Assay Detail
Functional
CHEMBL747509
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonistic activity against N-methyl-D-aspartate glutamate receptor 1/2A.
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor; Grin1/Grin2a (CHEMBL2096680) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 4.44 | 4.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL56543 | — | — | 1 | 4.72 |
| CHEMBL113830 | (S,R)-IFENPRODIL | — | 1 | 4.70 |
| CHEMBL114255 | — | — | 1 | 4.64 |
| CHEMBL431860 | — | — | 1 | 4.35 |
| CHEMBL114246 | — | — | 1 | 4.31 |
| CHEMBL305195 | — | — | 1 | 4.28 |
| CHEMBL60230 | — | — | 1 | 4.11 |
| CHEMBL64286 | N-P-COUMAROYL TYRAMINE | — | 1 | - |
| CHEMBL325749 | — | — | 1 | - |
| CHEMBL116684 | — | — | 1 | - |
| CHEMBL417554 | — | — | 1 | - |
| CHEMBL62044 | — | — | 1 | - |
| CHEMBL62181 | — | — | 1 | - |
| CHEMBL325974 | — | — | 1 | - |
| CHEMBL56731 | — | — | 1 | - |
| CHEMBL440298 | — | — | 1 | - |
| CHEMBL114252 | — | — | 1 | - |
| CHEMBL61060 | — | — | 1 | - |
| CHEMBL417389 | — | — | 1 | - |
| CHEMBL115388 | — | — | 1 | - |
| CHEMBL114512 | — | — | 1 | - |
| CHEMBL293749 | — | — | 1 | - |
| CHEMBL439600 | — | — | 1 | - |
| CHEMBL17350 | TRAXOPRODIL | 2.0 | 1 | - |
| CHEMBL60247 | — | — | 1 | - |
| CHEMBL113919 | — | — | 1 | - |
| CHEMBL114620 | — | — | 1 | - |
| CHEMBL113786 | — | — | 1 | - |
| CHEMBL62130 | — | — | 1 | - |
| CHEMBL116681 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL56543 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL113830 | (S,R)-IFENPRODIL | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL114255 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL431860 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL114246 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL305195 | — | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL60230 | — | IC50 | = | 78000.0 | nM | 4.11 |
| CHEMBL417554 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL53898 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL62044 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL62181 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL325974 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL56731 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL440298 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL114252 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL61060 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL325749 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL115340 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL114793 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL441161 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL113990 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL116684 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL64286 | N-P-COUMAROYL TYRAMINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL417389 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL115388 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL114512 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL293749 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL439600 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL17350 | TRAXOPRODIL | IC50 | > | 100000.0 | nM | - |
| CHEMBL60247 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL113919 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL114620 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL113786 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL62130 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL116681 | — | IC50 | > | 100000.0 | nM | - |