Reaction Details Report a problem with these data
Target
Inhibitor of nuclear factor kappa-B kinase subunit beta
Ligand
BDBM50402409
Substrate
n/a
Meas. Tech.
ChEMBL_886358 (CHEMBL2212848)
IC50
375.4±n/a nM
Citation
Forsyth, T; Kearney, PC; Kim, BG; Johnson, HW; Aay, N; Arcalas, A; Brown, DS; Chan, V; Chen, J; Du, H; Epshteyn, S; Galan, AA; Huynh, TP; Ibrahim, MA; Kane, B; Koltun, ES; Mann, G; Meyr, LE; Lee, MS; Lewis, GL; Noguchi, RT; Pack, M; Ridgway, BH; Shi, X; Takeuchi, CS; Zu, P; Leahy, JW; Nuss, JM; Aoyama, R; Engst, S; Gendreau, SB; Kassees, R; Li, J; Lin, SH; Martini, JF; Stout, T; Tong, P; Woolfrey, J; Zhang, W; Yu, P SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors. Bioorg Med Chem Lett 22:7653-8 (2012) [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