General Information of the Protein
Protein ID
PT00924
Protein Name
Protein kinase C zeta type
Secondarily
Protein Name
nPKC-zeta
Gene Name
PRKCZ
Secondarily
Gene Name
PKC2
Sequence
MPSRTGPKMEGSGGRVRLKAHYGGDIFITSVDAATTFEELCEEVRDMCRLHQQHPLTLKWVDSEGDPCTVSSQMELEEAFRLARQCRDEGLIIHVFPSTPEQPGLPCPGEDKSIYRRGARRWRKLYRANGHLFQAKRFNRRAYCGQCSERIWGLARQGYRCINCKLLVHKRCHGLVPLTCRKHMDSVMPSQEPPVDDKNEDADLPSEETDGIAYISSSRKHDSIKDDSEDLKPVIDGMDGIKISQGLGLQDFDLIRVIGRGSYAKVLLVRLKKNDQIYAMKVVKKELVHDDEDIDWVQTEKHVFEQASSNPFLVGLHSCFQTTSRLFLVIEYVNGGDLMFHMQRQRKLPEEHARFYAAEICIALNFLHERGIIYRDLKLDNVLLDADGHIKLTDYGMCKEGLGPGDTTSTFCGTPNYIAPEILRGEEYGFSVDWWALGVLMFEMMAGRSPFDIITDNPDMNTEDYLFQVILEKPIRIPRFLSVKASHVLKGFLNKDPKERLGCRPQTGFSDIKSHAFFRSIDWDLLEKKQALPPFQPQITDDYGLDNFDTQFTSEPVQLTPDDEDAIKRIDQSEFEGFEYINPLLLSTEESV
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
AGC protein kinase group
>
AGC protein kinase PKC family
>
AGC protein kinase PKC iota subfamily
Function
Calcium- and diacylglycerol-independent serine/threonine-protein kinase that functions in phosphatidylinositol 3-kinase (PI3K) pathway and mitogen-activated protein (MAP) kinase cascade, and is involved in NF-kappa-B activation, mitogenic signaling, cell proliferation, cell polarity, inflammatory response and maintenance of long-term potentiation (LTP). Upon lipopolysaccharide (LPS) treatment in macrophages, or following mitogenic stimuli, functions downstream of PI3K to activate MAP2K1/MEK1-MAPK1/ERK2 signaling cascade independently of RAF1 activation. Required for insulin-dependent activation of AKT3, but may function as an adapter rather than a direct activator. Upon insulin treatment may act as a downstream effector of PI3K and contribute to the activation of translocation of the glucose transporter SLC2A4/GLUT4 and subsequent glucose transport in adipocytes. In EGF-induced cells, binds and activates MAP2K5/MEK5-MAPK7/ERK5 independently of its kinase activity and can activate JUN promoter through MEF2C. Through binding with SQSTM1/p62, functions in interleukin-1 signaling and activation of NF-kappa-B with the specific adapters RIPK1 and TRAF6. Participates in TNF-dependent transactivation of NF-kappa-B by phosphorylating and activating IKBKB kinase, which in turn leads to the degradation of NF-kappa-B inhibitors. In migrating astrocytes, forms a cytoplasmic complex with PARD6A and is recruited by CDC42 to function in the establishment of cell polarity along with the microtubule motor and dynein. In association with FEZ1, stimulates neuronal differentiation in PC12 cells. In the inflammatory response, is required for the T-helper 2 (Th2) differentiation process, including interleukin production, efficient activation of JAK1 and the subsequent phosphorylation and nuclear translocation of STAT6. May be involved in development of allergic airway inflammation (asthma), a process dependent on Th2 immune response. In the NF-kappa-B-mediated inflammatory response, can relieve SETD6-dependent repression of NF-kappa-B target genes by phosphorylating the RELA subunit at 'Ser-311'. Phosphorylates VAMP2 in vitro (PubMed:17313651).
