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Target
MAP kinase-interacting serine/threonine-protein kinase 2
Ligand
BDBM168214
Substrate
n/a
Meas. Tech.
ChEBML_1697750
IC50
1.8±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
More Info.:
Target
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
Inhibitor
Name:
BDBM168214
Synonyms:
US9669031, 207 6′-((6-aminopyrimidin-4-yl)amino)-8′-(hydroxymethyl)-2′H-spiro[cyclohexane-1,3′-imidazo[1,5-a]pyridine]-1′,5′-dione (Cpd. No. 207) | US9669031, 45 N-(6-((8′-chloro-1′,5′-dioxo-1′,5′-dihydro-2′H-spiro[cyclohexane-1,3′-imidazo[1,5-a]pyridin]-6′-yl)amino)pyrimidin-4-yl)cyclopropanecarboxamide (Cpd. No. 45)
Type:
Small organic molecule
Emp. Form.:
C20H21ClN6O3
Mol. Mass.:
428.872
SMILES:
Clc1cc(Nc2cc(NC(=O)C3CC3)ncn2)c(=O)n2c1C(=O)NC21CCCCC1