General Information of the Protein
Protein ID
PT03071
Protein Name
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
Secondarily
Protein Name
Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit gamma
Phosphoinositide-3-kinase catalytic gamma polypeptide
Serine/threonine protein kinase PIK3CG
p120-PI3K
Gene Name
PIK3CG
Secondarily
Gene Name
Pi3kg1
Sequence
MELENYEQPVVLREDNLRRRRRMKPRSAAGSLSSMELIPIEFVLPTSQRISKTPETALLHVAGHGNVEQMKAQVWLRALETSVAAEFYHRLGPDQFLLLYQKKGQWYEIYDRYQVVQTLDCLHYWKLMHKSPGQIHVVQRHVPSEETLAFQKQLTSLIGYDVTDISNVHDDELEFTRRRLVTPRMAEVAGRDAKLYAMHPWVTSKPLPDYLSKKIANNCIFIVIHRGTTSQTIKVSADDTPGTILQSFFTKMAKKKSLMNISESQSEQDFVLRVCGRDEYLVGETPLKNFQWVRQCLKNGDEIHLVLDTPPDPALDEVRKEEWPLVDDCTGVTGYHEQLTIHGKDHESVFTVSLWDCDRKFRVKIRGIDIPVLPRNTDLTVFVEANIQHGQQVLCQRRTSPKPFAEEVLWNVWLEFGIKIKDLPKGALLNLQIYCCKTPSLSSKASAETPGSESKGKAQLLYYVNLLLIDHRFLLRHGDYVLHMWQISGKAEEQGSFNADKLTSATNPDKENSMSISILLDNYCHPIALPKHRPTPDPEGDRVRAEMPNQLRKQLEAIIATDPLNPLTAEDKELLWHFRYESLKHPKAYPKLFSSVKWGQQEIVAKTYQLLARREIWDQSALDVGLTMQLLDCNFSDENVRAIAVQKLESLEDDDVLHYLLQLVQAVKFEPYHDSALARFLLKRGLRNKRIGHFLFWFLRSEIAQSRHYQQRFAVILEAYLRGCGTAMLQDFTQQVHVIEMLQKVTIDIKSLSAEKYDVSSQVISQLKQKLESLQNSNLPESFRVPYDPGLKAGTLVIEKCKVMASKKKPLWLEFKCADPTVLSNETIGIIFKHGDDLRQDMLILQILRIMESIWETESLDLCLLPYGCISTGDKIGMIEIVKDATTIAQIQQSTVGNTGAFKDEVLNHWLKEKCPIEEKFQAAVERFVYSCAGYCVATFVLGIGDRHNDNIMISETGNLFHIDFGHILGNYKSFLGINKERVPFVLTPDFLFVMGSSGKKTSPHFQKFQDVCVRAYLALRHHTNLLIILFSMMLMTGMPQLTSKEDIEYIRDALTVGKSEEDAKKYFLDQIEVCRDKGWTVQFNWFLHLVLGIKQGEKHSA
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Organism
Mus musculus, Mouse
Protein Classification
Enzyme
>
Transferase
Function
Phosphoinositide-3-kinase (PI3K) that phosphorylates 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. Links G-protein coupled receptor activation to PIP3 production. Involved in immune, inflammatory and allergic responses. Modulates leukocyte chemotaxis to inflammatory sites and in response to chemoattractant agents. May control leukocyte polarization and migration by regulating the spatial accumulation of PIP3 and by regulating the organization of F-actin formation and integrin-based adhesion at the leading edge. Controls motility of dendritic cells. Together with PIK3CD is involved in natural killer (NK) cell development and migration towards the sites of inflammation. Participates in T-lymphocyte migration. Regulates T-lymphocyte proliferation, activation and cytokine production. Together with PIK3CD participates in T-lymphocyte development. Required for B-lymphocyte development and signaling. Together with PIK3CD participates in neutrophil respiratory burst. Together with PIK3CD is involved in neutrophil chemotaxis and extravasation. Together with PIK3CB promotes platelet aggregation and thrombosis. Regulates alpha-IIb/beta-3 integrins (ITGA2B/ ITGB3) adhesive function in platelets downstream of P2Y12 through a lipid kinase activity-independent mechanism. May have also a lipid kinase activity-dependent function in platelet aggregation. Involved in endothelial progenitor cell migration. Negative regulator of cardiac contractility. Modulates cardiac contractility by anchoring protein kinase A (PKA) and PDE3B activation, reducing cAMP levels. Regulates cardiac contractility also by promoting beta-adrenergic receptor internalization by binding to GRK2 and by non-muscle tropomyosin phosphorylation. Also has serine/threonine protein kinase activity: both lipid and protein kinase activities are required for beta-adrenergic receptor endocytosis. May also have a scaffolding role in modulating cardiac contractility. Contribute to cardiac hypertrophy under pathological stress. Through simultaneous binding of PDE3B to RAPGEF3 and PIK3R6 is assembled in a signaling complex in which the PI3K gamma complex is activated by RAPGEF3 and which is involved in angiogenesis (By similarity).
