Assay Detail
Binding
CHEMBL748089
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity was determined towards NMDA receptor using [3H]thienylcyclidine as radioligand
34
Total Activities
31
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
Identification, synthesis, and characterization of a unique class of N-methyl-D-aspartate antagonists. The 6,11-ethanobenzo[b]quinolizinium cation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 7.07 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL344151 | DIZOCILPINE MALEATE | -1.0 | 1 | 8.62 |
| CHEMBL139641 | — | — | 1 | 8.40 |
| CHEMBL52124 | — | — | 3 | 8.40 |
| CHEMBL335351 | — | — | 1 | 8.10 |
| CHEMBL140288 | — | — | 1 | 7.96 |
| CHEMBL436008 | — | — | 1 | 7.96 |
| CHEMBL342885 | — | — | 1 | 7.92 |
| CHEMBL139348 | — | — | 1 | 7.92 |
| CHEMBL139199 | — | — | 1 | 7.89 |
| CHEMBL344854 | — | — | 1 | 7.58 |
| CHEMBL423729 | — | — | 1 | 7.58 |
| CHEMBL138837 | — | — | 1 | 7.47 |
| CHEMBL275528 | PHENCYCLIDINE | 2.0 | 1 | 7.42 |
| CHEMBL140421 | — | — | 1 | 7.34 |
| CHEMBL139360 | — | — | 1 | 7.32 |
| CHEMBL138943 | — | — | 1 | 7.28 |
| CHEMBL139306 | — | — | 1 | 6.99 |
| CHEMBL424476 | — | — | 1 | 6.91 |
| CHEMBL342181 | — | — | 1 | 6.88 |
| CHEMBL138966 | — | — | 1 | 6.50 |
| CHEMBL136466 | — | — | 1 | 6.40 |
| CHEMBL139525 | — | — | 1 | 6.34 |
| CHEMBL139305 | — | — | 2 | 6.33 |
| CHEMBL139296 | — | — | 1 | 5.73 |
| CHEMBL139047 | — | — | 1 | 5.56 |
| CHEMBL139911 | — | — | 1 | 5.54 |
| CHEMBL141458 | — | — | 1 | 5.46 |
| CHEMBL140343 | — | — | 1 | 5.42 |
| CHEMBL344371 | — | — | 1 | 5.30 |
| CHEMBL344581 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL344151 | DIZOCILPINE MALEATE | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL52124 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL139641 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL335351 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL52124 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL140288 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL436008 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL52124 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL139348 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL342885 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL139199 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL344854 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL423729 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL138837 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL275528 | PHENCYCLIDINE | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL140421 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL139360 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL138943 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL139306 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL424476 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL342181 | — | Ki | = | 132.0 | nM | 6.88 |
| CHEMBL138966 | — | Ki | = | 314.0 | nM | 6.50 |
| CHEMBL136466 | — | Ki | = | 401.0 | nM | 6.40 |
| CHEMBL139525 | — | Ki | = | 455.0 | nM | 6.34 |
| CHEMBL139305 | — | Ki | = | 465.0 | nM | 6.33 |
| CHEMBL139305 | — | Ki | = | 1878.0 | nM | 5.73 |
| CHEMBL139296 | — | Ki | = | 1843.0 | nM | 5.73 |
| CHEMBL139047 | — | Ki | = | 2764.0 | nM | 5.56 |
| CHEMBL139911 | — | Ki | = | 2899.0 | nM | 5.54 |
| CHEMBL141458 | — | Ki | = | 3456.0 | nM | 5.46 |
| CHEMBL140343 | — | Ki | = | 3805.0 | nM | 5.42 |
| CHEMBL344371 | — | Ki | = | 4987.0 | nM | 5.30 |
| CHEMBL336891 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL344581 | — | Ki | > | 10000.0 | nM | - |