Reaction Details |
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Target | 3-phosphoinositide-dependent protein kinase 1 |
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Ligand | BDBM50499153 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1537761 (CHEMBL3737518) |
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IC50 | 998±n/a nM |
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Citation | Sestito, S; Nesi, G; Daniele, S; Martelli, A; Digiacomo, M; Borghini, A; Pietra, D; Calderone, V; Lapucci, A; Falasca, M; Parrella, P; Notarangelo, A; Breschi, MC; Macchia, M; Martini, C; Rapposelli, S Design and synthesis of 2-oxindole based multi-targeted inhibitors of PDK1/Akt signaling pathway for the treatment of glioblastoma multiforme. Eur J Med Chem105:274-88 (2015) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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3-phosphoinositide-dependent protein kinase 1 |
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Name: | 3-phosphoinositide-dependent protein kinase 1 |
Synonyms: | 3-Phosphoinositide-Dependent Protein Kinase 1 (PDK1) | 3-phosphoinositide dependent protein kinase-1 | 3-phosphoinositide-dependent protein kinase 1 | 3-phosphoinositide-dependent protein kinase 1 (PDK) | 3-phosphoinositide-dependent protein kinase 1 (PDK-1) | 3-phosphoinositide-dependent protein kinase 1 (PDK1)(Δ1-50) | Isoform 2 of 3-phosphoinositide-dependent protein kinase 1 | PDK1 | PDPK1 | PDPK1_HUMAN | Phosphoinositide-dependent protein kinase 1 (PDK1) | Pyruvate dehydrogenase kinase isoenzyme 1 (PDK1) | hPDK1 |
Type: | Enzyme |
Mol. Mass.: | 63157.65 |
Organism: | Homo sapiens (Human) |
Description: | O15530 |
Residue: | 556 |
Sequence: | MARTTSQLYDAVPIQSSVVLCSCPSPSMVRTQTESSTPPGIPGGSRQGPAMDGTAAEPRP
GAGSLQHAQPPPQPRKKRPEDFKFGKILGEGSFSTVVLARELATSREYAIKILEKRHIIK
ENKVPYVTRERDVMSRLDHPFFVKLYFTFQDDEKLYFGLSYAKNGELLKYIRKIGSFDET
CTRFYTAEIVSALEYLHGKGIIHRDLKPENILLNEDMHIQITDFGTAKVLSPESKQARAN
SFVGTAQYVSPELLTEKSACKSSDLWALGCIIYQLVAGLPPFRAGNEYLIFQKIIKLEYD
FPEKFFPKARDLVEKLLVLDATKRLGCEEMEGYGPLKAHPFFESVTWENLHQQTPPKLTA
YLPAMSEDDEDCYGNYDNLLSQFGCMQVSSSSSSHSLSASDTGLPQRSGSNIEQYIHDLD
SNSFELDLQFSEDEKRLLLEKQAGGNPWHQFVENNLILKMGPVDKRKGLFARRRQLLLTE
GPHLYYVDPVNKVLKGEIPWSQELRPEAKNFKTFFVHTPNRTYYLMDPSGNAHKWCRKIQ
EVWRQRYQSHPDAAVQ
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BDBM50499153 |
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n/a |
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Name | BDBM50499153 |
Synonyms: | CHEMBL3091673 |
Type | Small organic molecule |
Emp. Form. | C25H25N5O4 |
Mol. Mass. | 459.4971 |
SMILES | COc1cc2CCN(CC(=O)Nc3ccc4NC(=O)\C(=C/c5cnc[nH]5)c4c3)Cc2cc1OC |
Structure |
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