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Assay Detail

CHEMBL4055338

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

Binding
Displacement of 5-carboxyfluorescein-GY(PO3H2)LVLDKW from STAT5A SH2 domain (unknown origin) pretreated for 1 hr followed by fluorescent tracer addition after 1 hr by fluorescence polarization assay
13
Total Activities
13
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 13 5.06 5.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4104462 1 5.14
CHEMBL4104019 1 5.14
CHEMBL4077592 1 5.13
CHEMBL4085646 1 5.12
CHEMBL4103576 1 5.08
CHEMBL4093849 1 5.08
CHEMBL4080740 1 5.07
CHEMBL4080219 1 5.05
CHEMBL4075745 1 5.04
CHEMBL4066274 1 5.01
CHEMBL4076474 1 4.98
CHEMBL4086096 1 4.97
CHEMBL4062751 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4104462 IC50 = 7200.0 nM 5.14
CHEMBL4104019 IC50 = 7300.0 nM 5.14
CHEMBL4077592 IC50 = 7400.0 nM 5.13
CHEMBL4085646 IC50 = 7600.0 nM 5.12
CHEMBL4103576 IC50 = 8400.0 nM 5.08
CHEMBL4093849 IC50 = 8300.0 nM 5.08
CHEMBL4080740 IC50 = 8600.0 nM 5.07
CHEMBL4080219 IC50 = 8900.0 nM 5.05
CHEMBL4075745 IC50 = 9100.0 nM 5.04
CHEMBL4066274 IC50 = 9700.0 nM 5.01
CHEMBL4076474 IC50 = 10500.0 nM 4.98
CHEMBL4086096 IC50 = 10600.0 nM 4.97
CHEMBL4062751 IC50 = 11900.0 nM 4.92