Assay Detail
Binding
CHEMBL4396283
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H] ifenprodil from GluN2B/GluN1a (unknown origin) expressed in mouse L(tk-) cell membranes incubated for 120 mins by scintillation counting method
26
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Tetrahydro-3-benzazepines with fluorinated side chains as NMDA and σ<sub>1</sub> receptor antagonists: Synthesis, receptor affinity, selectivity and antiallodynic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 6.88 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4588347 | — | — | 1 | 8.00 |
| CHEMBL49623 | (R,S)-IFENPRODIL | — | 1 | 8.00 |
| CHEMBL28564 | ELIPRODIL | 2.0 | 1 | 7.89 |
| CHEMBL4440895 | — | — | 3 | 7.80 |
| CHEMBL4575948 | — | — | 1 | 7.52 |
| CHEMBL4565798 | — | — | 1 | 7.26 |
| CHEMBL1289626 | — | — | 1 | 7.08 |
| CHEMBL4459710 | — | — | 1 | 7.07 |
| CHEMBL4457961 | — | — | 1 | 6.92 |
| CHEMBL4536158 | — | — | 1 | 6.62 |
| CHEMBL4435229 | — | — | 1 | 6.60 |
| CHEMBL4466227 | — | — | 1 | 6.46 |
| CHEMBL4514409 | — | — | 1 | 6.38 |
| CHEMBL4574220 | — | — | 1 | 6.30 |
| CHEMBL1290051 | — | — | 1 | 6.30 |
| CHEMBL4457995 | — | — | 1 | 6.22 |
| CHEMBL4473837 | — | — | 1 | 6.20 |
| CHEMBL1289403 | — | — | 1 | 6.15 |
| CHEMBL4562406 | — | — | 1 | 6.11 |
| CHEMBL4573419 | — | — | 1 | 6.09 |
| CHEMBL1165411 | DEXOXADROL | 2.0 | 1 | - |
| CHEMBL284237 | DIZOCILPINE | 2.0 | 1 | - |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | - |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4588347 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL49623 | (R,S)-IFENPRODIL | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL28564 | ELIPRODIL | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4440895 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4575948 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL4440895 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL4565798 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL4440895 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL1289626 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL4459710 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL4457961 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL4536158 | — | Ki | = | 239.0 | nM | 6.62 |
| CHEMBL4435229 | — | Ki | = | 249.0 | nM | 6.60 |
| CHEMBL4466227 | — | Ki | = | 348.0 | nM | 6.46 |
| CHEMBL4514409 | — | Ki | = | 422.0 | nM | 6.38 |
| CHEMBL1290051 | — | Ki | = | 505.0 | nM | 6.30 |
| CHEMBL4574220 | — | Ki | = | 506.0 | nM | 6.30 |
| CHEMBL4457995 | — | Ki | = | 602.0 | nM | 6.22 |
| CHEMBL4473837 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL1289403 | — | Ki | = | 706.0 | nM | 6.15 |
| CHEMBL4562406 | — | Ki | = | 784.0 | nM | 6.11 |
| CHEMBL4573419 | — | Ki | = | 813.0 | nM | 6.09 |
| CHEMBL1165411 | DEXOXADROL | Ki | - | — | - | |
| CHEMBL284237 | DIZOCILPINE | Ki | - | — | - | |
| CHEMBL54 | HALOPERIDOL | Ki | - | — | - | |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | - | — | - |