Reaction Details |
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Target | 3-phosphoinositide-dependent protein kinase 1 |
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Ligand | BDBM26198 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Proliferation Assay |
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EC50 | 1±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 |
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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BDBM26198 |
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n/a |
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Name | BDBM26198 |
Synonyms: | 4-tert-butyl-15-fluoro-3,5,10-triazatetracyclo[11.4.0.0^{2,6}.0^{7,12}]heptadeca-1(13),2(6),3,7(12),8,14,16-heptaen-11-one | CHEMBL21156 | Compound # 2 | Jak Inhibitor 1 | PDK1 inhibitor, 1 | Tetracyclic Pyridone, 1 |
Type | Small organic molecule |
Emp. Form. | C18H16FN3O |
Mol. Mass. | 309.3375 |
SMILES | CC(C)(C)c1nc2c([nH]1)c1ccc(F)cc1c1c2cc[nH]c1=O |
Structure |
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