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Assay Detail

CHEMBL895666

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Functional
Agonist activity at GluR3 expressed in HEK293 cells by Fluo-4/Ca2+ assay
12
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Glutamate receptor 3 (CHEMBL3595)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Functional characterization of Tet-AMPA [tetrazolyl-2-amino-3-(3-hydroxy-5-methyl- 4-isoxazolyl)propionic acid] analogues at ionotropic glutamate receptors GluR1-GluR4. The molecular basis for the functional selectivity profile of 2-Bn-Tet-AMPA.
Jensen AA, Christesen T, Bølcho U, Greenwood JR, Postorino G, Vogensen SB, Johansen TN, Egebjerg J, Bräuner-Osborne H, Clausen RP.
J Med Chem (2007) 50 : 4177 -4185
PubMed 17672447 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 4.46 4.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370941 2 4.75
CHEMBL575060 GLUTAMIC ACID 3.0 2 4.17
CHEMBL317790 2 -
CHEMBL388746 2 -
CHEMBL193087 2 -
CHEMBL372643 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370941 EC50 = 18000.0 nM 4.75
CHEMBL575060 GLUTAMIC ACID EC50 = 67000.0 nM 4.17
CHEMBL575060 GLUTAMIC ACID EC50 = 15848931924611.11 nM -
CHEMBL317790 EC50 > 3000000.0 nM -
CHEMBL317790 EC50 < 316227766016.84 nM -
CHEMBL388746 EC50 = 1000000.0 nM -
CHEMBL388746 EC50 = 1000000000000.0 nM -
CHEMBL193087 EC50 = 700000.0 nM -
CHEMBL193087 EC50 = 1584893192461.11 nM -
CHEMBL372643 EC50 = 450000.0 nM -
CHEMBL372643 EC50 = 2511886431509.58 nM -
CHEMBL370941 EC50 = 63095734448019.43 nM -