General Information of the Protein
Protein ID
PT06232
Protein Name
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform
Secondarily
Protein Name
Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit beta
Serine/threonine protein kinase PIK3CB
Gene Name
PIK3CB
Sequence
MCFRSIMPPAMADTLDIWAVDSQIASDGSISVDFLLPTGIYIQLEVPREATISYIKQMLWKQVHNYPMFNLLMDIDSYMFACVNQTAVYEELEDETRRLCDVRPFLPVLKLVTRSCDPAEKLDSKIGVLIGKGLHEFDALKDPEVNEFRRKMRKFSEDKIQSLVGLSWIDWLKHTYPPEHEPSVLENLEDKLYGGKLVVAVHFENSQDVFSFQVSPNLNPIKINELAIQKRLTIRGKEEEASPCDYVLQVSGRVEYVFGDHPLIQFQYIRNCVMNRTLPHFILVECCKIKKMYEQEMIAIEAAINRNSSSLPLPLPPKKTRVISHVWGNNNPFQIVLVKGNKLNTEETVKVHVRAGLFHGTELLCKTVVSSEISGKNDHIWNEQLEFDINICDLPRMARLCFAVYAVLDKVKTKKSTKTINPSKYQTIRKAGKVHYPVAWVNTMVFDFKGQLRSGDVILHSWSSFPDELEEMLNPMGTVQTNPYAENATALHIKFPENKKQPYYYPPFDKIIEKAAEIASGDSANVSSRGGKKFLAVLKEILDRDPLSQLCENEMDLIWTLRQDCRENFPQSLPKLLLSIKWNKLEDVAQLQALLQIWPKLPPREALELLDFNYPDQYVREYAVGCLRQMSDEELSQYLLQLVQVLKYEPFLDCALSRFLLERALDNRRIGQFLFWHLRSEVHTPAVSIQFGVILEAYCRGSVGHMKVLSKQVEALNKLKTLNSLIKLNAMKLNRAKGKEAMHTCLKQSAYREALSDLQSPLNPCVILSELYVEKCRYMDSKMKPLWLVYSNRAFGEDAVGVIFKNGDDLRQDMLTLQMLRLMDLLWKEAGLDLRMLPYGCLATGDRSGLIEVVSTSETIADIQLNSSNVAATAAFNKDALLNWLKEYNSGDDLDRAIEEFTLSCAGYCVASYVLGIGDRHSDNIMVKKTGQLFHIDFGHILGNFKSKFGIKRERVPFILTYDFIHVIQQGKTGNTEKFGRFRQCCEDAYLILRRHGNLFITLFALMLTAGLPELTSVKDIQYLKDSLALGKSEEEALKQFKQKFDEALRESWTTKVNWMAHTVRKDYRS
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Organism
Rattus norvegicus, Rat
Protein Classification
Enzyme
>
Transferase
Function
Phosphoinositide-3-kinase (PI3K) phosphorylates phosphatidylinositol (PI) derivatives at position 3 of the inositol ring to produce 3-phosphoinositides. Uses ATP and PtdIns(4,5)P2 (phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role by recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in cell growth, survival, proliferation, motility and morphology. Involved in the activation of AKT1 upon stimulation by G-protein coupled receptors (GPCRs) ligands such as CXCL12, sphingosine 1-phosphate, and lysophosphatidic acid. May also act downstream receptor tyrosine kinases. Required in different signaling pathways for stable platelet adhesion and aggregation. Plays a role in platelet activation signaling triggered by GPCRs, alpha-IIb/beta-3 integrins (ITGA2B/ ITGB3) and ITAM (immunoreceptor tyrosine-based activation motif)-bearing receptors such as GP6. Regulates the strength of adhesion of ITGA2B/ ITGB3 activated receptors necessary for the cellular transmission of contractile forces. Required for platelet aggregation induced by F2 (thrombin) and thromboxane A2 (TXA2). Has a role in cell survival. May have a role in cell migration. Involved in the early stage of autophagosome formation. Modulates the intracellular level of PtdIns3P (phosphatidylinositol 3-phosphate) and activates PIK3C3 kinase activity. May act as a scaffold, independently of its lipid kinase activity to positively regulate autophagy. May have a role in insulin signaling as scaffolding protein in which the lipid kinase activity is not required. May have a kinase-independent function in regulating cell proliferation and in clathrin-mediated endocytosis. Mediator of oncogenic signal in cell lines lacking PTEN. The lipid kinase activity is necessary for its role in oncogenic transformation. Required for the growth of ERBB2 and RAS driven tumors. Has also a protein kinase activity showing autophosphorylation.