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Uniprot ID
Primary ID:
Q9JHG7

Secondarily ID:
Q80V09
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Ensembl ID
ENSG00000105851
Subcellular Location
Cytoplasm
Cell membrane
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: CL000014 , RAW 264.7
Compound ID Compound Name Compound Formula
CP0006058
2-amino-N-[(1S)-1-[8-[2-(1-methylpyrazol-4-yl)ethynyl]-1-oxo-2-phenylisoquinolin-3-yl]ethyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
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C30H24N8O2
 1
1
IC50 = 1.2 nM
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CP0019791
N-[5-[2-[(1S)-1-cyclopropylethyl]-7-(methanesulfonamido)-1-oxo-3H-isoindol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide
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C20H24N4O4S2
 1
1
IC50 = 2.512 nM
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CP0019793
N-[5-[2-[(1S)-1-cyclopropylethyl]-7-(methylsulfamoyl)-1-oxo-3H-isoindol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide
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C20H24N4O4S2
 1
1
IC50 = 5.012 nM
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CP0012179
N-[5-[2-[(1S)-1-cyclopropylethyl]-7-methyl-1-oxo-3H-isoindol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide
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C20H23N3O2S
 1
1
IC50 = 6.31 nM
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CP0024001
N-[5-[2-[(1S)-1-cyclopropylethyl]-7-(2-methoxyethylsulfonylamino)-1-oxo-3H-isoindol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide
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C22H28N4O5S2
 1
1
IC50 = 6.31 nM
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CP0031524
N-[5-[7-chloro-2-[(1S)-1-cyclopropylethyl]-1-oxo-3H-isoindol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide
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C19H20ClN3O2S
 1
1
IC50 = 6.31 nM
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CP0017013
N-[5-[2-[(1S)-1-cyclopropylethyl]-7-methylsulfonyl-1-oxo-3H-isoindol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide
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C20H23N3O4S2
 1
1
IC50 = 7.943 nM
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CP0017098
N-[5-[2-[(1S)-1-cyclopropylethyl]-1-oxo-7-sulfamoyl-3H-isoindol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide
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C19H22N4O4S2
 1
1
IC50 = 19.95 nM
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CP0019794
N-[5-[2-[(1S)-1-cyclopropylethyl]-7-(2-methoxyethylsulfamoyl)-1-oxo-3H-isoindol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide
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C22H28N4O5S2
 1
1
IC50 = 19.95 nM
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CP0353655
4-amino-6-[[(1S)-1-(6-methyl-4-oxo-3-phenylquinolizin-2-yl)ethyl]amino]pyrimidine-5-carbonitrile
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C23H20N6O
 1
1
IC50 = 30 nM
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CP0017012
N-[5-[7-chloro-2-[(1S)-1-cyclopropylethyl]-1-oxo-3H-isoindol-5-yl]-1,3-thiazol-2-yl]acetamide
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C18H18ClN3O2S
 1
1
IC50 = 31.62 nM
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CP0026318
5-chloro-3-phenyl-2-[(1S)-1-(7H-purin-6-ylamino)ethyl]quinazolin-4-one
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C21H16ClN7O
 1
1
IC50 = 39 nM
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CP0024003
N-[5-[7-chloro-2-[(1R)-1-cyclopropylethyl]-1-oxo-3H-isoindol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide
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C19H20ClN3O2S
 1
1
IC50 = 39.81 nM
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CP0077387
N-[4-methyl-5-(2-pyridin-3-yl-1,3-oxazol-5-yl)-1,3-thiazol-2-yl]acetamide
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C14H12N4O2S
 1
1
IC50 = 59 nM
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CP0136524
