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Target Report Card

Target Name and Classification

Target ID CHEMBL2534
Preferred Name 3-phosphoinositide dependent protein kinase-1
Synonyms 3-phosphoinositide-dependent protein kinase 1 | PDK1 | PDPK1 | hPDK1
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > agc protein kinase group > agc protein kinase pdk1 subfamily

Target Components

Component Description Relationship Accession
3-phosphoinositide-dependent protein kinase 1 SINGLE PROTEIN O15530

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL574737 (7S)-HYDROXYL-STAUROSPORINE 3-phosphoinositide dependent protein kinase-1 inhibitor 2 Other PubMed PubMed
CHEMBL1650595 AR-12 3-phosphoinositide dependent protein kinase-1 inhibitor 1 PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000140992
Ensembl ENSG00000140992
GO Cellular Component GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0005737 (cytoplasm)
GO:0005829 (cytosol)
GO:0005886 (plasma membrane)
GO:0005925 (focal adhesion)
GO:0016020 (membrane)
GO:0016023 (cytoplasmic, membrane-bounded vesicle)
GO:0030054 (cell junction)
GO:0042995 (cell projection)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0004672 (protein kinase activity)
GO:0004674 (protein serine/threonine kinase activity)
GO:0004676 (3-phosphoinositide-dependent protein kinase activity)
GO:0005158 (insulin receptor binding)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0016004 (phospholipase activator activity)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0019901 (protein kinase binding)
GO:0043274 (phospholipase binding)
GO Biological Process GO:0002223 (stimulatory C-type lectin receptor signaling pathway)
GO:0003323 (type B pancreatic cell development)
GO:0006351 (transcription, DNA-templated)
GO:0006355 (regulation of transcription, DNA-templated)
GO:0006468 (protein phosphorylation)
GO:0006469 (negative regulation of protein kinase activity)
GO:0006972 (hyperosmotic response)
GO:0007173 (epidermal growth factor receptor signaling pathway)
GO:0010518 (positive regulation of phospholipase activity)
GO:0010594 (regulation of endothelial cell migration)
GO:0010667 (negative regulation of cardiac muscle cell apoptotic process)
GO:0016310 (phosphorylation)
GO:0016477 (cell migration)
GO:0018105 (peptidyl-serine phosphorylation)
GO:0018107 (peptidyl-threonine phosphorylation)
GO:0019722 (calcium-mediated signaling)
GO:0030036 (actin cytoskeleton organization)
GO:0030168 (platelet activation)
GO:0030512 (negative regulation of transforming growth factor beta receptor signaling pathway)
GO:0031295 (T cell costimulation)
GO:0032148 (activation of protein kinase B activity)
GO:0032869 (cellular response to insulin stimulus)
GO:0034122 (negative regulation of toll-like receptor signaling pathway)
GO:0035556 (intracellular signal transduction)
GO:0038095 (Fc-epsilon receptor signaling pathway)
GO:0043122 (regulation of I-kappaB kinase/NF-kappaB signaling)
GO:0043304 (regulation of mast cell degranulation)
GO:0046777 (protein autophosphorylation)
GO:0048015 (phosphatidylinositol-mediated signaling)
GO:0048041 (focal adhesion assembly)
GO:0050852 (T cell receptor signaling pathway)
GO:0051281 (positive regulation of release of sequestered calcium ion into cytosol)
GO:0071364 (cellular response to epidermal growth factor stimulus)
GO:0090004 (positive regulation of establishment of protein localization to plasma membrane)
GO:0097191 (extrinsic apoptotic signaling pathway)
Wikipedia Phosphoinositide-dependent_kinase-1

Target Cross References - Protein

canSAR O15530
Human Protein Atlas ENSG00000140992
IntAct O15530
Guide to Pharmacology 1519
Open Targets ENSG00000140992
PharmGKB PA33160
Pharos O15530 (Tchem)
Reactome R-HSA-114604 (GPVI-mediated activation cascade.)
R-HSA-1257604 (PIP3 activates AKT signaling.)
R-HSA-165158 (Activation of AKT2.)
R-HSA-202424 (Downstream TCR signaling.)
R-HSA-2730905 (Role of LAT2/NTAL/LAB on calcium mobilization.)
R-HSA-2871837 (FCERI mediated NF-kB activation.)
R-HSA-354192 (Integrin alphaIIb beta3 signaling.)
R-HSA-389357 (CD28 dependent PI3K/Akt signaling.)
R-HSA-389513 (CTLA4 inhibitory signaling.)
R-HSA-392451 (G beta:gamma signalling through PI3Kgamma.)
R-HSA-444257 (RSK activation.)
R-HSA-5218920 (VEGFR2 mediated vascular permeability.)
R-HSA-5218921 (VEGFR2 mediated cell proliferation.)
R-HSA-5607764 (CLEC7A (Dectin-1) signaling.)
R-HSA-5625740 (RHO GTPases activate PKNs.)
R-HSA-5674400 (Constitutive Signaling by AKT1 E17K in Cancer.)
R-HSA-6804757 (Regulation of TP53 Degradation.)
UniProt H0Y4Z0 O15530 Q59EH6 Q6FI20 Q8IV52 Q9BRD5

Target Cross References - Domain

InterPro IPR000719 (Prot_kinase_dom.)
IPR008271 (Ser/Thr_kinase_AS.)
IPR011009 (Kinase-like_dom.)
IPR011993 (PH_dom-like.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR033931 (PDK1-typ_PH.)
Pfam PF00069 (Pkinase)
PF14593 (PH_3)

Target Cross References - Structure

PDBe 1H1W 1OKY 1OKZ 1UU3 1UU7 1UU8 1UU9 1UVR 1W1D 1W1G 1W1H 1Z5M 2BIY 2PE0 2PE1 2PE2 2R7B 2VKI 2XCH 2XCK 3H9O 3HRC 3HRF 3ION More...
CREDO 1H1W 1OKY 1OKZ 1UU3 1UU7 1UU8 1UU9 1UVR 1W1D 1W1G 1W1H 1Z5M 2BIY 2PE0 2PE1 2PE2 2R7B 2VKI 2XCH 2XCK 3H9O 3HRC 3HRF 3ION More...