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Target Report Card

Target Name and Classification

Target ID CHEMBL4282
Preferred Name Serine/threonine-protein kinase AKT
Synonyms AKT1 | PKB alpha | PKB | PKB | Protein kinase B alpha | Protein kinase B | Proto-oncogene c-Akt | RAC | RAC-PK-alpha | RAC-alpha serine/threonine-protein kinase
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > agc protein kinase group > agc protein kinase akt family

Target Components

Component Description Relationship Accession
RAC-alpha serine/threonine-protein kinase SINGLE PROTEIN P31749

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2111353 Serine/threonine-protein kinase AKT PROTEIN FAMILY
CHEMBL3885629 RAC-alpha serine/threonine-protein kinase/Ribosomal protein S6 kinase beta-1 PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL3545003 MSC-2363318A Serine/threonine-protein kinase AKT inhibitor 1 Other
CHEMBL3545049 BAY-1125976 Serine/threonine-protein kinase AKT inhibitor 1 DOI DOI
CHEMBL3545143 SR-13668 Serine/threonine-protein kinase AKT inhibitor 1 PubMed PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000142208
Ensembl ENSG00000142208
GO Cellular Component GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0005737 (cytoplasm)
GO:0005739 (mitochondrion)
GO:0005819 (spindle)
GO:0005829 (cytosol)
GO:0005886 (plasma membrane)
GO:0005911 (cell-cell junction)
GO:0015630 (microtubule cytoskeleton)
GO:0016020 (membrane)
GO:0031982 (vesicle)
GO:0032991 (macromolecular complex)
GO:0036064 (ciliary basal body)
GO:0098794 (postsynapse)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0004672 (protein kinase activity)
GO:0004674 (protein serine/threonine kinase activity)
GO:0004712 (protein serine/threonine/tyrosine kinase activity)
GO:0005080 (protein kinase C binding)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0005547 (phosphatidylinositol-3,4,5-trisphosphate binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0019899 (enzyme binding)
GO:0019901 (protein kinase binding)
GO:0030235 (nitric-oxide synthase regulator activity)
GO:0032794 (GTPase activating protein binding)
GO:0042802 (identical protein binding)
GO:0042803 (protein homodimerization activity)
GO:0043325 (phosphatidylinositol-3,4-bisphosphate binding)
GO:0051721 (protein phosphatase 2A binding)
GO:0071889 (14-3-3 protein binding)
GO Biological Process GO:0000060 (protein import into nucleus, translocation)
GO:0001649 (osteoblast differentiation)
GO:0001893 (maternal placenta development)
GO:0001934 (positive regulation of protein phosphorylation)
GO:0001938 (positive regulation of endothelial cell proliferation)
GO:0005975 (carbohydrate metabolic process)
GO:0005977 (glycogen metabolic process)
GO:0005978 (glycogen biosynthetic process)
GO:0005979 (regulation of glycogen biosynthetic process)
GO:0006006 (glucose metabolic process)
GO:0006412 (translation)
GO:0006417 (regulation of translation)
GO:0006464 (cellular protein modification process)
GO:0006468 (protein phosphorylation)
GO:0006469 (negative regulation of protein kinase activity)
GO:0006809 (nitric oxide biosynthetic process)
GO:0006915 (apoptotic process)
GO:0006924 (activation-induced cell death of T cells)
GO:0006954 (inflammatory response)
GO:0006974 (cellular response to DNA damage stimulus)
GO:0006979 (response to oxidative stress)
GO:0007165 (signal transduction)
GO:0007173 (epidermal growth factor receptor signaling pathway)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0007249 (I-kappaB kinase/NF-kappaB signaling)
GO:0007275 (multicellular organism development)
GO:0007281 (germ cell development)
GO:0007399 (nervous system development)
GO:0007568 (aging)
GO:0008283 (cell proliferation)
GO:0008284 (positive regulation of cell proliferation)
GO:0008286 (insulin receptor signaling pathway)
GO:0008637 (apoptotic mitochondrial changes)
GO:0008643 (carbohydrate transport)
GO:0009408 (response to heat)
GO:0009725 (response to hormone)
GO:0010033 (response to organic substance)
GO:0010507 (negative regulation of autophagy)
GO:0010628 (positive regulation of gene expression)
GO:0010629 (negative regulation of gene expression)
GO:0010748 (negative regulation of plasma membrane long-chain fatty acid transport)
GO:0010763 (positive regulation of fibroblast migration)
GO:0010765 (positive regulation of sodium ion transport)
GO:0010907 (positive regulation of glucose metabolic process)
GO:0010918 (positive regulation of mitochondrial membrane potential)
GO:0010951 (negative regulation of endopeptidase activity)
GO:0010975 (regulation of neuron projection development)
GO:0014065 (phosphatidylinositol 3-kinase signaling)
GO:0016242 (negative regulation of macroautophagy)
GO:0016310 (phosphorylation)
GO:0016567 (protein ubiquitination)
GO:0018105 (peptidyl-serine phosphorylation)
GO:0018107 (peptidyl-threonine phosphorylation)
GO:0019221 (cytokine-mediated signaling pathway)
GO:0021510 (spinal cord development)
GO:0030030 (cell projection organization)
GO:0030154 (cell differentiation)
GO:0030163 (protein catabolic process)
GO:0030168 (platelet activation)
GO:0030212 (hyaluronan metabolic process)
GO:0030307 (positive regulation of cell growth)
GO:0030334 (regulation of cell migration)
