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL280814 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL22168 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL28838 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL29072 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL28609 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL28713 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL418204 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL280850 | — | IC50 | = | 4080.0 | nM | 5.39 |
| CHEMBL2114361 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL280846 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL29634 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL28900 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL30021 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL436148 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL280828 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL284895 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL282794 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL433238 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL27859 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL29613 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL29788 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL280911 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL279533 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL29081 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL29340 | — | IC50 | = | 61000.0 | nM | 4.21 |
| CHEMBL282119 | — | IC50 | = | 74000.0 | nM | 4.13 |
| CHEMBL442149 | — | IC50 | = | 83000.0 | nM | 4.08 |
| CHEMBL28931 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL287624 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL28784 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL417846 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL29432 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL280549 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL28582 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL417847 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL282546 | — | IC50 | > | 100000.0 | nM | - |