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Assay Detail

CHEMBL748011

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Binding
Tested for in vitro inhibition of the displacement of (+)-[3H]dizocilpine from NMDA receptor
2
Total Activities
2
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.
Linders JT, Monn JA, Mattson MV, George C, Jacobson AE, Rice KC.
J Med Chem (1993) 36 : 2499 -2507
PubMed 8355251 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.02 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284237 DIZOCILPINE 2.0 1 8.60
CHEMBL312471 1 7.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284237 DIZOCILPINE Ki = 2.5 nM 8.60
CHEMBL312471 Ki = 37.0 nM 7.43