Assay Detail
Binding
CHEMBL749340
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-methyl-D-aspartate glutamate receptor by using [3H]CPP as a radioligand from the rat cortical membranes.
17
Total Activities
17
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
New and versatile approaches to the synthesis of CPP-related competitive NMDA antagonists. Preliminary structure-activity relationships and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.59 | 7.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL39664 | SELFOTEL | 2.0 | 1 | 7.19 |
| CHEMBL22304 | — | — | 1 | 7.10 |
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 1 | 6.77 |
| CHEMBL274440 | AP-7 | — | 1 | 6.12 |
| CHEMBL98870 | — | — | 1 | 6.11 |
| CHEMBL318872 | — | — | 1 | 6.07 |
| CHEMBL29624 | — | — | 1 | 5.24 |
| CHEMBL436148 | — | — | 1 | 5.01 |
| CHEMBL98814 | — | — | 1 | 4.80 |
| CHEMBL280911 | — | — | 1 | 4.32 |
| CHEMBL279533 | — | — | 1 | 4.32 |
| CHEMBL317007 | — | — | 1 | 4.08 |
| CHEMBL99250 | — | — | 1 | - |
| CHEMBL99380 | — | — | 1 | - |
| CHEMBL98445 | — | — | 1 | - |
| CHEMBL449705 | — | — | 1 | - |
| CHEMBL99333 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL39664 | SELFOTEL | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL22304 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL575060 | GLUTAMIC ACID | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL274440 | AP-7 | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL98870 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL318872 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL29624 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL436148 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL98814 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL280911 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL279533 | — | IC50 | = | 47700.0 | nM | 4.32 |
| CHEMBL317007 | — | IC50 | = | 83000.0 | nM | 4.08 |
| CHEMBL99250 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL99380 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL98445 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL449705 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL99333 | — | IC50 | > | 100000.0 | nM | - |