Reaction Details |
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Target | Inhibitor of nuclear factor kappa-B kinase subunit epsilon |
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Ligand | BDBM276943 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Biological Assay for TBK1 and IKKs |
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pH | 7±n/a |
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IC50 | 1.22±n/a nM |
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Comments | extracted |
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Citation | Du, Z; Guerrero, JA; Kaplan, JA; Knox, Jr., JE; Naduthambi, D; Phillips, BW; Venkataramani, C; Wang, P; Watkins, WJ; Zablocki, J Tank-binding kinase inhibitor compounds US Patent US10072001 Publication Date 9/11/2018 |
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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 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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BDBM276943 |
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n/a |
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Name | BDBM276943 |
Synonyms: | US10072001, Example 119 | US10259811, Example 119 |
Type | Small organic molecule |
Emp. Form. | C28H24N6O2 |
Mol. Mass. | 476.5292 |
SMILES | N#Cc1cc(ccc1OC1CCOCC1)-c1ncnc2[nH]c(cc12)-c1cccc(Cn2ccnc2)c1 |
Structure |
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