Assay Detail
Functional
CHEMBL746725
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Affinity for glycine site of N-methyl-D-aspartate glutamate receptor determined by displacement of tritium labeled selective glycine antagonist [3H]- SM-18400
9
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, NMDA 1 (CHEMBL330) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Tricyclic indole-2-carboxylic acids: highly in vivo active and selective antagonists for the glycine binding site of the NMDA receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.21 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL85567 | — | — | 1 | 9.00 |
| CHEMBL161406 | — | — | 2 | 8.92 |
| CHEMBL350974 | — | — | 1 | 8.82 |
| CHEMBL349136 | — | — | 1 | 8.57 |
| CHEMBL159896 | — | — | 1 | 8.12 |
| CHEMBL162693 | — | — | 1 | 7.75 |
| CHEMBL351097 | — | — | 1 | 7.72 |
| CHEMBL348165 | — | — | 1 | 7.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL85567 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL161406 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL350974 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL349136 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL159896 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL162693 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL351097 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL348165 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL161406 | — | IC50 | = | 33.0 | nM | 7.48 |