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Assay Detail

CHEMBL4345239

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Binding
Inhibition of N-terminal GST-tagged full length human PIKFYVE (1 to 2098 residues) using PI(3)P and Phosphatidylserine as substrate by ADP-Glo assay
1
Total Activities
1
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

1-phosphatidylinositol 3-phosphate 5-kinase (CHEMBL1938222)
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 1 7.40 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4446338 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4446338 IC50 = 40.1 nM 7.40