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Assay Detail

CHEMBL5209616

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

Functional
Inhibition of the Excitatory Amino Acid Transporter 1 (EAAT1, SLC1A3) as assessed by a phenotypic impedance-based assay detecting changes in cell morphology by L-glutamate uptake in HEK-293 JumpIN-SLC1A3 cells (PubChem AID: 1745862)
6
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Excitatory amino acid transporter 1 (CHEMBL3085)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Impedance-Based Phenotypic Readout of Transporter Function: A Case for Glutamate Transporters
Hubert J. Sijben; Laura Dall' Acqua; Rongfang Liu; Abigail Jarret; Eirini Christodoulaki; Svenja Onstein; Gernot Wolf; Simone J. Verburgt; Sylvia E. Le Dévédec; Tabea Wiedmer; Giulio Superti-Furga; Adriaan P. Ijzerman; Laura H. Heitman
Front Pharmacol (2022) 13 : 872335
PubMed 35677430 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 - -
IC50 2 5.95 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1257519 1 6.70
CHEMBL474133 1 5.20
CHEMBL575060 GLUTAMIC ACID 3.0 1 -
CHEMBL76232 D-GLUTAMATE 1 -
CHEMBL274323 ASPARTIC ACID 3.0 1 -
CHEMBL29757 D-ASPARTATE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1257519 IC50 = 200.0 nM 6.70
CHEMBL474133 IC50 = 6300.0 nM 5.20
CHEMBL575060 GLUTAMIC ACID EC50 = 398000.0 nM -
CHEMBL76232 D-GLUTAMATE EC50 > 1000000.0 nM -
CHEMBL274323 ASPARTIC ACID EC50 = 398000.0 nM -
CHEMBL29757 D-ASPARTATE EC50 = 398000.0 nM -