Assay Detail
Binding
CHEMBL753020
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Inhibitory activity against Xenopus oocytes expressing rat N-Methyl-D-aspartate (NR1A/2B) Receptor subtype.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Oocyte |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor; Grin1/Grin2b (CHEMBL2096666) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Synthesis of N-substituted 4-(4-hydroxyphenyl)piperidines, 4-(4-hydroxybenzyl)piperidines, and (+/-)-3-(4-hydroxyphenyl)pyrrolidines: selective antagonists at the 1A/2B NMDA receptor subtype.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.01 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1203902 | — | — | 1 | 7.96 |
| CHEMBL174632 | — | — | 1 | 7.92 |
| CHEMBL175170 | — | — | 1 | 7.77 |
| CHEMBL1201889 | — | — | 1 | 7.72 |
| CHEMBL177620 | — | — | 1 | 7.72 |
| CHEMBL1202296 | — | — | 1 | 7.66 |
| CHEMBL177624 | — | — | 1 | 7.58 |
| CHEMBL175086 | — | — | 1 | 7.23 |
| CHEMBL1202295 | — | — | 1 | 7.15 |
| CHEMBL1203909 | — | — | 1 | 7.13 |
| CHEMBL1203901 | — | — | 1 | 7.12 |
| CHEMBL175318 | — | — | 1 | 6.89 |
| CHEMBL407274 | — | — | 1 | 6.75 |
| CHEMBL1203914 | — | — | 1 | 6.64 |
| CHEMBL366983 | — | — | 1 | 6.10 |
| CHEMBL1788131 | — | — | 1 | 5.66 |
| CHEMBL1202294 | — | — | 1 | 4.21 |
| CHEMBL1203894 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1203902 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL174632 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL175170 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1201889 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL177620 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1202296 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL177624 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL175086 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL1202295 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL1203909 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL1203901 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL175318 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL407274 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1203914 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL366983 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL1788131 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL1202294 | — | IC50 | = | 61000.0 | nM | 4.21 |
| CHEMBL1203894 | — | IC50 | > | 100000.0 | nM | - |