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Target
Phosphatidylinositol 3-kinase catalytic subunit type 3
Ligand
BDBM535569
Substrate
n/a
Meas. Tech.
PI3KC3 (hVPS34) Kinase Assay
IC50
2100±n/a nM
Citation
 Stocking, EM; Wrasidlo, WJ Morpholine derivates as inhibitors of Vps34 US Patent  US11236079 Publication Date 2/1/2022 
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:
BDBM535569
Synonyms:
(R)-5-(3-morpholino-5- ((tetrahydrofuran-3- yl)sulfonyl)phenyl)-4- (trifluoromethyl)thiazol-2-amine | US11236079, Example 2
Type:
Small organic molecule
Emp. Form.:
C18H20F3N3O4S2
Mol. Mass.:
463.494
SMILES:
Nc1nc(c(s1)-c1cc(cc(c1)S(=O)(=O)[C@@H]1CCOC1)N1CCOCC1)C(F)(F)F |r|
Structure:
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