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Assay Detail

CHEMBL2317650

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

Binding
Displacement of [3H]AMPA from full length recombinant rat GluKA2(R) receptor expressed in sf9 cells by liquid scintillation counting
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glutamate receptor 2 (CHEMBL3503)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Chemoenzymatic synthesis of new 2,4-syn-functionalized (S)-glutamate analogues and structure-activity relationship studies at ionotropic glutamate receptors and excitatory amino acid transporters.
Assaf Z, Larsen AP, Venskutonytė R, Han L, Abrahamsen B, Nielsen B, Gajhede M, Kastrup JS, Jensen AA, Pickering DS, Frydenvang K, Gefflaut T, Bunch L.
J Med Chem (2013) 56 : 1614 -1628
PubMed 23414088 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 4.66 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL575060 GLUTAMIC ACID 3.0 1 6.55
CHEMBL2312396 1 5.09
CHEMBL2312403 1 4.39
CHEMBL2312398 1 4.31
CHEMBL2312680 1 4.27
CHEMBL2312683 1 4.25
CHEMBL2312397 1 4.25
CHEMBL2312400 1 4.15
CHEMBL2312402 1 -
CHEMBL2312401 1 -
CHEMBL2312399 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL575060 GLUTAMIC ACID Ki = 282.0 nM 6.55
CHEMBL2312396 Ki = 8050.0 nM 5.09
CHEMBL2312403 Ki = 40800.0 nM 4.39
CHEMBL2312398 Ki = 49200.0 nM 4.31
CHEMBL2312680 Ki = 53300.0 nM 4.27
CHEMBL2312683 Ki = 56500.0 nM 4.25
CHEMBL2312397 Ki = 56200.0 nM 4.25
CHEMBL2312400 Ki = 71100.0 nM 4.15
CHEMBL2312402 Ki > 100000.0 nM -
CHEMBL2312401 Ki > 100000.0 nM -
CHEMBL2312399 Ki > 100000.0 nM -