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ChEMBL

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Target Report Card

Target Name and Classification

Target ID CHEMBL2487
Target Type SINGLE PROTEIN
Preferred Name Beta amyloid A4 protein
Synonyms A4 | ABPP | AD1 | AICD-50 | AICD-57 | AICD-59 | AID(50) | AID(57) | AID(59) | APP | APP | APPI | Abeta40 | Abeta42 | Alpha-CTF | Alpha-secretase C-terminal fragment | Alzheimer disease amyloid protein | Amyloid intracellular domain 50 | Amyloid intracellular domain 57 | Amyloid intracellular domain 59 | Amyloid precursor protein | Amyloid-beta A4 protein | Amyloid-beta precursor protein | Amyloid-beta protein 40 | Amyloid-beta protein 42 | Beta-APP40 | Beta-APP42 | Beta-CTF | Beta-secretase C-terminal fragment | C31 | C80 | C83 | C99 | CVAP | Cerebral vascular amyloid peptide | Gamma-CTF(50) | Gamma-CTF(57) | Gamma-CTF(59) | Gamma-secretase C-terminal fragment 50 | Gamma-secretase C-terminal fragment 57 | Gamma-secretase C-terminal fragment 59 | N-APP | P3(40) | P3(42) | PN-II | PreA4 | Protease nexin-II | S-APP-alpha | S-APP-beta | Soluble APP-alpha | Soluble APP-beta
Organism Homo sapiens
Species Group No
Protein Target Classification
  • membrane receptor

Target Components

Component Description Relationship Accession
Amyloid-beta A4 protein SINGLE PROTEIN P05067

