General Information of the Protein
Protein ID
PT02680
Protein Name
Phosphatidylinositol 3-kinase catalytic subunit type 3
Secondarily
Protein Name
Phosphatidylinositol 3-kinase p100 subunit
Phosphoinositide-3-kinase class 3
hVps34
Gene Name
PIK3C3
Secondarily
Gene Name
VPS34
Sequence
MGEAEKFHYIYSCDLDINVQLKIGSLEGKREQKSYKAVLEDPMLKFSGLYQETCSDLYVTCQVFAEGKPLALPVRTSYKAFSTRWNWNEWLKLPVKYPDLPRNAQVALTIWDVYGPGKAVPVGGTTVSLFGKYGMFRQGMHDLKVWPNVEADGSEPTKTPGRTSSTLSEDQMSRLAKLTKAHRQGHMVKVDWLDRLTFREIEMINESEKRSSNFMYLMVEFRCVKCDDKEYGIVYYEKDGDESSPILTSFELVKVPDPQMSMENLVESKHHKLARSLRSGPSDHDLKPNAATRDQLNIIVSYPPTKQLTYEEQDLVWKFRYYLTNQEKALTKFLKCVNWDLPQEAKQALELLGKWKPMDVEDSLELLSSHYTNPTVRRYAVARLRQADDEDLLMYLLQLVQALKYENFDDIKNGLEPTKKDSQSSVSENVSNSGINSAEIDSSQIITSPLPSVSSPPPASKTKEVPDGENLEQDLCTFLISRACKNSTLANYLYWYVIVECEDQDTQQRDPKTHEMYLNVMRRFSQALLKGDKSVRVMRSLLAAQQTFVDRLVHLMKAVQRESGNRKKKNERLQALLGDNEKMNLSDVELIPLPLEPQVKIRGIIPETATLFKSALMPAQLFFKTEDGGKYPVIFKHGDDLRQDQLILQIISLMDKLLRKENLDLKLTPYKVLATSTKHGFMQFIQSVPVAEVLDTEGSIQNFFRKYAPSENGPNGISAEVMDTYVKSCAGYCVITYILGVGDRHLDNLLLTKTGKLFHIDFGYILGRDPKPLPPPMKLNKEMVEGMGGTQSEQYQEFRKQCYTAFLHLRRYSNLILNLFSLMVDANIPDIALEPDKTVKKVQDKFRLDLSDEEAVHYMQSLIDESVHALFAAVVEQIHKFAQYWRK
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Transferase
Function
Catalytic subunit of the PI3K complex that mediates formation of phosphatidylinositol 3-phosphate; different complex forms are believed to play a role in multiple membrane trafficking pathways: PI3KC3-C1 is involved in initiation of autophagosomes and PI3KC3-C2 in maturation of autophagosomes and endocytosis (PubMed:14617358, PubMed:7628435, PubMed:33637724). As part of PI3KC3-C1, promotes endoplasmic reticulum membrane curvature formation prior to vesicle budding (PubMed:32690950). Involved in regulation of degradative endocytic trafficking and required for the abcission step in cytokinesis, probably in the context of PI3KC3-C2 (PubMed:20208530, PubMed:20643123). Involved in the transport of lysosomal enzyme precursors to lysosomes (By similarity). Required for transport from early to late endosomes (By similarity).
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Uniprot ID
Primary ID:
Q8NEB9

Secondarily ID:
Q15134
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Ensembl ID
ENSG00000078142
HGNC ID
HGNC:8974
Subcellular Location
Midbody
Late endosome
Cytoplasmic vesicle
Autophagosome
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000012 , Sf21
Compound ID Compound Name Compound Formula
CP0564578
2-[2-(2,4-difluorophenyl)-1,2,4-triazol-3-yl]-4,5-dihydro-[1]benzoxepino[5,4-d][1,3]thiazole-8-carboxamide
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C20H13F2N5O2S
 1
1
IC50 = 1.7 nM
   TI
   LI
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CP0550417
N-[6-[4-(2-chlorophenyl)-1,2,4-triazol-3-yl]isoquinolin-3-yl]-2-fluorocyclopropane-1-carboxamide
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C21H15ClFN5O
 1
1
IC50 = 3 nM
   TI
   LI
   LO
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CP0570964
N-[4-[(7R)-4-oxo-7-propan-2-yl-6,7-dihydro-5H-pyrazolo[1,5-a]pyrazin-2-yl]pyridin-2-yl]cyclopropanecarboxamide
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C18H21N5O2
 1
1
IC50 = 13 nM
   TI
   LI
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CP0576970
N-(4-imidazo[1,2-a]pyridin-7-ylpyridin-2-yl)cyclopropanecarboxamide
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C16H14N4O
 1
1
IC50 = 20 nM
   TI
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CP0543610
(R)-2-((R)-3-methylmorpholino)-6-(trifluoromethyl)-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one
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C12H15F3N4O2
 1
1
IC50 = 37 nM
   TI
   LI
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   TS
CP0571364
(R)-7-(tert-butyl)-2-((R)-3-methylmorpholino)-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one
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C15H24N4O2
 1
1
IC50 = 43 nM
   TI
   LI
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   TS
CP0571798
N-[5-methyl-4-[(7R)-4-oxo-7-propan-2-yl-6,7-dihydro-5H-pyrazolo[1,5-a]pyrazin-2-yl]pyridin-2-yl]cyclopropanecarboxamide
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C19H23N5O2
 1
1
IC50 = 48 nM
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CP0577592
N-[4-(benzimidazol-1-yl)pyridin-2-yl]cyclopropanecarboxamide
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C16H14N4O
 1
1
IC50 = 53 nM
   TI
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CP0569807
(R)-7-isopropyl-2-((R)-3-methylmorpholino)-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one
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C14H22N4O2
 1
1
IC50 = 78 nM
   TI
   LI
   LO
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CP0577891
(5aS,8aR)-2-((R)-3-methylmorpholino)-5,5a,6,7,8,8a-hexahydro-4H-cyclopenta[e]pyrazolo[1,5-a]pyrazin-4-one
