Assay Detail
Binding
CHEMBL751883
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity for the glycine binding site on rat N-methyl-D-aspartate glutamate receptor 1, determined by displacement of the glycine site antagonist [3H]L-689,560 from rat cortical membranes
76
Total Activities
76
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
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 76 | 6.99 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL44793 | GAVESTINEL | 2.0 | 1 | 9.00 |
| CHEMBL132660 | — | — | 1 | 8.89 |
| CHEMBL32076 | — | — | 1 | 8.85 |
| CHEMBL131504 | — | — | 1 | 8.71 |
| CHEMBL31741 | — | — | 1 | 8.70 |
| CHEMBL31718 | — | — | 1 | 8.66 |
| CHEMBL129974 | — | — | 1 | 8.62 |
| CHEMBL289832 | LICOSTINEL | 2.0 | 1 | 8.55 |
| CHEMBL129888 | — | — | 1 | 8.48 |
| CHEMBL336068 | — | — | 1 | 8.44 |
| CHEMBL335059 | — | — | 1 | 8.44 |
| CHEMBL32240 | — | — | 1 | 8.40 |
| CHEMBL133796 | — | — | 1 | 8.40 |
| CHEMBL31049 | — | — | 1 | 8.35 |
| CHEMBL130144 | — | — | 1 | 8.22 |
| CHEMBL322420 | — | — | 1 | 8.16 |
| CHEMBL133396 | — | — | 1 | 8.11 |
| CHEMBL131569 | — | — | 1 | 8.10 |
| CHEMBL130778 | — | — | 1 | 8.05 |
| CHEMBL131832 | — | — | 1 | 8.05 |
| CHEMBL131315 | — | — | 1 | 8.02 |
| CHEMBL130575 | — | — | 1 | 7.99 |
| CHEMBL130879 | — | — | 1 | 7.96 |
| CHEMBL129925 | — | — | 1 | 7.93 |
| CHEMBL334378 | — | — | 1 | 7.92 |
| CHEMBL131385 | — | — | 1 | 7.91 |
| CHEMBL130399 | — | — | 1 | 7.64 |
| CHEMBL290738 | — | — | 1 | 7.62 |
| CHEMBL340946 | — | — | 1 | 7.55 |
| CHEMBL130951 | — | — | 1 | 7.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL44793 | GAVESTINEL | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL132660 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL32076 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL131504 | — | IC50 | = | 1.95 | nM | 8.71 |
| CHEMBL31741 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL31718 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL129974 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL289832 | LICOSTINEL | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL129888 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL336068 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL335059 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL32240 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL133796 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL31049 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL130144 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL322420 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL133396 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL131569 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL130778 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL131832 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL131315 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL130575 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL130879 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL129925 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL334378 | — | IC50 | = | 12.1 | nM | 7.92 |
| CHEMBL131385 | — | IC50 | = | 12.2 | nM | 7.91 |
| CHEMBL130399 | — | IC50 | = | 22.8 | nM | 7.64 |
| CHEMBL290738 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL340946 | — | IC50 | = | 27.9 | nM | 7.55 |
| CHEMBL130951 | — | IC50 | = | 32.6 | nM | 7.49 |
| CHEMBL130535 | — | IC50 | = | 34.3 | nM | 7.46 |
| CHEMBL43372 | — | IC50 | = | 36.4 | nM | 7.44 |
| CHEMBL129996 | — | IC50 | = | 37.8 | nM | 7.42 |
| CHEMBL133163 | — | IC50 | = | 38.5 | nM | 7.42 |
| CHEMBL335840 | — | IC50 | = | 42.7 | nM | 7.37 |
| CHEMBL50267 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL132062 | — | IC50 | = | 75.6 | nM | 7.12 |
| CHEMBL336729 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL131076 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL434620 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL323335 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL31661 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL113660 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL336156 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL311389 | 7-CHLOROKYNURENIC ACID | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL132903 | — | IC50 | = | 352.0 | nM | 6.45 |
| CHEMBL130735 | — | IC50 | = | 391.0 | nM | 6.41 |
| CHEMBL130895 | — | IC50 | = | 421.0 | nM | 6.38 |
| CHEMBL102574 | — | IC50 | = | 414.0 | nM | 6.38 |
| CHEMBL115225 | — | IC50 | = | 419.0 | nM | 6.38 |