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TargetInhibitor of nuclear factor kappa-B kinase subunit alpha
LigandBDBM27476
Substrate/CompetitorI-kappa-B-alpha
Meas. Tech.IKK Kinase Inhibition Assay
pH7.4±n/a
Temperature295.15±n/a K
IC50 79±n/a nM
Citation Christopher, JAAvitabile, BGBamborough, PChampigny, ACCutler, GJDyos, SLGrace, KGKerns, JKKitson, JDMellor, GWMorey, JVMorse, MAO'Malley, CFPatel, CBProbst, NRumsey, WSmith, CAWilson, MJ The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-alpha and IKK-beta kinases. Bioorg Med Chem Lett17:3972-7 (2007) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Inhibitor of nuclear factor kappa-B kinase subunit alpha
Name:Inhibitor of nuclear factor kappa-B kinase subunit alpha
Synonyms:CHUK | Conserved helix-loop-helix ubiquitous kinase | I-kappa-B kinase 1 | I-kappa-B kinase alpha | IKK-A | IKK-alpha | IKK1 | IKK2/IKK1 | IKKA | IKKA_HUMAN | IkBKA | IkappaB kinase | Inhibitor of NF-kappa-B kinase alpha/beta | NFKBIKA | Nuclear factor NF-kappa-B inhibitor kinase alpha | TCF-16 | TCF16 | Transcription factor 16
Type:PROTEIN
Mol. Mass.:84642.21
Organism:Homo sapiens (Human)
Description:ChEMBL_327453
Residue:745
Sequence:
MERPPGLRPGAGGPWEMRERLGTGGFGNVCLYQHRELDLKIAIKSCRLELSTKNRERWCH
EIQIMKKLNHANVVKACDVPEELNILIHDVPLLAMEYCSGGDLRKLLNKPENCCGLKESQ
ILSLLSDIGSGIRYLHENKIIHRDLKPENIVLQDVGGKIIHKIIDLGYAKDVDQGSLCTS
FVGTLQYLAPELFENKPYTATVDYWSFGTMVFECIAGYRPFLHHLQPFTWHEKIKKKDPK
CIFACEEMSGEVRFSSHLPQPNSLCSLVVEPMENWLQLMLNWDPQQRGGPVDLTLKQPRC
FVLMDHILNLKIVHILNMTSAKIISFLLPPDESLHSLQSRIERETGINTGSQELLSETGI
SLDPRKPASQCVLDGVRGCDSYMVYLFDKSKTVYEGPFASRSLSDCVNYIVQDSKIQLPI
IQLRKVWAEAVHYVSGLKEDYSRLFQGQRAAMLSLLRYNANLTKMKNTLISASQQLKAKL
EFFHKSIQLDLERYSEQMTYGISSEKMLKAWKEMEEKAIHYAEVGVIGYLEDQIMSLHAE
IMELQKSPYGRRQGDLMESLEQRAIDLYKQLKHRPSDHSYSDSTEMVKIIVHTVQSQDRV
LKELFGHLSKLLGCKQKIIDLLPKVEVALSNIKEADNTVMFMQGKRQKEIWHLLKIACTQ
SSARSLVGSSLEGAVTPQTSAWLPPTSAEHDHSLSCVVTPQDGETSAQMIEENLNCLGHL
STIIHEANEEQGNSMMNLDWSWLTE
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  Blast E-value cutoff:
BDBM27476
I-kappa-B-alpha
Name:NF-kappa-B inhibitor alpha
Synonyms:I-kappa-B-alpha | IKBA | IKBA_HUMAN | MAD3 | NF-kappa-B inhibitor alpha | NFKBI | NFKBIA
Type:GST fusion protein
Mol. Mass.:35584.84
Organism:Homo sapiens (Human)
Description:It was produced in E. coli as GST-tagged fusion protein (Santa Cruz Biotechnology).
Residue:317
Sequence:
MFQAAERPQEWAMEGPRDGLKKERLLDDRHDSGLDSMKDEEYEQMVKELQEIRLEPQEVP
RGSEPWKQQLTEDGDSFLHLAIIHEEKALTMEVIRQVKGDLAFLNFQNNLQQTPLHLAVI
TNQPEIAEALLGAGCDPELRDFRGNTPLHLACEQGCLASVGVLTQSCTTPHLHSILKATN
YNGHTCLHLASIHGYLGIVELLVSLGADVNAQEPCNGRTALHLAVDLQNPDLVSLLLKCG
ADVNRVTYQGYSPYQLTWGRPSTRIQQQLGQLTLENLQMLPESEDEESYDTESEFTEFTE
DELPYDDCVFGGQRLTL
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  Blast E-value cutoff: