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TargetInhibitor of nuclear factor kappa-B kinase subunit beta
LigandBDBM50031747
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1432590 (CHEMBL3388149)
IC50 24689±n/a nM
Citation Menet, CJFletcher, SRVan Lommen, GGeney, RBlanc, JSmits, KJouannigot, NDeprez, Pvan der Aar, EMClement-Lacroix, PLepescheux, LGalien, RVayssiere, BNelles, LChristophe, TBrys, RUhring, MCiesielski, FVan Rompaey, L Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634. J Med Chem57:9323-42 (2014) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Inhibitor of nuclear factor kappa-B kinase subunit beta
Name:Inhibitor of nuclear factor kappa-B kinase subunit beta
Synonyms:I-kappa-B Kinase 2 (IKK-beta) | I-kappa-B kinase 2 | I-kappa-B-kinase beta | I-kappa-B-kinase beta (IKKB) | IKBKB | IKK-B | IKK-beta | IKK2 | IKK2/IKK1 | IKKB | IKKB_HUMAN | Inhibitor of NF-kappa-B kinase alpha/beta | Inhibitor of nuclear factor kappa B kinase beta subunit | NFKBIKB | Nuclear factor NF-kappa-B inhibitor kinase beta
Type:Serine/threonine-protein kinase
Mol. Mass.:86554.39
Organism:Homo sapiens (Human)
Description:GST-tagged IKK-2 was expressed in High Five cells and purified.
Residue:756
Sequence:
MSWSPSLTTQTCGAWEMKERLGTGGFGNVIRWHNQETGEQIAIKQCRQELSPRNRERWCL
EIQIMRRLTHPNVVAARDVPEGMQNLAPNDLPLLAMEYCQGGDLRKYLNQFENCCGLREG
AILTLLSDIASALRYLHENRIIHRDLKPENIVLQQGEQRLIHKIIDLGYAKELDQGSLCT
SFVGTLQYLAPELLEQQKYTVTVDYWSFGTLAFECITGFRPFLPNWQPVQWHSKVRQKSE
VDIVVSEDLNGTVKFSSSLPYPNNLNSVLAERLEKWLQLMLMWHPRQRGTDPTYGPNGCF
KALDDILNLKLVHILNMVTGTIHTYPVTEDESLQSLKARIQQDTGIPEEDQELLQEAGLA
LIPDKPATQCISDGKLNEGHTLDMDLVFLFDNSKITYETQISPRPQPESVSCILQEPKRN
LAFFQLRKVWGQVWHSIQTLKEDCNRLQQGQRAAMMNLLRNNSCLSKMKNSMASMSQQLK
AKLDFFKTSIQIDLEKYSEQTEFGITSDKLLLAWREMEQAVELCGRENEVKLLVERMMAL
QTDIVDLQRSPMGRKQGGTLDDLEEQARELYRRLREKPRDQRTEGDSQEMVRLLLQAIQS
FEKKVRVIYTQLSKTVVCKQKALELLPKVEEVVSLMNEDEKTVVRLQEKRQKELWNLLKI
ACSKVRGPVSGSPDSMNASRLSQPGQLMSQPSTASNSLPEPAKKSEELVAEAHNLCTLLE
NAIQDTVREQDQSFTALDWSWLQTEEEEHSCLEQAS
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  Blast E-value cutoff:
BDBM50031747
n/a
NameBDBM50031747
Synonyms:CHEMBL3360318
TypeSmall organic molecule
Emp. Form.C17H16N4O2
Mol. Mass.308.3345
SMILESCOc1ccc(cc1)-c1cccc2nc(NC(=O)C3CC3)nn12
Structure
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