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Assay Detail

CHEMBL920804

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

Binding
Displacement of [3H]AMPA from rat recombinant GluR2 expressed in Sf9 cells
6
Total Activities
6
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 Intermediate

Target

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

Publication

A tetrazolyl-substituted subtype-selective AMPA receptor agonist.
Vogensen SB, Frydenvang K, Greenwood JR, Postorino G, Nielsen B, Pickering DS, Ebert B, Bølcho U, Egebjerg J, Gajhede M, Kastrup JS, Johansen TN, Clausen RP, Krogsgaard-Larsen P.
J Med Chem (2007) 50 : 2408 -2414
PubMed 17455929 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 9.47 10.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13378 (R,S)-AMPA 1 10.77
CHEMBL370941 1 10.10
CHEMBL388746 1 9.12
CHEMBL372643 1 8.80
CHEMBL193087 1 8.54
CHEMBL370038 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13378 (R,S)-AMPA Ki = 0.017 nM 10.77
CHEMBL370941 Ki = 0.08 nM 10.10
CHEMBL388746 Ki = 0.75 nM 9.12
CHEMBL372643 Ki = 1.6 nM 8.80
CHEMBL193087 Ki = 2.9 nM 8.54
CHEMBL370038 Ki = 0.0039 nM -