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Assay Detail

CHEMBL750152

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

Binding
Inhibitory activity evaluated by its ability to displace [3H]CPP from N-methyl-D-aspartate glutamate receptor in rat cortical membranes at 10E-5 concentration of the compound
4
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

Exploration of N-phosphonoalkyl-, N-phosphonoalkenyl-, and N-(phosphonoalkyl)phenyl-spaced alpha-amino acids as competitive N-methyl-D-aspartic acid antagonists.
Bigge CF, Johnson G, Ortwine DF, Drummond JT, Retz DM, Brahce LJ, Coughenour LL, Marcoux FW, Probert AW.
J Med Chem (1992) 35 : 1371 -1384
PubMed 1533423 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.70 6.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL28862 1 6.54
CHEMBL274440 AP-7 1 6.11
CHEMBL443231 1 5.40
CHEMBL284880 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL28862 IC50 = 290.0 nM 6.54
CHEMBL274440 AP-7 IC50 = 770.0 nM 6.11
CHEMBL443231 IC50 = 4000.0 nM 5.40
CHEMBL284880 IC50 = 18000.0 nM 4.75