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Target
Inhibitor of nuclear factor kappa-B kinase subunit beta
Ligand
BDBM50208911
Substrate
n/a
Meas. Tech.
ChEMBL_1633278 (CHEMBL3876070)
IC50
10000±n/a nM
Citation
Katz, JD; Haidle, A; Childers, KK; Zabierek, AA; Jewell, JP; Hou, Y; Altman, MD; Szewczak, A; Chen, D; Harsch, A; Hayashi, M; Warren, L; Hutton, M; Nuthall, H; Su, HP; Munshi, S; Stanton, MG; Davies, IW; Munoz, B; Northrup, A Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors. Bioorg Med Chem Lett 27:114-120 (2017) [PubMed] Article
More Info.:
Target
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:
MSWSPSLTTQTCGAWEMKERLGTGGFGNVIRWHNQETGEQIAIKQCRQELSPRNRERWCLEIQIMRRLTHPNVVAARDVPEGMQNLAPNDLPLLAMEYCQGGDLRKYLNQFENCCGLREGAILTLLSDIASALRYLHENRIIHRDLKPENIVLQQGEQRLIHKIIDLGYAKELDQGSLCTSFVGTLQYLAPELLEQQKYTVTVDYWSFGTLAFECITGFRPFLPNWQPVQWHSKVRQKSEVDIVVSEDLNGTVKFSSSLPYPNNLNSVLAERLEKWLQLMLMWHPRQRGTDPTYGPNGCFKALDDILNLKLVHILNMVTGTIHTYPVTEDESLQSLKARIQQDTGIPEEDQELLQEAGLALIPDKPATQCISDGKLNEGHTLDMDLVFLFDNSKITYETQISPRPQPESVSCILQEPKRNLAFFQLRKVWGQVWHSIQTLKEDCNRLQQGQRAAMMNLLRNNSCLSKMKNSMASMSQQLKAKLDFFKTSIQIDLEKYSEQTEFGITSDKLLLAWREMEQAVELCGRENEVKLLVERMMALQTDIVDLQRSPMGRKQGGTLDDLEEQARELYRRLREKPRDQRTEGDSQEMVRLLLQAIQSFEKKVRVIYTQLSKTVVCKQKALELLPKVEEVVSLMNEDEKTVVRLQEKRQKELWNLLKIACSKVRGPVSGSPDSMNASRLSQPGQLMSQPSTASNSLPEPAKKSEELVAEAHNLCTLLENAIQDTVREQDQSFTALDWSWLQTEEEEHSCLEQAS