Reaction Details Report a problem with these data
Target
MAP kinase-interacting serine/threonine-protein kinase 1
Ligand
BDBM164271
Substrate
n/a
Meas. Tech.
ChEBML_1697749
IC50
2.7±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
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:
BDBM164271
Synonyms:
US9669031, 10 N-(6-((3,3-dimethyl-1,5-dioxo-1,2,3,5-tetrahydroimidazo[1,5-a]pyridin-6-yl)amino)pyrimidin-4-yl)cyclopropanecarboxamide (Cpd. No. 10)
Type:
Small organic molecule
Emp. Form.:
C17H18N6O3
Mol. Mass.:
354.3632
SMILES:
CC1(C)NC(=O)c2ccc(Nc3cc(NC(=O)C4CC4)ncn3)c(=O)n12
Structure:
Search PDB for entries with ligand similarity: