Assay Detail
Binding
CHEMBL752917
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro radioligand binding assay for the N-methyl-D-aspartate glutamate receptor is performed using [3H]MK-801 and rat brain membrane suspensions
71
Total Activities
71
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis and pharmacological evaluation of N-(2,5-disubstituted phenyl)-N'-(3-substituted phenyl)-N'-methylguanidines as N-methyl-D-aspartate receptor ion-channel blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 71 | 7.20 | 8.78 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL545311 | — | — | 1 | 8.78 |
| CHEMBL284237 | DIZOCILPINE | 2.0 | 1 | 8.77 |
| CHEMBL545312 | — | — | 1 | 8.73 |
| CHEMBL2093907 | — | — | 1 | 8.61 |
| CHEMBL543200 | — | — | 1 | 8.41 |
| CHEMBL540838 | — | — | 1 | 8.41 |
| CHEMBL543196 | — | — | 1 | 8.38 |
| CHEMBL545537 | — | — | 1 | 8.37 |
| CHEMBL538052 | — | — | 1 | 8.29 |
| CHEMBL545769 | — | — | 1 | 8.19 |
| CHEMBL543199 | — | — | 1 | 8.16 |
| CHEMBL555606 | — | — | 1 | 8.01 |
| CHEMBL543427 | — | — | 1 | 7.93 |
| CHEMBL552605 | — | — | 1 | 7.91 |
| CHEMBL543192 | — | — | 1 | 7.89 |
| CHEMBL543664 | — | — | 1 | 7.80 |
| CHEMBL541848 | — | — | 1 | 7.71 |
| CHEMBL553747 | — | — | 1 | 7.58 |
| CHEMBL542486 | — | — | 1 | 7.57 |
| CHEMBL554054 | APTIGANEL HYDROCHLORIDE | -1.0 | 1 | 7.54 |
| CHEMBL553034 | — | — | 1 | 7.54 |
| CHEMBL542487 | — | — | 1 | 7.46 |
| CHEMBL545542 | — | — | 1 | 7.43 |
| CHEMBL543428 | — | — | 1 | 7.39 |
| CHEMBL542736 | — | — | 1 | 7.36 |
| CHEMBL554868 | — | — | 1 | 7.34 |
| CHEMBL552829 | — | — | 1 | 7.30 |
| CHEMBL544842 | — | — | 1 | 7.29 |
| CHEMBL545079 | — | — | 1 | 7.23 |
| CHEMBL543673 | — | — | 1 | 7.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL545311 | — | Ki | = | 1.65 | nM | 8.78 |
| CHEMBL284237 | DIZOCILPINE | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL545312 | — | Ki | = | 1.87 | nM | 8.73 |
| CHEMBL2093907 | — | Ki | = | 2.45 | nM | 8.61 |
| CHEMBL543200 | — | Ki | = | 3.85 | nM | 8.41 |
| CHEMBL540838 | — | Ki | = | 3.92 | nM | 8.41 |
| CHEMBL543196 | — | Ki | = | 4.13 | nM | 8.38 |
| CHEMBL545537 | — | Ki | = | 4.27 | nM | 8.37 |
| CHEMBL538052 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL545769 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL543199 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL555606 | — | Ki | = | 9.69 | nM | 8.01 |
| CHEMBL543427 | — | Ki | = | 11.8 | nM | 7.93 |
| CHEMBL552605 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL543192 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL543664 | — | Ki | = | 15.7 | nM | 7.80 |
| CHEMBL541848 | — | Ki | = | 19.7 | nM | 7.71 |
| CHEMBL553747 | — | Ki | = | 26.1 | nM | 7.58 |
| CHEMBL542486 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL554054 | APTIGANEL HYDROCHLORIDE | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL553034 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL542487 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL545542 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL543428 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL542736 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL554868 | — | Ki | = | 45.6 | nM | 7.34 |
| CHEMBL552829 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL544842 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL545079 | — | Ki | = | 59.2 | nM | 7.23 |
| CHEMBL543673 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL542478 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL553312 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL542481 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL553749 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL542956 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL540841 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL544144 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL545544 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL542730 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL538283 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL542238 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL542957 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL543436 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL545076 | — | Ki | = | 111.0 | nM | 6.96 |
| CHEMBL554355 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL555698 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL542959 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL553167 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL552831 | — | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL543433 | — | Ki | = | 133.0 | nM | 6.88 |