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Target Report Card

Target Name and Classification

Target ID CHEMBL4282
Target Type SINGLE PROTEIN
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
CHEMBL3038463 AKT/p21CIP1 PROTEIN COMPLEX
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

PDBe 1H10 1UNP 1UNQ 1UNR 2UVM 2UZR 2UZS 3CQU 3CQW 3MV5 3MVH 3O96 3OCB 3OW4 3QKK 3QKL 3QKM 4EJN 4EKK 4EKL 4GV1 5KCV
CREDO 1H10 1UNP 1UNQ 1UNR 2UVM 2UZR 2UZS 3CQU 3CQW 3MV5 3MVH 3O96 3OCB 3OW4 3QKK 3QKL 3QKM 4EJN 4EKK 4EKL 4GV1 5KCV
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