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Assay Detail

CHEMBL4345229

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

Binding
Inhibition of PI5P4Kbeta (unknown origin) incubated for 15 mins in presence of ATP by ADP-Glo assay
17
Total Activities
17
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

Structure-Activity Relationship Study of Covalent Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors.
Manz TD, Sivakumaren SC, Yasgar A, Hall MD, Davis MI, Seo HS, Card JD, Ficarro SB, Shim H, Marto JA, Dhe-Paganon S, Sasaki AT, Boxer MB, Simeonov A, Cantley LC, Shen M, Zhang T, Ferguson FM, Gray NS.
ACS Med Chem Lett (2020) 11 : 346 -352
PubMed 32184968 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 4.85 5.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2104863 IMANIXIL 2.0 1 5.42
CHEMBL4446338 1 5.23
CHEMBL4461694 1 5.21
CHEMBL4472811 1 5.20
CHEMBL4533123 1 5.05
CHEMBL4439287 1 5.00
CHEMBL4449493 1 5.00
CHEMBL4571099 1 4.96
CHEMBL4454740 1 4.80
CHEMBL4518868 1 4.69
CHEMBL4537067 1 4.61
CHEMBL4550598 1 4.53
CHEMBL4563077 1 4.52
CHEMBL4517979 1 4.50
CHEMBL4464636 1 4.47
CHEMBL4572941 1 4.45
CHEMBL4520888 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2104863 IMANIXIL IC50 = 3800.0 nM 5.42
CHEMBL4446338 IC50 = 5900.0 nM 5.23
CHEMBL4461694 IC50 = 6200.0 nM 5.21
CHEMBL4472811 IC50 = 6300.0 nM 5.20
CHEMBL4533123 IC50 = 8900.0 nM 5.05
CHEMBL4439287 IC50 = 9900.0 nM 5.00
CHEMBL4449493 IC50 = 10100.0 nM 5.00
CHEMBL4571099 IC50 = 10900.0 nM 4.96
CHEMBL4454740 IC50 = 15800.0 nM 4.80
CHEMBL4518868 IC50 = 20500.0 nM 4.69
CHEMBL4537067 IC50 = 24500.0 nM 4.61
CHEMBL4550598 IC50 = 29800.0 nM 4.53
CHEMBL4563077 IC50 = 30400.0 nM 4.52
CHEMBL4517979 IC50 = 31800.0 nM 4.50
CHEMBL4464636 IC50 = 33600.0 nM 4.47
CHEMBL4572941 IC50 = 35600.0 nM 4.45
CHEMBL4520888 IC50 - -