2,4-diamino-6-[[(1S)-1-(7-fluoro-4-oxo-3-phenylquinolizin-2-yl)ethyl]amino]pyrimidine-5-carbonitrile
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C22H18FN7O
 1
1
IC50 = 75 nM
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CP0276259
N-[4-methyl-5-[2-(2,2,2-trifluoroethyl)-1,3-oxazol-5-yl]-1,3-thiazol-2-yl]acetamide
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C11H10F3N3O2S
 1
1
IC50 = 88 nM
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CP0219705
2-amino-4-[[(1S)-1-[7-fluoro-1-(4-fluorophenyl)-4-oxo-3-phenylquinolizin-2-yl]ethyl]amino]-6-methylpyrimidine-5-carbonitrile
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C29H22F2N6O
 1
1
IC50 = 90 nM
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CP0077385
N-[5-(2-tert-butyl-1,3-oxazol-5-yl)-4-methyl-1,3-thiazol-2-yl]acetamide
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C13H17N3O2S
 1
1
IC50 = 113 nM
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CP0252714
N-[5-[3-(3-hydroxy-2,2-dimethylbutyl)-1,2,4-oxadiazol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide
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C14H20N4O3S
 1
1
IC50 = 155 nM
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CP0176936
2,4-diamino-6-[[(1S)-1-[7-fluoro-1-(4-fluorophenyl)-4-oxo-3-phenylquinolizin-2-yl]ethyl]amino]pyrimidine-5-carbonitrile
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C28H21F2N7O
 1
1
IC50 = 177 nM
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CP0134073
N-[5-[3-(3-hydroxy-2,2-dimethylpropyl)-1,2,4-oxadiazol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide
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C13H18N4O3S
 1
1
IC50 = 191 nM
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CP0224694
N-[4-methyl-5-(2-methylsulfonyl-1,3-oxazol-5-yl)-1,3-thiazol-2-yl]acetamide
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C10H11N3O4S2
 1
1
IC50 = 222 nM
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CP0134074
N-[5-(3-tert-butyl-1,2,4-oxadiazol-5-yl)-4-methyl-1,3-thiazol-2-yl]acetamide
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C12H16N4O2S
 1
1
IC50 = 231 nM
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CP0224695
N-[5-[2-(3-hydroxypiperidin-1-yl)-1,3-oxazol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide
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C14H18N4O3S
 1
1
IC50 = 237 nM
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CP0019790
N-[5-[2-[(1S)-1-cyclopropylethyl]-7-(3-hydroxypropylsulfonyl)-1-oxo-3H-isoindol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide
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C22H27N3O5S2
 1
1
IC50 = 251.19 nM
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CP0262745
N-[4-methyl-5-[3-(2,2,2-trifluoroethyl)-1,2,4-oxadiazol-5-yl]-1,3-thiazol-2-yl]acetamide
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C10H9F3N4O2S
 1
1
IC50 = 278 nM
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CP0245832
N-[4-methyl-5-(2-pyridin-3-ylsulfanyl-1,3-oxazol-5-yl)-1,3-thiazol-2-yl]acetamide
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C14H12N4O2S2
 1
1
IC50 = 279 nM
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CP0067381
N-[5-[3-(3-hydroxypiperidin-1-yl)-1,2,4-oxadiazol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide
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C13H17N5O3S
 1
1
IC50 = 294 nM
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CP0122221
N-[4-methyl-5-(2-methylsulfanyl-1,3-oxazol-5-yl)-1,3-thiazol-2-yl]acetamide
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C10H11N3O2S2
 1
1
IC50 = 322 nM
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CP0245831
N-[5-[2-(2-hydroxypropan-2-yl)-1,3-oxazol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide
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C12H15N3O3S
 1
1
IC50 = 369 nM
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CP0016620
3-amino-6-[2-[(1S)-1-cyclopropylethyl]-7-methyl-1-oxo-3H-isoindol-5-yl]-N-methylpyrazine-2-carboxamide
