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Target Report Card

Target Name and Classification

Target ID CHEMBL4040
Preferred Name MAP kinase ERK2
Synonyms ERK-2 | ERK2 | ERT1 | Extracellular signal-regulated kinase 2 | MAP kinase 1 | MAP kinase 2 | MAP kinase isoform p42 | MAPK 1 | MAPK 2 | MAPK1 | Mitogen-activated protein kinase 1 | Mitogen-activated protein kinase 2 | PRKM1 | PRKM2 | p42-MAPK
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > cmgc protein kinase group > cmgc protein kinase mapk family > cmgc protein kinase erk subfamily

Target Components

Component Description Relationship Accession
Mitogen-activated protein kinase 1 SINGLE PROTEIN P28482

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL1907606 Mitogen-activated protein kinase; ERK1/ERK2 PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL3545022 Ulixertinib MAP kinase ERK2 inhibitor 2 DOI Other
CHEMBL3544964 GDC-0994 MAP kinase ERK2 inhibitor 1 Other
CHEMBL3545001 MK-8353 MAP kinase ERK2 inhibitor 1 Other

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000100030
Ensembl ENSG00000100030
GO Cellular Component GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0005737 (cytoplasm)
GO:0005739 (mitochondrion)
GO:0005769 (early endosome)
GO:0005770 (late endosome)
GO:0005794 (Golgi apparatus)
GO:0005815 (microtubule organizing center)
GO:0005819 (spindle)
GO:0005829 (cytosol)
GO:0005856 (cytoskeleton)
GO:0005901 (caveola)
GO:0005925 (focal adhesion)
GO:0015630 (microtubule cytoskeleton)
GO:0030424 (axon)
GO:0031143 (pseudopodium)
GO:0032839 (dendrite cytoplasm)
GO:0043204 (perikaryon)
GO:0043234 (protein complex)
GO:0070062 (extracellular exosome)
GO:0072686 (mitotic spindle)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0001784 (phosphotyrosine binding)
GO:0003677 (DNA binding)
GO:0004672 (protein kinase activity)
GO:0004674 (protein serine/threonine kinase activity)
GO:0004707 (MAP kinase activity)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0008134 (transcription factor binding)
GO:0008353 (RNA polymerase II carboxy-terminal domain kinase activity)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0019901 (protein kinase binding)
GO:0019902 (phosphatase binding)
GO:0031435 (mitogen-activated protein kinase kinase kinase binding)
GO:0042802 (identical protein binding)
GO Biological Process GO:0000165 (MAPK cascade)
GO:0000187 (activation of MAPK activity)
GO:0000189 (MAPK import into nucleus)
GO:0006351 (transcription, DNA-templated)
GO:0006355 (regulation of transcription, DNA-templated)
GO:0006468 (protein phosphorylation)
GO:0006915 (apoptotic process)
GO:0006935 (chemotaxis)
GO:0006950 (response to stress)
GO:0006974 (cellular response to DNA damage stimulus)
GO:0007049 (cell cycle)
GO:0007165 (signal transduction)
GO:0007268 (chemical synaptic transmission)
GO:0007411 (axon guidance)
GO:0007507 (heart development)
GO:0008284 (positive regulation of cell proliferation)
GO:0008543 (fibroblast growth factor receptor signaling pathway)
GO:0009636 (response to toxic substance)
GO:0009887 (organ morphogenesis)
GO:0010800 (positive regulation of peptidyl-threonine phosphorylation)
GO:0014032 (neural crest cell development)
GO:0014066 (regulation of phosphatidylinositol 3-kinase signaling)
GO:0016032 (viral process)
GO:0016310 (phosphorylation)
GO:0018105 (peptidyl-serine phosphorylation)
GO:0018107 (peptidyl-threonine phosphorylation)
GO:0019233 (sensory perception of pain)
GO:0019858 (cytosine metabolic process)
GO:0030168 (platelet activation)
GO:0030335 (positive regulation of cell migration)
GO:0030878 (thyroid gland development)
GO:0031647 (regulation of protein stability)
GO:0031663 (lipopolysaccharide-mediated signaling pathway)
GO:0032212 (positive regulation of telomere maintenance via telomerase)
GO:0032496 (response to lipopolysaccharide)
GO:0032872 (regulation of stress-activated MAPK cascade)
GO:0033598 (mammary gland epithelial cell proliferation)
GO:0035556 (intracellular signal transduction)
GO:0038095 (Fc-epsilon receptor signaling pathway)
GO:0038096 (Fc-gamma receptor signaling pathway involved in phagocytosis)
GO:0038127 (ERBB signaling pathway)
GO:0042473 (outer ear morphogenesis)
GO:0043330 (response to exogenous dsRNA)
GO:0043627 (response to estrogen)
GO:0045596 (negative regulation of cell differentiation)
GO:0045727 (positive regulation of translation)
GO:0045893 (positive regulation of transcription, DNA-templated)
GO:0048538 (thymus development)
GO:0050852 (T cell receptor signaling pathway)
GO:0050853 (B cell receptor signaling pathway)
GO:0051090 (regulation of sequence-specific DNA binding transcription factor activity)
GO:0051493 (regulation of cytoskeleton organization)
GO:0051973 (positive regulation of telomerase activity)
GO:0060020 (Bergmann glial cell differentiation)
GO:0060291 (long-term synaptic potentiation)
GO:0060324 (face development)
GO:0060397 (JAK-STAT cascade involved in growth hormone signaling pathway)
GO:0060425 (lung morphogenesis)
GO:0060440 (trachea formation)
GO:0060716 (labyrinthine layer blood vessel development)
GO:0061308 (cardiac neural crest cell development involved in heart development)
GO:0070371 (ERK1 and ERK2 cascade)
GO:0070849 (response to epidermal growth factor)
GO:0071310 (cellular response to organic substance)
GO:0072584 (caveolin-mediated endocytosis)
GO:0090170 (regulation of Golgi inheritance)
GO:0097011 (cellular response to granulocyte macrophage colony-stimulating factor stimulus)
GO:1900034 (regulation of cellular response to heat)
GO:1904355 (positive regulation of telomere capping)
GO:2000641 (regulation of early endosome to late endosome transport)
Wikipedia MAPK1

