Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4712508

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

Binding
Inhibition of oligonucleotide [32P]-labelled 5'-AGCITCATTTCCCGTAAATCCCTA probe binding to STAT1/STAT3 heterodimer in mouse NIH3T3 nuclear extract preincubated for 30 mins followed by hSIE probe addition by EMSA analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type NIH3T3
Subcellular Nucleus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Signal transducer and activator of transcription 1/ 3 (CHEMBL3885638)
Type PROTEIN COMPLEX
Organism Mus musculus

Publication

Discovery of Novel Azetidine Amides as Potent Small-Molecule STAT3 Inhibitors.
Brotherton-Pleiss C,Yue P,Zhu Y,Nakamura K,Chen W,Fu W,Kubota C,Chen J,Alonso-Valenteen F,Mikhael S,Medina-Kauwe L,Tius MA,Lopez-Tapia F,Turkson J
J Med Chem (2021) 64 : 695 -710
PubMed 33352047 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.51 5.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4778873 1 5.84
CHEMBL4746031 1 5.58
CHEMBL4753131 1 5.50
CHEMBL4787896 1 5.33
CHEMBL4760561 1 5.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4778873 IC50 = 1460.0 nM 5.84
CHEMBL4746031 IC50 = 2610.0 nM 5.58
CHEMBL4753131 IC50 = 3140.0 nM 5.50
CHEMBL4787896 IC50 = 4710.0 nM 5.33
CHEMBL4760561 IC50 = 4920.0 nM 5.31