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Target
MAP kinase-interacting serine/threonine-protein kinase 1/2
Ligand
BDBM50263270
Substrate
n/a
Meas. Tech.
ChEBML_1697751
IC50
0.084000±n/a nM
Citation
 Reich, SH; Sprengeler, PA; Chiang, GG; Appleman, JR; Chen, J; Clarine, J; Eam, B; Ernst, JT; Han, Q; Goel, VK; Han, EZR; Huang, V; Hung, INJ; Jemison, A; Jessen, KA; Molter, J; Murphy, D; Neal, M; Parker, GS; Shaghafi, M; Sperry, S; Staunton, J; Stumpf, CR; Thompson, PA; Tran, C; Webber, SE; Wegerski, CJ; Zheng, H; Webster, KR Structure-based Design of Pyridone-Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition. J Med Chem 61:3516-3540 (2018) [PubMed]  Article 
Target
Name:
MAP kinase-interacting serine/threonine-protein kinase 1/2
Synonyms:
n/a
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of ChEMBL is 1879554
Components:
This complex has 2 components.
Component 1
Name:
MAP kinase-interacting serine/threonine-protein kinase 2
Synonyms:
GPRK7 | MAP kinase signal-integrating kinase 2 | MAP kinase-interacting serine/threonine-protein kinase 2 (MKNK2) | MAP kinase-interacting serine/threonine-protein kinase 2 (MnK2) | MAP-kinase interacting kinase 2 (MNK2) | MKNK2 | MKNK2_HUMAN | MNK2
Type:
Protein
Mol. Mass.:
51870.79
Organism:
Homo sapiens (Human)
Description:
Q9HBH9
Residue:
465
Sequence:
MVQKKPAELQGFHRSFKGQNPFELAFSLDQPDHGDSDFGLQCSARPDMPASQPIDIPDAKKRGKKKKRGRATDSFSGRFEDVYQLQEDVLGEGAHARVQTCINLITSQEYAVKIIEKQPGHIRSRVFREVEMLYQCQGHRNVLELIEFFEEEDRFYLVFEKMRGGSILSHIHKRRHFNELEASVVVQDVASALDFLHNKGIAHRDLKPENILCEHPNQVSPVKICDFDLGSGIKLNGDCSPISTPELLTPCGSAEYMAPEVVEAFSEEASIYDKRCDLWSLGVILYILLSGYPPFVGRCGSDCGWDRGEACPACQNMLFESIQEGKYEFPDKDWAHISCAAKDLISKLLVRDAKQRLSAAQVLQHPWVQGCAPENTLPTPMVLQRNSCAKDLTSFAAEAIAMNRQLAQHDEDLAEEEAAGQGQPVLVRATSRCLQLSPPSQSKLAQRRQRASLSSAPVVLVGDHA
  
Component 2
Name:
MAP kinase-interacting serine/threonine-protein kinase 1
Synonyms:
MAP Kinase-Interacting Protein Kinase (MNK1) | MAP kinase signal-integrating kinase 1 | MAP kinase-interacting serine/threonine-protein kinase 1 (MnK1) | MAP kinase-interacting serine/threonine-protein kinase MNK1 | MAP-kinase interacting kinase 1 (MNK1) | MAPK signal-integrating kinase 1 | MKNK1 | MKNK1_HUMAN | MNK1
Type:
Serine/threonine-protein kinase
Mol. Mass.:
51342.85
Organism:
Homo sapiens (Human)
Description:
Q9BUB5
Residue:
465
Sequence:
MVSSQKLEKPIEMGSSEPLPIADGDRRRKKKRRGRATDSLPGKFEDMYKLTSELLGEGAYAKVQGAVSLQNGKEYAVKIIEKQAGHSRSRVFREVETLYQCQGNKNILELIEFFEDDTRFYLVFEKLQGGSILAHIQKQKHFNEREASRVVRDVAAALDFLHTKDKVSLCHLGWSAMAPSGLTAAPTSLGSSDPPTSASQVAGTTGIAHRDLKPENILCESPEKVSPVKICDFDLGSGMKLNNSCTPITTPELTTPCGSAEYMAPEVVEVFTDQATFYDKRCDLWSLGVVLYIMLSGYPPFVGHCGADCGWDRGEVCRVCQNKLFESIQEGKYEFPDKDWAHISSEAKDLISKLLVRDAKQRLSAAQVLQHPWVQGQAPEKGLPTPQVLQRNSSTMDLTLFAAEAIALNRQLSQHEENELAEEPEALADGLCSMKLSPPCKSRLARRRALAQAGRGEDRSPPTAL
  
Inhibitor
Name:
BDBM50263270
Synonyms:
CHEMBL4086747
Type:
Small organic molecule
Emp. Form.:
C16H16Cl2N6O2
Mol. Mass.:
395.243
SMILES:
Nc1ncnc(Nc2cc(Cl)c3C(=O)NC4(CCCCC4)n3c2=O)c1Cl
Structure:
Search PDB for entries with ligand similarity: