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Target3-phosphoinositide-dependent protein kinase 1
LigandBDBM50321582
Substrate/Competitorn/a
Meas. Tech.ChEMBL_639726 (CHEMBL1175615)
IC50 85±n/a nM
Citation Angiolini, MBanfi, PCasale, ECasuscelli, FFiorelli, CSaccardo, MBSilvagni, MZuccotto, F Structure-based optimization of potent PDK1 inhibitors. Bioorg Med Chem Lett20:4095-9 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
3-phosphoinositide-dependent protein kinase 1
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50321582
n/a
NameBDBM50321582
Synonyms:1-(3-aminopropyl)-8-(3-(2-(dimethylamino)-2-oxoethyl)phenylamino)-N-((2-methylpyridin-4-yl)methyl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL1172241
TypeSmall organic molecule
Emp. Form.C30H35N9O2
Mol. Mass.553.658
SMILESCN(C)C(=O)Cc1cccc(Nc2ncc3CCc4c(nn(CCCN)c4-c3n2)C(=O)NCc2ccnc(C)c2)c1
Structure
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