General Information of the Protein
Protein ID
PT01379
Protein Name
Dual specificity mitogen-activated protein kinase kinase 2
Secondarily
Protein Name
ERK activator kinase 2
MAPK/ERK kinase 2
Gene Name
MAP2K2
Secondarily
Gene Name
MEK2
MKK2
PRKMK2
Sequence
MLARRKPVLPALTINPTIAEGPSPTSEGASEANLVDLQKKLEELELDEQQKKRLEAFLTQKAKVGELKDDDFERISELGAGNGGVVTKVQHRPSGLIMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKEAKRIPEEILGKVSIAVLRGLAYLREKHQIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMAPERLQGTHYSVQSDIWSMGLSLVELAVGRYPIPPPDAKELEAIFGRPVVDGEEGEPHSISPRPRPPGRPVSGHGMDSRPAMAIFELLDYIVNEPPPKLPNGVFTPDFQEFVNKCLIKNPAERADLKMLTNHTFIKRSEVEEVDFAGWLCKTLRLNQPGTPTRTAV
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
STE protein kinase group
>
STE protein kinase STE7 family
Function
Catalyzes the concomitant phosphorylation of a threonine and a tyrosine residue in a Thr-Glu-Tyr sequence located in MAP kinases. Activates the ERK1 and ERK2 MAP kinases (By similarity). Activates BRAF in a KSR1 or KSR2-dependent manner; by binding to KSR1 or KSR2 releases the inhibitory intramolecular interaction between KSR1 or KSR2 protein kinase and N-terminal domains which promotes KSR1 or KSR2-BRAF dimerization and BRAF activation (PubMed:29433126).
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Uniprot ID
P36507
Ensembl ID
ENSG00000126934
HGNC ID
HGNC:6842
Subcellular Location
Cytoplasm
Membrane
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: CL000624 , B6
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0447664
 Compound Info 
2,2-dimethyl-N-[2-[[(2S)-1'-methyl-2',4'-dioxospiro[1,3-dihydroindene-2,5'-imidazolidine]-5-yl]amino]-2-oxoethyl]-N-[(1R)-1-phenylethyl]propanamide
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C27H32N4O4
  1
1
Ki = 670 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0327608
 Compound Info 
(S)-N-benzyl-N-(2-(3-methyl-2,5-dioxo-1',3'-dihydrospiro[imidazolidine-4,2'-indene]-5'-ylamino)-2-oxoethyl)pivalamide
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C26H30N4O4
  1
1
Ki = 710 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0428910
 Compound Info 
(+/-)-N-(3-fluorobenzyl)-N-(2-(3-methyl-2,5-dioxo-1',3'-dihydrospiro[imidazolidine-4,2'-indene]-5'-ylamino)-2-oxoethyl)pivalamide
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C26H29FN4O4
  1
1
Ki = 1400 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0447680
 Compound Info 
(+/-)-N-(3-chlorobenzyl)-N-(2-(3-methyl-2,5-dioxo-1',3'-dihydrospiro[imidazolidine-4,2'-indene]-5'-ylamino)-2-oxoethyl)pivalamide
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C26H29ClN4O4
  1
1
Ki = 1400 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0485748
 Compound Info 
N-[(1R)-1-(3,5-difluorophenyl)ethyl]-2,2-dimethyl-N-[2-[[(2S)-1'-methyl-2',4'-dioxospiro[1,3-dihydroindene-2,5'-imidazolidine]-5-yl]amino]-2-oxoethyl]propanamide
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C27H30F2N4O4
  1
1
Ki = 1400 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0428911
 Compound Info 
(S)-N-(3-chloro-5-fluorobenzyl)-N-(2-(3-methyl-2,5-dioxo-1',3'-dihydrospiro[imidazolidine-4,2'-indene]-5'-ylamino)-2-oxoethyl)pivalamide
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C26H28ClFN4O4
  1
1
Ki = 1800 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0469942