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C20H23N5O2
 1
1
IC50 = 398.11 nM
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CP0017099
2-[(1S)-1-cyclopropylethyl]-7-methyl-5-(5H-pyrrolo[2,3-b]pyrazin-2-yl)-3H-isoindol-1-one
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C20H20N4O
 1
1
IC50 = 398.11 nM
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CP0122220
N-[4-methyl-5-[2-(pyridin-3-ylamino)-1,3-oxazol-5-yl]-1,3-thiazol-2-yl]acetamide
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C14H13N5O2S
 1
1
IC50 = 431 nM
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CP0252713
N-[4-methyl-5-[3-(oxolan-3-yl)-1,2,4-oxadiazol-5-yl]-1,3-thiazol-2-yl]acetamide
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C12H14N4O3S
 1
1
IC50 = 558 nM
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CP0284911
N-[4-methyl-5-(2-morpholin-4-yl-1,3-oxazol-5-yl)-1,3-thiazol-2-yl]acetamide
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C13H16N4O3S
 1
1
IC50 = 599 nM
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CP0024002
5-(2-aminopyrimidin-5-yl)-7-chloro-2-[(1S)-1-cyclopropylethyl]-3H-isoindol-1-one
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C17H17ClN4O
 1
1
IC50 = 630.96 nM
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CP0057640
N-[5-[2-[(6-chloropyridin-3-yl)amino]-1,3-oxazol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide
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C14H12ClN5O2S
 1
1
IC50 = 1040 nM
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CP0316180
N-[5-[2-(dimethylamino)-1,3-oxazol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide
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C11H14N4O2S
 1
1
IC50 = 1222 nM
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CP0473312
7-methyl-2-((7-methyl-[1,2,4]triazolo[1,5-a]pyridin-6-yl)amino)-9-(tetrahydro-2H-pyran-4-yl)-7,9-dihydro-8H-purin-8-one
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C18H20N8O2
 1
1
IC50 = 1370 nM
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CP0077388
N-[4-methyl-5-(2-pyridin-3-yloxy-1,3-oxazol-5-yl)-1,3-thiazol-2-yl]acetamide
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C14H12N4O3S
 1
1
IC50 = 1666 nM
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CP0030807
3-(5-tert-butyl-1,3,4-oxadiazol-2-yl)-5-[1-methyl-5-(1-phenylcyclopropyl)-1,2,4-triazol-3-yl]pyrazin-2-amine
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C22H24N8O
 1
1
IC50 = 3700 nM
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CP0029667
5-(3-aminopyrazin-2-yl)-2-[(1S)-1-cyclopropylethyl]-7-methyl-3H-isoindol-1-one
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C18H20N4O
 1
1
IC50 = 7943.28 nM
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CP0221106
3-[[5-(2-acetamido-4-methyl-1,3-thiazol-5-yl)-1,3-oxazol-2-yl]amino]benzoic acid
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C16H14N4O4S
 1
1
IC50 > 10000 nM
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CP0335247
3-[[5-(2-acetamido-4-methyl-1,3-thiazol-5-yl)-1,3-oxazol-2-yl]methyl]benzoic acid
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C17H15N3O4S
 1
1
IC50 > 10000 nM
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CP0016012
4-[3-amino-6-[1-methyl-5-(1-phenylcyclopropyl)-1,2,4-triazol-3-yl]pyrazin-2-yl]-N,N-dimethylpyrazole-1-sulfonamide
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C21H23N9O2S
 1
1
IC50 > 10000 nM
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CP0033023
N-[4-methyl-5-(7-methyl-1-oxo-2,3-dihydroisoindol-5-yl)-1,3-thiazol-2-yl]acetamide
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C15H15N3O2S
 1
1
IC50 > 1000 nM
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CP0702721
(S)-2-(1-((9H-Purin-6-yl)amino)ethyl)-7-fluoro-3-phenyl-4H-quinolizin-4-one
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C22H17FN6O
 1
1
IC50 > 3000 nM
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Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT01029 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens, Human