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Assay Detail

CHEMBL1838752

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

Functional
Increase of EAAT2 expression in mouse primary astrocytes after 24 hrs by Western blot analysis relative to beta-actin protein expression
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type Astrocyte
Confidence 1 — Organism
Curated By Autocuration

Target

Astrocyte (CHEMBL614871)
Type CELL-LINE

Publication

Structure-activity relationship study of pyridazine derivatives as glutamate transporter EAAT2 activators.
Xing X, Chang LC, Kong Q, Colton CK, Lai L, Glicksman MA, Lin CL, Cuny GD.
Bioorg Med Chem Lett (2011) 21 : 5774 -5777
PubMed 21875806 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 5.62 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1834147 1 6.30
CHEMBL1834143 1 5.77
CHEMBL1834157 1 5.72
CHEMBL1834154 1 5.62
CHEMBL1834131 1 5.58
CHEMBL1834177 1 5.58
CHEMBL1834164 1 5.58
CHEMBL1834133 1 5.57
CHEMBL1834129 1 5.48
CHEMBL1834168 1 5.48
CHEMBL1834127 1 5.41
CHEMBL1834155 1 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1834147 EC50 = 500.0 nM 6.30
CHEMBL1834143 EC50 = 1700.0 nM 5.77
CHEMBL1834157 EC50 = 1900.0 nM 5.72
CHEMBL1834154 EC50 = 2400.0 nM 5.62
CHEMBL1834131 EC50 = 2600.0 nM 5.58
CHEMBL1834177 EC50 = 2600.0 nM 5.58
CHEMBL1834164 EC50 = 2600.0 nM 5.58
CHEMBL1834133 EC50 = 2700.0 nM 5.57
CHEMBL1834129 EC50 = 3300.0 nM 5.48
CHEMBL1834168 EC50 = 3300.0 nM 5.48
CHEMBL1834127 EC50 = 3900.0 nM 5.41
CHEMBL1834155 EC50 = 4700.0 nM 5.33