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C14H20N4O2
 1
1
IC50 = 83 nM
   TI
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CP0580148
(R)-7'-cyclopropyl-2'-((R)-3-methylmorpholino)-7'H-spiro[cyclopropane-1,6'-pyrazolo[1,5-a]pyrazin]-4'(5'H)-one
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C16H22N4O2
 1
1
IC50 = 84 nM
   TI
   LI
   LO
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CP0577005
(S)-2-((R)-3-methylmorpholino)-7-(trifluoromethyl)-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one
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C12H15F3N4O2
 1
1
IC50 = 92 nM
   TI
   LI
   LO
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CP0564579
2-[2-(2,4-difluorophenyl)-1,2,4-triazol-3-yl]-4-methyl-4,5-dihydro-[1]benzoxepino[5,4-d][1,3]thiazole-8-carboxamide
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C21H15F2N5O2S
 1
1
IC50 = 130 nM
   TI
   LI
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CP0577004
N-[4-[(7R)-7-methyl-4-oxo-6,7-dihydro-5H-pyrazolo[1,5-a]pyrazin-2-yl]pyridin-2-yl]cyclopropanecarboxamide
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C16H17N5O2
 1
1
IC50 = 130 nM
   TI
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CP0550418
(S)-7-(2-hydroxypropan-2-yl)-2-((R)-3-methylmorpholino)-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one
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C14H22N4O3
 1
1
IC50 = 170 nM
   TI
   LI
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CP0578494
(6S,7R)-7-cyclopropyl-6-methyl-2-((R)-3-methylmorpholino)-6,7- dihydropyrazolo[1,5-a]pyrazin-4(5H)-one
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C15H22N4O2
 1
1
IC50 = 170 nM
   TI
   LI
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CP0571362
(7R)-7-cyclopropyl-2-[(3R)-3-methylmorpholin-4-yl]-6,7-dihydro-5H-pyrazolo[1,5-a]pyrazin-4-one
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C14H20N4O2
 1
1
IC50 = 240 nM
   TI
   LI
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CP0571363
(R)-7-cyclobutyl-2-((R)-3-methylmorpholino)-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one
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C15H22N4O2
 1
1
IC50 = 240 nM
   TI
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CP0576945
2-[[2-(cyclopropanecarbonylamino)pyridin-4-yl]amino]benzamide
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C16H16N4O2
 1
1
IC50 = 320 nM
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CP0578672
(R)-7-cyclopentyl-2-((R)-3-methylmorpholino)-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one
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C16H24N4O2
 1
1
IC50 = 350 nM
   TI
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CP0578822
N-[4-(1-methyl-2-oxopyridin-4-yl)pyridin-2-yl]cyclopropanecarboxamide
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C15H15N3O2
 1
1
IC50 = 470 nM
   TI
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CP0577609
(6S,7R)-6,7-dicyclopropyl-2-((R)-3-methylmorpholino)-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one
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C17H24N4O2
 1
1
IC50 = 560 nM
   TI
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CP0564576
(7R)-2-morpholin-4-yl-7-propan-2-yl-6,7-dihydro-5H-pyrazolo[1,5-a]pyrazin-4-one
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C13H20N4O2
 1
1
IC50 = 710 nM
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CP0564577
(R)-7-cyclopropyl-6,6-dimethyl-2-((R)-3-methylmorpholino)-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one
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C16H24N4O2
 1
1
IC50 = 1400 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0102496
4-(cyclopropylmethyl)-5-[2-(pyridin-4-ylamino)pyrimidin-4-yl]pyrimidin-2-amine
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C17H17N7
 1
1 IC50 = 0.018 nM
CP0115688
(8S)-9-[(5-chloropyridin-3-yl)methyl]-2-[(3R)-3-methylmorpholin-4-yl]-8-(trifluoromethyl)-7,8-dihydro-6H-pyrimido[1,2-a]pyrimidin-4-one
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C19H21ClF3N5O2
 1
1 IC50 = 1.2 nM
CP0058485
1-[[4-(cyclopropylmethyl)-5-[2-(pyridin-4-ylamino)pyrimidin-4-yl]pyrimidin-2-yl]amino]-2-methylpropan-2-ol
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C21H25N7O
 1
1 IC50 = 15 nM
CP0058491
4-(cyclopropylmethyl)-N-methyl-5-[2-(pyridin-4-ylamino)pyrimidin-4-yl]pyrimidin-2-amine
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C18H19N7
 1
1 IC50 = 37 nM
CP0174724
4-[4-(cyclopropylmethyl)pyrimidin-5-yl]-N-pyridin-4-ylpyrimidin-2-amine
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C17H16N6
 1
1 IC50 = 210 nM
CP0079006
4-(cyclopropylmethyl)-N-(oxan-4-yl)-5-[2-(pyridin-4-ylamino)pyrimidin-4-yl]pyrimidin-2-amine
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C22H25N7O
 1
1 IC50 = 240 nM