Target
MAP kinase-interacting serine/threonine-protein kinase 1/2
Ligand
BDBM297342
Substrate
n/a
Meas. Tech.
ChEBML_1697751
IC50
28000±n/a nM
Citation
 Reich, SHSprengeler, PAChiang, GGAppleman, JRChen, JClarine, JEam, BErnst, JTHan, QGoel, VKHan, EZRHuang, VHung, INJJemison, AJessen, KAMolter, JMurphy, DNeal, MParker, GSShaghafi, MSperry, SStaunton, JStumpf, CRThompson, PATran, CWebber, SEWegerski, CJZheng, HWebster, 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:
BDBM297342
Synonyms:
3-methyl-5-(pyrimidin-4-ylamino)isoindolin-1-one (Cpd. No. 8) | US10112955, Example 8
Type:
Small organic molecule
Emp. Form.:
C13H12N4O
Mol. Mass.:
240.2606
SMILES:
CC1NC(=O)c2ccc(Nc3ccncn3)cc12
Structure:
Search PDB for entries with ligand similarity: