General Information of the Protein
Protein ID
PT02162
Protein Name
Mitogen-activated protein kinase 6
Secondarily
Protein Name
Extracellular signal-regulated kinase 3
MAP kinase isoform p97
Gene Name
MAPK6
Secondarily
Gene Name
ERK3
PRKM6
Sequence
MAEKFESLMNIHGFDLGSRYMDLKPLGCGGNGLVFSAVDNDCDKRVAIKKIVLTDPQSVKHALREIKIIRRLDHDNIVKVFEILGPSGSQLTDDVGSLTELNSVYIVQEYMETDLANVLEQGPLLEEHARLFMYQLLRGLKYIHSANVLHRDLKPANLFINTEDLVLKIGDFGLARIMDPHYSHKGHLSEGLVTKWYRSPRLLLSPNNYTKAIDMWAAGCIFAEMLTGKTLFAGAHELEQMQLILESIPVVHEEDRQELLSVIPVYIRNDMTEPHKPLTQLLPGISREALDFLEQILTFSPMDRLTAEEALSHPYMSIYSFPMDEPISSHPFHIEDEVDDILLMDETHSHIYNWERYHDCQFSEHDWPVHNNFDIDEVQLDPRALSDVTDEEEVQVDPRKYLDGDREKYLEDPAFDTNYSTEPCWQYSDHHENKYCDLECSHTCNYKTRSSSYLDNLVWRESEVNHYYEPKLIIDLSNWKEQSKEKSDKKGKSKCERNGLVKAQIALEEASQQLAGKEREKNQGFDFDSFIAGTIQLSSQHEPTDVVDKLNDLNSSVSQLELKSLISKSVSQEKQEKGMANLAQLEALYQSSWDSQFVSGGEDCFFINQFCEVRKDEQVEKENTYTSYLDKFFSRKEDTEMLETEPVEDGKLGERGHEEGFLNNSGEFLFNKQLESIGIPQFHSPVGSPLKSIQATLTPSAMKSSPQIPHQTYSSILKHLN
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
CMGC protein kinase group
>
CMGC protein kinase MAPK family
>
CMGC protein kinase ERK3
Function
Atypical MAPK protein. Phosphorylates microtubule-associated protein 2 (MAP2) and MAPKAPK5. The precise role of the complex formed with MAPKAPK5 is still unclear, but the complex follows a complex set of phosphorylation events: upon interaction with atypical MAPKAPK5, ERK3/MAPK6 is phosphorylated at Ser-189 and then mediates phosphorylation and activation of MAPKAPK5, which in turn phosphorylates ERK3/MAPK6. May promote entry in the cell cycle (By similarity).
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Uniprot ID
Primary ID:
Q16659

Secondarily ID:
B2R945
B5BU65
Q68DH4
Q8IYN8
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Ensembl ID
ENSG00000069956
HGNC ID
HGNC:6879
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: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0507566
3-(4-ethoxyphenyl)-N-[1-(1-methylpiperidin-4-yl)pyrazol-4-yl]triazolo[4,5-d]pyrimidin-5-amine
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C21H25N9O
 1
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0548561
3-(4-methoxyphenyl)-N-[(3R)-1-pyridin-4-ylpyrrolidin-3-yl]triazolo[4,5-d]pyrimidin-5-amine
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C20H20N8O
 1
1
IC50 = 38 nM
   TI
   LI
   LO
   TS
CP0553235
5-fluoro-2-[5-[[1-(1-methylpiperidin-4-yl)pyrazol-4-yl]amino]triazolo[4,5-d]pyrimidin-3-yl]benzonitrile
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C20H19FN10
 1
1
IC50 = 55 nM
   TI
   LI
   LO
   TS
CP0548555
N-[1-(1-methylpiperidin-4-yl)pyrazol-4-yl]-3-(1-methylpyrazol-3-yl)triazolo[4,5-d]pyrimidin-5-amine
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C17H21N11
 1
1
IC50 = 165 nM
   TI
   LI
   LO
   TS
CP0451009
N-[4-(aminomethyl)cyclohexyl]-3-(4-methoxyphenyl)triazolo[4,5-d]pyrimidin-5-amine
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C18H23N7O
 1
1
IC50 = 368 nM
   TI
   LI
   LO
   TS
CP0451006
4-N-[3-(4-methoxyphenyl)triazolo[4,5-d]pyrimidin-5-yl]cyclohexane-1,4-diamine
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C17H21N7O
 1
1
IC50 = 549 nM
   TI
   LI
   LO
   TS
CP0444137
(1R,3R)-3-N-[3-(4-methoxyphenyl)triazolo[4,5-d]pyrimidin-5-yl]cyclopentane-1,3-diamine
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C16H19N7O
 1
1
IC50 = 736 nM
   TI
   LI
   LO
   TS
CP0451007
(1S,3S)-3-N-[3-(4-methoxyphenyl)triazolo[4,5-d]pyrimidin-5-yl]cyclopentane-1,3-diamine
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C16H19N7O
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0551813
(1S,3R)-3-N-[3-(4-methoxyphenyl)triazolo[4,5-d]pyrimidin-5-yl]cyclopentane-1,3-diamine
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C16H19N7O
 1
1
IC50 = 3400 nM
   TI
   LI
   LO
   TS
CP0955839
(1R,3R)-N3-[3-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]cyclopentane-1,3-diamine
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C17H20N6O
 1
1
IC50 = 7160 nM
   TI
   LI
   LO
   TS
CP0451008
