Assay Detail
Binding
CHEMBL750514
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to the glutamate site of the NMDA receptor was measured by competitive inhibition of binding of [3H]-CGP- 39653 to rat or porcine cerebral cortex membranes
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
New heteroaryl-spaced phosphono -amino acids are competitive NMDA antagonists with analgesic activity
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.32 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42990 | — | — | 1 | 8.47 |
| CHEMBL44185 | — | — | 1 | 8.40 |
| CHEMBL42064 | — | — | 1 | 8.40 |
| CHEMBL43266 | — | — | 1 | 8.30 |
| CHEMBL44348 | — | — | 1 | 8.30 |
| CHEMBL43480 | — | — | 1 | 7.89 |
| CHEMBL43536 | — | — | 1 | 7.74 |
| CHEMBL442543 | — | — | 1 | 7.70 |
| CHEMBL39664 | SELFOTEL | 2.0 | 1 | 7.54 |
| CHEMBL43804 | — | — | 1 | 7.54 |
| CHEMBL46695 | — | — | 1 | 7.54 |
| CHEMBL296485 | — | — | 1 | 7.27 |
| CHEMBL40449 | — | — | 1 | 7.24 |
| CHEMBL281190 | — | — | 1 | 7.19 |
| CHEMBL46713 | — | — | 1 | 7.13 |
| CHEMBL295021 | — | — | 1 | 6.92 |
| CHEMBL288908 | — | — | 1 | 6.91 |
| CHEMBL298242 | — | — | 1 | 6.85 |
| CHEMBL297411 | — | — | 1 | 6.85 |
| CHEMBL43899 | — | — | 1 | 6.37 |
| CHEMBL297853 | — | — | 1 | 6.14 |
| CHEMBL43267 | — | — | 1 | 6.02 |
| CHEMBL42604 | — | — | 1 | 5.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42990 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL44185 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL42064 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL43266 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL44348 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL43480 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL43536 | — | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL442543 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL39664 | SELFOTEL | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL43804 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL46695 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL296485 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL40449 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL281190 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL46713 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL295021 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL288908 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL298242 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL297411 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL43899 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL297853 | — | Ki | = | 722.0 | nM | 6.14 |
| CHEMBL43267 | — | Ki | = | 950.0 | nM | 6.02 |
| CHEMBL42604 | — | Ki | = | 2700.0 | nM | 5.57 |