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Assay Detail

CHEMBL751135

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

Binding
Tested for the ability to inhibit the specific binding of [3H]-CGS- 19755 to NMDA recognition sites on rat brain membranes
8
Total Activities
7
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

Pharmacology of (2R, 4R, 5S)-2-amino-4,5-(1,2-cyclohexyl)-7-phosphonoheptanoic acid (NPC 17742); a selective, systemically active, competitive NMDA antagonist
Ferkany J, Willetts J, Borosky D, Clissold E, Karbon, Hamilton G
Bioorg Med Chem Lett (1993) 3 : 33 -38
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.84 7.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39664 SELFOTEL 2.0 1 7.06
CHEMBL22304 1 6.72
CHEMBL107660 1 6.57
CHEMBL107961 1 5.62
CHEMBL108823 1 5.58
CHEMBL340085 2 5.39
CHEMBL108096 1 5.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39664 SELFOTEL IC50 = 87.0 nM 7.06
CHEMBL22304 IC50 = 190.0 nM 6.72
CHEMBL107660 IC50 = 270.0 nM 6.57
CHEMBL107961 IC50 = 2400.0 nM 5.62
CHEMBL108823 IC50 = 2600.0 nM 5.58
CHEMBL340085 IC50 = 4050.0 nM 5.39
CHEMBL108096 IC50 = 5600.0 nM 5.25
CHEMBL340085 IC50 = 28000.0 nM 4.55