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Assay Detail

CHEMBL751565

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

Binding
Inhibition of [3H]-CGS- 19755 binding to N-methyl-D-aspartic acid receptors in rat crude synaptic membranes
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Glutamate NMDA receptor (CHEMBL1907608)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

4-(Phosphonoalkyl)- and 4-(phosphonoalkenyl)-2-piperidinecarboxylic acids: synthesis, activity at N-methyl-D-aspartic acid receptors, and anticonvulsant activity.
Hutchison AJ, Williams M, Angst C, de Jesus R, Blanchard L, Jackson RH, Wilusz EJ, Murphy DE, Bernard PS, Schneider J.
J Med Chem (1989) 32 : 2171 -2178
PubMed 2549246 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.73 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39664 SELFOTEL 2.0 1 7.50
CHEMBL68517 1 7.01
CHEMBL22304 1 6.66
CHEMBL71898 1 6.46
CHEMBL302783 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39664 SELFOTEL IC50 = 32.0 nM 7.50
CHEMBL68517 IC50 = 98.0 nM 7.01
CHEMBL22304 IC50 = 220.0 nM 6.66
CHEMBL71898 IC50 = 350.0 nM 6.46
CHEMBL302783 IC50 = 912.0 nM 6.04