Assay Detail
Binding
CHEMBL746728
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Concentration required to inhibit 50% of the specific binding of [3H]glycine to NMDA receptor prepared from rat cerebral cortex and hippocampus
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Hippocampus |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
2-Carboxytetrahydroquinolines. Conformational and stereochemical requirements for antagonism of the glycine site on the NMDA receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 5.66 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL22895 | — | — | 1 | 7.50 |
| CHEMBL278854 | — | — | 1 | 7.07 |
| CHEMBL293523 | — | — | 1 | 6.87 |
| CHEMBL50267 | — | — | 1 | 6.70 |
| CHEMBL61315 | — | — | 1 | 6.44 |
| CHEMBL416006 | — | — | 1 | 6.27 |
| CHEMBL311389 | 7-CHLOROKYNURENIC ACID | -1.0 | 1 | 6.25 |
| CHEMBL305137 | — | — | 1 | 6.22 |
| CHEMBL429233 | — | — | 1 | 6.19 |
| CHEMBL294419 | — | — | 1 | 6.14 |
| CHEMBL293634 | — | — | 1 | 5.98 |
| CHEMBL61298 | — | — | 1 | 5.92 |
| CHEMBL61502 | — | — | 1 | 5.89 |
| CHEMBL294697 | — | — | 1 | 5.73 |
| CHEMBL61297 | — | — | 1 | 5.69 |
| CHEMBL58586 | — | — | 1 | 5.64 |
| CHEMBL58163 | — | — | 1 | 5.63 |
| CHEMBL292683 | — | — | 1 | 5.63 |
| CHEMBL60644 | — | — | 1 | 5.61 |
| CHEMBL301420 | — | — | 1 | 5.60 |
| CHEMBL60222 | — | — | 1 | 5.54 |
| CHEMBL292650 | — | — | 1 | 5.51 |
| CHEMBL293275 | — | — | 1 | 5.46 |
| CHEMBL58249 | — | — | 1 | 5.42 |
| CHEMBL61296 | — | — | 1 | 5.38 |
| CHEMBL291706 | — | — | 1 | 5.30 |
| CHEMBL22493 | — | — | 1 | 5.28 |
| CHEMBL57955 | — | — | 1 | 5.19 |
| CHEMBL58164 | — | — | 1 | 5.16 |
| CHEMBL417386 | — | — | 1 | 4.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL22895 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL278854 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL293523 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL50267 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL61315 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL416006 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL311389 | 7-CHLOROKYNURENIC ACID | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL305137 | — | IC50 | = | 603.0 | nM | 6.22 |
| CHEMBL429233 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL294419 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL293634 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL61298 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL61502 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL294697 | — | IC50 | = | 1860.0 | nM | 5.73 |
| CHEMBL61297 | — | IC50 | = | 2050.0 | nM | 5.69 |
| CHEMBL58586 | — | IC50 | = | 2310.0 | nM | 5.64 |
| CHEMBL58163 | — | IC50 | = | 2360.0 | nM | 5.63 |
| CHEMBL292683 | — | IC50 | = | 2330.0 | nM | 5.63 |
| CHEMBL60644 | — | IC50 | = | 2470.0 | nM | 5.61 |
| CHEMBL301420 | — | IC50 | = | 2530.0 | nM | 5.60 |
| CHEMBL60222 | — | IC50 | = | 2890.0 | nM | 5.54 |
| CHEMBL292650 | — | IC50 | = | 3090.0 | nM | 5.51 |
| CHEMBL293275 | — | IC50 | = | 3440.0 | nM | 5.46 |
| CHEMBL58249 | — | IC50 | = | 3840.0 | nM | 5.42 |
| CHEMBL61296 | — | IC50 | = | 4180.0 | nM | 5.38 |
| CHEMBL291706 | — | IC50 | = | 5020.0 | nM | 5.30 |
| CHEMBL22493 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL57955 | — | IC50 | = | 6390.0 | nM | 5.19 |
| CHEMBL58164 | — | IC50 | = | 6960.0 | nM | 5.16 |
| CHEMBL417386 | — | IC50 | = | 13700.0 | nM | 4.86 |
| CHEMBL58171 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL60701 | — | IC50 | = | 16900.0 | nM | 4.77 |
| CHEMBL60652 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL57956 | — | IC50 | = | 26100.0 | nM | 4.58 |
| CHEMBL264976 | — | IC50 | = | 31400.0 | nM | 4.50 |
| CHEMBL299155 | TRANSTORINE | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL58404 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL58368 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL60875 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL60984 | — | IC50 | = | 176000.0 | nM | - |