Assay Detail
Binding
CHEMBL747502
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]glycine to glycine binding site, associated with the N-methyl-D-aspartate glutamate receptor 1 in crude synaptic membranes prepared from adult rat cerebral cortex.
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Glutamate receptor ionotropic, NMDA 1 (CHEMBL330) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Substituted indole-2-carboxylates as in vivo potent antagonists acting as the strychnine-insensitive glycine binding site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 35 | 7.72 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL31741 | — | — | 1 | 9.00 |
| CHEMBL117627 | — | — | 1 | 8.90 |
| CHEMBL117691 | — | — | 1 | 8.80 |
| CHEMBL168394 | — | — | 1 | 8.70 |
| CHEMBL168754 | — | — | 1 | 8.50 |
| CHEMBL419045 | GAVESTINEL SODIUM | — | 1 | 8.50 |
| CHEMBL355109 | — | — | 1 | 8.40 |
| CHEMBL166552 | — | — | 1 | 8.40 |
| CHEMBL169566 | — | — | 1 | 8.30 |
| CHEMBL354980 | — | — | 1 | 8.30 |
| CHEMBL433725 | — | — | 1 | 8.30 |
| CHEMBL262537 | — | — | 1 | 8.30 |
| CHEMBL287327 | — | — | 1 | 8.20 |
| CHEMBL168465 | — | — | 1 | 8.20 |
| CHEMBL289832 | LICOSTINEL | 2.0 | 1 | 8.10 |
| CHEMBL168470 | — | — | 1 | 8.10 |
| CHEMBL169013 | — | — | 1 | 8.00 |
| CHEMBL354793 | — | — | 1 | 7.90 |
| CHEMBL169368 | — | — | 1 | 7.70 |
| CHEMBL168503 | — | — | 1 | 7.70 |
| CHEMBL168828 | — | — | 1 | 7.60 |
| CHEMBL352435 | — | — | 1 | 7.60 |
| CHEMBL169227 | — | — | 1 | 7.50 |
| CHEMBL169776 | — | — | 1 | 7.40 |
| CHEMBL354484 | — | — | 1 | 7.30 |
| CHEMBL353977 | — | — | 1 | 7.20 |
| CHEMBL353272 | — | — | 1 | 7.00 |
| CHEMBL352310 | — | — | 1 | 7.00 |
| CHEMBL323628 | — | — | 1 | 6.90 |
| CHEMBL354375 | — | — | 1 | 6.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL31741 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL117627 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL117691 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL168394 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL168754 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL419045 | GAVESTINEL SODIUM | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL355109 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL166552 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL169566 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL354980 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL433725 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL262537 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL287327 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL168465 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL168470 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL289832 | LICOSTINEL | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL169013 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL354793 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL168503 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL169368 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL168828 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL352435 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL169227 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL169776 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL354484 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL353977 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL353272 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL352310 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL323628 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL354375 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL169890 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL355298 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL435473 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL352828 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL168924 | — | Ki | = | 1995.26 | nM | 5.70 |