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Assay Detail

CHEMBL2025841

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

Binding
Displacement of fluorescein-labeled phosphotyrosine-peptide derived from the interleukin-6 receptor subunit gp130 from the STAT3 after 15 mins by fluorescent polarization assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Signal transducer and activator of transcription 3 (CHEMBL4026)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Small molecule STAT5-SH2 domain inhibitors exhibit potent antileukemia activity.
Page BD, Khoury H, Laister RC, Fletcher S, Vellozo M, Manzoli A, Yue P, Turkson J, Minden MD, Gunning PT.
J Med Chem (2012) 55 : 1047 -1055
PubMed 22148584 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 5.07 5.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2023985 1 5.55
CHEMBL1829870 1 5.21
CHEMBL1829862 1 5.10
CHEMBL2023989 1 5.10
CHEMBL2023986 1 5.08
CHEMBL2023987 1 5.08
CHEMBL1829874 1 4.96
CHEMBL1829786 1 4.81
CHEMBL2023988 1 4.75
CHEMBL2024086 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2023985 Ki = 2800.0 nM 5.55
CHEMBL1829870 Ki = 6200.0 nM 5.21
CHEMBL1829862 Ki = 8000.0 nM 5.10
CHEMBL2023989 Ki = 7900.0 nM 5.10
CHEMBL2023986 Ki = 8400.0 nM 5.08
CHEMBL2023987 Ki = 8400.0 nM 5.08
CHEMBL1829874 Ki = 11000.0 nM 4.96
CHEMBL1829786 Ki = 15500.0 nM 4.81
CHEMBL2023988 Ki = 17600.0 nM 4.75
CHEMBL2024086 Ki > 25000.0 nM -