Assay Detail
Functional
CHEMBL887322
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human NMDA NR1 receptor
29
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, NMDA 1 (CHEMBL2015) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
N-(6,7-dichloro-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)-N-alkylsulfonamides as peripherally restricted N-methyl-D-aspartate receptor antagonists for the treatment of pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.54 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL248247 | — | — | 1 | 9.00 |
| CHEMBL401848 | — | — | 1 | 8.70 |
| CHEMBL246004 | — | — | 1 | 8.70 |
| CHEMBL429296 | — | — | 1 | 8.40 |
| CHEMBL399275 | — | — | 3 | 8.10 |
| CHEMBL248443 | — | — | 3 | 7.96 |
| CHEMBL247035 | — | — | 1 | 7.92 |
| CHEMBL401849 | — | — | 1 | 7.85 |
| CHEMBL400508 | — | — | 1 | 7.72 |
| CHEMBL399519 | — | — | 3 | 7.70 |
| CHEMBL248439 | — | — | 1 | 7.42 |
| CHEMBL399075 | — | — | 1 | 7.41 |
| CHEMBL247034 | — | — | 1 | 7.40 |
| CHEMBL401100 | — | — | 1 | 7.39 |
| CHEMBL248436 | — | — | 1 | 7.35 |
| CHEMBL248446 | — | — | 1 | 7.31 |
| CHEMBL401253 | — | — | 1 | 7.24 |
| CHEMBL248438 | — | — | 1 | 7.23 |
| CHEMBL248445 | — | — | 1 | 7.13 |
| CHEMBL248444 | — | — | 1 | 7.11 |
| CHEMBL399274 | — | — | 1 | 6.78 |
| CHEMBL248442 | — | — | 1 | 6.68 |
| CHEMBL399700 | — | — | 1 | 6.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL248247 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL401848 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL246004 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL429296 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL399275 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL248443 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL247035 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL401849 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL248443 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL400508 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL399519 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL248443 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL399275 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL399519 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL248439 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL399075 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL247034 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL401100 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL248436 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL248446 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL401253 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL248438 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL248445 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL248444 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL399519 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL399274 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL248442 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL399275 | — | IC50 | = | 282.0 | nM | 6.55 |
| CHEMBL399700 | — | IC50 | = | 728.0 | nM | 6.14 |