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Assay Detail

CHEMBL4351325

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

Binding
Displacement of (RS)-[3H]AMPA from recombinant rat GluA1 expressed in baculovirus infected Sf9 insect cell membranes
9
Total Activities
9
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 1 (CHEMBL3753)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands.
Sainas S, Temperini P, Farnsworth JC, Yi F, Møllerud S, Jensen AA, Nielsen B, Passoni A, Kastrup JS, Hansen KB, Boschi D, Pickering DS, Clausen RP, Lolli ML.
J Med Chem (2019) 62 : 4467 -4482
PubMed 30943028 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 5.70 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL94859 1 8.28
CHEMBL276815 (S)-AMPA 1 7.66
CHEMBL4529665 1 5.04
CHEMBL3742451 1 4.80
CHEMBL4556711 1 4.27
CHEMBL3742450 1 4.14
CHEMBL4448290 1 -
CHEMBL4451018 1 -
CHEMBL388746 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL94859 Ki = 5.2 nM 8.28
CHEMBL276815 (S)-AMPA Ki = 22.0 nM 7.66
CHEMBL4529665 Ki = 9020.0 nM 5.04
CHEMBL3742451 Ki = 15700.0 nM 4.80
CHEMBL4556711 Ki = 54100.0 nM 4.27
CHEMBL3742450 Ki = 73000.0 nM 4.14
CHEMBL4448290 Ki > 100000.0 nM -
CHEMBL4451018 Ki > 100000.0 nM -
CHEMBL388746 Ki = 7700.0 nM -