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Target
3-phosphoinositide-dependent protein kinase 1
Ligand
BDBM50296953
Substrate
n/a
Meas. Tech.
ChEMBL_580930 (CHEMBL1054895)
Kd
5900±n/a nM
Citation
 Stroba, A; Schaeffer, F; Hindie, V; Lopez-Garcia, L; Adrian, I; Fröhner, W; Hartmann, RW; Biondi, RM; Engel, M 3,5-Diphenylpent-2-enoic acids as allosteric activators of the protein kinase PDK1: structure-activity relationships and thermodynamic characterization of binding as paradigms for PIF-binding pocket-targeting compounds. J Med Chem 52:4683-93 (2009) [PubMed]  Article 
Target
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:
MARTTSQLYDAVPIQSSVVLCSCPSPSMVRTQTESSTPPGIPGGSRQGPAMDGTAAEPRPGAGSLQHAQPPPQPRKKRPEDFKFGKILGEGSFSTVVLARELATSREYAIKILEKRHIIKENKVPYVTRERDVMSRLDHPFFVKLYFTFQDDEKLYFGLSYAKNGELLKYIRKIGSFDETCTRFYTAEIVSALEYLHGKGIIHRDLKPENILLNEDMHIQITDFGTAKVLSPESKQARANSFVGTAQYVSPELLTEKSACKSSDLWALGCIIYQLVAGLPPFRAGNEYLIFQKIIKLEYDFPEKFFPKARDLVEKLLVLDATKRLGCEEMEGYGPLKAHPFFESVTWENLHQQTPPKLTAYLPAMSEDDEDCYGNYDNLLSQFGCMQVSSSSSSHSLSASDTGLPQRSGSNIEQYIHDLDSNSFELDLQFSEDEKRLLLEKQAGGNPWHQFVENNLILKMGPVDKRKGLFARRRQLLLTEGPHLYYVDPVNKVLKGEIPWSQELRPEAKNFKTFFVHTPNRTYYLMDPSGNAHKWCRKIQEVWRQRYQSHPDAAVQ
  
Inhibitor
Name:
BDBM50296953
Synonyms:
(Z)-5-(2,4-Dichlorophenyl)-3-phenylpent-2-enoic Acid | CHEMBL550195
Type:
Small organic molecule
Emp. Form.:
C17H14Cl2O2
Mol. Mass.:
321.198
SMILES:
OC(=O)\C=C(\CCc1ccc(Cl)cc1Cl)c1ccccc1
Structure:
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