Assay Detail
Binding
CHEMBL751237
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CPP from rat brain synaptic membrane N-methyl-D-aspartate glutamate receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Design and synthesis of [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)-ethyl]phosphonic acid (EAA-090), a potent N-methyl-D-aspartate antagonist, via the use of 3-cyclobutene-1,2-dione as an achiral alpha-amino acid bioisostere.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.02 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL79314 | — | — | 1 | 7.72 |
| CHEMBL39664 | SELFOTEL | 2.0 | 1 | 7.55 |
| CHEMBL452461 | PERZINFOTEL | 2.0 | 1 | 7.52 |
| CHEMBL79960 | — | — | 1 | 7.42 |
| CHEMBL310445 | — | — | 1 | 7.31 |
| CHEMBL309544 | — | — | 1 | 7.04 |
| CHEMBL79596 | — | — | 1 | 6.55 |
| CHEMBL84553 | — | — | 1 | 6.47 |
| CHEMBL83688 | — | — | 1 | 6.33 |
| CHEMBL79961 | — | — | 1 | 6.26 |
| CHEMBL79949 | — | — | 1 | - |
| CHEMBL415691 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL79314 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL39664 | SELFOTEL | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL452461 | PERZINFOTEL | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL79960 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL310445 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL309544 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL79596 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL84553 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL83688 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL79961 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL79949 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL415691 | — | IC50 | > | 1000.0 | nM | - |