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Assay Detail

CHEMBL5053563

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

Binding
Inhibition of human SHIP2 catalytic domain (419 to 832 residues) phosphatase activity assessed as inhibition of Ins(1,3,4,5)P4 production using Ins(1,3,4,5)P4 as substrate incubated for 20 mins measured using microplate reader
11
Total Activities
11
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 11 5.49 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5087243 1 6.16
CHEMBL5078323 1 6.05
CHEMBL5081948 1 5.60
CHEMBL1601846 1 5.58
CHEMBL5080660 1 5.57
CHEMBL5092991 1 5.47
CHEMBL66953 PURPUROGALLIN 1 5.14
CHEMBL1756 ESTRAMUSTINE PHOSPHATE 4.0 1 4.38
CHEMBL23552 1 -
CHEMBL234338 1 -
CHEMBL2337806 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5087243 IC50 = 700.0 nM 6.16
CHEMBL5078323 IC50 = 900.0 nM 6.05
CHEMBL5081948 IC50 = 2500.0 nM 5.60
CHEMBL1601846 IC50 = 2600.0 nM 5.58
CHEMBL5080660 IC50 = 2700.0 nM 5.57
CHEMBL5092991 IC50 = 3400.0 nM 5.47
CHEMBL66953 PURPUROGALLIN IC50 = 7300.0 nM 5.14
CHEMBL1756 ESTRAMUSTINE PHOSPHATE IC50 = 41700.0 nM 4.38
CHEMBL23552 IC50 - -
CHEMBL234338 IC50 - -
CHEMBL2337806 IC50 - -