3-(4-methoxyphenyl)-N-[(3S)-1-pyridin-4-ylpyrrolidin-3-yl]triazolo[4,5-d]pyrimidin-5-amine
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C20H20N8O
 1
1
IC50 = 8600 nM
   TI
   LI
   LO
   TS
CP0552747
(1R,3S)-3-N-[3-(4-methoxyphenyl)triazolo[4,5-d]pyrimidin-5-yl]cyclopentane-1,3-diamine
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C16H19N7O
 1
1
IC50 = 9360 nM
   TI
   LI
   LO
   TS
CP0551811
(1R,3R)-3-N-[1-(4-methoxyphenyl)triazolo[4,5-c]pyridin-6-yl]cyclopentane-1,3-diamine
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C17H20N6O
 1
1
IC50 = 13500 nM
   TI
   LI
   LO
   TS
CP0095473
US10525036, Example GDC-0994
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C21H18ClFN6O2
 1
1
IC50 = 21800 nM
   TI
   LI
   LO
   TS
CP0553236
[4-[[3-(4-methoxyphenyl)triazolo[4,5-d]pyrimidin-5-yl]amino]cyclohexyl]methanol
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C18H22N6O2
 1
1
IC50 = 26000 nM
   TI
   LI
   LO
   TS
CP0554919
(1R,3S)-3-N-[1-(4-methoxyphenyl)pyrazolo[3,4-d]pyrimidin-6-yl]cyclopentane-1,3-diamine
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C17H20N6O
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0560233
(1R,3R)-3-N-[9-(4-methoxyphenyl)purin-2-yl]cyclopentane-1,3-diamine
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C17H20N6O
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0507566
3-(4-ethoxyphenyl)-N-[1-(1-methylpiperidin-4-yl)pyrazol-4-yl]triazolo[4,5-d]pyrimidin-5-amine
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C21H25N9O
 1
1 IC50 = 33 nM
CP0548555
N-[1-(1-methylpiperidin-4-yl)pyrazol-4-yl]-3-(1-methylpyrazol-3-yl)triazolo[4,5-d]pyrimidin-5-amine
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C17H21N11
 1
1 IC50 = 49 nM
CP0548561
3-(4-methoxyphenyl)-N-[(3R)-1-pyridin-4-ylpyrrolidin-3-yl]triazolo[4,5-d]pyrimidin-5-amine
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C20H20N8O
 1
1 IC50 = 73 nM
CP0451009
CHEMBL4784697
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C18H23N7O
 1
1 IC50 = 143 nM
CP0444137
(1R,3R)-3-N-[3-(4-methoxyphenyl)triazolo[4,5-d]pyrimidin-5-yl]cyclopentane-1,3-diamine
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C16H19N7O
 1
1 IC50 = 157 nM
CP0553235
5-fluoro-2-[5-[[1-(1-methylpiperidin-4-yl)pyrazol-4-yl]amino]triazolo[4,5-d]pyrimidin-3-yl]benzonitrile
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C20H19FN10
 1
1 IC50 = 177 nM
CP0451006
CHEMBL4759319
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C17H21N7O
 1
1 IC50 = 300 nM
CP0551813
(1S,3R)-3-N-[3-(4-methoxyphenyl)triazolo[4,5-d]pyrimidin-5-yl]cyclopentane-1,3-diamine
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C16H19N7O
 1
1 IC50 = 860 nM
CP0451007
(1S,3S)-3-N-[3-(4-methoxyphenyl)triazolo[4,5-d]pyrimidin-5-yl]cyclopentane-1,3-diamine
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C16H19N7O
 1
1 IC50 = 1970 nM
CP0451008
3-(4-methoxyphenyl)-N-[(3S)-1-pyridin-4-ylpyrrolidin-3-yl]triazolo[4,5-d]pyrimidin-5-amine
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C20H20N8O
 1
1 IC50 = 2200 nM
CP0552747
(1R,3S)-3-N-[3-(4-methoxyphenyl)triazolo[4,5-d]pyrimidin-5-yl]cyclopentane-1,3-diamine
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C16H19N7O
 1
1 IC50 = 5000 nM
CP0955839
(1R,3R)-N3-[3-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]cyclopentane-1,3-diamine
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C17H20N6O
 1
1 IC50 = 6000 nM
CP0551811
(1R,3R)-3-N-[1-(4-methoxyphenyl)triazolo[4,5-c]pyridin-6-yl]cyclopentane-1,3-diamine
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C17H20N6O
 1
1 IC50 = 18000 nM
CP0553236
CHEMBL4764076
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C18H22N6O2
 1
1 IC50 > 30000 nM
CP0554919
(1R,3S)-3-N-[1-(4-methoxyphenyl)pyrazolo[3,4-d]pyrimidin-6-yl]cyclopentane-1,3-diamine
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C17H20N6O
 1
1 IC50 > 30000 nM
CP0560233
(1R,3R)-3-N-[9-(4-methoxyphenyl)purin-2-yl]cyclopentane-1,3-diamine
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C17H20N6O
 1
1 IC50 > 30000 nM