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Target
Inhibitor of nuclear factor kappa-B kinase subunit epsilon
Ligand
BDBM199250
Substrate
n/a
Meas. Tech.
ChEMBL_1330228 (CHEMBL3224484)
IC50
<1.000000±n/a nM
Citation
 Pireddu, R; Forinash, KD; Sun, NN; Martin, MP; Sung, SS; Alexander, B; Zhu, JY; Guida, WC; Schönbrunn, E; Sebti, SM; Lawrence, NJ Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2). Medchemcomm 3:699-709 (2012) [PubMed]  Article 
Target
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:
MQSTANYLWHTDDLLGQGATASVYKARNKKSGELVAVKVFNTTSYLRPREVQVREFEVLRKLNHQNIVKLFAVEETGGSRQKVLVMEYCSSGSLLSVLESPENAFGLPEDEFLVVLRCVVAGMNHLRENGIVHRDIKPGNIMRLVGEEGQSIYKLTDFGAARELDDDEKFVSVYGTEEYLHPDMYERAVLRKPQQKAFGVTVDLWSIGVTLYHAATGSLPFIPFGGPRRNKEIMYRITTEKPAGAIAGAQRRENGPLEWSYTLPITCQLSLGLQSQLVPILANILEVEQAKCWGFDQFFAETSDILQRVVVHVFSLSQAVLHHIYIHAHNTIAIFQEAVHKQTSVAPRHQEYLFEGHLCVLEPSVSAQHIAHTTASSPLTLFSTAIPKGLAFRDPALDVPKFVPKVDLQADYNTAKGVLGAGYQALRLARALLDGQELMFRGLHWVMEVLQATCRRTLEVARTSLLYLSSSLGTERFSSVAGTPEIQELKAAAELRSRLRTLAEVLSRCSQNITETQESLSSLNRELVKSRDQVHEDRSIQQIQCCLDKMNFIYKQFKKSRMRPGLGYNEEQIHKLDKVNFSHLAKRLLQVFQEECVQKYQASLVTHGKRMRVVHETRNHLRLVGCSVAACNTEAQGVQESLSKLLEELSHQLLQDRAKGAQASPPPIAPYPSPTRKDLLLHMQELCEGMKLLASDLLDNNRIIERLNRVPAPPDV
  
Inhibitor
Name:
BDBM199250
Synonyms:
US9221808, 1bo | US9221808, 1bo-HCl | US9221808, 1bo-Mes
Type:
Small organic molecule
Emp. Form.:
C16H14N4O2S
Mol. Mass.:
326.373
SMILES:
Oc1cccc(CNC(=O)Nc2nc(cs2)-c2ccncc2)c1
Structure:
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