Assay Detail
Binding
CHEMBL748551
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Tested for the inhibition of [3H]dizocilpine binding to N-methyl-D-aspartate (NMDA) receptor-coupled phencyclidine binding site
5
Total Activities
4
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
Synthesis and binding properties of MK-801 isothiocyanates; (+)-3-isothiocyanato-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten- 5,10-imine hydrochloride: a new, potent and selective electrophilic affinity ligand for the NMDA receptor-coupled phencyclidine binding site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 6.58 | 7.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL312471 | — | — | 2 | 7.43 |
| CHEMBL282383 | — | — | 1 | 7.03 |
| CHEMBL41541 | METHAPHIT | — | 1 | 6.27 |
| CHEMBL314256 | — | — | 1 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL312471 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL282383 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL41541 | METHAPHIT | Ki | = | 535.0 | nM | 6.27 |
| CHEMBL312471 | — | Ki | = | 838.0 | nM | 6.08 |
| CHEMBL314256 | — | Ki | = | 843.0 | nM | 6.07 |