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Assay Detail

CHEMBL846478

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Tested for in vitro inhibition of the displacement of (+)-[3H]pentazocine from sigma opioid receptor
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL3602)
Type SINGLE PROTEIN
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 4.78 5.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL312471 1 5.32
CHEMBL284237 DIZOCILPINE 2.0 1 4.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL312471 Ki = 4815.0 nM 5.32
CHEMBL284237 DIZOCILPINE Ki = 59167.0 nM 4.23