Assay Detail
Binding
CHEMBL753011
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Inhibitory activity against Xenopus oocytes expressing rat N-Methyl-D-aspartate (NR1A/2A) 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/Grin2a (CHEMBL2096680) ↗| 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 | 4.26 | 4.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL175170 | — | — | 1 | 4.39 |
| CHEMBL1203914 | — | — | 1 | 4.37 |
| CHEMBL1203909 | — | — | 1 | 4.29 |
| CHEMBL175318 | — | — | 1 | 4.28 |
| CHEMBL1201889 | — | — | 1 | 4.23 |
| CHEMBL174632 | — | — | 1 | 4.21 |
| CHEMBL177624 | — | — | 1 | 4.03 |
| CHEMBL366983 | — | — | 1 | - |
| CHEMBL175086 | — | — | 1 | - |
| CHEMBL177620 | — | — | 1 | - |
| CHEMBL1203902 | — | — | 1 | - |
| CHEMBL1788131 | — | — | 1 | - |
| CHEMBL1202294 | — | — | 1 | - |
| CHEMBL1203894 | — | — | 1 | - |
| CHEMBL1202295 | — | — | 1 | - |
| CHEMBL1202296 | — | — | 1 | - |
| CHEMBL1203901 | — | — | 1 | - |
| CHEMBL407274 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL175170 | — | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL1203914 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL1203909 | — | IC50 | = | 51000.0 | nM | 4.29 |
| CHEMBL175318 | — | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL1201889 | — | IC50 | = | 59000.0 | nM | 4.23 |
| CHEMBL174632 | — | IC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL177624 | — | IC50 | = | 93000.0 | nM | 4.03 |
| CHEMBL366983 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL175086 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL177620 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1203902 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1788131 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1202294 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1203894 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1202295 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1202296 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1203901 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL407274 | — | IC50 | > | 100000.0 | nM | - |