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Target
Glutathione S-transferase P/Isoform 2 of MAP kinase-interacting serine/threonine-protein kinase 1 (MNK1a) [T344D]
Ligand
BDBM259281
Substrate
n/a
Meas. Tech.
Kinase High ATP Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
17±n/a nM
Comments
extracted
Citation
 Eis, K; Puehler, F; Zorn, L; Scholz, A; Lienau, P; Gnoth, MJ; Bömer, U; Günther, J; Hitchcock, M Amino-substituted imidazopyridazines US Patent  US9499547 Publication Date 11/22/2016 
Target
Name:
Glutathione S-transferase P/Isoform 2 of MAP kinase-interacting serine/threonine-protein kinase 1 (MNK1a) [T344D]
Synonyms:
GST-MAP kinase-interacting serine/threonine-protein kinase 1 (MKNK1) (T344D) | Glutathione S-transferase P/MAP kinase-interacting serine/threonine-protein kinase 1 (MNK1a) [T344D]
Type:
Enzyme
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
Glutathione S-transferase P
Synonyms:
FAEES3 | GST class-pi | GST3 | GSTP1 | GSTP1-1 | GSTP1_HUMAN | Glutathione S-transferase | Glutathione S-transferase (GST) | Glutathione S-transferase P | Glutathione S-transferase Pi | Glutathione transferase (GST)
Type:
Enzyme
Mol. Mass.:
23353.53
Organism:
Homo sapiens (Human)
Description:
P09211
Residue:
210
Sequence:
MPPYTVVYFPVRGRCAALRMLLADQGQSWKEEVVTVETWQEGSLKASCLYGQLPKFQDGDLTLYQSNTILRHLGRTLGLYGKDQQEAALVDMVNDGVEDLRCKYISLIYTNYEAGKDDYVKALPGQLKPFETLLSQNQGGKTFIVGDQISFADYNLLDLLLIHEVLAPGCLDAFPLLSAYVGRLSARPKLKAFLASPEYVNLPINGNGKQ
  
Component 2
Name:
Isoform 2 of MAP kinase-interacting serine/threonine-protein kinase 1 (MNK1a) 344D]
Synonyms:
Isoform 2 of MAP kinase-interacting serine/threonine-protein kinase 1 (MNK1a) 344D] | Isoform 2 of MAP kinase-interacting serine/threonine-protein kinase 1 (MNK1a) [T344D] | MAP kinase signal-integrating kinase 1 (MNK1) (T344D) | MAP kinase-interacting serine/threonine-protein kinase 1 (MKNK1) | MAP kinase-interacting serine/threonine-protein kinase 1 (MKNK1) (T344D) | MAP kinase-interacting serine/threonine-protein kinase 1 (MKNK1)(T344D) | MAP kinase-interacting serine/threonine-protein kinase 1 (MNK1a) [T344D] | MAP kinase-interacting serine/threonine-protein kinase 1 (T344D) | MKNK1 | MKNK1 (aa 1-424) T344D | MKNK1_HUMAN | MNK1 | MNK1a
Type:
Protein
Mol. Mass.:
47416.00
Organism:
Homo sapiens (Human)
Description:
Q9BUB5-2 with T344D
Residue:
424
Sequence:
MVSSQKLEKPIEMGSSEPLPIADGDRRRKKKRRGRATDSLPGKFEDMYKLTSELLGEGAYAKVQGAVSLQNGKEYAVKIIEKQAGHSRSRVFREVETLYQCQGNKNILELIEFFEDDTRFYLVFEKLQGGSILAHIQKQKHFNEREASRVVRDVAAALDFLHTKGIAHRDLKPENILCESPEKVSPVKICDFDLGSGMKLNNSCTPITTPELTTPCGSAEYMAPEVVEVFTDQATFYDKRCDLWSLGVVLYIMLSGYPPFVGHCGADCGWDRGEVCRVCQNKLFESIQEGKYEFPDKDWAHISSEAKDLISKLLVRDAKQRLSAAQVLQHPWVQGQAPEKGLPDPQVLQRNSSTMDLTLFAAEAIALNRQLSQHEENELAEEPEALADGLCSMKLSPPCKSRLARRRALAQAGRGEDRSPPTAL
  
Inhibitor
Name:
BDBM259281
Synonyms:
US9499547, 22
Type:
Small organic molecule
Emp. Form.:
C19H18N4O2
Mol. Mass.:
334.3718
SMILES:
N[C@H]1C[C@H](COc2ccc3ncc(-c4cc5ccccc5o4)n3n2)C1 |r,wU:3.3,wD:1.0,(-7.18,-.29,;-5.85,.48,;-4.36,.08,;-3.96,1.57,;-2.63,2.34,;-1.29,1.57,;.04,2.34,;.04,3.88,;1.37,4.65,;2.71,3.88,;4.17,4.36,;5.08,3.11,;4.17,1.87,;4.57,.38,;3.67,-.87,;4.57,-2.11,;4.25,-3.62,;5.4,-4.65,;6.86,-4.18,;7.18,-2.67,;6.04,-1.64,;6.04,-.1,;2.71,2.34,;1.37,1.57,;-5.45,1.97,)|
Structure:
Search PDB for entries with ligand similarity: