Assay Detail
Binding
CHEMBL744072
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Inhibition of strychnine-insensitive [3H]glycine binding to the N-methyl-D-aspartate glutamate receptor of synaptic plasma membranes(SPM) prepared from rat forebrain
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain/Plasma |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Novel indole-2-carboxylates as ligands for the strychnine-insensitive N-methyl-D-aspartate-linked glycine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 53 | 5.22 | 6.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL23120 | — | — | 1 | 6.33 |
| CHEMBL277479 | — | — | 1 | 6.20 |
| CHEMBL277411 | — | — | 1 | 6.17 |
| CHEMBL283355 | — | — | 1 | 6.16 |
| CHEMBL286782 | — | — | 1 | 6.04 |
| CHEMBL280179 | — | — | 1 | 5.93 |
| CHEMBL415462 | — | — | 1 | 5.81 |
| CHEMBL23255 | — | — | 1 | 5.79 |
| CHEMBL25875 | — | — | 1 | 5.42 |
| CHEMBL278800 | — | — | 1 | 5.17 |
| CHEMBL24207 | — | — | 1 | 5.08 |
| CHEMBL23134 | — | — | 1 | 5.00 |
| CHEMBL286375 | — | — | 1 | 4.99 |
| CHEMBL23930 | — | — | 1 | 4.96 |
| CHEMBL23953 | — | — | 1 | 4.95 |
| CHEMBL23637 | — | — | 1 | 4.94 |
| CHEMBL23396 | — | — | 1 | 4.88 |
| CHEMBL283379 | — | — | 1 | 4.85 |
| CHEMBL22868 | — | — | 1 | 4.68 |
| CHEMBL23754 | — | — | 1 | 4.61 |
| CHEMBL434007 | — | — | 1 | 4.54 |
| CHEMBL286530 | — | — | 1 | 4.53 |
| CHEMBL277189 | — | — | 1 | 4.12 |
| CHEMBL23507 | 5-FLUOROINDOLE-2-CARBOXYLIC ACID | — | 1 | 4.04 |
| CHEMBL278390 | INDOLE-2-CARBOXYLIC ACID | — | 1 | - |
| CHEMBL288092 | — | — | 1 | - |
| CHEMBL22435 | — | — | 1 | - |
| CHEMBL24490 | — | — | 1 | - |
| CHEMBL22813 | — | — | 1 | - |
| CHEMBL25599 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL23120 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL277479 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL277411 | — | Ki | = | 680.0 | nM | 6.17 |
| CHEMBL283355 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL286782 | — | Ki | = | 920.0 | nM | 6.04 |
| CHEMBL280179 | — | Ki | = | 1180.0 | nM | 5.93 |
| CHEMBL415462 | — | Ki | = | 1560.0 | nM | 5.81 |
| CHEMBL23255 | — | Ki | = | 1610.0 | nM | 5.79 |
| CHEMBL25875 | — | Ki | = | 3850.0 | nM | 5.42 |
| CHEMBL278800 | — | Ki | = | 6800.0 | nM | 5.17 |
| CHEMBL24207 | — | Ki | = | 8250.0 | nM | 5.08 |
| CHEMBL23134 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL286375 | — | Ki | = | 10300.0 | nM | 4.99 |
| CHEMBL23930 | — | Ki | = | 10900.0 | nM | 4.96 |
| CHEMBL23953 | — | Ki | = | 11200.0 | nM | 4.95 |
| CHEMBL23637 | — | Ki | = | 11400.0 | nM | 4.94 |
| CHEMBL23396 | — | Ki | = | 13200.0 | nM | 4.88 |
| CHEMBL283379 | — | Ki | = | 14100.0 | nM | 4.85 |
| CHEMBL22868 | — | Ki | = | 20900.0 | nM | 4.68 |
| CHEMBL23754 | — | Ki | = | 24800.0 | nM | 4.61 |
| CHEMBL434007 | — | Ki | = | 29200.0 | nM | 4.54 |
| CHEMBL286530 | — | Ki | = | 29600.0 | nM | 4.53 |
| CHEMBL277189 | — | Ki | = | 75100.0 | nM | 4.12 |
| CHEMBL23507 | 5-FLUOROINDOLE-2-CARBOXYLIC ACID | Ki | = | 91000.0 | nM | 4.04 |
| CHEMBL23328 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL283333 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL22299 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL23399 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL285303 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL23481 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL23488 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL23906 | 5-CHLOROINDOLE-2-CARBOXYLIC ACID | Ki | > | 100000.0 | nM | - |
| CHEMBL280891 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL280901 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL285007 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL24658 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL282875 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL278097 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL23081 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL25324 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL24438 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL23961 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL279300 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL285694 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL25599 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL22813 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL24490 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL22435 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL288092 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL278390 | INDOLE-2-CARBOXYLIC ACID | Ki | > | 100000.0 | nM | - |