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Uniprot ID
Primary ID:
Q05513

Secondarily ID:
A8K4N0
A8MU64
B7Z2J7
E9PCW2
Q15207
Q5SYT5
Q969S4
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Ensembl ID
ENSG00000067606
HGNC ID
HGNC:9412
Subcellular Location
Cytoplasm
Endosome
Cell junction
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: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0043188
US8889672, 317-094-001
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C13H14N2O2S
 1
1
EC50 = 1 nM
   TI
   LI
   LO
   TS
CP0156976
US8889672, 317-052-004
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C21H21NO5S
 1
1
EC50 = 1 nM
   TI
   LI
   LO
   TS
CP0156979
US8889672, 317-080-001
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C15H18N2O2S
 1
1
EC50 = 1 nM
   TI
   LI
   LO
   TS
CP0054786
US8889672, 268-020-002
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C14H13NO4S
 1
1
EC50 = 2 nM
   TI
   LI
   LO
   TS
CP0187938
US8889672, 252-036-001
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C20H19NO4S
 1
1
EC50 = 2 nM
   TI
   LI
   LO
   TS
CP0009085
(4-(4-(benzo[b]thiophen-2-yl)pyrimidin-2-ylamino)phenyl)(4-(pyrrolidin-1-yl)piperidin-1-yl)methanone
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C28H29N5OS
 1
1
EC50 = 3 nM
   TI
   LI
   LO
   TS
CP0056629
US8889672, 194-074-007
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C16H19NO4S
 1
1
EC50 = 3 nM
   TI
   LI
   LO
   TS
CP0054791
US8889672, 317-054-001
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C14H14FNO3S
 1
1
EC50 = 10 nM
   TI
   LI
   LO
   TS
CP0482636
4-[2-(3-chlorophenyl)-3-(3-fluoro-4-hydroxyphenyl)-3,4-dihydropyrazol-5-yl]benzene-1,3-diol
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C21H16ClFN2O3
 1
1
IC50 < 100 nM
   TI
   LI
   LO
   TS
CP0671568
4-(1,5-bis(4-Chlorophenyl)-4,5-dihydro-1H-pyrazol-3-yl)benzene-1,2-diol
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C21H16Cl2N2O2
 1
1
IC50 < 100 nM
   TI
   LI
   LO
   TS
CP0944312
4-(1-(3-Chlorophenyl)-5-(4-chlorophenyl)-4,5-dihydro-1H-pyrazol-3-yl)phenol
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C21H16Cl2N2O
 1
1
IC50 < 100 nM
   TI
   LI
   LO
   TS
CP0944313
4-(5-(3-Chlorophenyl)-1-(4-chlorophenyl)-4,5-dihydro-1H-pyrazol-3-yl)phenol
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C21H16Cl2N2O
 1
1
IC50 < 100 nM
   TI
   LI
   LO
   TS
CP0860817
4-(1,5-bis(3-Chlorophenyl)-4,5-dihydro-1H-pyrazol-3-yl)phenol
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C21H16Cl2N2O
 2
1
IC50 = 400 nM
   TI
   LI
   LO
   TS
2
IC50 = 4100 nM
   TI
   LI
   LO
   TS
CP0042841
4-[2-(3-chlorophenyl)-5-(2-hydroxyphenyl)-3,4-dihydropyrazol-3-yl]-2-fluorophenol
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C21H16ClFN2O2
 1
1
IC50 = 2900 nM
   TI
   LI
   LO
   TS
CP0855272
4-(1,5-bis(4-Chlorophenyl)-4,5-dihydro-1H-pyrazol-3-yl)benzene-1,3-diol
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C21H16Cl2N2O2
 2
1
IC50 = 4300 nM
   TI
   LI
   LO
   TS
2
IC50 = 9700 nM
   TI
   LI
   LO
   TS
CP0900116
4-(1,5-bis(4-Chlorophenyl)-4,5-dihydro-1H-pyrazol-3-yl)phenol
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C21H16Cl2N2O
 2
1
IC50 = 6200 nM
   TI
   LI
   LO
   TS
2
IC50 = 20800 nM
   TI
   LI
   LO
   TS
CP0955633
3-(1,5-bis(4-Chlorophenyl)-4,5-dihydro-1H-pyrazol-3-yl)phenol
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C21H16Cl2N2O
 1
1
IC50 = 6500 nM
   TI
   LI
   LO
   TS
CP0883759
4-(1,5-bis(2-Chlorophenyl)-4,5-dihydro-1H-pyrazol-3-yl)phenol
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C21H16Cl2N2O
 1
1
IC50 = 21300 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0357869
7-(4-amino-2-fluorophenyl)-N-[(3S)-azepan-3-yl]isoquinolin-5-amine
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C21H23FN4
 1
1 IC50 = 0.1 nM
CP0698479
6-[(3S)-pyrrolidin-3-yl]oxy-4-(1H-pyrrolo[2,3-b]pyridin-5-yl)isoquinoline
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C20H18N4O
 1
1 IC50 = 13 nM
CP0482636
4-[2-(3-chlorophenyl)-3-(3-fluoro-4-hydroxyphenyl)-3,4-dihydropyrazol-5-yl]benzene-1,3-diol
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C21H16ClFN2O3
 1
1 IC50 < 100 nM
CP0042881
5-[5-tert-butyl-2-(3-chlorophenyl)-3,4-dihydropyrazol-3-yl]-2-fluorophenol
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C19H20ClFN2O
 1
1 IC50 = 300 nM
CP0042879
4-[5-thiophen-2-yl-2-[4-(trifluoromethyl)phenyl]-3,4-dihydropyrazol-3-yl]phenol
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C20H15F3N2OS
 1
1 IC50 = 400 nM
CP0508955
4-[5-tert-butyl-2-(3,4-difluorophenyl)-3,4-dihydropyrazol-3-yl]phenol
