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Assay Detail

CHEMBL1013084

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

Binding
Displacement of [3H]AMPA from AMPA receptor in rat synaptosomes
14
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7.
Sagot E, Pickering DS, Pu X, Umberti M, Stensbøl TB, Nielsen B, Chapelet M, Bolte J, Gefflaut T, Bunch L.
J Med Chem (2008) 51 : 4093 -4103
PubMed 18578478 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 4.42 4.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL479804 2 4.60
CHEMBL500042 2 4.51
CHEMBL482080 2 4.51
CHEMBL500448 2 4.36
CHEMBL479805 2 4.13
CHEMBL518313 1 -
CHEMBL482081 1 -
CHEMBL479797 1 -
CHEMBL446256 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL479804 IC50 = 25000.0 nM 4.60
CHEMBL479804 IC50 = 25118.86 nM 4.60
CHEMBL500042 IC50 = 30902.95 nM 4.51
CHEMBL482080 IC50 = 31000.0 nM 4.51
CHEMBL482080 IC50 = 30902.95 nM 4.51
CHEMBL500042 IC50 = 32000.0 nM 4.50
CHEMBL500448 IC50 = 44000.0 nM 4.36
CHEMBL500448 IC50 = 44668.36 nM 4.35
CHEMBL479805 IC50 = 74000.0 nM 4.13
CHEMBL479805 IC50 = 74131.02 nM 4.13
CHEMBL518313 IC50 > 100000.0 nM -
CHEMBL482081 IC50 > 100000.0 nM -
CHEMBL479797 IC50 > 100000.0 nM -
CHEMBL446256 IC50 > 100000.0 nM -