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Assay Detail

CHEMBL865634

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

Binding
Displacement of [3H]kainate from rat GLUK6 expressed in HEK293 cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

Glutamate receptor ionotropic, kainate 2 (CHEMBL3607)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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
Ki 15 5.73 5.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9790 1 5.98
CHEMBL575060 GLUTAMIC ACID 3.0 1 5.48
CHEMBL200737 1 -
CHEMBL206407 1 -
CHEMBL202786 1 -
CHEMBL379442 1 -
CHEMBL438974 1 -
CHEMBL446188 1 -
CHEMBL382774 1 -
CHEMBL382687 1 -
CHEMBL208483 1 -
CHEMBL207046 1 -
CHEMBL383062 1 -
CHEMBL372797 1 -
CHEMBL200337 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9790 Ki = 1050.0 nM 5.98
CHEMBL575060 GLUTAMIC ACID Ki = 3280.0 nM 5.48
CHEMBL200737 Ki > 1000000.0 nM -
CHEMBL206407 Ki > 100000.0 nM -
CHEMBL202786 Ki > 1000000.0 nM -
CHEMBL379442 Ki > 100000.0 nM -
CHEMBL438974 Ki - -
CHEMBL446188 Ki > 100000.0 nM -
CHEMBL382774 Ki > 1000000.0 nM -
CHEMBL382687 Ki - -
CHEMBL208483 Ki > 100000.0 nM -
CHEMBL207046 Ki > 100000.0 nM -
CHEMBL383062 Ki - -
CHEMBL372797 Ki > 1000000.0 nM -
CHEMBL200337 Ki > 100000.0 nM -