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Assay Detail

CHEMBL2175187

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

Binding
Inhibition of STAT3 dimerization in v-Src transformed mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT3-DNA interaction in nucleus after 30 mins by EMSA
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type NIH3T3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Signal transducer and activator of transcription 3 (CHEMBL5402)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein.
Debnath B, Xu S, Neamati N.
J Med Chem (2012) 55 : 6645 -6668
PubMed 22650325 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 4.35 4.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2171897 1 4.60
CHEMBL2172017 1 4.55
CHEMBL2172015 1 4.48
CHEMBL1829786 1 4.46
CHEMBL392556 1 4.38
CHEMBL2023986 1 4.37
CHEMBL2172013 1 4.37
CHEMBL2172014 1 4.35
CHEMBL2023987 1 4.30
CHEMBL2172018 1 4.24
CHEMBL477936 1 4.07
CHEMBL2172016 1 4.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2171897 IC50 = 25000.0 nM 4.60
CHEMBL2172017 IC50 = 28000.0 nM 4.55
CHEMBL2172015 IC50 = 33000.0 nM 4.48
CHEMBL1829786 IC50 = 35000.0 nM 4.46
CHEMBL392556 IC50 = 42000.0 nM 4.38
CHEMBL2023986 IC50 = 43000.0 nM 4.37
CHEMBL2172013 IC50 = 43000.0 nM 4.37
CHEMBL2172014 IC50 = 45000.0 nM 4.35
CHEMBL2023987 IC50 = 50000.0 nM 4.30
CHEMBL2172018 IC50 = 58000.0 nM 4.24
CHEMBL477936 IC50 = 86000.0 nM 4.07
CHEMBL2172016 IC50 = 90000.0 nM 4.05