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Assay Detail

CHEMBL4406334

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

Binding
Inhibition of GST-tagged recombinant PI5P4Kbeta (unknown origin) incubated for 1 hr in presence of DPPS and PI5P by ADP-Glo assay
24
Total Activities
24
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

Phosphatidylinositol 5-phosphate 4-kinase type-2 beta (CHEMBL5667)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Structure-Activity Relationship Study of (Z)-5-Methylenethiazolidin-4-one Derivatives as Potent and Selective Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors.
Manz TD, Sivakumaren SC, Ferguson FM, Zhang T, Yasgar A, Seo HS, Ficarro SB, Card JD, Shim H, Miduturu CV, Simeonov A, Shen M, Marto JA, Dhe-Paganon S, Hall MD, Cantley LC, Gray NS.
J Med Chem (2020) 63 : 4880 -4895
PubMed 32298120 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 4.86 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4436648 1 5.77
CHEMBL4447308 1 5.72
CHEMBL4454033 1 5.57
CHEMBL4519752 1 5.37
CHEMBL4577337 1 5.07
CHEMBL4455633 1 5.03
CHEMBL4467678 1 4.82
CHEMBL4456203 1 4.66
CHEMBL4573568 1 4.60
CHEMBL4436057 1 4.60
CHEMBL4475338 1 4.58
CHEMBL4559878 1 4.57
CHEMBL4441998 1 4.55
CHEMBL4440465 1 4.54
CHEMBL4567681 1 4.44
CHEMBL4449110 1 4.37
CHEMBL4454398 1 4.35
CHEMBL4527801 1 -
CHEMBL4459957 1 -
CHEMBL4538609 1 -
CHEMBL4443959 1 -
CHEMBL4458985 1 -
CHEMBL4436523 1 -
CHEMBL4540008 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4436648 IC50 = 1700.0 nM 5.77
CHEMBL4447308 IC50 = 1900.0 nM 5.72
CHEMBL4454033 IC50 = 2700.0 nM 5.57
CHEMBL4519752 IC50 = 4300.0 nM 5.37
CHEMBL4577337 IC50 = 8600.0 nM 5.07
CHEMBL4455633 IC50 = 9400.0 nM 5.03
CHEMBL4467678 IC50 = 15000.0 nM 4.82
CHEMBL4456203 IC50 = 22000.0 nM 4.66
CHEMBL4573568 IC50 = 25000.0 nM 4.60
CHEMBL4436057 IC50 = 25000.0 nM 4.60
CHEMBL4475338 IC50 = 26000.0 nM 4.58
CHEMBL4559878 IC50 = 27000.0 nM 4.57
CHEMBL4441998 IC50 = 28000.0 nM 4.55
CHEMBL4440465 IC50 = 29000.0 nM 4.54
CHEMBL4567681 IC50 = 36000.0 nM 4.44
CHEMBL4449110 IC50 = 43000.0 nM 4.37
CHEMBL4454398 IC50 = 45000.0 nM 4.35
CHEMBL4527801 IC50 > 50000.0 nM -
CHEMBL4459957 IC50 > 50000.0 nM -
CHEMBL4538609 IC50 > 50000.0 nM -
CHEMBL4443959 IC50 > 50000.0 nM -
CHEMBL4458985 IC50 > 50000.0 nM -
CHEMBL4436523 IC50 > 50000.0 nM -
CHEMBL4540008 IC50 > 50000.0 nM -