General Information of the Protein
Protein ID
PT01383
Protein Name
MAP/microtubule affinity-regulating kinase 3
Secondarily
Protein Name
C-TAK1
Cdc25C-associated protein kinase 1
ELKL motif kinase 2
Protein kinase STK10
Ser/Thr protein kinase PAR-1
Serine/threonine-protein kinase p78
Gene Name
MARK3
Secondarily
Gene Name
CTAK1
EMK2
Sequence
MSTRTPLPTVNERDTENHTSHGDGRQEVTSRTSRSGARCRNSIASCADEQPHIGNYRLLKTIGKGNFAKVKLARHILTGREVAIKIIDKTQLNPTSLQKLFREVRIMKILNHPNIVKLFEVIETEKTLYLIMEYASGGEVFDYLVAHGRMKEKEARSKFRQIVSAVQYCHQKRIVHRDLKAENLLLDADMNIKIADFGFSNEFTVGGKLDTFCGSPPYAAPELFQGKKYDGPEVDVWSLGVILYTLVSGSLPFDGQNLKELRERVLRGKYRIPFYMSTDCENLLKRFLVLNPIKRGTLEQIMKDRWINAGHEEDELKPFVEPELDISDQKRIDIMVGMGYSQEEIQESLSKMKYDEITATYLLLGRKSSELDASDSSSSSNLSLAKVRPSSDLNNSTGQSPHHKVQRSVSSSQKQRRYSDHAGPAIPSVVAYPKRSQTSTADSDLKEDGISSRKSSGSAVGGKGIAPASPMLGNASNPNKADIPERKKSSTVPSSNTASGGMTRRNTYVCSERTTADRHSVIQNGKENSTIPDQRTPVASTHSISSAATPDRIRFPRGTASRSTFHGQPRERRTATYNGPPASPSLSHEATPLSQTRSRGSTNLFSKLTSKLTRRNMSFRFIKRLPTEYERNGRYEGSSRNVSAEQKDENKEAKPRSLRFTWSMKTTSSMDPGDMMREIRKVLDANNCDYEQRERFLLFCVHGDGHAENLVQWEMEVCKLPRLSLNGVRFKRISGTSIAFKNIASKIANELKL
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
CAMK protein kinase group
>
CAMK protein kinase CAMK1 family
>
CAMK protein kinase MARK subfamily
Function
Serine/threonine-protein kinase (PubMed:16822840, PubMed:16980613, PubMed:23666762). Involved in the specific phosphorylation of microtubule-associated proteins for MAP2 and MAP4. Phosphorylates the microtubule-associated protein MAPT/TAU (PubMed:23666762). Phosphorylates CDC25C on 'Ser-216' (PubMed:12941695). Regulates localization and activity of some histone deacetylases by mediating phosphorylation of HDAC7, promoting subsequent interaction between HDAC7 and 14-3-3 and export from the nucleus (PubMed:16980613). Regulates localization and activity of MITF by mediating its phosphorylation, promoting subsequent interaction between MITF and 14-3-3 and retention in the cytosol (PubMed:16822840). Negatively regulates the Hippo signaling pathway and antagonizes the phosphorylation of LATS1. Cooperates with DLG5 to inhibit the kinase activity of STK3/MST2 toward LATS1 (PubMed:28087714). Phosphorylates PKP2 and KSR1 (PubMed:12941695).
