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Assay Detail

CHEMBL697426

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 1 using cell membranes prepared from HEK293 cells
26
Total Activities
26
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 1 (CHEMBL1918)
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 26 6.23 7.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301536 1 7.83
CHEMBL51660 1 7.49
CHEMBL52295 1 7.22
CHEMBL50041 1 7.09
CHEMBL52742 1 7.07
CHEMBL298800 1 7.03
CHEMBL297919 1 6.82
CHEMBL299291 1 6.82
CHEMBL275040 KAINIC ACID 2.0 1 6.75
CHEMBL299365 1 6.65
CHEMBL51395 1 6.63
CHEMBL51008 1 6.62
CHEMBL38499 1 6.57
CHEMBL51054 1 6.33
CHEMBL300928 1 6.29
CHEMBL575060 GLUTAMIC ACID 3.0 1 6.15
CHEMBL52514 1 5.66
CHEMBL54291 1 5.44
CHEMBL54238 1 5.29
CHEMBL53702 1 5.22
CHEMBL298779 1 4.86
CHEMBL53775 1 4.77
CHEMBL53194 1 4.54
CHEMBL297283 1 4.38
CHEMBL54073 1 -
CHEMBL53655 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301536 Ki = 14.8 nM 7.83
CHEMBL51660 Ki = 32.6 nM 7.49
CHEMBL52295 Ki = 60.5 nM 7.22
CHEMBL50041 Ki = 80.4 nM 7.09
CHEMBL52742 Ki = 85.7 nM 7.07
CHEMBL298800 Ki = 93.6 nM 7.03
CHEMBL297919 Ki = 150.0 nM 6.82
CHEMBL299291 Ki = 152.0 nM 6.82
CHEMBL275040 KAINIC ACID Ki = 177.0 nM 6.75
CHEMBL299365 Ki = 224.0 nM 6.65
CHEMBL51395 Ki = 236.0 nM 6.63
CHEMBL51008 Ki = 241.0 nM 6.62
CHEMBL38499 Ki = 270.0 nM 6.57
CHEMBL51054 Ki = 470.0 nM 6.33
CHEMBL300928 Ki = 511.0 nM 6.29
CHEMBL575060 GLUTAMIC ACID Ki = 701.0 nM 6.15
CHEMBL52514 Ki = 2200.0 nM 5.66
CHEMBL54291 Ki = 3620.0 nM 5.44
CHEMBL54238 Ki = 5130.0 nM 5.29
CHEMBL53702 Ki = 6060.0 nM 5.22
CHEMBL298779 Ki = 13900.0 nM 4.86
CHEMBL53775 Ki = 17100.0 nM 4.77
CHEMBL53194 Ki = 29100.0 nM 4.54
CHEMBL297283 Ki = 41200.0 nM 4.38
CHEMBL54073 Ki > 1000.0 nM -
CHEMBL53655 Ki > 1000.0 nM -