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TargetInhibitor of nuclear factor kappa-B kinase subunit epsilon
LigandBDBM2579
Substrate/Competitorn/a
Meas. Tech.ChEMBL_586823
Kd 5.1±n/a nM
Citation Karaman MWHerrgard STreiber DKGallant PAtteridge CECampbell BTChan KWCiceri PDavis MIEdeen PTFaraoni RFloyd MHunt JPLockhart DJMilanov ZVMorrison MJPallares GPatel HKPritchard SWodicka LMZarrinkar PP A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol 26:127-32 (2008) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Inhibitor of nuclear factor kappa-B kinase subunit epsilon
Name:Inhibitor of nuclear factor kappa-B kinase subunit epsilon
Synonyms:I kappa-B kinase epsilon | I-kappa-B Kinase 3 (IKK-epsilon) | I-kappa-B kinase epsilon (IKK-E) | I-kappa-B kinase epsilon (IKKE) | IKK-E | IKK-epsilon | IKK-i | IkBKE | Inducible I kappa-B kinase
Type:Serine/threonine-protein kinase
Mol. Mass.:80475.98
Organism:Homo sapiens (Human)
Description:Kinase inhibitory activity was determined using recombinant human IKK-epsilon expressed in baculovirus as a FLAG-tagged fusion protein.
Residue:716
Sequence:
MQSTANYLWHTDDLLGQGATASVYKARNKKSGELVAVKVFNTTSYLRPREVQVREFEVLR
KLNHQNIVKLFAVEETGGSRQKVLVMEYCSSGSLLSVLESPENAFGLPEDEFLVVLRCVV
AGMNHLRENGIVHRDIKPGNIMRLVGEEGQSIYKLTDFGAARELDDDEKFVSVYGTEEYL
HPDMYERAVLRKPQQKAFGVTVDLWSIGVTLYHAATGSLPFIPFGGPRRNKEIMYRITTE
KPAGAIAGAQRRENGPLEWSYTLPITCQLSLGLQSQLVPILANILEVEQAKCWGFDQFFA
ETSDILQRVVVHVFSLSQAVLHHIYIHAHNTIAIFQEAVHKQTSVAPRHQEYLFEGHLCV
LEPSVSAQHIAHTTASSPLTLFSTAIPKGLAFRDPALDVPKFVPKVDLQADYNTAKGVLG
AGYQALRLARALLDGQELMFRGLHWVMEVLQATCRRTLEVARTSLLYLSSSLGTERFSSV
AGTPEIQELKAAAELRSRLRTLAEVLSRCSQNITETQESLSSLNRELVKSRDQVHEDRSI
QQIQCCLDKMNFIYKQFKKSRMRPGLGYNEEQIHKLDKVNFSHLAKRLLQVFQEECVQKY
QASLVTHGKRMRVVHETRNHLRLVGCSVAACNTEAQGVQESLSKLLEELSHQLLQDRAKG
AQASPPPIAPYPSPTRKDLLLHMQELCEGMKLLASDLLDNNRIIERLNRVPAPPDV
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  Blast E-value cutoff:
BDBM2579
n/a
NameBDBM2579
Synonyms:(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one | CHEMBL388978 | Staurosporin, 4 | Staurosporine | Staurosporine, 8 | US9206188, Staurosporine | US9226923, Staurosporine
TypeSmall organic molecule
Emp. Form.C28H26N4O3
Mol. Mass.466.531
SMILESCN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r|
Structure
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