Reaction Details |
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Target | Inhibitor of nuclear factor kappa-B kinase subunit epsilon |
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Ligand | BDBM27468 |
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Substrate/Competitor | I-kappa-B-alpha |
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Meas. Tech. | IKK Kinase Inhibition Assay |
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IC50 | >15849±n/a nM |
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Citation | Christopher, JA; Avitabile, BG; Bamborough, P; Champigny, AC; Cutler, GJ; Dyos, SL; Grace, KG; Kerns, JK; Kitson, JD; Mellor, GW; Morey, JV; Morse, MA; O'Malley, CF; Patel, CB; Probst, N; Rumsey, W; Smith, CA; Wilson, 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 |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Inhibitor of nuclear factor kappa-B kinase subunit epsilon |
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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) | IKBKE | IKK-E | IKK-epsilon | IKK-i | IKKE | IKKE_HUMAN | IKKI | Inducible I kappa-B kinase | KIAA0151 | von Hippel-Lindau disease tumor suppressor/Inhibitor of nuclear factor kappa-B kinase subunit epsilon |
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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BDBM27468 |
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I-kappa-B-alpha |
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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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