GO:0031018 (endocrine pancreas development)
GO:0031295 (T cell costimulation)
GO:0031397 (negative regulation of protein ubiquitination)
GO:0031641 (regulation of myelination)
GO:0031659 (positive regulation of cyclin-dependent protein serine/threonine kinase activity involved in G1/S transition of mitotic cell cycle)
GO:0031663 (lipopolysaccharide-mediated signaling pathway)
GO:0031929 (TOR signaling)
GO:0031999 (negative regulation of fatty acid beta-oxidation)
GO:0032079 (positive regulation of endodeoxyribonuclease activity)
GO:0032091 (negative regulation of protein binding)
GO:0032094 (response to food)
GO:0032148 (activation of protein kinase B activity)
GO:0032270 (positive regulation of cellular protein metabolic process)
GO:0032287 (peripheral nervous system myelin maintenance)
GO:0032436 (positive regulation of proteasomal ubiquitin-dependent protein catabolic process)
GO:0032869 (cellular response to insulin stimulus)
GO:0032880 (regulation of protein localization)
GO:0033138 (positive regulation of peptidyl-serine phosphorylation)
GO:0034405 (response to fluid shear stress)
GO:0034614 (cellular response to reactive oxygen species)
GO:0035556 (intracellular signal transduction)
GO:0035655 (interleukin-18-mediated signaling pathway)
GO:0035924 (cellular response to vascular endothelial growth factor stimulus)
GO:0036294 (cellular response to decreased oxygen levels)
GO:0038061 (NIK/NF-kappaB signaling)
GO:0042593 (glucose homeostasis)
GO:0042981 (regulation of apoptotic process)
GO:0043065 (positive regulation of apoptotic process)
GO:0043066 (negative regulation of apoptotic process)
GO:0043154 (negative regulation of cysteine-type endopeptidase activity involved in apoptotic process)
GO:0043276 (anoikis)
GO:0043488 (regulation of mRNA stability)
GO:0043491 (protein kinase B signaling)
GO:0043536 (positive regulation of blood vessel endothelial cell migration)
GO:0045429 (positive regulation of nitric oxide biosynthetic process)
GO:0045600 (positive regulation of fat cell differentiation)
GO:0045725 (positive regulation of glycogen biosynthetic process)
GO:0045742 (positive regulation of epidermal growth factor receptor signaling pathway)
GO:0045792 (negative regulation of cell size)
GO:0045861 (negative regulation of proteolysis)
GO:0045893 (positive regulation of transcription, DNA-templated)
GO:0045907 (positive regulation of vasoconstriction)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0046326 (positive regulation of glucose import)
GO:0046329 (negative regulation of JNK cascade)
GO:0046622 (positive regulation of organ growth)
GO:0046777 (protein autophosphorylation)
GO:0046889 (positive regulation of lipid biosynthetic process)
GO:0048009 (insulin-like growth factor receptor signaling pathway)
GO:0048661 (positive regulation of smooth muscle cell proliferation)
GO:0050999 (regulation of nitric-oxide synthase activity)
GO:0051000 (positive regulation of nitric-oxide synthase activity)
GO:0051091 (positive regulation of sequence-specific DNA binding transcription factor activity)
GO:0051146 (striated muscle cell differentiation)
GO:0051186 (cofactor metabolic process)
GO:0051898 (negative regulation of protein kinase B signaling)
GO:0060079 (excitatory postsynaptic potential)
GO:0060416 (response to growth hormone)
GO:0060644 (mammary gland epithelial cell differentiation)
GO:0060709 (glycogen cell differentiation involved in embryonic placenta development)
GO:0060716 (labyrinthine layer blood vessel development)
GO:0070141 (response to UV-A)
GO:0071260 (cellular response to mechanical stimulus)
GO:0071276 (cellular response to cadmium ion)
GO:0071356 (cellular response to tumor necrosis factor)
GO:0071363 (cellular response to growth factor stimulus)
GO:0071364 (cellular response to epidermal growth factor stimulus)
GO:0071380 (cellular response to prostaglandin E stimulus)
GO:0071407 (cellular response to organic cyclic compound)
GO:0071456 (cellular response to hypoxia)
GO:0071901 (negative regulation of protein serine/threonine kinase activity)
GO:0072655 (establishment of protein localization to mitochondrion)
GO:0072656 (maintenance of protein location in mitochondrion)
GO:0090201 (negative regulation of release of cytochrome c from mitochondria)
GO:0097011 (cellular response to granulocyte macrophage colony-stimulating factor stimulus)
GO:0097194 (execution phase of apoptosis)
GO:0100002 (negative regulation of protein kinase activity by protein phosphorylation)
GO:1900182 (positive regulation of protein localization to nucleus)
GO:1901215 (negative regulation of neuron death)
GO:1901653 (cellular response to peptide)
GO:1901796 (regulation of signal transduction by p53 class mediator)
GO:1902176 (negative regulation of oxidative stress-induced intrinsic apoptotic signaling pathway)
GO:1903078 (positive regulation of protein localization to plasma membrane)
GO:1903721 (positive regulation of I-kappaB phosphorylation)
GO:1990090 (cellular response to nerve growth factor stimulus)
GO:1990418 (response to insulin-like growth factor stimulus)
GO:2000010 (positive regulation of protein localization to cell surface)
GO:2001240 (negative regulation of extrinsic apoptotic signaling pathway in absence of ligand)
Wikipedia AKT1

