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Assay Detail

CHEMBL1687315

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

Binding
Inhibition of STAT3 dimerization in mouse NIH3T3 cells expressing v-Src assessed as disruption of STAT3-STAT3: DNA complexation in nucleus after 30 mins by electrophoretic mobility shift assay
14
Total Activities
14
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

Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
Shahani VM, Yue P, Fletcher S, Sharmeen S, Sukhai MA, Luu DP, Zhang X, Sun H, Zhao W, Schimmer AD, Turkson J, Gunning PT.
Bioorg Med Chem (2011) 19 : 1823 -1838
PubMed 21216604 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 4.35 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1681824 1 5.30
CHEMBL1684873 1 4.48
CHEMBL1684879 1 4.40
CHEMBL1681825 1 4.22
CHEMBL1684877 1 4.21
CHEMBL1684878 1 4.19
CHEMBL1681829 1 4.18
CHEMBL1684872 1 4.14
CHEMBL1681828 1 4.04
CHEMBL1684875 1 -
CHEMBL1684876 1 -
CHEMBL1681827 1 -
CHEMBL1681826 1 -
CHEMBL1684874 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1681824 IC50 = 5000.0 nM 5.30
CHEMBL1684873 IC50 = 33000.0 nM 4.48
CHEMBL1684879 IC50 = 40000.0 nM 4.40
CHEMBL1681825 IC50 = 60000.0 nM 4.22
CHEMBL1684877 IC50 = 62000.0 nM 4.21
CHEMBL1684878 IC50 = 64000.0 nM 4.19
CHEMBL1681829 IC50 = 66000.0 nM 4.18
CHEMBL1684872 IC50 = 73100.0 nM 4.14
CHEMBL1681828 IC50 = 92000.0 nM 4.04
CHEMBL1684875 IC50 = 103000.0 nM -
CHEMBL1684876 IC50 = 190000.0 nM -
CHEMBL1681827 IC50 = 188000.0 nM -
CHEMBL1681826 IC50 = 112000.0 nM -
CHEMBL1684874 IC50 > 200000.0 nM -