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Assay Detail

CHEMBL751242

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

Binding
The compound was tested for its affinity against N-methyl-D-aspartate glutamate receptor in rats using [3H]CPP as radioligand
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

Bioisosteric replacement of the alpha-amino carboxylic acid functionality in 2-amino-5-phosphonopentanoic acid yields unique 3,4-diamino-3-cyclobutene-1,2-dione containing NMDA antagonists.
Kinney WA, Lee NE, Garrison DT, Podlesny EJ, Simmonds JT, Bramlett D, Notvest RR, Kowal DM, Tasse RP.
J Med Chem (1992) 35 : 4720 -4726
PubMed 1361582 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.97 6.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL83688 1 6.33
CHEMBL143852 1 6.00
CHEMBL145806 1 5.58
CHEMBL142917 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL83688 IC50 = 470.0 nM 6.33
CHEMBL143852 IC50 = 1000.0 nM 6.00
CHEMBL145806 IC50 = 2600.0 nM 5.58
CHEMBL142917 IC50 > 10000.0 nM -