| Reaction Details |
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 | Report a problem with these data |
| Target | 3-phosphoinositide-dependent protein kinase 1 |
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| Ligand | BDBM17051 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | Proliferation Assay |
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| EC50 | 26±0.0 nM |
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| Citation |  Nagashima, K; Shumway, SD; Sathyanarayanan, S; Chen, AH; Dolinski, B; Xu, Y; Keilhack, H; Nguyen, T; Wiznerowicz, M; Li, L; Lutterbach, BA; Chi, A; Paweletz, C; Allison, T; Yan, Y; Munshi, SK; Klippel, A; Kraus, M; Bobkova, EV; Deshmukh, S; Xu, Z; Mueller, U; Szewczak, AA; Pan, BS; Richon, V; Pollock, R; Blume-Jensen, P; Northrup, A; Andersen, JN Genetic and pharmacological inhibition of PDK1 in cancer cells: characterization of a selective allosteric kinase inhibitor. J Biol Chem286:6433-48 (2011) [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 |
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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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| BDBM17051 |
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| n/a |
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| Name | BDBM17051 |
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| Synonyms: | BX-795 | BX-795, 3 | N-(3-{[5-iodo-4-({3-[(thiophen-2-ylcarbonyl)amino]propyl}amino)pyrimidin-2-yl]amino}phenyl)pyrrolidine-1-carboxamide | N-{3-[(5-iodo-4-{[3-(thiophen-2-ylformamido)propyl]amino}pyrimidin-2-yl)amino]phenyl}pyrrolidine-1-carboxamide |
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| Type | Small organic molecule |
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| Emp. Form. | C23H26IN7O2S |
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| Mol. Mass. | 591.468 |
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| SMILES | Ic1cnc(Nc2cccc(NC(=O)N3CCCC3)c2)nc1NCCCNC(=O)c1cccs1 |
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| Structure | 
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