Reaction Details Report a problem with these data
Target
Inhibitor of nuclear factor kappa-B kinase subunit epsilon
Ligand
BDBM50329427
Substrate
n/a
Meas. Tech.
ChEMBL_673926 (CHEMBL1275103)
IC50
>10000±n/a nM
Citation
Menichincheri, M; Albanese, C; Alli, C; Ballinari, D; Bargiotti, A; Caldarelli, M; Ciavolella, A; Cirla, A; Colombo, M; Colotta, F; Croci, V; D'Alessio, R; D'Anello, M; Ermoli, A; Fiorentini, F; Forte, B; Galvani, A; Giordano, P; Isacchi, A; Martina, K; Molinari, A; Moll, JK; Montagnoli, A; Orsini, P; Orzi, F; Pesenti, E; Pillan, A; Roletto, F; Scolaro, A; Tatò, M; Tibolla, M; Valsasina, B; Varasi, M; Vianello, P; Volpi, D; Santocanale, C; Vanotti, E Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding. J Med Chem 53:7296-315 (2010) [PubMed] Article
More Info.:
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