 Compound Info 
(+/-)-N-(2-(3-methyl-2,5-dioxo-1',3'-dihydrospiro[imidazolidine-4,2'-indene]-5'-ylamino)-2-oxoethyl)-N-(3-methylbenzyl)pivalamide
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C27H32N4O4
  1
1
Ki = 1800 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0415042
 Compound Info 
(S)-N-(3,5-dichlorobenzyl)-N-(2-(3-methyl-2,5-dioxo-1',3'-dihydrospiro[imidazolidine-4,2'-indene]-5'-ylamino)-2-oxoethyl)pivalamide
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C26H28Cl2N4O4
  1
1
Ki = 2100 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0401577
 Compound Info 
(S)-N-(3,5-difluorobenzyl)-N-(2-(3-methyl-2,5-dioxo-1',3'-dihydrospiro[imidazolidine-4,2'-indene]-5'-ylamino)-2-oxoethyl)pivalamide
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C26H28F2N4O4
  1
1
Ki = 2400 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0397184
 Compound Info 
(+/-)-N-(4-fluorobenzyl)-N-(2-(3-methyl-2,5-dioxo-1',3'-dihydrospiro[imidazolidine-4,2'-indene]-5'-ylamino)-2-oxoethyl)pivalamide
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C26H29FN4O4
  1
1
Ki = 3700 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0388412
 Compound Info 
(+/-)-N-(2-(3-methyl-2,5-dioxo-1',3'-dihydrospiro[imidazolidine-4,2'-indene]-5'-ylamino)-2-oxoethyl)-N-(4-(trifluoromethyl)benzyl)pivalamide
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C27H29F3N4O4
  1
1
Ki = 6200 nM
 Bioactivity Info 
   TI
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   LO
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CP0415041
 Compound Info 
(+/-)-N-(3-methoxybenzyl)-N-(2-(3-methyl-2,5-dioxo-1',3'-dihydrospiro[imidazolidine-4,2'-indene]-5'-ylamino)-2-oxoethyl)pivalamide
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C27H32N4O5
  1
1
Ki = 9700 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0430164
 Compound Info 
(+/-)-N-(3-cyanobenzyl)-N-(2-(3-methyl-2,5-dioxo-1',3'-dihydrospiro[imidazolidine-4,2'-indene]-5'-ylamino)-2-oxoethyl)pivalamide
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C27H29N5O4
  1
1
Ki = 13000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0388352
 Compound Info 
2,2-dimethyl-N-[2-[[(2S)-1'-methyl-2',4'-dioxospiro[1,3-dihydroindene-2,5'-imidazolidine]-5-yl]amino]-2-oxoethyl]-N-[(1S)-1-phenylethyl]propanamide
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C27H32N4O4
  1
1
Ki = 16000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Clinical Information about the Protein
Target 1 ( ERK activator kinase 2 (MEK2) )
Target Type Clinical trial Target
Disease 2 Target-related Diseases  2
1 Melanoma [ICD-11: 2C30]
2 Cardiac arrest [ICD-11: MC82]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 Selumetinib
 Drug Info 
Phase 3
Melanoma
Investigative Drug(s) 1 Investigative Drug  1
1 PD98059
 Drug Info 
Investigative
Cardiac arrest
Target 2 ( MEK2 messenger RNA (MEK2 mRNA) )
Target Type Literature-reported Target
Target 3 ( HUMAN ERK activator kinase 2 (MEK2) )
Target Type Unknown Type Target
Disease 2 Target-related Diseases  2
1 Neurofibromatosis type 1 [ICD-11: LD2D.10]
2 Metastatic melanoma [ICD-11: 2E2Z]
Investigative Drug(s) 2 Investigative Drugs  2
1 Selumetinib
 Drug Info 
Approved
Neurofibromatosis type 1
2 Trametinib
 Drug Info 
Approved
Metastatic melanoma