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Target
Glutathione S-transferase P/Isoform 2 of MAP kinase-interacting serine/threonine-protein kinase 1 (MNK1a) [T344D]
Ligand
BDBM259298
Substrate
n/a
Meas. Tech.
MKNK1 TR-FRET Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
3±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:
BDBM259298
Synonyms:
US9499547, 39
Type:
Small organic molecule
Emp. Form.:
C18H15FN4O2
Mol. Mass.:
338.3357
SMILES:
N[C@H]1C[C@@H](C1)Oc1ccc2ncc(-c3cc4cc(F)ccc4o3)n2n1 |r,wU:1.0,wD:3.5,(-6.7,4.88,;-5.37,4.11,;-3.88,4.5,;-3.48,3.02,;-4.97,2.62,;-2.15,2.25,;-.81,3.02,;-.81,4.56,;.52,5.33,;1.85,4.56,;3.32,5.03,;4.22,3.79,;3.32,2.54,;4.09,1.21,;3.18,-.04,;4.09,-1.28,;3.77,-2.79,;4.92,-3.82,;4.6,-5.33,;6.38,-3.34,;6.7,-1.84,;5.55,-.81,;5.55,.73,;1.85,3.02,;.52,2.25,)|
Structure:
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