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Assay Detail

CHEMBL5548355

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

Binding
Positive allosteric modulation of EAAT3 (unknown origin) transfected in African green monkey COS-7 cells assessed as increase in glutamate uptake preincubated for 10 mins followed by 3-H-L-glutamate addition and measured after 10 mins by scintillation counter analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Excitatory amino acid transporter 3 (CHEMBL2721)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and Structure-Activity Relationships for Glutamate Transporter Allosteric Modulators.
Fontana ACK, Poli ANR, Gour J, Srikanth YVV, Anastasi N, Ashok D, Khatiwada A, Reeb KL, Cheng MH, Bahar I, Rawls SM, Salvino JM.
J Med Chem (2024) 67 : 6119 -6143
PubMed 38626917 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 8.47 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5593916 1 9.70
CHEMBL5564905 1 8.81
CHEMBL5594077 1 8.60
CHEMBL5583680 1 8.37
CHEMBL1393473 1 6.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5593916 EC50 = 0.2 nM 9.70
CHEMBL5564905 EC50 = 1.55 nM 8.81
CHEMBL5594077 EC50 = 2.5 nM 8.60
CHEMBL5583680 EC50 = 4.3 nM 8.37
CHEMBL1393473 EC50 = 132.0 nM 6.88