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Assay Detail

CHEMBL865006

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

Functional
Inhibition of glutamate-induced calcium influx in HEK293 cells expressing human GLUK5/GLUK6 by FLIPR assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structure-activity relationship studies on N3-substituted willardiine derivatives acting as AMPA or kainate receptor antagonists.
Dolman NP, More JC, Alt A, Knauss JL, Troop HM, Bleakman D, Collingridge GL, Jane DE.
J Med Chem (2006) 49 : 2579 -2592
PubMed 16610801 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.38 6.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL379442 1 6.21
CHEMBL222519 NBQX 1 4.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL379442 IC50 = 620.0 nM 6.21
CHEMBL222519 NBQX IC50 = 28000.0 nM 4.55