Assay Detail
Binding
CHEMBL761030
Review assay metadata, readout intent, target linkage, and publication context from the same page.
The compound was tested for its ability to block PCP N-methyl-D-aspartate glutamate receptor at the PCP (phencyclidine) binding site in postmortem human frontal cortex.
27
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Quantitative analysis of the structural requirements for blockade of the N-methyl-D-aspartate receptor at the phencyclidine binding site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 5.79 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL284237 | DIZOCILPINE | 2.0 | 2 | 8.92 |
| CHEMBL275528 | PHENCYCLIDINE | 2.0 | 1 | 7.64 |
| CHEMBL341050 | — | — | 1 | 6.72 |
| CHEMBL1254766 | DEXTRORPHAN | 2.0 | 1 | 6.66 |
| CHEMBL742 | KETAMINE | 4.0 | 1 | 6.38 |
| CHEMBL807 | MEMANTINE | 4.0 | 1 | 6.27 |
| CHEMBL132442 | — | — | 1 | 6.22 |
| CHEMBL130274 | — | — | 1 | 6.10 |
| CHEMBL338354 | — | — | 1 | 5.79 |
| CHEMBL52440 | DEXTROMETHORPHAN | 4.0 | 1 | 5.78 |
| CHEMBL86715 | PROCYCLIDINE | 4.0 | 1 | 5.77 |
| CHEMBL131610 | — | — | 1 | 5.76 |
| CHEMBL341013 | — | — | 1 | 5.42 |
| CHEMBL338523 | — | — | 1 | 5.39 |
| CHEMBL130497 | — | — | 1 | 5.39 |
| CHEMBL130240 | — | — | 1 | 5.35 |
| CHEMBL900 | ORPHENADRINE | 4.0 | 1 | 5.22 |
| CHEMBL132511 | — | — | 1 | 5.14 |
| CHEMBL128343 | — | — | 1 | 5.02 |
| CHEMBL660 | AMANTADINE | 4.0 | 1 | 4.98 |
| CHEMBL334491 | BUDIPINE | 2.0 | 1 | 4.93 |
| CHEMBL340215 | — | — | 1 | 4.82 |
| CHEMBL424261 | — | — | 1 | 4.76 |
| CHEMBL131460 | — | — | 1 | 4.68 |
| CHEMBL443286 | — | — | 1 | 4.66 |
| CHEMBL336585 | — | — | 1 | 4.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL284237 | DIZOCILPINE | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL284237 | DIZOCILPINE | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL275528 | PHENCYCLIDINE | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL341050 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL1254766 | DEXTRORPHAN | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL742 | KETAMINE | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL807 | MEMANTINE | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL132442 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL130274 | — | Ki | = | 790.0 | nM | 6.10 |
| CHEMBL338354 | — | Ki | = | 1610.0 | nM | 5.79 |
| CHEMBL52440 | DEXTROMETHORPHAN | Ki | = | 1680.0 | nM | 5.78 |
| CHEMBL86715 | PROCYCLIDINE | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL131610 | — | Ki | = | 1720.0 | nM | 5.76 |
| CHEMBL341013 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL338523 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL130497 | — | Ki | = | 4080.0 | nM | 5.39 |
| CHEMBL130240 | — | Ki | = | 4440.0 | nM | 5.35 |
| CHEMBL900 | ORPHENADRINE | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL132511 | — | Ki | = | 7210.0 | nM | 5.14 |
| CHEMBL128343 | — | Ki | = | 9500.0 | nM | 5.02 |
| CHEMBL660 | AMANTADINE | Ki | = | 10500.0 | nM | 4.98 |
| CHEMBL334491 | BUDIPINE | Ki | = | 11700.0 | nM | 4.93 |
| CHEMBL340215 | — | Ki | = | 15200.0 | nM | 4.82 |
| CHEMBL424261 | — | Ki | = | 17400.0 | nM | 4.76 |
| CHEMBL131460 | — | Ki | = | 20800.0 | nM | 4.68 |
| CHEMBL443286 | — | Ki | = | 21700.0 | nM | 4.66 |
| CHEMBL336585 | — | Ki | = | 33300.0 | nM | 4.48 |