Reaction Details |
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Target | 3-phosphoinositide-dependent protein kinase 1 |
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Ligand | BDBM92493 |
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Substrate/Competitor | n/a |
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Meas. Tech. | TR-Fret Assay |
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IC50 | 1.80e+4± 1.3e+3 nM |
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Citation | Bobkova, EV; Weber, MJ; Xu, Z; Zhang, YL; Jung, J; Blume-Jensen, P; Northrup, A; Kunapuli, P; Andersen, JN; Kariv, I Discovery of PDK1 kinase inhibitors with a novel mechanism of action by ultrahigh throughput screening. J Biol Chem285:18838-46 (2010) [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 |
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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BDBM92493 |
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n/a |
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Name | BDBM92493 |
Synonyms: | Alkaloid 2 |
Type | Small organic molecule |
Emp. Form. | C27H44N4O3 |
Mol. Mass. | 472.6633 |
SMILES | CCCCCNC(=O)O[C@@H]1CC[C@@H]2[C@H](C[C@H]1N2CCC(C)C)C(=O)Nc1ccc(cc1)N(C)C |r,THB:17:16:13.14:9.11.10| |
Structure |
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