Assay Detail
Binding
CHEMBL4045543
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ifenprodil from human NR1-1a/NR2B receptor expressed in Mouse L(tk-) cell membranes incubated for 120 mins by scintillation counting method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor; GRIN1/GRIN2B (CHEMBL1907603) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Replacement of benzylic hydroxy group by vinyl or hydroxymethyl moiety at the 3-benzazepine scaffold retaining GluN2B affinity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.76 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL319706 | (S)-IFENPRODIL | — | 1 | 8.00 |
| CHEMBL1289626 | — | — | 1 | 7.08 |
| CHEMBL4075349 | — | — | 1 | 6.80 |
| CHEMBL4065052 | — | — | 1 | 6.33 |
| CHEMBL4088218 | — | — | 1 | 6.22 |
| CHEMBL1289403 | — | — | 1 | 6.15 |
| CHEMBL1165411 | DEXOXADROL | 2.0 | 1 | - |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | - |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL319706 | (S)-IFENPRODIL | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1289626 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL4075349 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL4065052 | — | Ki | = | 472.0 | nM | 6.33 |
| CHEMBL4088218 | — | Ki | = | 606.0 | nM | 6.22 |
| CHEMBL1289403 | — | Ki | = | 706.0 | nM | 6.15 |
| CHEMBL1165411 | DEXOXADROL | Ki | - | — | - | |
| CHEMBL54 | HALOPERIDOL | Ki | - | — | - | |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | - | — | - |