Reaction Details |
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Target | 3-phosphoinositide-dependent protein kinase 1 |
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Ligand | BDBM50341244 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_742336 (CHEMBL1768785) |
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IC50 | >29300±n/a nM |
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Citation | Medina, JR; Becker, CJ; Blackledge, CW; Duquenne, C; Feng, Y; Grant, SW; Heerding, D; Li, WH; Miller, WH; Romeril, SP; Scherzer, D; Shu, A; Bobko, MA; Chadderton, AR; Dumble, M; Gardiner, CM; Gilbert, S; Liu, Q; Rabindran, SK; Sudakin, V; Xiang, H; Brady, PG; Campobasso, N; Ward, P; Axten, JM Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors. J Med Chem54:1871-95 (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 |
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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BDBM50341244 |
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n/a |
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Name | BDBM50341244 |
Synonyms: | (2S,5R)-4-[2-Amino-6-(3-amino-1H-indazol-6-yl)-4-pyrimidinyl]-5-methyl-N-phenyl-2-morpholinecarboxamide | CHEMBL1765741 |
Type | Small organic molecule |
Emp. Form. | C23H24N8O2 |
Mol. Mass. | 444.4891 |
SMILES | C[C@@H]1CO[C@@H](CN1c1cc(nc(N)n1)-c1ccc2c(N)n[nH]c2c1)C(=O)Nc1ccccc1 |r| |
Structure |
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