General Information of the Protein
Protein ID
PT03500
Protein Name
Mitogen-activated protein kinase 1
Secondarily
Protein Name
ERT1
Extracellular signal-regulated kinase 2
MAP kinase isoform p42
Mitogen-activated protein kinase 2
Gene Name
MAPK1
Secondarily
Gene Name
Erk2
Mapk
Prkm1
Sequence
MAAAAAAGPEMVRGQVFDVGPRYTNLSYIGEGAYGMVCSAYDNLNKVRVAIKKISPFEHQTYCQRTLREIKILLRFRHENIIGINDIIRAPTIEQMKDVYIVQDLMETDLYKLLKTQHLSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLLNTTCDLKICDFGLARVADPDHDHTGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLSNRPIFPGKHYLDQLNHILGILGSPSQEDLNCIINLKARNYLLSLPHKNKVPWNRLFPNADSKALDLLDKMLTFNPHKRIEVEQALAHPYLEQYYDPSDEPIAEAPFKFDMELDDLPKEKLKELIFEETARFQPGYRS
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Organism
Mus musculus, Mouse
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
CMGC protein kinase group
>
CMGC protein kinase MAPK family
>
CMGC protein kinase ERK subfamily
Function
Serine/threonine kinase which acts as an essential component of the MAP kinase signal transduction pathway. MAPK1/ERK2 and MAPK3/ERK1 are the 2 MAPKs which play an important role in the MAPK/ERK cascade. They participate also in a signaling cascade initiated by activated KIT and KITLG/SCF. Depending on the cellular context, the MAPK/ERK cascade mediates diverse biological functions such as cell growth, adhesion, survival and differentiation through the regulation of transcription, translation, cytoskeletal rearrangements. The MAPK/ERK cascade also plays a role in initiation and regulation of meiosis, mitosis, and postmitotic functions in differentiated cells by phosphorylating a number of transcription factors. About 160 substrates have already been discovered for ERKs. Many of these substrates are localized in the nucleus, and seem to participate in the regulation of transcription upon stimulation. However, other substrates are found in the cytosol as well as in other cellular organelles, and those are responsible for processes such as translation, mitosis and apoptosis. Moreover, the MAPK/ERK cascade is also involved in the regulation of the endosomal dynamics, including lysosome processing and endosome cycling through the perinuclear recycling compartment (PNRC); as well as in the fragmentation of the Golgi apparatus during mitosis. The substrates include transcription factors (such as ATF2, BCL6, ELK1, ERF, FOS, HSF4 or SPZ1), cytoskeletal elements (such as CANX, CTTN, GJA1, MAP2, MAPT, PXN, SORBS3 or STMN1), regulators of apoptosis (such as BAD, BTG2, CASP9, DAPK1, IER3, MCL1 or PPARG), regulators of translation (such as EIF4EBP1 and FXR1) and a variety of other signaling-related molecules (like ARHGEF2, DCC, FRS2 or GRB10). Protein kinases (such as RAF1, RPS6KA1/RSK1, RPS6KA3/RSK2, RPS6KA2/RSK3, RPS6KA6/RSK4, SYK, MKNK1/MNK1, MKNK2/MNK2, RPS6KA5/MSK1, RPS6KA4/MSK2, MAPKAPK3 or MAPKAPK5) and phosphatases (such as DUSP1, DUSP4, DUSP6 or DUSP16) are other substrates which enable the propagation the MAPK/ERK signal to additional cytosolic and nuclear targets, thereby extending the specificity of the cascade. Mediates phosphorylation of TPR in response to EGF stimulation. May play a role in the spindle assembly checkpoint. Phosphorylates PML and promotes its interaction with PIN1, leading to PML degradation. Phosphorylates CDK2AP2 (By similarity).
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Uniprot ID
Primary ID:
P63085

Secondarily ID:
P27703
Q3V1U6
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Ensembl ID
ENSG00000100030
Subcellular Location
Cytoplasm
Cytoskeleton
Spindle
Nucleus
Cytoplasm
Cytoskeleton
Microtubule organizing center
Centrosome
Cytoplasm
Membrane
Caveola
Cell junction
Focal adhesion
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: CL000169 , P19
Compound ID Compound Name Compound Formula
CP0004106
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one
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C28H26N4O3
 1
1
IC50 > 10000 nM
   TI
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CP0005230
3-(1-Benzo[b]thiophen-2-yl-1H-indol-3-yl)-4-[1-(3-dimethylamino-propyl)-1H-indazol-3-yl]-pyrrole-2,5-dione
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C32H27N5O2S
 1
1
IC50 > 10000 nM
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CP0005235
3-[1-(3-Dimethylamino-propyl)-1H-indazol-3-yl]-4-[1-(1,4,4a,8a-tetrahydro-naphthalen-1-yl)-1H-indol-3-yl]-pyrrole-2,5-dione
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C34H29N5O2
 1
1
IC50 > 10000 nM
   TI
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CP0008384
3-[1-(3-Dimethylamino-propyl)-1H-indazol-3-yl]-4-[1-(1,4,4a,8a-tetrahydro-naphthalen-2-yl)-1H-indol-3-yl]-pyrrole-2,5-dione
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C34H29N5O2
 1
1
IC50 > 10000 nM
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CP0008485
3-[1-(3-Dimethylamino-propyl)-1H-indazol-3-yl]-4-(1-pyridin-3-yl-1H-indol-3-yl)-pyrrole-2,5-dione
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C29H26N6O2
 1
1
IC50 > 10000 nM
   TI
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CP0013045
3-[1-(3-Dimethylamino-propyl)-1H-indazol-3-yl]-4-(1-quinolin-3-yl-1H-indol-3-yl)-pyrrole-2,5-dione
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C33H28N6O2
 1
1
IC50 > 10000 nM
   TI
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CP0013222
3-[1-(3-Dimethylamino-propyl)-1H-indazol-3-yl]-4-(1-thiophen-2-yl-1H-indol-3-yl)-pyrrole-2,5-dione
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C28H25N5O2S
 1
1
IC50 > 10000 nM
   TI
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   TS