General Information of the Protein
Protein ID
PT02258
Protein Name
MAP kinase-interacting serine/threonine-protein kinase 1
Secondarily
Protein Name
MAP kinase signal-integrating kinase 1
Gene Name
MKNK1
Secondarily
Gene Name
MNK1
Sequence
MVSSQKLEKPIEMGSSEPLPIADGDRRRKKKRRGRATDSLPGKFEDMYKLTSELLGEGAYAKVQGAVSLQNGKEYAVKIIEKQAGHSRSRVFREVETLYQCQGNKNILELIEFFEDDTRFYLVFEKLQGGSILAHIQKQKHFNEREASRVVRDVAAALDFLHTKDKVSLCHLGWSAMAPSGLTAAPTSLGSSDPPTSASQVAGTTGIAHRDLKPENILCESPEKVSPVKICDFDLGSGMKLNNSCTPITTPELTTPCGSAEYMAPEVVEVFTDQATFYDKRCDLWSLGVVLYIMLSGYPPFVGHCGADCGWDRGEVCRVCQNKLFESIQEGKYEFPDKDWAHISSEAKDLISKLLVRDAKQRLSAAQVLQHPWVQGQAPEKGLPTPQVLQRNSSTMDLTLFAAEAIALNRQLSQHEENELAEEPEALADGLCSMKLSPPCKSRLARRRALAQAGRGEDRSPPTAL
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
CAMK protein kinase group
>
CAMK protein kinase MAPKAPK family
>
CAMK protein kinase MNK subfamily
Function
May play a role in the response to environmental stress and cytokines. Appears to regulate translation by phosphorylating EIF4E, thus increasing the affinity of this protein for the 7-methylguanosine-containing mRNA cap.
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Uniprot ID
Primary ID:
Q9BUB5

Secondarily ID:
D3DQ20
D3DQ21
O00312
Q5TC06
Q5TC07
Q6V0N6
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Ensembl ID
ENSG00000079277
HGNC ID
HGNC:7110
Subcellular Location
Cytoplasm
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: CL000012 , Sf21
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0571091
 Compound Info 
[(3S)-3-aminopiperidin-1-yl]-[4-(3-isoquinolin-6-ylimidazo[1,2-b]pyridazin-6-yl)phenyl]methanone
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C27H24N6O
  1
1
IC50 = 2.3 nM
 Bioactivity Info 
   TI
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CP0550874
 Compound Info 
[4-(3-isoquinolin-6-ylimidazo[1,2-a]pyridin-6-yl)phenyl]-(4-piperidin-1-ylpiperidin-1-yl)methanone
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C33H33N5O
  1
1
IC50 = 2.4 nM
 Bioactivity Info 
   TI
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CP0572219
 Compound Info 
[(3S)-3-aminopiperidin-1-yl]-[4-(3-isoquinolin-6-ylimidazo[1,2-a]pyridin-6-yl)phenyl]methanone
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C28H25N5O
  1
1
IC50 = 2.5 nM
 Bioactivity Info 
   TI
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CP0569513
 Compound Info 
[4-(3-isoquinolin-6-ylimidazo[1,2-a]pyridin-6-yl)phenyl]-(4-morpholin-4-ylpiperidin-1-yl)methanone
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C32H31N5O2
  1
1
IC50 = 4 nM
 Bioactivity Info 
   TI
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CP0550873
 Compound Info 
[4-(3-isoquinolin-6-ylimidazo[1,2-a]pyridin-6-yl)phenyl]-morpholin-4-ylmethanone
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C27H22N4O2
  1
1
IC50 = 7 nM
 Bioactivity Info 
   TI
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CP0565075
 Compound Info 
[(3R)-3-aminopiperidin-1-yl]-[4-(3-isoquinolin-6-ylimidazo[1,2-a]pyridin-6-yl)phenyl]methanone
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C28H25N5O
  1
1
IC50 = 7.7 nM
 Bioactivity Info 
   TI
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CP0550876
 Compound Info 
[(3R)-3-aminopiperidin-1-yl]-[4-(3-isoquinolin-6-ylimidazo[1,2-b]pyridazin-6-yl)phenyl]methanone
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C27H24N6O
  1
1
IC50 = 9.4 nM
 Bioactivity Info 
   TI
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CP0570182
 Compound Info 
[4-(3-isoquinolin-6-ylimidazo[1,2-a]pyridin-6-yl)phenyl]-piperazin-1-ylmethanone
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C27H23N5O
  1
1
IC50 = 9.4 nM
 Bioactivity Info 
   TI
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CP0491640
 Compound Info 
4-(6-(4-(morpholine-4-carbonyl)phenyl)imidazo[1,2-a]pyridin-3-yl)benzonitrile
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C25H20N4O2
  1
1
IC50 = 10.6 nM
 Bioactivity Info 
   TI
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CP0563463
 Compound Info 
(4-aminopiperidin-1-yl)-[4-(3-isoquinolin-6-ylimidazo[1,2-b]pyridazin-6-yl)phenyl]methanone
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C27H24N6O
  1
1
IC50 = 14.5 nM
 Bioactivity Info 
   TI
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CP0569548
 Compound Info 
(4-aminopiperidin-1-yl)-[4-(3-isoquinolin-6-ylimidazo[1,2-a]pyridin-6-yl)phenyl]methanone
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C28H25N5O
  1
1
IC50 = 16.8 nM
 Bioactivity Info 
   TI
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CP0564225
 Compound Info 
[(3S)-3-aminopiperidin-1-yl]-[4-(3-isoquinolin-6-ylimidazo[1,2-a]pyrazin-6-yl)phenyl]methanone
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C27H24N6O
  1
1
IC50 = 27.3 nM
 Bioactivity Info 
   TI
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CP0569583
 Compound Info 
(4-aminopiperidin-1-yl)-[4-(3-isoquinolin-6-ylimidazo[1,2-a]pyrazin-6-yl)phenyl]methanone
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C27H24N6O
  1
1
IC50 = 32.1 nM
 Bioactivity Info 
   TI
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CP0569550
 Compound Info 
[(3R)-3-aminopiperidin-1-yl]-[4-(3-isoquinolin-6-ylimidazo[1,2-a]pyrazin-6-yl)phenyl]methanone
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C27H24N6O
  1
1
IC50 = 42 nM
 Bioactivity Info 
   TI
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CP0550877
 Compound Info 
piperazin-1-yl-[4-(3-quinolin-3-ylimidazo[1,2-a]pyridin-6-yl)phenyl]methanone
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C27H23N5O
  1
1
IC50 = 67.6 nM
 Bioactivity Info 
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CP0563538
 Compound Info 
morpholin-4-yl-[4-(3-quinolin-3-ylimidazo[1,2-a]pyridin-6-yl)phenyl]methanone
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C27H22N4O2
  1
1
IC50 = 153.7 nM
 Bioactivity Info 
   TI
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CP0550875
 Compound Info 
morpholin-4-yl-[4-(3-quinolin-6-ylimidazo[1,2-a]pyridin-6-yl)phenyl]methanone
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C27H22N4O2
  1
1
IC50 = 370.8 nM
 Bioactivity Info 
   TI
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0015547
 Compound Info 
CGP-57380
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C11H9FN6
  4
1 IC50 = 850 nM
2 IC50 = 870 nM
3 IC50 = 2740 nM
4 Ki = 1010 nM
Clinical Information about the Protein
Target 1 ( MAPK signal-integrating kinase 1 (MKNK1) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Colorectal cancer [ICD-11: 2B91.Z]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 EFT508
 Drug Info 
Phase 2
Colorectal cancer