Assay Detail
Binding
CHEMBL750147
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of stimulated [3H](+)-MK-801 binding to N-methyl-D-aspartate glutamate receptor in rat cortical membranes incubated with 10 uM glycine.
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
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 |
|---|---|---|---|
| IC50 | 17 | 5.16 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL274588 | — | — | 1 | 6.52 |
| CHEMBL8693 | — | — | 1 | 6.10 |
| CHEMBL9281 | — | — | 1 | 6.05 |
| CHEMBL9044 | — | — | 1 | 5.75 |
| CHEMBL275106 | — | — | 1 | 5.68 |
| CHEMBL266998 | — | — | 1 | 5.62 |
| CHEMBL276624 | — | — | 1 | 5.36 |
| CHEMBL267504 | — | — | 1 | 5.22 |
| CHEMBL267256 | — | — | 1 | 4.98 |
| CHEMBL427734 | — | — | 1 | 4.87 |
| CHEMBL9037 | — | — | 1 | 4.79 |
| CHEMBL9159 | — | — | 1 | 4.79 |
| CHEMBL8829 | — | — | 1 | 4.77 |
| CHEMBL8992 | — | — | 1 | 4.76 |
| CHEMBL267929 | — | — | 1 | 4.34 |
| CHEMBL267259 | — | — | 1 | 4.04 |
| CHEMBL268445 | — | — | 1 | 4.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL274588 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL8693 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL9281 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL9044 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL275106 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL266998 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL276624 | — | IC50 | = | 4330.0 | nM | 5.36 |
| CHEMBL267504 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL267256 | — | IC50 | = | 10400.0 | nM | 4.98 |
| CHEMBL427734 | — | IC50 | = | 13400.0 | nM | 4.87 |
| CHEMBL9037 | — | IC50 | = | 16100.0 | nM | 4.79 |
| CHEMBL9159 | — | IC50 | = | 16200.0 | nM | 4.79 |
| CHEMBL8829 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL8992 | — | IC50 | = | 17500.0 | nM | 4.76 |
| CHEMBL267929 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL267259 | — | IC50 | = | 92000.0 | nM | 4.04 |
| CHEMBL268445 | — | IC50 | = | 91000.0 | nM | 4.04 |