Target Cross References - Protein

canSAR P28482
Human Protein Atlas ENSG00000100030
IntAct P28482
Guide to Pharmacology 1495
Open Targets ENSG00000100030
PharmGKB PA30616
Pharos P28482 (Tchem)
Reactome R-HSA-111995 (phospho-PLA2 pathway.)
R-HSA-112409 (RAF-independent MAPK1/3 activation.)
R-HSA-112411 (MAPK1 (ERK2) activation.)
R-HSA-1295596 (Spry regulation of FGF signaling.)
R-HSA-162658 (Golgi Cisternae Pericentriolar Stack Reorganization.)
R-HSA-198753 (ERK/MAPK targets.)
R-HSA-202670 (ERKs are inactivated.)
R-HSA-2029482 (Regulation of actin dynamics for phagocytic cup formation.)
R-HSA-2559580 (Oxidative Stress Induced Senescence.)
R-HSA-2559582 (Senescence-Associated Secretory Phenotype (SASP).)
R-HSA-2559585 (Oncogene Induced Senescence.)
R-HSA-2871796 (FCERI mediated MAPK activation.)
R-HSA-3371453 (Regulation of HSF1-mediated heat shock response.)
R-HSA-375165 (NCAM signaling for neurite out-growth.)
R-HSA-437239 (Recycling pathway of L1.)
R-HSA-442742 (CREB phosphorylation through the activation of Ras.)
R-HSA-444257 (RSK activation.)
R-HSA-445144 (Signal transduction by L1.)
R-HSA-450341 (Activation of the AP-1 family of transcription factors.)
R-HSA-456926 (Thrombin signalling through proteinase activated receptors (PARs).)
R-HSA-5654726 (Negative regulation of FGFR1 signaling.)
R-HSA-5654727 (Negative regulation of FGFR2 signaling.)
R-HSA-5654732 (Negative regulation of FGFR3 signaling.)
R-HSA-5654733 (Negative regulation of FGFR4 signaling.)
R-HSA-5663213 (RHO GTPases Activate WASPs and WAVEs.)
R-HSA-5673001 (RAF/MAP kinase cascade.)
R-HSA-5674135 (MAP2K and MAPK activation.)
R-HSA-5674499 (Negative feedback regulation of MAPK pathway.)
R-HSA-5675221 (Negative regulation of MAPK pathway.)
R-HSA-6798695 (Neutrophil degranulation.)
R-HSA-6802946 (Signaling by moderate kinase activity BRAF mutants.)
R-HSA-6802948 (Signaling by high-kinase activity BRAF mutants.)
R-HSA-6802949 (Signaling by RAS mutants.)
R-HSA-6802952 (Signaling by BRAF and RAF fusions.)
R-HSA-6802955 (Paradoxical activation of RAF signaling by kinase inactive BRAF.)
R-HSA-6811558 (PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling.)
R-HSA-74749 (Signal attenuation.)
R-HSA-879415 (Advanced glycosylation endproduct receptor signaling.)
R-HSA-881907 (Gastrin-CREB signalling pathway via PKC and MAPK.)
R-HSA-982772 (Growth hormone receptor signaling.)
UniProt A8CZ64 P28482

Target Cross References - Domain

InterPro IPR000719 (Prot_kinase_dom.)
IPR003527 (MAP_kinase_CS.)
IPR008271 (Ser/Thr_kinase_AS.)
IPR008349 (MAPK_ERK1/2.)
IPR011009 (Kinase-like_dom.)
IPR017441 (Protein_kinase_ATP_BS.)
Pfam PF00069 (Pkinase)

Target Cross References - Structure

PDBe 1PME 1TVO 1WZY 2OJG 2OJI 2OJJ 2Y9Q 3D42 3D44 3I5Z 3I60 3SA0 3TEI 3W55 4FMQ 4FUX 4FUY 4FV0 4FV1 4FV2 4FV3 4FV4 4FV5 4FV6 More...
CREDO 1PME 1TVO 1WZY 2OJG 2OJI 2OJJ 2Y9Q 3D42 3D44 3I5Z 3I60 3SA0 3TEI 3W55 4FMQ 4FUX 4FUY 4FV0 4FV1 4FV2 4FV3 4FV4 4FV5 4FV6 More...