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Assay Detail

CHEMBL751564

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-aspartate glutamate receptor in rat crude synaptic membranes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 5 — Multiple protein complex / RNA
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 12 6.51 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26475 1 7.85
CHEMBL283032 1 7.41
CHEMBL29692 1 7.14
CHEMBL284445 1 7.11
CHEMBL28523 1 7.10
CHEMBL68966 1 6.98
CHEMBL30161 1 6.34
CHEMBL281485 1 6.10
CHEMBL29465 1 5.89
CHEMBL30127 1 5.89
CHEMBL282162 1 5.80
CHEMBL69691 1 4.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26475 IC50 = 14.0 nM 7.85
CHEMBL283032 IC50 = 39.0 nM 7.41
CHEMBL29692 IC50 = 72.0 nM 7.14
CHEMBL284445 IC50 = 78.0 nM 7.11
CHEMBL28523 IC50 = 80.0 nM 7.10
CHEMBL68966 IC50 = 105.0 nM 6.98
CHEMBL30161 IC50 = 452.0 nM 6.34
CHEMBL281485 IC50 = 800.0 nM 6.10
CHEMBL29465 IC50 = 1300.0 nM 5.89
CHEMBL30127 IC50 = 1300.0 nM 5.89
CHEMBL282162 IC50 = 1600.0 nM 5.80
CHEMBL69691 IC50 = 28000.0 nM 4.55