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL1743004 CRENEZUMAB Beta amyloid A4 protein inhibitor 3 Other Other PubMed
CHEMBL1743025 GANTENERUMAB Beta amyloid A4 protein other 3 PubMed
CHEMBL1743072 SOLANEZUMAB Beta amyloid A4 protein other 3 PubMed
CHEMBL2108576 BAPINEUZUMAB Beta amyloid A4 protein other 3 PubMed
CHEMBL3039540 ADUCANUMAB Beta amyloid A4 protein other 3 PubMed
CHEMBL1743058 PONEZUMAB Beta amyloid A4 protein other 2 PubMed
CHEMBL2109300 GSK933776 Beta amyloid A4 protein other 2 PubMed
CHEMBL3833321 BAN2401 Beta amyloid A4 protein inhibitor 2 PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000142192
Ensembl ENSG00000142192
GO Cellular Component GO:0005576 (extracellular region)
GO:0005615 (extracellular space)
GO:0005622 (intracellular)
GO:0005641 (nuclear envelope lumen)
GO:0005737 (cytoplasm)
GO:0005764 (lysosome)
GO:0005768 (endosome)
GO:0005769 (early endosome)
GO:0005788 (endoplasmic reticulum lumen)
GO:0005790 (smooth endoplasmic reticulum)
GO:0005791 (rough endoplasmic reticulum)
GO:0005794 (Golgi apparatus)
GO:0005796 (Golgi lumen)
GO:0005829 (cytosol)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0005905 (clathrin-coated pit)
GO:0005911 (cell-cell junction)
GO:0009986 (cell surface)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0030134 (ER to Golgi transport vesicle)
GO:0030424 (axon)
GO:0030425 (dendrite)
GO:0030426 (growth cone)
GO:0031093 (platelet alpha granule lumen)
GO:0031232 (extrinsic component of external side of plasma membrane)
GO:0031410 (cytoplasmic vesicle)
GO:0031594 (neuromuscular junction)
GO:0031904 (endosome lumen)
GO:0032588 (trans-Golgi network membrane)
GO:0032590 (dendrite membrane)
GO:0032991 (macromolecular complex)
GO:0034361 (very-low-density lipoprotein particle)
GO:0034362 (low-density lipoprotein particle)
GO:0034363 (intermediate-density lipoprotein particle)
GO:0034364 (high-density lipoprotein particle)
GO:0035253 (ciliary rootlet)
GO:0043005 (neuron projection)
GO:0043197 (dendritic spine)
GO:0043198 (dendritic shaft)
GO:0043235 (receptor complex)
GO:0044297 (cell body)
GO:0044304 (main axon)
GO:0045121 (membrane raft)
GO:0045177 (apical part of cell)
GO:0045202 (synapse)
GO:0048471 (perinuclear region of cytoplasm)
GO:0051233 (spindle midzone)
GO:0070062 (extracellular exosome)
GO:0070381 (endosome to plasma membrane transport vesicle)
GO:0097060 (synaptic membrane)
GO:0097449 (astrocyte projection)
GO:0098793 (presynapse)
GO:0098794 (postsynapse)
GO:0106003 (amyloid-beta complex)
GO:1990761 (growth cone lamellipodium)
GO:1990777 (lipoprotein particle)
GO:1990812 (growth cone filopodium)
GO Molecular Function GO:0003677 (DNA binding)
GO:0004867 (serine-type endopeptidase inhibitor activity)
GO:0005102 (receptor binding)
GO:0005109 (frizzled binding)
GO:0005158 (insulin receptor binding)
GO:0005178 (integrin binding)
GO:0005515 (protein binding)
GO:0008201 (heparin binding)
GO:0016504 (peptidase activator activity)
GO:0019899 (enzyme binding)
GO:0030414 (peptidase inhibitor activity)
GO:0030546 (receptor activator activity)
GO:0030549 (acetylcholine receptor activator activity)
GO:0033130 (acetylcholine receptor binding)
GO:0034185 (apolipoprotein binding)
GO:0042056 (chemoattractant activity)
GO:0042802 (identical protein binding)
GO:0042803 (protein homodimerization activity)
GO:0043395 (heparan sulfate proteoglycan binding)
GO:0046872 (metal ion binding)
GO:0046875 (ephrin receptor binding)
GO:0046914 (transition metal ion binding)
GO:0046982 (protein heterodimerization activity)
GO:0046983 (protein dimerization activity)
GO:0050750 (low-density lipoprotein particle receptor binding)
GO:0051087 (chaperone binding)
GO:0051425 (PTB domain binding)
GO:0070851 (growth factor receptor binding)
GO:0097645 (amylin binding)
GO:1904399 (heparan sulfate binding)
GO Biological Process GO:0000122 (negative regulation of transcription from RNA polymerase II promoter)
GO:0000185 (activation of MAPKKK activity)
GO:0000187 (activation of MAPK activity)
GO:0001774 (microglial cell activation)
GO:0001878 (response to yeast)
GO:0001934 (positive regulation of protein phosphorylation)
GO:0001967 (suckling behavior)
GO:0002265 (astrocyte activation involved in immune response)
GO:0002576 (platelet degranulation)
GO:0006378 (mRNA polyadenylation)
GO:0006417 (regulation of translation)
GO:0006468 (protein phosphorylation)
GO:0006878 (cellular copper ion homeostasis)
GO:0006897 (endocytosis)
GO:0006915 (apoptotic process)
GO:0006979 (response to oxidative stress)
GO:0006990 (positive regulation of transcription from RNA polymerase II promoter involved in unfolded protein response)
GO:0007155 (cell adhesion)
GO:0007176 (regulation of epidermal growth factor-activated receptor activity)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0007193 (adenylate cyclase-inhibiting G-protein coupled receptor signaling pathway)
GO:0007204 (positive regulation of cytosolic calcium ion concentration)
GO:0007219 (Notch signaling pathway)
GO:0007268 (chemical synaptic transmission)
GO:0007399 (nervous system development)
GO:0007409 (axonogenesis)
GO:0007611 (learning or memory)
GO:0007612 (learning)
GO:0007613 (memory)
GO:0007617 (mating behavior)
GO:0007626 (locomotory behavior)
GO:0008088 (axo-dendritic transport)
GO:0008203 (cholesterol metabolic process)
GO:0008285 (negative regulation of cell proliferation)
GO:0008306 (associative learning)
GO:0008344 (adult locomotory behavior)
GO:0008542 (visual learning)
GO:0009987 (cellular process)
GO:0010288 (response to lead ion)
GO:0010466 (negative regulation of peptidase activity)
GO:0010468 (regulation of gene expression)
GO:0010628 (positive regulation of gene expression)
GO:0010629 (negative regulation of gene expression)
GO:0010739 (positive regulation of protein kinase A signaling)
GO:0010800 (positive regulation of peptidyl-threonine phosphorylation)
GO:0010823 (negative regulation of mitochondrion organization)
GO:0010951 (negative regulation of endopeptidase activity)
GO:0010952 (positive regulation of peptidase activity)
