Assay Detail
Binding
CHEMBL749643
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro concentration required to inhibit specific [3H]MK-801 radioligand binding to N-methyl-D-aspartate (NMDA) receptor on rat brain membrane
59
Total Activities
59
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 structure-activity studies of N,N'-diarylguanidine derivatives. N-(1-naphthyl)-N'-(3-ethylphenyl)-N'-methylguanidine: a new, selective noncompetitive NMDA receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 59 | 6.02 | 7.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL92484 | APTIGANEL | 2.0 | 1 | 7.44 |
| CHEMBL91713 | — | — | 1 | 7.41 |
| CHEMBL314379 | — | — | 1 | 7.28 |
| CHEMBL90326 | — | — | 1 | 7.19 |
| CHEMBL88161 | — | — | 1 | 7.16 |
| CHEMBL420245 | — | — | 1 | 7.14 |
| CHEMBL420979 | — | — | 1 | 7.07 |
| CHEMBL421364 | — | — | 1 | 7.06 |
| CHEMBL88146 | — | — | 1 | 7.01 |
| CHEMBL89811 | — | — | 1 | 7.00 |
| CHEMBL89344 | — | — | 1 | 6.99 |
| CHEMBL88465 | — | — | 1 | 6.94 |
| CHEMBL90809 | — | — | 1 | 6.93 |
| CHEMBL78777 | — | — | 1 | 6.78 |
| CHEMBL88932 | — | — | 1 | 6.72 |
| CHEMBL90508 | — | — | 1 | 6.68 |
| CHEMBL91628 | — | — | 1 | 6.67 |
| CHEMBL280243 | — | — | 1 | 6.66 |
| CHEMBL312600 | — | — | 1 | 6.64 |
| CHEMBL79509 | — | — | 1 | 6.48 |
| CHEMBL309603 | — | — | 1 | 6.47 |
| CHEMBL82078 | — | — | 1 | 6.39 |
| CHEMBL90288 | — | — | 1 | 6.33 |
| CHEMBL313649 | — | — | 1 | 6.32 |
| CHEMBL91222 | — | — | 1 | 6.31 |
| CHEMBL315051 | — | — | 1 | 6.30 |
| CHEMBL328986 | — | — | 1 | 6.27 |
| CHEMBL310170 | — | — | 1 | 6.09 |
| CHEMBL91828 | — | — | 1 | 6.07 |
| CHEMBL90643 | — | — | 1 | 5.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL92484 | APTIGANEL | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL91713 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL314379 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL90326 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL88161 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL420245 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL420979 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL421364 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL88146 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL89811 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL89344 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL88465 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL90809 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL78777 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL88932 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL90508 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL91628 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL280243 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL312600 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL79509 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL309603 | — | IC50 | = | 335.0 | nM | 6.47 |
| CHEMBL82078 | — | IC50 | = | 407.0 | nM | 6.39 |
| CHEMBL90288 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL313649 | — | IC50 | = | 484.0 | nM | 6.32 |
| CHEMBL91222 | — | IC50 | = | 493.0 | nM | 6.31 |
| CHEMBL315051 | — | IC50 | = | 506.0 | nM | 6.30 |
| CHEMBL328986 | — | IC50 | = | 537.0 | nM | 6.27 |
| CHEMBL310170 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL91828 | — | IC50 | = | 859.0 | nM | 6.07 |
| CHEMBL90643 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL81678 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL310729 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL78306 | — | IC50 | = | 1570.0 | nM | 5.80 |
| CHEMBL431462 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL314423 | — | IC50 | = | 1870.0 | nM | 5.73 |
| CHEMBL92095 | — | IC50 | = | 1880.0 | nM | 5.73 |
| CHEMBL330551 | — | IC50 | = | 1990.0 | nM | 5.70 |
| CHEMBL79437 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL91946 | — | IC50 | = | 2070.0 | nM | 5.68 |
| CHEMBL329623 | — | IC50 | = | 2540.0 | nM | 5.59 |
| CHEMBL265549 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL90975 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL77675 | — | IC50 | = | 3450.0 | nM | 5.46 |
| CHEMBL430455 | — | IC50 | = | 5130.0 | nM | 5.29 |
| CHEMBL282433 | DITOLYLGUANIDINE | IC50 | = | 9120.0 | nM | 5.04 |
| CHEMBL91145 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL81594 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL314710 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL412674 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL88660 | — | IC50 | = | 10000.0 | nM | 5.00 |