Assay Detail
Binding
CHEMBL751569
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]glycine binding to glycine site of N-methyl-D-aspartate glutamate receptor in rat cortical membranes
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Kynurenic acid derivatives. Structure-activity relationships for excitatory amino acid antagonism and identification of potent and selective antagonists at the glycine site on the N-methyl-D-aspartate receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 51 | 5.66 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL22895 | — | — | 1 | 7.50 |
| CHEMBL22338 | — | — | 1 | 7.18 |
| CHEMBL278854 | — | — | 1 | 7.07 |
| CHEMBL50267 | — | — | 1 | 6.70 |
| CHEMBL25054 | — | — | 1 | 6.58 |
| CHEMBL21856 | — | — | 1 | 6.57 |
| CHEMBL416006 | — | — | 1 | 6.27 |
| CHEMBL311389 | 7-CHLOROKYNURENIC ACID | -1.0 | 1 | 6.25 |
| CHEMBL22462 | — | — | 1 | 6.20 |
| CHEMBL429233 | — | — | 1 | 6.19 |
| CHEMBL22239 | — | — | 1 | 6.09 |
| CHEMBL22026 | — | — | 1 | 6.07 |
| CHEMBL440462 | — | — | 1 | 5.96 |
| CHEMBL21529 | — | — | 1 | 5.92 |
| CHEMBL21587 | — | — | 1 | 5.75 |
| CHEMBL22807 | — | — | 1 | 5.68 |
| CHEMBL22720 | — | — | 1 | 5.64 |
| CHEMBL22530 | — | — | 1 | 5.62 |
| CHEMBL284028 | 2,3-DIHYDROXY-6,7-DICHLOROQUINOXALINE | — | 1 | 5.51 |
| CHEMBL22894 | — | — | 1 | 5.50 |
| CHEMBL282003 | — | — | 1 | 5.47 |
| CHEMBL279489 | — | — | 1 | 5.44 |
| CHEMBL22933 | — | — | 1 | 5.32 |
| CHEMBL418747 | — | — | 1 | 5.31 |
| CHEMBL22493 | — | — | 1 | 5.28 |
| CHEMBL22586 | — | — | 1 | 5.25 |
| CHEMBL416555 | — | — | 1 | 5.18 |
| CHEMBL22083 | — | — | 1 | 5.17 |
| CHEMBL21641 | — | — | 1 | 5.08 |
| CHEMBL23044 | — | — | 1 | 5.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL22895 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL22338 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL278854 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL50267 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL25054 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL21856 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL416006 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL311389 | 7-CHLOROKYNURENIC ACID | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL22462 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL429233 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL22239 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL22026 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL440462 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL21529 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL21587 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL22807 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL22720 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL22530 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL284028 | 2,3-DIHYDROXY-6,7-DICHLOROQUINOXALINE | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL22894 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL282003 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL279489 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL22933 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL418747 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL22493 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL22586 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL416555 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL22083 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL21641 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL23044 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL282672 | — | IC50 | = | 38600.0 | nM | 4.41 |
| CHEMBL299155 | TRANSTORINE | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL21349 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL22608 | — | IC50 | = | 56300.0 | nM | 4.25 |
| CHEMBL22700 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL22082 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL283345 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL22274 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL22588 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL278325 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL21826 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL279740 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL22339 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL22640 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL21978 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL277675 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL283805 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL22222 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL22527 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL280701 | — | IC50 | > | 100000.0 | nM | - |