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Uniprot ID
Q9Z1L0
Ensembl ID
ENSG00000051382
Subcellular Location
Cytoplasm
Nucleus
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: CL000019 , Rat1
Compound ID Compound Name Compound Formula
CP0001158
US9284315, BEZ-235
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C30H23N5O
 1
1
IC50 = 10 nM
   TI
   LI
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CP0579027
(4S,5S)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-5-(hydroxymethyl)-4-methyl-1,3-oxazolidin-2-one
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C18H20F3N7O4
 1
1
IC50 = 36 nM
   TI
   LI
   LO
   TS
CP0577015
(3aS,6aS)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-3a,4,6,6a-tetrahydrofuro[3,4-d][1,3]oxazol-2-one
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C18H18F3N7O4
 1
1
IC50 = 37 nM
   TI
   LI
   LO
   TS
CP0576744
(4S)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-4-methyl-1,3-oxazolidin-2-one
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C17H18F3N7O3
 1
1
IC50 = 65 nM
   TI
   LI
   LO
   TS
CP0576748
(4S,5R)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-4-(hydroxymethyl)-5-methyl-1,3-oxazolidin-2-one
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C18H20F3N7O4
 1
1
IC50 = 65 nM
   TI
   LI
   LO
   TS
CP0545313
(4S)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-4-(hydroxymethyl)-1,3-oxazolidin-2-one
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C17H18F3N7O4
 1
1
IC50 = 96 nM
   TI
   LI
   LO
   TS
CP0577684
5-[6-(7-methoxy-2,3-dihydro-1,4-benzoxazin-4-yl)-2-morpholin-4-ylpyrimidin-4-yl]pyrimidin-2-amine
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C21H23N7O3
 1
1
IC50 = 101 nM
   TI
   LI
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   TS
CP0125999
2-amino-5-(2,6-dimorpholin-4-ylpyrimidin-4-yl)-1H-pyrimidin-6-one
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C16H21N7O3
 1
1
IC50 = 104 nM
   TI
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CP0545315
(4S,5R)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-5-(hydroxymethyl)-4-methyl-1,3-oxazolidin-2-one
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C18H20F3N7O4
 1
1
IC50 = 109 nM
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   LI
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CP0576745
(5R)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one
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C17H18F3N7O4
 1
1
IC50 = 124 nM
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CP0007893
4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpiperazin-1-yl)methyl]thieno[3,2-d]pyrimidin-4-yl]morpholine
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C23H27N7O3S2
 1
1
IC50 = 146 nM
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CP0548467
(4S,5S)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-4-(hydroxymethyl)-5-methyl-1,3-oxazolidin-2-one
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C18H20F3N7O4
 1
1
IC50 = 147 nM
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CP0546964
1-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]pyrrolidin-2-one
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C18H19F3N6O2
 1
1
IC50 = 157 nM
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CP0576741
(5S)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one
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C17H18F3N7O4
 1
1
IC50 = 157 nM
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   LI
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CP0576740
3-[6-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-2-morpholin-4-ylpyrimidin-4-yl]-1,3-oxazolidin-2-one
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C16H16F3N7O3
 1
1
IC50 = 184 nM
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CP0188346
5-(2,6-dimorpholin-4-ylpyrimidin-4-yl)-4-(trifluoromethyl)pyrimidin-2-amine
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C17H20F3N7O2
 1
1
IC50 = 191 nM
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CP0579376
3-[6-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-2-morpholin-4-ylpyrimidin-4-yl]-1,3-oxazinan-2-one
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C17H18F3N7O3
 1
1
IC50 = 203 nM
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CP0548095
2-[(4S,5R)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-5-methyl-2-oxo-1,3-oxazolidin-4-yl]acetonitrile
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C19H19F3N8O3
 1
1
IC50 = 237 nM
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CP0543348
(4R)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-4-(hydroxymethyl)-1,3-oxazolidin-2-one
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C17H18F3N7O4
 1
1
IC50 = 264 nM
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CP0543347
(4S)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-4-(hydroxymethyl)-5,5-dimethyl-1,3-oxazolidin-2-one
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C19H22F3N7O4
 1
1
IC50 = 278 nM
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CP0573794
(4S)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-4-[(1S)-1-hydroxyethyl]-1,3-oxazolidin-2-one
