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TargetPhosphatidylinositol 3-kinase catalytic subunit type 3
LigandBDBM50396820
Substrate/Competitorn/a
Meas. Tech.ChEMBL_861943
IC50>10000±n/a nM
Citation Norman MHAndrews KLBo YYBooker SKCaenepeel SCee VJD'Angelo NDFreeman DJHerberich BJHong FTJackson CLJiang JLanman BALiu LMcCarter JDMullady ELNishimura NPettus LHReed ABMiguel TSSmith ALStec MMTadesse STasker AAidasani DZhu XSubramanian RTamayo NAWang LWhittington DAWu BWu TWurz RPYang KZalameda LZhang NHughes PE Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. J Med Chem 55:7796-816 (2012) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Phosphatidylinositol 3-kinase catalytic subunit type 3
Name:Phosphatidylinositol 3-kinase catalytic subunit type 3
Synonyms:BC033004 | PI3K type 3 | Phosphatidylinositol 3-kinase catalytic subunit type 3 (PIK3C3) | Phosphatidylinositol 3-kinase p100 subunit | Phosphoinositide 3-Kinase (PI3K), Vps34 | Phosphoinositide-3-kinase class 3 | PtdIns-3-kinase type 3 | hVPS34
Type:Enzyme
Mol. Mass.:101551.30
Organism:Homo sapiens (Human)
Description:Recombinant human Vps34 protein was expressed as monomeric GST-fusion and purified.
Residue:887
Sequence:
MGEAEKFHYIYSCDLDINVQLKIGSLEGKREQKSYKAVLEDPMLKFSGLYQETCSDLYVT
CQVFAEGKPLALPVRTSYKAFSTRWNWNEWLKLPVKYPDLPRNAQVALTIWDVYGPGKAV
PVGGTTVSLFGKYGMFRQGMHDLKVWPNVEADGSEPTKTPGRTSSTLSEDQMSRLAKLTK
AHRQGHMVKVDWLDRLTFREIEMINESEKRSSNFMYLMVEFRCVKCDDKEYGIVYYEKDG
DESSPILTSFELVKVPDPQMSMENLVESKHHKLARSLRSGPSDHDLKPNAATRDQLNIIV
SYPPTKQLTYEEQDLVWKFRYYLTNQEKALTKFLKCVNWDLPQEAKQALELLGKWKPMDV
EDSLELLSSHYTNPTVRRYAVARLRQADDEDLLMYLLQLVQALKYENFDDIKNGLEPTKK
DSQSSVSENVSNSGINSAEIDSSQIITSPLPSVSSPPPASKTKEVPDGENLEQDLCTFLI
SRACKNSTLANYLYWYVIVECEDQDTQQRDPKTHEMYLNVMRRFSQALLKGDKSVRVMRS
LLAAQQTFVDRLVHLMKAVQRESGNRKKKNERLQALLGDNEKMNLSDVELIPLPLEPQVK
IRGIIPETATLFKSALMPAQLFFKTEDGGKYPVIFKHGDDLRQDQLILQIISLMDKLLRK
ENLDLKLTPYKVLATSTKHGFMQFIQSVPVAEVLDTEGSIQNFFRKYAPSENGPNGISAE
VMDTYVKSCAGYCVITYILGVGDRHLDNLLLTKTGKLFHIDFGYILGRDPKPLPPPMKLN
KEMVEGMGGTQSEQYQEFRKQCYTAFLHLRRYSNLILNLFSLMVDANIPDIALEPDKTVK
KVQDKFRLDLSDEEAVHYMQSLIDESVHALFAAVVEQIHKFAQYWRK
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  Blast E-value cutoff:
BDBM50396820
n/a
NameBDBM50396820
Synonyms:CHEMBL2170088 | US8772480, 272
TypeSmall organic molecule
Emp. Form.C23H30FN9O3S
Mol. Mass.531.606
SMILESCOc1ncc(Nc2ncc(cc2-c2nc(C)nc(N)n2)[C@@H](C)N2CCN(C[C@@H]2C)S(C)(=O)=O)cc1F |r|
Structure
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