Reaction Details |
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Target | Inhibitor of nuclear factor kappa-B kinase subunit beta |
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Ligand | BDBM41575 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_631419 (CHEMBL1111956) |
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IC50 | >10000±n/a nM |
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Citation | Beria, I; Ballinari, D; Bertrand, JA; Borghi, D; Bossi, RT; Brasca, MG; Cappella, P; Caruso, M; Ceccarelli, W; Ciavolella, A; Cristiani, C; Croci, V; De Ponti, A; Fachin, G; Ferguson, RD; Lansen, J; Moll, JK; Pesenti, E; Posteri, H; Perego, R; Rocchetti, M; Storici, P; Volpi, D; Valsasina, B Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors. J Med Chem53:3532-51 (2010) [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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BDBM41575 |
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n/a |
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Name | BDBM41575 |
Synonyms: | CHEMBL1094408 | US8614220, A85B1C1Z |
Type | n/a |
Emp. Form. | C23H28N8O2 |
Mol. Mass. | 448.5208 |
SMILES | COc1ccc(cc1Nc1ncc2CCc3c(nn(C)c3-c2n1)C(N)=O)N1CCN(C)CC1 |
Structure |
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