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Assay Detail

CHEMBL698072

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Binding
Binding affinity against human ionotropic glutamate receptor kainate 1 in HK293 cells using [3H]kainate as radioligand
ChEMBL ↗
48
Total Activities
47
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-Alkyl- and 4-cinnamylglutamic acid analogues are potent GluR5 kainate receptor agonists.
Pedregal C, Collado I, Escribano A, Ezquerra J, Domínguez C, Mateo AI, Rubio A, Baker SR, Goldsworthy J, Kamboj RK, Ballyk BA, Hoo K, Bleakman D.
J Med Chem (2000) 43 : 1958 -1968
PubMed 10821708 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 48 6.85 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288166 2S,4R-4-METHYLGLUTAMATE — 1 8.52
CHEMBL61751 — — 1 8.15
CHEMBL58590 — — 1 8.10
CHEMBL59551 — — 1 7.94
CHEMBL294139 — — 1 7.68
CHEMBL59284 — — 2 7.58
CHEMBL62086 — — 1 7.54
CHEMBL301915 — — 1 7.52
CHEMBL300368 — — 1 7.50
CHEMBL305346 — — 1 7.40
CHEMBL60406 — — 1 7.39
CHEMBL58095 — — 1 7.36
CHEMBL293118 — — 1 7.31
CHEMBL291491 — — 1 7.28
CHEMBL62057 — — 1 7.25
CHEMBL302680 — — 1 7.24
CHEMBL60168 — — 1 7.23
CHEMBL58054 — — 1 7.22
CHEMBL294683 — — 1 7.11
CHEMBL61997 — — 1 6.91
CHEMBL59297 — — 1 6.88
CHEMBL292896 — — 1 6.88
CHEMBL58808 — — 1 6.80
CHEMBL2111523 — — 1 6.80
CHEMBL304434 — — 1 6.79
CHEMBL292745 — — 1 6.76
CHEMBL275040 KAINIC ACID 2.0 1 6.75
CHEMBL60114 — — 1 6.59
CHEMBL293548 — — 1 6.59
CHEMBL58027 — — 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL288166 2S,4R-4-METHYLGLUTAMATE Ki = 3.0 nM 8.52
CHEMBL61751 — Ki = 7.0 nM 8.15
CHEMBL58590 — Ki = 8.0 nM 8.10
CHEMBL59551 — Ki = 11.6 nM 7.94
CHEMBL294139 — Ki = 21.0 nM 7.68
CHEMBL59284 — Ki = 26.0 nM 7.58
CHEMBL62086 — Ki = 28.9 nM 7.54
CHEMBL59284 — Ki = 30.0 nM 7.52
CHEMBL301915 — Ki = 30.0 nM 7.52
CHEMBL300368 — Ki = 32.0 nM 7.50
CHEMBL305346 — Ki = 40.0 nM 7.40
CHEMBL60406 — Ki = 41.0 nM 7.39
CHEMBL58095 — Ki = 44.0 nM 7.36
CHEMBL293118 — Ki = 49.0 nM 7.31
CHEMBL291491 — Ki = 52.0 nM 7.28
CHEMBL62057 — Ki = 56.0 nM 7.25
CHEMBL302680 — Ki = 58.0 nM 7.24
CHEMBL60168 — Ki = 59.0 nM 7.23
CHEMBL58054 — Ki = 60.0 nM 7.22
CHEMBL294683 — Ki = 78.0 nM 7.11
CHEMBL61997 — Ki = 123.0 nM 6.91
CHEMBL59297 — Ki = 131.0 nM 6.88
CHEMBL292896 — Ki = 133.0 nM 6.88
CHEMBL2111523 — Ki = 160.0 nM 6.80
CHEMBL58808 — Ki = 157.0 nM 6.80
CHEMBL304434 — Ki = 161.0 nM 6.79
CHEMBL292745 — Ki = 172.0 nM 6.76
CHEMBL275040 KAINIC ACID Ki = 177.0 nM 6.75
CHEMBL60114 — Ki = 254.0 nM 6.59
CHEMBL293548 — Ki = 254.0 nM 6.59
CHEMBL58027 — Ki = 267.0 nM 6.57
CHEMBL59299 — Ki = 284.0 nM 6.55
CHEMBL58718 — Ki = 307.0 nM 6.51
CHEMBL59792 — Ki = 337.0 nM 6.47
CHEMBL293829 — Ki = 367.0 nM 6.43
CHEMBL59948 — Ki = 540.0 nM 6.27
CHEMBL61307 — Ki = 577.0 nM 6.24
CHEMBL61697 — Ki = 670.0 nM 6.17
CHEMBL575060 GLUTAMIC ACID Ki = 701.0 nM 6.15
CHEMBL58541 — Ki = 831.0 nM 6.08
CHEMBL59286 — Ki = 1015.0 nM 5.99
CHEMBL305387 — Ki = 1190.0 nM 5.92
CHEMBL62055 — Ki = 1300.0 nM 5.89
CHEMBL299449 — Ki = 1464.0 nM 5.83
CHEMBL62053 — Ki = 2376.0 nM 5.62
CHEMBL61434 — Ki = 3590.0 nM 5.45
CHEMBL302402 — Ki = 3606.0 nM 5.44
CHEMBL301536 — Ki > 10000.0 nM -