GO:0010971 (positive regulation of G2/M transition of mitotic cell cycle)
GO:0010996 (response to auditory stimulus)
GO:0014005 (microglia development)
GO:0016199 (axon midline choice point recognition)
GO:0016322 (neuron remodeling)
GO:0016358 (dendrite development)
GO:0019722 (calcium-mediated signaling)
GO:0019731 (antibacterial humoral response)
GO:0019732 (antifungal humoral response)
GO:0030111 (regulation of Wnt signaling pathway)
GO:0030198 (extracellular matrix organization)
GO:0030816 (positive regulation of cAMP metabolic process)
GO:0030900 (forebrain development)
GO:0031175 (neuron projection development)
GO:0032092 (positive regulation of protein binding)
GO:0032640 (tumor necrosis factor production)
GO:0032930 (positive regulation of superoxide anion generation)
GO:0033138 (positive regulation of peptidyl-serine phosphorylation)
GO:0034121 (regulation of toll-like receptor signaling pathway)
GO:0035235 (ionotropic glutamate receptor signaling pathway)
GO:0040014 (regulation of multicellular organism growth)
GO:0042157 (lipoprotein metabolic process)
GO:0042327 (positive regulation of phosphorylation)
GO:0043065 (positive regulation of apoptotic process)
GO:0043280 (positive regulation of cysteine-type endopeptidase activity involved in apoptotic process)
GO:0043393 (regulation of protein binding)
GO:0043410 (positive regulation of MAPK cascade)
GO:0043687 (post-translational protein modification)
GO:0044267 (cellular protein metabolic process)
GO:0045087 (innate immune response)
GO:0045429 (positive regulation of nitric oxide biosynthetic process)
GO:0045665 (negative regulation of neuron differentiation)
GO:0045666 (positive regulation of neuron differentiation)
GO:0045745 (positive regulation of G-protein coupled receptor protein signaling pathway)
GO:0045931 (positive regulation of mitotic cell cycle)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0046330 (positive regulation of JNK cascade)
GO:0048143 (astrocyte activation)
GO:0048169 (regulation of long-term neuronal synaptic plasticity)
GO:0048669 (collateral sprouting in absence of injury)
GO:0050730 (regulation of peptidyl-tyrosine phosphorylation)
GO:0050731 (positive regulation of peptidyl-tyrosine phosphorylation)
GO:0050803 (regulation of synapse structure or activity)
GO:0050808 (synapse organization)
GO:0050829 (defense response to Gram-negative bacterium)
GO:0050830 (defense response to Gram-positive bacterium)
GO:0050867 (positive regulation of cell activation)
GO:0050885 (neuromuscular process controlling balance)
GO:0050918 (positive chemotaxis)
GO:0051044 (positive regulation of membrane protein ectodomain proteolysis)
GO:0051091 (positive regulation of sequence-specific DNA binding transcription factor activity)
GO:0051092 (positive regulation of NF-kappaB transcription factor activity)
GO:0051124 (synaptic growth at neuromuscular junction)
GO:0051247 (positive regulation of protein metabolic process)
GO:0051260 (protein homooligomerization)
GO:0051262 (protein tetramerization)
GO:0051402 (neuron apoptotic process)
GO:0051563 (smooth endoplasmic reticulum calcium ion homeostasis)
GO:0051897 (positive regulation of protein kinase B signaling)
GO:0061098 (positive regulation of protein tyrosine kinase activity)
GO:0061844 (antimicrobial humoral immune response mediated by antimicrobial peptide)
GO:0061890 (positive regulation of astrocyte activation)
GO:0061903 (positive regulation of 1-phosphatidylinositol-3-kinase activity)
GO:0070206 (protein trimerization)
GO:0070374 (positive regulation of ERK1 and ERK2 cascade)
GO:0071320 (cellular response to cAMP)
GO:0071874 (cellular response to norepinephrine stimulus)
GO:0090026 (positive regulation of monocyte chemotaxis)
GO:0090090 (negative regulation of canonical Wnt signaling pathway)
GO:0090647 (modulation of age-related behavioral decline)
GO:0098815 (modulation of excitatory postsynaptic potential)
GO:0150003 (regulation of spontaneous synaptic transmission)
GO:1900122 (positive regulation of receptor binding)
GO:1900181 (negative regulation of protein localization to nucleus)
GO:1900272 (negative regulation of long-term synaptic potentiation)
GO:1900273 (positive regulation of long-term synaptic potentiation)
GO:1901215 (negative regulation of neuron death)
GO:1901216 (positive regulation of neuron death)
GO:1901224 (positive regulation of NIK/NF-kappaB signaling)
GO:1902003 (regulation of amyloid-beta formation)
GO:1902004 (positive regulation of beta-amyloid formation)
GO:1902514 (regulation of calcium ion transmembrane transport via high voltage-gated calcium channel)
GO:1902949 (positive regulation of tau-protein kinase activity)
GO:1902950 (regulation of dendritic spine maintenance)
GO:1903048 (regulation of acetylcholine-gated cation channel activity)
GO:1903223 (positive regulation of oxidative stress-induced neuron death)
GO:1903980 (positive regulation of microglial cell activation)
GO:1904022 (positive regulation of G-protein coupled receptor internalization)
GO:1904591 (positive regulation of protein import)
GO:1904646 (cellular response to beta-amyloid)
GO:1905598 (negative regulation of low-density lipoprotein receptor activity)
GO:1905893 (positive regulation of cellular response to thapsigargin)
GO:1905896 (positive regulation of cellular response to tunicamycin)
GO:1905898 (positive regulation of response to endoplasmic reticulum stress)
GO:1905906 (regulation of amyloid fibril formation)
GO:1905908 (positive regulation of amyloid fibril formation)
GO:1905945 (regulation of response to calcium ion)
GO:1990000 (amyloid fibril formation)
GO:1990090 (cellular response to nerve growth factor stimulus)
GO:1990535 (neuron projection maintenance)
GO:2000273 (positive regulation of receptor activity)
GO:2000310 (regulation of N-methyl-D-aspartate selective glutamate receptor activity)
GO:2000406 (positive regulation of T cell migration)
GO:2000463 (positive regulation of excitatory postsynaptic potential)
Wikipedia Amyloid_precursor_protein