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Uniprot ID
Primary ID:
P27448

Secondarily ID:
A0A0A0MQR8
A0A0A0MST9
A0A0A0MT23
O60219
Q86TT8
Q8TB41
Q8WX83
Q96RG1
Q9UMY9
Q9UN34
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Ensembl ID
ENSG00000075413
HGNC ID
HGNC:6897
Subcellular Location
Cell membrane
Cell projection
Dendrite
Cytoplasm
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
CP0496360
N-[3-[[5-bromo-4-[3-(cyclobutanecarbonylamino)propylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide
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C23H30BrN7O2
 1
1
IC50 = 137 nM
   TI
   LI
   LO
   TS
CP0201442
N-[3-[[5-cyclopropyl-2-[3-(morpholin-4-ylmethyl)anilino]pyrimidin-4-yl]amino]propyl]cyclobutanecarboxamide
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C26H36N6O2
 1
1
IC50 = 328 nM
   TI
   LI
   LO
   TS
CP0275665
5-bromo-4-N-[2-(1H-imidazol-5-yl)ethyl]-2-N-[3-(morpholin-4-ylmethyl)phenyl]pyrimidine-2,4-diamine
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C20H24BrN7O
 1
1
IC50 = 872 nM
   TI
   LI
   LO
   TS
CP0275666
N-[3-[[4-[3-(cyclobutanecarbonylamino)propylamino]-5-cyclopropylpyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide
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C26H35N7O2
 1
1
IC50 = 2001 nM
   TI
   LI
   LO
   TS
CP0237749
BX-912
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C20H23BrN8O
 1
1
IC50 = 3333 nM
   TI
   LI
   LO
   TS
CP0275671
5-cyclopropyl-4-N-[2-(1H-imidazol-5-yl)ethyl]-2-N-[3-(morpholin-4-ylmethyl)phenyl]pyrimidine-2,4-diamine
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C23H29N7O
 1
1
IC50 = 4015 nM
   TI
   LI
   LO
   TS
CP0169053
4-[[[5-bromo-2-[[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]amino]pyrimidin-4-yl]amino]methyl]benzenesulfonamide
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C17H17BrF3N7O2S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0260709
4-N-[2-(1H-imidazol-5-yl)ethyl]-2-N-[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]pyrimidine-2,4-diamine
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C15H17F3N8
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0273555
4-[[[5-cyclopropyl-2-[3-(morpholin-4-ylmethyl)anilino]pyrimidin-4-yl]amino]methyl]benzenesulfonamide
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C25H30N6O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0275668
4-[[[5-bromo-2-[3-(morpholin-4-ylmethyl)anilino]pyrimidin-4-yl]amino]methyl]benzenesulfonamide
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C22H25BrN6O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0275670
4-[[[2-[3-(morpholin-4-ylmethyl)anilino]pyrimidin-4-yl]amino]methyl]benzenesulfonamide
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C22H26N6O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0275672
N-[3-[[4-[3-(cyclobutanecarbonylamino)propylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide
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C23H31N7O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0275673
N-[3-[[5-bromo-4-[(4-sulfamoylphenyl)methylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide
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C22H24BrN7O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0275674
5-cyclopropyl-4-N-[2-(1H-imidazol-5-yl)ethyl]-2-N-[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]pyrimidine-2,4-diamine
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C18H21F3N8
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0344151
4-N-[2-(1H-imidazol-5-yl)ethyl]-2-N-[3-(morpholin-4-ylmethyl)phenyl]pyrimidine-2,4-diamine
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C20H25N7O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0496361
N-[3-[[5-bromo-2-[[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]amino]pyrimidin-4-yl]amino]propyl]cyclobutanecarboxamide
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C18H23BrF3N7O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0496362
5-bromo-4-N-[2-(1H-imidazol-5-yl)ethyl]-2-N-[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]pyrimidine-2,4-diamine
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C15H16BrF3N8
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0496364
4-[[[2-[[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]amino]pyrimidin-4-yl]amino]methyl]benzenesulfonamide
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C17H18F3N7O2S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0543933
N-[3-[[5-cyclopropyl-4-[(4-sulfamoylphenyl)methylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide
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C25H29N7O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0551443
4-[[[5-cyclopropyl-2-[[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]amino]pyrimidin-4-yl]amino]methyl]benzenesulfonamide
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C20H22F3N7O2S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0551444
N-[3-[[4-[(4-sulfamoylphenyl)methylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide
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C22H25N7O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0567307
N-[3-[[5-cyclopropyl-2-[[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]amino]pyrimidin-4-yl]amino]propyl]cyclobutanecarboxamide
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C21H28F3N7O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0571203
N-[3-[[2-[[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]amino]pyrimidin-4-yl]amino]propyl]cyclobutanecarboxamide
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C18H24F3N7O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
Clinical Information about the Protein
Target 1 ( Microtubule affinity regulating kinase 3 (MARK3) )
Target Type Clinical trial Target
Target 2 ( HUMAN microtubule affinity regulating kinase 3 (MARK3) )
Target Type Unknown Type Target