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Assay Detail

CHEMBL3603390

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

Binding
Inhibition of N-terminal GST-tagged human full length recombinant PI4K3beta expressed in Sf9 cells using D-myo-phosphatidylinositol substrate and ATP incubated for 45 mins by ADP-Glo kinase Assay
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Phosphatidylinositol 4-kinase beta (CHEMBL3268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent, selective small molecule inhibitors of α-subtype of type III phosphatidylinositol-4-kinase (PI4KIIIα).
Raubo P, Andrews DM, McKelvie JC, Robb GR, Smith JM, Swarbrick ME, Waring MJ.
Bioorg Med Chem Lett (2015) 25 : 3189 -3193
PubMed 26087940 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 5.88 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3600785 1 6.60
CHEMBL3600782 1 6.50
CHEMBL3600778 1 6.50
CHEMBL3600777 1 6.50
CHEMBL3600685 1 6.50
CHEMBL3600781 1 6.40
CHEMBL97245 1 6.30
CHEMBL3600691 1 6.30
CHEMBL3600694 1 6.30
CHEMBL3600784 1 6.20
CHEMBL3600767 1 6.20
CHEMBL3600701 1 6.20
CHEMBL3600683 1 6.20
CHEMBL3600684 1 6.20
CHEMBL3600776 1 6.10
CHEMBL3600690 1 6.10
CHEMBL3600769 1 6.00
CHEMBL1645107 1 6.00
CHEMBL1645105 1 6.00
CHEMBL3600695 1 6.00
CHEMBL3600688 1 6.00
CHEMBL3600698 1 6.00
CHEMBL3600687 1 5.90
CHEMBL3600770 1 5.90
CHEMBL3600768 1 5.90
CHEMBL3600779 1 5.80
CHEMBL3600771 1 5.80
CHEMBL3600692 1 5.80
CHEMBL3600689 1 5.80
CHEMBL3600772 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3600785 IC50 = 251.19 nM 6.60
CHEMBL3600782 IC50 = 316.23 nM 6.50
CHEMBL3600778 IC50 = 316.23 nM 6.50
CHEMBL3600777 IC50 = 316.23 nM 6.50
CHEMBL3600685 IC50 = 316.23 nM 6.50
CHEMBL3600781 IC50 = 398.11 nM 6.40
CHEMBL97245 IC50 = 501.19 nM 6.30
CHEMBL3600691 IC50 = 501.19 nM 6.30
CHEMBL3600694 IC50 = 501.19 nM 6.30
CHEMBL3600683 IC50 = 630.96 nM 6.20
CHEMBL3600684 IC50 = 630.96 nM 6.20
CHEMBL3600701 IC50 = 630.96 nM 6.20
CHEMBL3600767 IC50 = 630.96 nM 6.20
CHEMBL3600784 IC50 = 630.96 nM 6.20
CHEMBL3600690 IC50 = 794.33 nM 6.10
CHEMBL3600776 IC50 = 794.33 nM 6.10
CHEMBL3600769 IC50 = 1000.0 nM 6.00
CHEMBL1645107 IC50 = 1000.0 nM 6.00
CHEMBL1645105 IC50 = 1000.0 nM 6.00
CHEMBL3600695 IC50 = 1000.0 nM 6.00
CHEMBL3600688 IC50 = 1000.0 nM 6.00
CHEMBL3600698 IC50 = 1000.0 nM 6.00
CHEMBL3600687 IC50 = 1258.93 nM 5.90
CHEMBL3600768 IC50 = 1258.93 nM 5.90
CHEMBL3600770 IC50 = 1258.93 nM 5.90
CHEMBL3600779 IC50 = 1584.89 nM 5.80
CHEMBL3600771 IC50 = 1584.89 nM 5.80
CHEMBL3600692 IC50 = 1584.89 nM 5.80
CHEMBL3600689 IC50 = 1584.89 nM 5.80
CHEMBL3600772 IC50 = 1995.26 nM 5.70
CHEMBL3600774 IC50 = 1995.26 nM 5.70
CHEMBL3600775 IC50 = 1995.26 nM 5.70
CHEMBL3600783 IC50 = 2511.89 nM 5.60
CHEMBL3600700 IC50 = 2511.89 nM 5.60
CHEMBL3600696 IC50 = 2511.89 nM 5.60
CHEMBL3600773 IC50 = 2511.89 nM 5.60
CHEMBL3600686 IC50 = 3162.28 nM 5.50
CHEMBL3600766 IC50 = 3981.07 nM 5.40
CHEMBL3600699 IC50 = 3981.07 nM 5.40
CHEMBL3600765 IC50 = 6309.57 nM 5.20
CHEMBL3600702 IC50 = 6309.57 nM 5.20
CHEMBL3600693 IC50 = 7943.28 nM 5.10
CHEMBL3600780 IC50 = 10000.0 nM 5.00
CHEMBL3600697 IC50 = 39810.72 nM 4.40