Assay Detail
Binding
CHEMBL747485
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Binding affinity against phencyclidine (PCP) site of N-methyl-D-aspartate glutamate receptor from rat brain, using [3H]- TCP as radioligand.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Novel NMDA antagonists: replacement of the pyridinium ring of 6,11-ethanobenzo[b]quinolizinium cations with heteroisoquinolinium cations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.76 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL299087 | — | — | 1 | 8.74 |
| CHEMBL284237 | DIZOCILPINE | 2.0 | 1 | 8.66 |
| CHEMBL298994 | — | — | 1 | 8.54 |
| CHEMBL53273 | — | — | 1 | 8.54 |
| CHEMBL52124 | — | — | 1 | 8.28 |
| CHEMBL52782 | — | — | 1 | 8.21 |
| CHEMBL53944 | — | — | 1 | 8.11 |
| CHEMBL53067 | — | — | 1 | 8.09 |
| CHEMBL51549 | — | — | 1 | 8.00 |
| CHEMBL296165 | — | — | 1 | 7.85 |
| CHEMBL53472 | — | — | 1 | 7.52 |
| CHEMBL51755 | — | — | 1 | 7.44 |
| CHEMBL296170 | — | — | 1 | 7.28 |
| CHEMBL52666 | — | — | 1 | 7.17 |
| CHEMBL430779 | — | — | 1 | 6.51 |
| CHEMBL299819 | — | — | 1 | 6.48 |
| CHEMBL51800 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL299087 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL284237 | DIZOCILPINE | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL298994 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL53273 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL52124 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL52782 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL53944 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL53067 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL51549 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL296165 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL53472 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL51755 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL296170 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL52666 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL430779 | — | Ki | = | 306.0 | nM | 6.51 |
| CHEMBL299819 | — | Ki | = | 329.0 | nM | 6.48 |
| CHEMBL51800 | — | Ki | = | 330.0 | nM | 6.48 |