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Assay Detail

CHEMBL5053561

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

Binding
Inhibition of 2-FAM-InsP5 binding to human SHIP2 catalytic domain (419 to 832 residues) assessed as change in polarization by fluorescence polarization based displacement assay
15
Total Activities
15
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

Publication

Allosteric Site on SHIP2 Identified Through Fluorescent Ligand Screening and Crystallography: A Potential New Target for Intervention.
Whitfield H, Hemmings AM, Mills SJ, Baker K, White G, Rushworth S, Riley AM, Potter BVL, Brearley CA.
J Med Chem (2021) 64 : 3813 -3826
PubMed 33724834 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.28 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5087243 1 7.64
CHEMBL5078323 1 7.57
CHEMBL5092991 1 7.54
CHEMBL5080660 1 7.51
CHEMBL5081948 1 7.21
CHEMBL5092487 1 5.81
CHEMBL23552 1 5.64
CHEMBL66953 PURPUROGALLIN 1 5.26
CHEMBL601719 CRIZOTINIB 4.0 1 5.26
CHEMBL4473747 1 5.20
CHEMBL1756 ESTRAMUSTINE PHOSPHATE 4.0 1 4.45
CHEMBL1601846 1 -
CHEMBL234338 1 -
CHEMBL2337806 1 -
CHEMBL5094588 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5087243 IC50 = 23.0 nM 7.64
CHEMBL5078323 IC50 = 27.0 nM 7.57
CHEMBL5092991 IC50 = 29.0 nM 7.54
CHEMBL5080660 IC50 = 31.0 nM 7.51
CHEMBL5081948 IC50 = 61.0 nM 7.21
CHEMBL5092487 IC50 = 1540.0 nM 5.81
CHEMBL23552 IC50 = 2300.0 nM 5.64
CHEMBL66953 PURPUROGALLIN IC50 = 5500.0 nM 5.26
CHEMBL601719 CRIZOTINIB IC50 = 5500.0 nM 5.26
CHEMBL4473747 IC50 = 6250.0 nM 5.20
CHEMBL1756 ESTRAMUSTINE PHOSPHATE IC50 = 35500.0 nM 4.45
CHEMBL1601846 IC50 - -
CHEMBL234338 IC50 - -
CHEMBL2337806 IC50 - -
CHEMBL5094588 IC50 > 100000.0 nM -