Assay Detail
Binding
CHEMBL747072
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Concentration required for 50% Inhibition of responses at cloned NR1A/2AB NMDA expressed in Xenopus oocytes
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Oocyte |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Glutamate receptor ionotropic, NMDA 1 (CHEMBL2015) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Subtype-selective N-methyl-D-aspartate receptor antagonists: synthesis and biological evaluation of 1-(heteroarylalkynyl)-4-benzylpiperidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.88 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL117260 | — | — | 1 | 8.28 |
| CHEMBL19636 | — | — | 1 | 8.21 |
| CHEMBL19506 | — | — | 1 | 8.09 |
| CHEMBL116223 | — | — | 1 | 7.80 |
| CHEMBL419399 | — | — | 1 | 7.77 |
| CHEMBL325825 | — | — | 1 | 7.72 |
| CHEMBL326742 | — | — | 1 | 7.72 |
| CHEMBL326568 | — | — | 1 | 7.58 |
| CHEMBL325890 | — | — | 1 | 7.31 |
| CHEMBL117940 | — | — | 1 | 7.05 |
| CHEMBL116224 | — | — | 1 | 6.96 |
| CHEMBL113697 | — | — | 1 | 6.92 |
| CHEMBL115883 | — | — | 1 | 6.75 |
| CHEMBL114536 | — | — | 1 | 6.66 |
| CHEMBL324584 | — | — | 1 | 6.60 |
| CHEMBL114823 | — | — | 1 | 6.50 |
| CHEMBL114644 | — | — | 1 | 6.42 |
| CHEMBL115761 | — | — | 1 | 6.38 |
| CHEMBL324940 | — | — | 1 | 5.96 |
| CHEMBL113936 | — | — | 1 | 5.75 |
| CHEMBL113750 | — | — | 1 | 4.82 |
| CHEMBL114155 | — | — | 1 | 4.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL117260 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL19636 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL19506 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL116223 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL419399 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL325825 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL326742 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL326568 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL325890 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL117940 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL116224 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL113697 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL115883 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL114536 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL324584 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL114823 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL114644 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL115761 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL324940 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL113936 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL113750 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL114155 | — | IC50 | = | 62000.0 | nM | 4.21 |