Target Cross References - Protein

canSAR P31749
CGD Cowden syndrome 6; Proteus syndrome
Human Protein Atlas ENSG00000142208
IntAct P31749
Guide to Pharmacology 1479
Open Targets ENSG00000142208
PharmGKB PA24684
Pharos P31749 (Tchem)
Reactome R-HSA-111447 (Activation of BAD and translocation to mitochondria.)
R-HSA-114604 (GPVI-mediated activation cascade.)
R-HSA-1257604 (PIP3 activates AKT signaling.)
R-HSA-1358803 (Downregulation of ERBB2:ERBB3 signaling.)
R-HSA-1445148 (Translocation of GLUT4 to the plasma membrane.)
R-HSA-1474151 (Tetrahydrobiopterin (BH4) synthesis, recycling, salvage and regulation.)
R-HSA-165159 (mTOR signalling.)
R-HSA-198323 (AKT phosphorylates targets in the cytosol.)
R-HSA-198693 (AKT phosphorylates targets in the nucleus.)
R-HSA-199418 (Negative regulation of the PI3K/AKT network.)
R-HSA-203615 (eNOS activation.)
R-HSA-211163 (AKT-mediated inactivation of FOXO1A.)
R-HSA-354192 (Integrin alphaIIb beta3 signaling.)
R-HSA-3769402 (Deactivation of the beta-catenin transactivating complex.)
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-450385 (Butyrate Response Factor 1 (BRF1) binds and destabilizes mRNA.)
R-HSA-450604 (KSRP (KHSRP) binds and destabilizes mRNA.)
R-HSA-5218920 (VEGFR2 mediated vascular permeability.)
R-HSA-5628897 (TP53 Regulates Metabolic Genes.)
R-HSA-5674400 (Constitutive Signaling by AKT1 E17K in Cancer.)
R-HSA-6785807 (Interleukin-4 and 13 signaling.)
R-HSA-6804757 (Regulation of TP53 Degradation.)
R-HSA-6804758 (Regulation of TP53 Activity through Acetylation.)
R-HSA-6804759 (Regulation of TP53 Activity through Association with Co-factors.)
R-HSA-6811558 (PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling.)
R-HSA-69202 (Cyclin E associated events during G1/S transition.)
R-HSA-8849469 (PTK6 Regulates RTKs and Their Effectors AKT1 and DOK1.)
R-HSA-8876198 (RAB GEFs exchange GTP for GDP on RABs.)
R-HSA-8941332 (RUNX2 regulates genes involved in cell migration.)
R-HSA-8948751 (Regulation of PTEN stability and activity.)
UniProt B2RAM5 B7Z5R1 P31749 Q9BWB6

Target Cross References - Domain

InterPro IPR000719 (Prot_kinase_dom.)
IPR000961 (AGC-kinase_C.)
IPR001849 (PH_domain.)
IPR008271 (Ser/Thr_kinase_AS.)
IPR011009 (Kinase-like_dom_sf.)
IPR011993 (PH-like_dom_sf.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR017892 (Pkinase_C.)
IPR034676 (Akt1.)
Pfam PF00069 (Pkinase)
PF00169 (PH)
PF00433 (Pkinase_C)

Target Cross References - Structure