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Assay Detail

CHEMBL840052

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

Binding
Inhibition of [3H]AMPA binding to human Ionotropic glutamate receptor 2
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Glutamate receptor 2 (CHEMBL4016)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain.
Dominguez E, Iyengar S, Shannon HE, Bleakman D, Alt A, Arnold BM, Bell MG, Bleisch TJ, Buckmaster JL, Castano AM, Del Prado M, Escribano A, Filla SA, Ho KH, Hudziak KJ, Jones CK, Martinez-Perez JA, Mateo A, Mathes BM, Mattiuz EL, Ogden AM, Simmons RM, Stack DR, Stratford RE, Winter MA, Wu Z, Ornstein PL.
J Med Chem (2005) 48 : 4200 -4203
PubMed 15974569 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 5.66 5.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14935 TEZAMPANEL ANHYDROUS 2.0 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14935 TEZAMPANEL ANHYDROUS Ki = 2210.0 nM 5.66