Target Cross References - Protein

canSAR P05067
CGD Alzheimer disease, familial; Cerebral amyloid angiopathy
Human Protein Atlas ENSG00000142192
IntAct P05067
MICAD NBK23203 (Aggregates of Amyloid-beta peptide)
NBK23213 (Aggregates of Beta-amyloid peptides)
NBK23443 (Aggregates of Beta-amyloid peptide)
NBK32300 (Amyloid-beta peptide)
NBK57129 (Amyloid-beta peptide)
NBK82968 (Beta-amyloid)
NBK82969 (Beta-amyloid (A-beta))
NBK84117 (Beta-amyloid plaques)
Open Targets ENSG00000142192
PharmGKB PA24910
Reactome R-HSA-114608 (Platelet degranulation.)
R-HSA-1810476 (RIP-mediated NFkB activation via ZBP1.)
R-HSA-3000178 (ECM proteoglycans.)
R-HSA-3134963 (DEx/H-box helicases activate type I IFN and inflammatory cytokines production.)
R-HSA-381426 (Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs).)
R-HSA-416476 (G alpha (q) signalling events.)
R-HSA-418594 (G alpha (i) signalling events.)
R-HSA-432720 (Lysosome Vesicle Biogenesis.)
R-HSA-444473 (Formyl peptide receptors bind formyl peptides and many other ligands.)
R-HSA-445989 (TAK1 activates NFkB by phosphorylation and activation of IKKs complex.)
R-HSA-844456 (The NLRP3 inflammasome.)
R-HSA-879415 (Advanced glycosylation endproduct receptor signaling.)
R-HSA-8862803 (Deregulated CDK5 triggers multiple neurodegenerative pathways in Alzheimer's disease models.)
R-HSA-8957275 (Post-translational protein phosphorylation.)
R-HSA-933542 (TRAF6 mediated NF-kB activation.)
R-HSA-977225 (Amyloid fiber formation.)
UniProt B2R5V1 B4DII8 D3DSD1 D3DSD2 D3DSD3 P05067 P09000 P78438 Q13764 Q13778 Q13793 Q16011 Q16014 Q16019 Q16020 Q6GSC0 Q8WZ99 Q9BT38 Q9UC33 Q9UCA9 Q9UCB6 Q9UCC8 Q9UCD1 Q9UQ58

Target Cross References - Domain

InterPro IPR002223 (Kunitz_BPTI.)
IPR008154 (Amyloid_glyco_extra.)
IPR008155 (Amyloid_glyco.)
IPR011178 (Amyloid_glyco_Cu-bd.)
IPR011993 (PH-like_dom_sf.)
IPR013803 (Amyloid_glyco_Abeta.)
IPR015849 (Amyloid_glyco_heparin-bd.)
IPR019543 (APP_amyloid_C.)
IPR019744 (Amyloid_glyco_extracell_CS.)
IPR019745 (Amyloid_glyco_intracell_CS.)
IPR020901 (Prtase_inh_Kunz-CS.)
IPR024329 (Amyloid_glyco_E2_domain.)
IPR028866 (APP.)
IPR036176 (E2_sf.)
IPR036454 (Amyloid_glyco_heparin-bd_sf.)
IPR036669 (Amyloid_Cu-bd_sf.)
IPR036880 (Kunitz_BPTI_sf.)
IPR037071 (Amyloid_glyco_Abeta_sf.)
Pfam PF00014 (Kunitz_BPTI)
PF02177 (APP_N)
PF03494 (Beta-APP)
PF10515 (APP_amyloid)
PF12924 (APP_Cu_bd)
PF12925 (APP_E2)

Target Cross References - Structure

PDBe 1AAP 1BRC 1CA0 1MWP 1TAW 1X11 1ZJD 2FJZ 2FK1 2FK2 2FK3 2FKL 2FMA 2G47 2IPU 2R0W 2WK3 2Y29 2Y2A 2Y3J 2Y3K 2Y3L 3AYU 3BAE More...
CREDO 1AAP 1BRC 1CA0 1MWP 1TAW 1X11 1ZJD 2FJZ 2FK1 2FK2 2FK3 2FKL 2FMA 2G47 2IPU 2R0W 2WK3 2Y29 2Y2A 2Y3J 2Y3K 2Y3L 3AYU 3BAE More...
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