Reaction Details |
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Target | Inhibitor of nuclear factor kappa-B kinase subunit beta |
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Ligand | BDBM50126732 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_90392 (CHEMBL698195) |
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IC50 | 50000±n/a nM |
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Citation | Goldberg, DR; Butz, T; Cardozo, MG; Eckner, RJ; Hammach, A; Huang, J; Jakes, S; Kapadia, S; Kashem, M; Lukas, S; Morwick, TM; Panzenbeck, M; Patel, U; Pav, S; Peet, GW; Peterson, JD; Prokopowicz, AS; Snow, RJ; Sellati, R; Takahashi, H; Tan, J; Tschantz, MA; Wang, XJ; Wang, Y; Wolak, J; Xiong, P; Moss, N Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase. J Med Chem46:1337-49 (2003) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Inhibitor of nuclear factor kappa-B kinase subunit beta |
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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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BDBM50126732 |
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n/a |
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Name | BDBM50126732 |
Synonyms: | 2-(2,6-Dichloro-phenylamino)-7-(3-diethylamino-propenyl)-1,6-dimethyl-1,8-dihydro-imidazo[4,5-h]isoquinolin-9-one | CHEMBL281957 |
Type | Small organic molecule |
Emp. Form. | C25H27Cl2N5O |
Mol. Mass. | 484.421 |
SMILES | CCN(CC)CC=Cc1[nH]c(=O)c2c3n(C)c(Nc4c(Cl)cccc4Cl)nc3ccc2c1C |w:6.5| |
Structure |
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