Assay Detail
Binding
CHEMBL752505
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]glycine from N-methyl-D-aspartate glutamate receptor 1 in rat cortical membranes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Glutamate receptor ionotropic, NMDA 1 (CHEMBL330) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and biological evaluation of a new set of pyrazolo[1,5-c]quinazoline-2-carboxylates as novel excitatory amino acid antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 5.56 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL9281 | — | — | 1 | 6.80 |
| CHEMBL275106 | — | — | 1 | 6.62 |
| CHEMBL9044 | — | — | 1 | 6.32 |
| CHEMBL266998 | — | — | 1 | 5.89 |
| CHEMBL267256 | — | — | 1 | 5.85 |
| CHEMBL8992 | — | — | 1 | 5.70 |
| CHEMBL267504 | — | — | 1 | 5.40 |
| CHEMBL427734 | — | — | 1 | 5.08 |
| CHEMBL9037 | — | — | 1 | 4.97 |
| CHEMBL9159 | — | — | 1 | 4.97 |
| CHEMBL267259 | — | — | 1 | 4.58 |
| CHEMBL267929 | — | — | 1 | 4.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL9281 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL275106 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL9044 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL266998 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL267256 | — | Ki | = | 1410.0 | nM | 5.85 |
| CHEMBL8992 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL267504 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL427734 | — | Ki | = | 8300.0 | nM | 5.08 |
| CHEMBL9037 | — | Ki | = | 10600.0 | nM | 4.97 |
| CHEMBL9159 | — | Ki | = | 10600.0 | nM | 4.97 |
| CHEMBL267259 | — | Ki | = | 26500.0 | nM | 4.58 |
| CHEMBL267929 | — | Ki | = | 33300.0 | nM | 4.48 |