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Assay Detail

CHEMBL4055341

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

Binding
Displacement of 5-carboxyfluorescein-GY(PO3H2)LVLDKW from C-terminal His6-tagged/N-terminal maltose-binding protein-tagged STAT5A SH2 domain (unknown origin) (137 to 707 residues) Escherichia coli BL21(DE3) pretreated for 1 hr followed by fluorescent tracer addition after 1 hr by fluorescence polarization assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Signal transducer and activator of transcription 5A (CHEMBL5403)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Halogen-substituted catechol bisphosphates are potent and selective inhibitors of the transcription factor STAT5b.
Elumalai N, Natarajan K, Berg T.
Bioorg Med Chem (2017) 25 : 3871 -3882
PubMed 28559059 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.30 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4088092 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4088092 IC50 = 4970.0 nM 5.30