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C18H20F3N7O4
 1
1
IC50 = 285 nM
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CP0568134
(4S)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-4-(hydroxymethyl)-4-methyl-1,3-oxazolidin-2-one
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C18H20F3N7O4
 1
1
IC50 = 331 nM
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CP0568135
1-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]imidazolidin-2-one
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C17H18F3N7O2
 1
1
IC50 = 391 nM
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   LI
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CP0577685
3-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]-1,3-oxazolidin-2-one
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C17H17F3N6O3
 1
1
IC50 = 443 nM
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   LI
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CP0001930
5-(2,6-dimorpholin-4-ylpyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine
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C18H21F3N6O2
 1
1
IC50 = 523 nM
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CP0576738
2-amino-5-[6-[2-(2-hydroxyethyl)morpholin-4-yl]-2-morpholin-4-ylpyrimidin-4-yl]pyridine-4-carbonitrile
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C20H25N7O3
 1
1
IC50 = 811 nM
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CP0116130
N-[4-methyl-5-(2-propan-2-yl-1,3-thiazol-4-yl)-1,3-thiazol-2-yl]acetamide
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C12H15N3OS2
 1
1
IC50 = 950 nM
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CP0173899
(2S,4S)-1-N-[5-(2-tert-butyl-1,3-thiazol-4-yl)-4-methyl-1,3-thiazol-2-yl]-4-hydroxypyrrolidine-1,2-dicarboxamide
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C17H23N5O3S2
 1
1
IC50 = 1300 nM
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CP0574438
1-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]-1,3-dimethylurea
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C17H20F3N7O2
 1
1
IC50 = 1405 nM
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CP0552713
1-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]piperidin-2-one
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C19H21F3N6O2
 1
1
IC50 = 1540 nM
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CP0579375
1-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]-3-phenylimidazolidin-2-one
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C23H22F3N7O2
 1
1
IC50 = 1580 nM
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CP0545312
(4S)-3-[4-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-6-morpholin-4-ylpyrimidin-2-yl]-4-methyl-1,3-oxazolidin-2-one
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C18H19F3N6O3
 1
1
IC50 = 1979 nM
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CP0008405
(2S)-1-N-[4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C19H22F3N5O2S
 1
1
IC50 = 2200 nM
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CP0576737
5-(2,6-dimorpholin-4-ylpyridin-4-yl)-4-(trifluoromethyl)pyridin-2-amine
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C19H22F3N5O2
 1
1
IC50 = 2485 nM
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CP0109038
(2S)-1-N-[5-(2-tert-butylpyrimidin-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C18H24N6O2S
 1
1
IC50 = 3100 nM
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CP0574436
5-[2-morpholin-4-yl-6-(2-phenylmorpholin-4-yl)pyrimidin-4-yl]-4-(trifluoromethyl)pyridin-2-amine
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C24H25F3N6O2
 1
1
IC50 = 4035 nM
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CP0054686
(2S,4R)-1-N-[5-(2-tert-butyl-1,3-thiazol-4-yl)-4-methyl-1,3-thiazol-2-yl]-4-hydroxypyrrolidine-1,2-dicarboxamide
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C17H23N5O3S2
 1
1
IC50 = 4500 nM
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CP0041061
(2S)-1-N-[5-(2-tert-butyl-1,3-thiazol-4-yl)-4-methyl-1,3-thiazol-2-yl]-2-methylpyrrolidine-1,2-dicarboxamide
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C18H25N5O2S2
 1
1
IC50 = 5600 nM
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CP0041055
(2S,4R)-1-N-[5-(2-tert-butyl-1,3-thiazol-4-yl)-4-methyl-1,3-thiazol-2-yl]-4-fluoropyrrolidine-1,2-dicarboxamide
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C17H22FN5O2S2
 1
1
IC50 = 5800 nM
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CP0579116
[(3R)-4-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]morpholin-3-yl]methanol
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C19H23F3N6O3
 1
1
IC50 = 5800 nM
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CP0568133
1-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]-1-(2-hydroxyethyl)-3-methylurea
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C18H22F3N7O3
 1
1
IC50 = 5865 nM
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CP0101472
(2S,3S)-1-N-[5-(2-tert-butyl-1,3-thiazol-4-yl)-4-methyl-1,3-thiazol-2-yl]-3-hydroxypyrrolidine-1,2-dicarboxamide
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C17H23N5O3S2
