| Reaction Details |
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 | Report a problem with these data |
| Target | 3-phosphoinositide-dependent protein kinase 1 |
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| Ligand | BDBM16996 |
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| Substrate/Competitor | Serine/threonine-protein kinase AKT2 |
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| Meas. Tech. | PDK1-mediated AKT2 Activation Assay (cAKT2 33P-SPA) |
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| pH | 7.2±n/a |
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| Temperature | 295.15±n/a K |
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| IC50 | 4±n/a nM |
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| Citation |  Islam, I; Brown, G; Bryant, J; Hrvatin, P; Kochanny, MJ; Phillips, GB; Yuan, S; Adler, M; Whitlow, M; Lentz, D; Polokoff, MA; Wu, J; Shen, J; Walters, J; Ho, E; Subramanyam, B; Zhu, D; Feldman, RI; Arnaiz, DO Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517. Bioorg Med Chem Lett17:3819-25 (2007) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| 3-phosphoinositide-dependent protein kinase 1 |
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| Name: | 3-phosphoinositide-dependent protein kinase 1 |
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| 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 |
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| Type: | Enzyme |
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| Mol. Mass.: | 63157.65 |
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| Organism: | Homo sapiens (Human) |
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| Description: | O15530 |
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| Residue: | 556 |
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| Sequence: | MARTTSQLYDAVPIQSSVVLCSCPSPSMVRTQTESSTPPGIPGGSRQGPAMDGTAAEPRP
GAGSLQHAQPPPQPRKKRPEDFKFGKILGEGSFSTVVLARELATSREYAIKILEKRHIIK
ENKVPYVTRERDVMSRLDHPFFVKLYFTFQDDEKLYFGLSYAKNGELLKYIRKIGSFDET
CTRFYTAEIVSALEYLHGKGIIHRDLKPENILLNEDMHIQITDFGTAKVLSPESKQARAN
SFVGTAQYVSPELLTEKSACKSSDLWALGCIIYQLVAGLPPFRAGNEYLIFQKIIKLEYD
FPEKFFPKARDLVEKLLVLDATKRLGCEEMEGYGPLKAHPFFESVTWENLHQQTPPKLTA
YLPAMSEDDEDCYGNYDNLLSQFGCMQVSSSSSSHSLSASDTGLPQRSGSNIEQYIHDLD
SNSFELDLQFSEDEKRLLLEKQAGGNPWHQFVENNLILKMGPVDKRKGLFARRRQLLLTE
GPHLYYVDPVNKVLKGEIPWSQELRPEAKNFKTFFVHTPNRTYYLMDPSGNAHKWCRKIQ
EVWRQRYQSHPDAAVQ
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| BDBM16996 |
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| Serine/threonine-protein kinase AKT2 |
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| Name: | RAC-beta serine/threonine-protein kinase |
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| Synonyms: | AKT2 | AKT2_HUMAN | PKB beta | Protein kinase Akt-2 | Protein kinase B (Akt 2) | Protein kinase B beta (AKT2) | Protein kinase B, beta | RAC-PK-beta | RAC-alpha serine/threonine-protein kinase (AKT2) | RAC-beta serine/threonine-protein kinase | RAC-beta serine/threonine-protein kinase (AKT2) | Serine/threonine-protein kinase AKT | Serine/threonine-protein kinase AKT2 | Serine/threonine-protein kinase Rac alpha/beta |
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| Type: | Enzyme |
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| Mol. Mass.: | 55766.64 |
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| Organism: | Homo sapiens (Human) |
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| Description: | n/a |
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| Residue: | 481 |
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| Sequence: | MNEVSVIKEGWLHKRGEYIKTWRPRYFLLKSDGSFIGYKERPEAPDQTLPPLNNFSVAEC
QLMKTERPRPNTFVIRCLQWTTVIERTFHVDSPDEREEWMRAIQMVANSLKQRAPGEDPM
DYKCGSPSDSSTTEEMEVAVSKARAKVTMNDFDYLKLLGKGTFGKVILVREKATGRYYAM
KILRKEVIIAKDEVAHTVTESRVLQNTRHPFLTALKYAFQTHDRLCFVMEYANGGELFFH
LSRERVFTEERARFYGAEIVSALEYLHSRDVVYRDIKLENLMLDKDGHIKITDFGLCKEG
ISDGATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHERLFE
LILMEEIRFPRTLSPEAKSLLAGLLKKDPKQRLGGGPSDAKEVMEHRFFLSINWQDVVQK
KLLPPFKPQVTSEVDTRYFDDEFTAQSITITPPDRYDSLGLLELDQRTHFPQFSYSASIR
E
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