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C19H20F2N2O
 1
1 IC50 = 500 nM
CP0114334
4-[5-tert-butyl-2-(4-chlorophenyl)-3,4-dihydropyrazol-3-yl]-2-chlorophenol
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C19H20Cl2N2O
 1
1 IC50 = 700 nM
CP0381421
4-[5-tert-butyl-2-(2,3,4-trifluorophenyl)-3,4-dihydropyrazol-3-yl]phenol
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C19H19F3N2O
 1
1 IC50 = 700 nM
CP0156979
US8889672, 317-080-001
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C15H18N2O2S
 2
1 IC50 = 800 nM
2 IC50 = 1000 nM
CP0213661
4-[5-tert-butyl-2-(3-chloro-4-fluorophenyl)-3,4-dihydropyrazol-3-yl]phenol
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C19H20ClFN2O
 1
1 IC50 = 900 nM
CP0043188
US8889672, 317-094-001
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C13H14N2O2S
 1
1 IC50 = 2000 nM
CP0054786
US8889672, 268-020-002
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C14H13NO4S
 1
1 IC50 = 2000 nM
CP0156976
US8889672, 317-052-004
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C21H21NO5S
 2
1 IC50 = 2000 nM
2 IC50 = 5000 nM
CP0139871
4-[5-tert-butyl-2-[3-(trifluoromethyl)phenyl]-3,4-dihydropyrazol-3-yl]phenol
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C20H21F3N2O
 1
1 IC50 = 2700 nM
CP0042841
4-[2-(3-chlorophenyl)-5-(2-hydroxyphenyl)-3,4-dihydropyrazol-3-yl]-2-fluorophenol
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C21H16ClFN2O2
 1
1 IC50 = 2900 nM
CP0272072
4-[5-tert-butyl-2-(4-chlorophenyl)-3,4-dihydropyrazol-3-yl]-2-fluorophenol
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C19H20ClFN2O
 1
1 IC50 = 3800 nM
CP0054791
US8889672, 317-054-001
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C14H14FNO3S
 1
1 IC50 = 4000 nM
CP0250935
3-[5-tert-butyl-2-(4-chlorophenyl)-3,4-dihydropyrazol-3-yl]phenol
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C19H21ClN2O
 1
1 IC50 = 5300 nM
CP0056629
US8889672, 194-074-007
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C16H19NO4S
 2
1 IC50 = 6000 nM
2 IC50 = 20000 nM
CP0187938
US8889672, 252-036-001
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C20H19NO4S
 1
1 IC50 = 6000 nM
CP0139872
4-[2-(3-chlorophenyl)-5-(2-hydroxyphenyl)-3,4-dihydropyrazol-3-yl]-2,3-difluorophenol
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C21H15ClF2N2O2
 1
1 IC50 = 6600 nM
CP0042880
4-[5-tert-butyl-2-(4-chlorophenyl)-3,4-dihydropyrazol-3-yl]phenol
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C19H21ClN2O
 1
1 IC50 = 10700 nM
CP0410481
4-[2-(3-chlorophenyl)-5-(2-hydroxyphenyl)-3,4-dihydropyrazol-3-yl]-2,6-difluorophenol
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C21H15ClF2N2O2
 1
1 IC50 = 11100 nM
CP0241979
3-(3,4-dichlorophenyl)-4-(6-iodo-1H-benzimidazol-2-yl)butanoic acid
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C17H13Cl2IN2O2
 2
1 IC50 = 15900 nM
2 IC50 = 18000 nM
CP0114668
4-[5-tert-butyl-2-(4-chlorophenyl)pyrazol-3-yl]-2-chlorophenol
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C19H18Cl2N2O
 1
1 IC50 = 17400 nM
CP0235572
3-(4-tert-butylphenyl)-4-(6-iodo-1H-benzimidazol-2-yl)butanoic acid
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C21H23IN2O2
 1
1 IC50 = 23000 nM
CP0253770
4-(6-iodo-1H-benzimidazol-2-yl)-3-(4-propylphenyl)butanoic acid
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C20H21IN2O2
 1
1 IC50 = 33000 nM
CP0281966
3-(4-chlorophenyl)-4-(6-iodo-1H-benzimidazol-2-yl)butanoic acid
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C17H14ClIN2O2
 1
1 IC50 = 33000 nM
CP0282571
3-(4-chlorophenyl)-4-(4,6-dichloro-1H-benzimidazol-2-yl)butanoic acid
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C17H13Cl3N2O2
 1
1 IC50 = 38000 nM
CP0218996
4-(6-chloro-1H-benzimidazol-2-yl)-3-(3,4-dichlorophenyl)butanoic acid
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C17H13Cl3N2O2
 1
1 IC50 = 39000 nM
CP0090763
4-(6-chloro-1H-benzimidazol-2-yl)-3-[4-chloro-3-(trifluoromethyl)phenyl]butanoic acid
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C18H13Cl2F3N2O2
 1
1 IC50 = 43000 nM
CP0282569
4-(6-chloro-4-methyl-1H-benzimidazol-2-yl)-3-(4-chlorophenyl)butanoic acid
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C18H16Cl2N2O2
 1
1 IC50 = 55000 nM
Clinical Information about the Protein
Target 1 ( Protein kinase C zeta (PRKCZ) )
Target Type Patented-recorded Target
Disease 1 Target-related Disease  1
1 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Investigative Drug(s) 1 Investigative Drug  1
1 G6976 Investigative
Solid tumour/cancer
Target 2 ( PKC-zeta messenger RNA (PRKCZ mRNA) )
Target Type Literature-reported Target