Assay Detail
Binding
CHEMBL751626
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Ability to displace [3H]L-689560 from NMDA receptor glycine site in rat brain membranes
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis and SAR of diiodotyrosine-derived glycine-site N-methyl-D-aspartate receptor ligands
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.64 | 6.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL559 | DEXTROTHYROXINE | 4.0 | 1 | 6.48 |
| CHEMBL277073 | — | — | 1 | 6.46 |
| CHEMBL15449 | — | — | 1 | 6.37 |
| CHEMBL15308 | — | — | 1 | 6.34 |
| CHEMBL15229 | — | — | 1 | 6.29 |
| CHEMBL280062 | — | — | 1 | 6.27 |
| CHEMBL15655 | — | — | 1 | 6.10 |
| CHEMBL15396 | — | — | 1 | 6.05 |
| CHEMBL15622 | — | — | 1 | 5.82 |
| CHEMBL557 | DETROTHYRONINE | 2.0 | 1 | 5.82 |
| CHEMBL555 | — | — | 1 | 5.39 |
| CHEMBL15274 | — | — | 1 | 5.14 |
| CHEMBL277545 | — | — | 1 | 4.00 |
| CHEMBL15557 | — | — | 1 | 4.00 |
| CHEMBL15543 | — | — | 1 | 4.00 |
| CHEMBL15701 | — | — | 1 | - |
| CHEMBL15475 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL559 | DEXTROTHYROXINE | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL277073 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL15449 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL15308 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL15229 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL280062 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL15655 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL15396 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL15622 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL557 | DETROTHYRONINE | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL555 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL15274 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL277545 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL15557 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL15543 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL15701 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL15475 | — | IC50 | > | 100000.0 | nM | - |