Top ▲

mitogen-activated protein kinase 7

Click here for help

Target not currently curated in GtoImmuPdb

Target id: 2093

Nomenclature: mitogen-activated protein kinase 7

Abbreviated Name: ERK5

Family: ERK subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 816 17p11.2 MAPK7 mitogen-activated protein kinase 7
Mouse - 806 11 B2 Mapk7 mitogen-activated protein kinase 7
Rat - 806 10q22 Mapk7 mitogen-activated protein kinase 7
Previous and Unofficial Names Click here for help
big MAP kinase 1 | BMK1 | MAP kinase 7 | PRKM7 | extracellular signal-regulated kinase 5
Database Links Click here for help
Alphafold Q13164 (Hs), Q9WVS8 (Mm), P0C865 (Rn)
BRENDA 2.7.11.24
CATH/Gene3D 1.25.10.10
ChEMBL Target CHEMBL5332 (Hs)
Ensembl Gene ENSG00000166484 (Hs), ENSMUSG00000001034 (Mm), ENSRNOG00000047907 (Rn)
Entrez Gene 5598 (Hs), 23939 (Mm), 114509 (Rn)
Human Protein Atlas ENSG00000166484 (Hs)
KEGG Enzyme 2.7.11.24
KEGG Gene hsa:5598 (Hs), mmu:23939 (Mm), rno:114509 (Rn)
OMIM 602521 (Hs)
Pharos Q13164 (Hs)
RefSeq Nucleotide NM_002749 (Hs), NM_011841 (Mm), NM_001191547 (Rn)
RefSeq Protein NP_002740 (Hs), NP_035971 (Mm), NP_001178476 (Rn)
SynPHARM 81091 (in complex with XMD8-92)
UniProtKB Q13164 (Hs), Q9WVS8 (Mm), P0C865 (Rn)
Wikipedia MAPK7 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of MAPK7 (ERK5) with inhibitor
PDB Id:  4B99
Resolution:  2.8Å
Species:  Human
References:  3
Enzyme Reaction Click here for help
EC Number: 2.7.11.24

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
XMD8-92 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.1 pKd 9
⤷ pKd 7.1 (Kd 8x10-8 M) [9]
AX15836 Small molecule or natural product Hs Inhibition 8.1 pIC50 5
⤷ pIC50 8.1 (IC50 8x10-9 M) [5]
BAY-885 Small molecule or natural product Primary target of this compound Hs Inhibition 7.5 pIC50 6
⤷ pIC50 7.5 (IC50 3.5x10-8 M) [6]
Description: Biochemical inhibition of phosphorylation of a synthetic peptide substrate.
BIX02189 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.2 pIC50 7
⤷ pIC50 7.2 (IC50 5.9x10-8 M) [7]
XMD17-109 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 6.8 pIC50 2
⤷ pIC50 6.8 (IC50 1.62x10-7 M) [2]
Description: In a cell-free biochemical assay.
BIX02188 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.1 pIC50 7
⤷ pIC50 6.1 (IC50 8.1x10-7 M) [7]
DCLK1-IN-1 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.7 pIC50 4
⤷ pIC50 5.7 (IC50 1.8x10-6 M) [4]
Description: Determined in a KinomeScan binding assay.
DiscoveRx KINOMEscan® screen Click here for help
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 1,8
Key to terms and symbols Click column headers to sort
Target used in screen: ERK5
Ligand Sp. Type Action Value Parameter
AT-7519 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
R547 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.3 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
BMS-345541 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 6.2 pKd
BMS-387032 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.0 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.8 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Immune regulation
Immuno Process:  Cytokine production & signalling

References

Show »

1. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1046-51. [PMID:22037378]

2. Deng X, Elkins JM, Zhang J, Yang Q, Erazo T, Gomez N, Choi HG, Wang J, Dzamko N, Lee JD et al.. (2013) Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. Eur J Med Chem, 70: 758-67. [PMID:24239623]

3. Elkins JM, Wang J, Deng X, Pattison MJ, Arthur JS, Erazo T, Gomez N, Lizcano JM, Gray NS, Knapp S. (2013) X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor. J Med Chem, 56 (11): 4413-21. [PMID:23656407]

4. Ferguson FM, Nabet B, Raghavan S, Liu Y, Leggett AL, Kuljanin M, Kalekar RL, Yang A, He S, Wang J et al.. (2020) Discovery of a selective inhibitor of doublecortin like kinase 1. Nat Chem Biol, 16 (6): 635-643. [PMID:32251410]

5. Lin EC, Amantea CM, Nomanbhoy TK, Weissig H, Ishiyama J, Hu Y, Sidique S, Li B, Kozarich JW, Rosenblum JS. (2016) ERK5 kinase activity is dispensable for cellular immune response and proliferation. Proc Natl Acad Sci U S A, 113 (42): 11865-11870. [PMID:27679845]

6. Nguyen D, Lemos C, Wortmann L, Eis K, Holton SJ, Boemer U, Moosmayer D, Eberspaecher U, Weiske J, Lechner C et al.. (2019) Discovery and Characterization of the Potent and Highly Selective (Piperidin-4-yl)pyrido[3,2- d]pyrimidine Based in Vitro Probe BAY-885 for the Kinase ERK5. J Med Chem, 62 (2): 928-940. [PMID:30563338]

7. Tatake RJ, O'Neill MM, Kennedy CA, Wayne AL, Jakes S, Wu D, Kugler Jr SZ, Kashem MA, Kaplita P, Snow RJ. (2008) Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem Biophys Res Commun, 377 (1): 120-5. [PMID:18834865]

8. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem Biol, 17 (11): 1241-9. [PMID:21095574]

9. Yang Q, Deng X, Lu B, Cameron M, Fearns C, Patricelli MP, Yates 3rd JR, Gray NS, Lee JD. (2010) Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell, 18 (3): 258-67. [PMID:20832753]

How to cite this page

ERK subfamily: mitogen-activated protein kinase 7. Last modified on 28/04/2022. Accessed on 11/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2093.