Assay Detail
Functional
CHEMBL748097
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonistic activity against N-methyl-D-aspartate glutamate receptor 1/2B.
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/Grin2b (CHEMBL2096666) ↗| 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 | 5.71 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL305195 | — | — | 1 | 8.05 |
| CHEMBL17350 | TRAXOPRODIL | 2.0 | 1 | 7.14 |
| CHEMBL115388 | — | — | 1 | 7.11 |
| CHEMBL113830 | (S,R)-IFENPRODIL | — | 1 | 6.96 |
| CHEMBL113919 | — | — | 1 | 6.92 |
| CHEMBL115340 | — | — | 1 | 6.90 |
| CHEMBL62130 | — | — | 1 | 6.77 |
| CHEMBL439600 | — | — | 1 | 6.54 |
| CHEMBL61060 | — | — | 1 | 6.48 |
| CHEMBL114512 | — | — | 1 | 6.37 |
| CHEMBL440298 | — | — | 1 | 6.25 |
| CHEMBL53898 | — | — | 1 | 6.18 |
| CHEMBL417389 | — | — | 1 | 6.17 |
| CHEMBL325749 | — | — | 1 | 5.82 |
| CHEMBL293749 | — | — | 1 | 5.77 |
| CHEMBL114255 | — | — | 1 | 5.75 |
| CHEMBL60230 | — | — | 1 | 5.47 |
| CHEMBL62181 | — | — | 1 | 5.13 |
| CHEMBL116681 | — | — | 1 | 5.08 |
| CHEMBL60247 | — | — | 1 | 5.05 |
| CHEMBL113990 | — | — | 1 | 4.72 |
| CHEMBL64286 | N-P-COUMAROYL TYRAMINE | — | 1 | 4.68 |
| CHEMBL116684 | — | — | 1 | 4.62 |
| CHEMBL114246 | — | — | 1 | 4.50 |
| CHEMBL56543 | — | — | 1 | 4.35 |
| CHEMBL114620 | — | — | 1 | 4.34 |
| CHEMBL431860 | — | — | 1 | 4.28 |
| CHEMBL113786 | — | — | 1 | 4.10 |
| CHEMBL56731 | — | — | 1 | 4.05 |
| CHEMBL114252 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL305195 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL17350 | TRAXOPRODIL | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL115388 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL113830 | (S,R)-IFENPRODIL | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL113919 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL115340 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL62130 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL439600 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL61060 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL114512 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL440298 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL53898 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL417389 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL325749 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL293749 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL114255 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL60230 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL62181 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL116681 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL60247 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL113990 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL64286 | N-P-COUMAROYL TYRAMINE | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL116684 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL114246 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL56543 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL114620 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL431860 | — | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL113786 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL56731 | — | IC50 | = | 90000.0 | nM | 4.05 |
| CHEMBL114252 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL325974 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL114793 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL441161 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL417554 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL62044 | — | IC50 | > | 100000.0 | nM | - |