Reaction Details |
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Target | 3-phosphoinositide-dependent protein kinase 1 |
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Ligand | BDBM50361650 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_799415 (CHEMBL1942167) |
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Ki | 1.3±n/a nM |
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Citation | Murphy, ST; Alton, G; Bailey, S; Baxi, SM; Burke, BJ; Chappie, TA; Ermolieff, J; Ferre, R; Greasley, S; Hickey, M; Humphrey, J; Kablaoui, N; Kath, J; Kazmirski, S; Kraus, M; Kupchinsky, S; Li, J; Lingardo, L; Marx, MA; Richter, D; Tanis, SP; Tran, K; Vernier, W; Xie, Z; Yin, MJ; Yu, XH Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1). J Med Chem54:8490-500 (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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BDBM50361650 |
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n/a |
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Name | BDBM50361650 |
Synonyms: | CHEMBL1940248 |
Type | Small organic molecule |
Emp. Form. | C24H24FN7O2 |
Mol. Mass. | 461.4915 |
SMILES | CC(C)n1cc(C(=O)c2cncc(N[C@@H]3CCO[C@@H]3c3ccc(F)cc3)n2)c2c(N)ncnc12 |r| |
Structure |
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