Assay Detail
Functional
CHEMBL751235
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Tested in vitro for antagonistic activity at N-methyl-D-aspartate glutamate receptor by measuring displacement of [3H]TCP from crude synaptic membrane preparations obtained from rat brain
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 4 — Cell-line / Tissue |
| 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 | 9 | 7.75 | 8.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL452461 | PERZINFOTEL | 2.0 | 1 | 8.12 |
| CHEMBL79314 | — | — | 1 | 8.00 |
| CHEMBL79960 | — | — | 1 | 7.75 |
| CHEMBL39664 | SELFOTEL | 2.0 | 1 | 7.66 |
| CHEMBL309544 | — | — | 1 | 7.54 |
| CHEMBL310445 | — | — | 1 | 7.44 |
| CHEMBL81836 | — | — | 1 | - |
| CHEMBL79949 | — | — | 1 | - |
| CHEMBL415691 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL452461 | PERZINFOTEL | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL79314 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL79960 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL39664 | SELFOTEL | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL309544 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL310445 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL81836 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL79949 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL415691 | — | IC50 | > | 100.0 | nM | - |