 1
1
IC50 = 6200 nM
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CP0054680
(2S,3S)-1-N-[5-(2-tert-butyl-1,3-thiazol-4-yl)-4-methyl-1,3-thiazol-2-yl]-3-methylpyrrolidine-1,2-dicarboxamide
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C18H25N5O2S2
 1
1
IC50 = 8100 nM
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CP0552712
5-[6-(1,1-dioxo-1,4-thiazinan-4-yl)-2-morpholin-4-ylpyrimidin-4-yl]-4-(trifluoromethyl)pyridin-2-amine
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C18H21F3N6O3S
 1
1
IC50 = 8220 nM
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CP0574440
2-[[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]amino]-3-phenylpropan-1-ol
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C23H25F3N6O2
 1
1
IC50 = 9290 nM
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CP0041010
(2S,4S)-1-N-[5-(2-tert-butyl-1,3-thiazol-4-yl)-4-methyl-1,3-thiazol-2-yl]-4-(dimethylamino)pyrrolidine-1,2-dicarboxamide
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C19H28N6O2S2
 1
1
IC50 > 10000 nM
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CP0041058
(2S,4R)-1-N-[5-(2-tert-butyl-1,3-thiazol-4-yl)-4-methyl-1,3-thiazol-2-yl]-4-(dimethylamino)pyrrolidine-1,2-dicarboxamide
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C19H28N6O2S2
 1
1
IC50 > 10000 nM
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CP0041059
(2S)-1-N-[5-(3-fluoro-4-methylsulfonylphenyl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C17H19FN4O4S2
 1
1
IC50 > 10000 nM
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CP0041060
(2S)-1-N-[5-[2-[(dimethylamino)methyl]-1,3-thiazol-4-yl]-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C16H22N6O2S2
 1
1
IC50 > 10000 nM
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CP0041063
(2S)-2-methyl-1-N-[4-methyl-5-[2-[1-(trifluoromethyl)cyclopropyl]-1,3-thiazol-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C18H20F3N5O2S2
 1
1
IC50 > 10000 nM
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CP0054682
(2S)-1-N-[5-(2-tert-butyl-1,3-thiazol-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C17H23N5O2S2
 1
1
IC50 > 10000 nM
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CP0054683
(2S)-1-N-[4-methyl-5-(2-propan-2-yl-1,3-thiazol-4-yl)-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C16H21N5O2S2
 1
1
IC50 > 10000 nM
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CP0055475
(2S)-1-N-[4-methyl-5-(2-pentan-3-yl-1,3-thiazol-4-yl)-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C18H25N5O2S2
 1
1
IC50 > 10000 nM
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CP0059185
(2S)-1-N-[5-(2-cyclobutyl-1,3-thiazol-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C17H21N5O2S2
 1
1
IC50 > 10000 nM
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CP0095468
(2S)-1-N-[4-methyl-5-[2-(1-methylcyclopropyl)-1,3-thiazol-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C17H21N5O2S2
 1
1
IC50 > 10000 nM
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CP0106216
(2S)-1-N-[5-[2-(2-fluorophenyl)-1,3-thiazol-4-yl]-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C19H18FN5O2S2
 1
1
IC50 > 10000 nM
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CP0106217
(2S)-1-N-[4-methyl-5-[2-[1-(trifluoromethyl)cyclopropyl]-1,3-thiazol-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C17H18F3N5O2S2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0116148
(2S,3R)-3-methyl-1-N-[4-methyl-5-[2-[1-(trifluoromethyl)cyclopropyl]-1,3-thiazol-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C18H20F3N5O2S2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0116166
(2S,3R)-3-hydroxy-1-N-[4-methyl-5-[2-[1-(trifluoromethyl)cyclopropyl]-1,3-thiazol-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C17H18F3N5O3S2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0127180
(2S,4R)-4-(dimethylamino)-1-N-[4-methyl-5-[2-(1-methylcyclopropyl)-1,3-thiazol-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C19H26N6O2S2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0186275
(2S)-1-N-[4-methyl-5-(2-pyridin-3-yl-1,3-thiazol-4-yl)-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C18H18N6O2S2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0186276
(1S,5R)-2-N-[5-(2-tert-butyl-1,3-thiazol-4-yl)-4-methyl-1,3-thiazol-2-yl]-2-azabicyclo[3.1.0]hexane-1,2-dicarboxamide
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C18H23N5O2S2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0235671
(2S)-1-N-[5-[2-(dimethylamino)-1,3-thiazol-4-yl]-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C15H20N6O2S2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0357025
(2S)-1-N-[5-[2-(cyclopropylmethyl)-1,3-thiazol-4-yl]-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C17H21N5O2S2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0545314
(4S,5R)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-5-methyl-4-[(1-oxo-1,4-thiazinan-4-yl)methyl]-1,3-oxazolidin-2-one
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C22H27F3N8O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT01033 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform Homo sapiens, Human