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Target
Phosphatidylinositol 3-kinase catalytic subunit type 3
Ligand
BDBM295074
Substrate
n/a
Meas. Tech.
Kinase Glo Luminescent Kinase Assay (Kglo) for PI 3-Kinase Alpha (A), PI 3-Kinase Beta (B), Vps34 (C), PI 4-Kinase Beta (D)
pH
7.5±n/a
Temperature
298.15±n/a K
IC50
>10000±n/a nM
Comments
extracted
Citation
 Bellenie, BR; Bloomfield, GC; Bruce, I; Culshaw, AJ; Hall, EC; Hollingworth, GJ; Neef, J; Spendiff, M; Watson, SJ Amino pyridine derivatives as phosphatidylinositol 3-kinase inhibitors US Patent  US10112926 Publication Date 10/30/2018 
Target
Name:
Phosphatidylinositol 3-kinase catalytic subunit type 3
Synonyms:
BC033004 | PI3K type 3 | PIK3C3 | PK3C3_HUMAN | 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 | VPS34 | 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:
MGEAEKFHYIYSCDLDINVQLKIGSLEGKREQKSYKAVLEDPMLKFSGLYQETCSDLYVTCQVFAEGKPLALPVRTSYKAFSTRWNWNEWLKLPVKYPDLPRNAQVALTIWDVYGPGKAVPVGGTTVSLFGKYGMFRQGMHDLKVWPNVEADGSEPTKTPGRTSSTLSEDQMSRLAKLTKAHRQGHMVKVDWLDRLTFREIEMINESEKRSSNFMYLMVEFRCVKCDDKEYGIVYYEKDGDESSPILTSFELVKVPDPQMSMENLVESKHHKLARSLRSGPSDHDLKPNAATRDQLNIIVSYPPTKQLTYEEQDLVWKFRYYLTNQEKALTKFLKCVNWDLPQEAKQALELLGKWKPMDVEDSLELLSSHYTNPTVRRYAVARLRQADDEDLLMYLLQLVQALKYENFDDIKNGLEPTKKDSQSSVSENVSNSGINSAEIDSSQIITSPLPSVSSPPPASKTKEVPDGENLEQDLCTFLISRACKNSTLANYLYWYVIVECEDQDTQQRDPKTHEMYLNVMRRFSQALLKGDKSVRVMRSLLAAQQTFVDRLVHLMKAVQRESGNRKKKNERLQALLGDNEKMNLSDVELIPLPLEPQVKIRGIIPETATLFKSALMPAQLFFKTEDGGKYPVIFKHGDDLRQDQLILQIISLMDKLLRKENLDLKLTPYKVLATSTKHGFMQFIQSVPVAEVLDTEGSIQNFFRKYAPSENGPNGISAEVMDTYVKSCAGYCVITYILGVGDRHLDNLLLTKTGKLFHIDFGYILGRDPKPLPPPMKLNKEMVEGMGGTQSEQYQEFRKQCYTAFLHLRRYSNLILNLFSLMVDANIPDIALEPDKTVKKVQDKFRLDLSDEEAVHYMQSLIDESVHALFAAVVEQIHKFAQYWRK
  
Inhibitor
Name:
BDBM295074
Synonyms:
5-(5-((2,2- dimethylpyrrolidin-1- yl)sulfonyl)-2- methylphenyl)-3-(3- methylisoxazol-5- yl)pyridin-2-amine trifluoroacetic acid salt | US10112926, Example 19.9
Type:
Small organic molecule
Emp. Form.:
C22H26N4O3S
Mol. Mass.:
426.532
SMILES:
Cc1cc(on1)-c1cc(cnc1N)-c1cc(ccc1C)S(=O)(=O)N1CCCC1(C)C
Structure:
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