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Assay Detail

CHEMBL699990

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

Binding
Binding affinity of compound was determined against Ionotropic glutamate receptor ionotropic kainate 2 using cell membranes prepared from HEK293 cells
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Glutamate receptor ionotropic, kainate 2 (CHEMBL3683)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists.
Baker SR, Bleakman D, Ezquerra J, Ballyk BA, Deverill M, Ho K, Kamboj RK, Collado I, Domínguez C, Escribano A, Mateo AI, Pedregal C, Rubio A.
Bioorg Med Chem Lett (2000) 10 : 1807 -1810
PubMed 10969973 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 5.13 7.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275040 KAINIC ACID 2.0 1 7.49
CHEMBL38499 1 6.35
CHEMBL575060 GLUTAMIC ACID 3.0 1 5.96
CHEMBL52514 1 5.60
CHEMBL301536 1 4.81
CHEMBL300928 1 4.79
CHEMBL52295 1 4.75
CHEMBL54291 1 4.33
CHEMBL50041 1 4.24
CHEMBL299180 1 4.08
CHEMBL299291 1 4.06
CHEMBL51008 1 -
CHEMBL298779 1 -
CHEMBL297919 1 -
CHEMBL53194 1 -
CHEMBL298800 1 -
CHEMBL53775 1 -
CHEMBL54238 1 -
CHEMBL54073 1 -
CHEMBL51054 1 -
CHEMBL51660 1 -
CHEMBL299365 1 -
CHEMBL52742 1 -
CHEMBL53702 1 -
CHEMBL297283 1 -
CHEMBL51395 1 -
CHEMBL53655 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275040 KAINIC ACID Ki = 32.4 nM 7.49
CHEMBL38499 Ki = 450.0 nM 6.35
CHEMBL575060 GLUTAMIC ACID Ki = 1106.0 nM 5.96
CHEMBL52514 Ki = 2500.0 nM 5.60
CHEMBL301536 Ki = 15410.0 nM 4.81
CHEMBL300928 Ki = 16300.0 nM 4.79
CHEMBL52295 Ki = 18000.0 nM 4.75
CHEMBL54291 Ki = 46300.0 nM 4.33
CHEMBL50041 Ki = 57200.0 nM 4.24
CHEMBL299180 Ki = 82500.0 nM 4.08
CHEMBL299291 Ki = 87600.0 nM 4.06
CHEMBL51008 Ki = 207000.0 nM -
CHEMBL298779 Ki > 400000.0 nM -
CHEMBL297919 Ki = 125000.0 nM -
CHEMBL53194 Ki > 100000.0 nM -
CHEMBL298800 Ki > 500000.0 nM -
CHEMBL53775 Ki = 205000.0 nM -
CHEMBL54238 Ki = 255000.0 nM -
CHEMBL54073 Ki > 10000.0 nM -
CHEMBL51054 Ki > 100000.0 nM -
CHEMBL51660 Ki > 100000.0 nM -
CHEMBL299365 Ki = 634000.0 nM -
CHEMBL52742 Ki > 100000.0 nM -
CHEMBL53702 Ki > 100010.0 nM -
CHEMBL297283 Ki = 193000.0 nM -
CHEMBL51395 Ki > 100000.0 nM -
CHEMBL53655 Ki > 100000.0 nM -