Assay Detail
Binding
CHEMBL831017
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory concentration against binding of the [3H]glycine to strychnine-insensitive glycine binding sites of rat N-methyl-D-aspartate glutamate receptor
8
Total Activities
8
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
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.53 | 8.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL180317 | — | — | 1 | 8.02 |
| CHEMBL180427 | — | — | 1 | 7.96 |
| CHEMBL31741 | — | — | 1 | 7.88 |
| CHEMBL419045 | GAVESTINEL SODIUM | — | 1 | 7.82 |
| CHEMBL289832 | LICOSTINEL | 2.0 | 1 | 7.70 |
| CHEMBL180365 | — | — | 1 | 7.61 |
| CHEMBL425691 | — | — | 1 | 6.94 |
| CHEMBL175989 | — | — | 1 | 6.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL180317 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL180427 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL31741 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL419045 | GAVESTINEL SODIUM | IC50 | = | 15.2 | nM | 7.82 |
| CHEMBL289832 | LICOSTINEL | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL180365 | — | IC50 | = | 24.3 | nM | 7.61 |
| CHEMBL425691 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL175989 | — | IC50 | = | 462.0 | nM | 6.33 |