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ChEMBL Statistics
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Target Report Card

Target Name and Classification

Target ID CHEMBL2929
Target Type SINGLE PROTEIN
Preferred Name Subtilisin/kexin type 9
Synonyms NARC-1 | NARC1 | Neural apoptosis-regulated convertase 1 | PC9 | PCSK9 | Proprotein convertase 9 | Proprotein convertase subtilisin/kexin type 9 | Subtilisin/kexin-like protease PC9
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > protease > serine protease > serine protease sb clan > serine protease s8a subfamily

Target Components

Component Description Relationship Accession
Proprotein convertase subtilisin/kexin type 9 SINGLE PROTEIN Q8NBP7

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL2109540 Alirocumab Subtilisin/kexin type 9 inhibitor 4 DailyMed
CHEMBL2364655 EVOLOCUMAB Subtilisin/kexin type 9 inhibitor 4 DailyMed
CHEMBL3137349 BOCOCIZUMAB Subtilisin/kexin type 9 inhibitor 3 PubMed PubMed
CHEMBL2109539 RG-7652 Subtilisin/kexin type 9 inhibitor 2 PubMed PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000169174
Ensembl ENSG00000169174
GO Cellular Component GO:0005576 (extracellular region)
GO:0005615 (extracellular space)
GO:0005737 (cytoplasm)
GO:0005764 (lysosome)
GO:0005768 (endosome)
GO:0005769 (early endosome)
GO:0005770 (late endosome)
GO:0005783 (endoplasmic reticulum)
GO:0005791 (rough endoplasmic reticulum)
GO:0005794 (Golgi apparatus)
GO:0005886 (plasma membrane)
GO:0009986 (cell surface)
GO:0030134 (ER to Golgi transport vesicle)
GO:0031232 (extrinsic component of external side of plasma membrane)
GO:0048471 (perinuclear region of cytoplasm)
GO:1990666 (PCSK9-LDLR complex)
GO:1990667 (PCSK9-AnxA2 complex)
GO Molecular Function GO:0004252 (serine-type endopeptidase activity)
GO:0005515 (protein binding)
GO:0008233 (peptidase activity)
GO:0008236 (serine-type peptidase activity)
GO:0016787 (hydrolase activity)
GO:0019871 (sodium channel inhibitor activity)
GO:0030169 (low-density lipoprotein particle binding)
GO:0030547 (receptor inhibitor activity)
GO:0034185 (apolipoprotein binding)
GO:0034189 (very-low-density lipoprotein particle binding)
GO:0034190 (apolipoprotein receptor binding)
GO:0043621 (protein self-association)
GO:0044822 (poly(A) RNA binding)
GO:0050750 (low-density lipoprotein particle receptor binding)
GO:0070326 (very-low-density lipoprotein particle receptor binding)
GO Biological Process GO:0001822 (kidney development)
GO:0001889 (liver development)
GO:0001920 (negative regulation of receptor recycling)
GO:0002092 (positive regulation of receptor internalization)
GO:0006508 (proteolysis)
GO:0006629 (lipid metabolic process)
GO:0006641 (triglyceride metabolic process)
GO:0006644 (phospholipid metabolic process)
GO:0006915 (apoptotic process)
GO:0007041 (lysosomal transport)
GO:0008202 (steroid metabolic process)
GO:0008203 (cholesterol metabolic process)
GO:0009267 (cellular response to starvation)
GO:0010469 (regulation of receptor activity)
GO:0010989 (negative regulation of low-density lipoprotein particle clearance)
GO:0016485 (protein processing)
GO:0016540 (protein autoprocessing)
GO:0022008 (neurogenesis)
GO:0030182 (neuron differentiation)
GO:0032799 (low-density lipoprotein receptor particle metabolic process)
GO:0032802 (low-density lipoprotein particle receptor catabolic process)
GO:0032803 (regulation of low-density lipoprotein particle receptor catabolic process)
GO:0032805 (positive regulation of low-density lipoprotein particle receptor catabolic process)
GO:0032869 (cellular response to insulin stimulus)
GO:0042157 (lipoprotein metabolic process)
GO:0042632 (cholesterol homeostasis)
GO:0043523 (regulation of neuron apoptotic process)
GO:0043525 (positive regulation of neuron apoptotic process)
GO:2000272 (negative regulation of receptor activity)
GO:2000650 (negative regulation of sodium ion transmembrane transporter activity)
Wikipedia PCSK9

Target Cross References - Protein

CGD Hypercholesterolemia, familial, 3
Human Protein Atlas ENSG00000169174
IntAct Q8NBP7
Guide to Pharmacology 2388
Open Targets ENSG00000169174
PharmGKB PA38617
Reactome R-HSA-171052 (LDL-mediated lipid transport.)
R-HSA-8866427 (VLDLR internalisation and degradation.)
UniProt A8T640 C0JYY9 Q5PSM5 Q5SZQ2 Q8NBP7

Target Cross References - Domain

InterPro IPR000209 (Peptidase_S8/S53_dom.)
IPR009020 (Propept_inh.)
IPR010259 (S8pro/Inhibitor_I9.)
IPR015500 (Peptidase_S8_subtilisin-rel.)
IPR034193 (PCSK9_ProteinaseK-like.)
Pfam PF00082 (Peptidase_S8)
PF05922 (Inhibitor_I9)

Target Cross References - Structure

PDBe 2P4E 2PMW 2QTW 2W2M 2W2N 2W2O 2W2P 2W2Q 2XTJ 3BPS 3GCW 3GCX 3H42 3M0C 3P5B 3P5C 3SQO 4K8R 4NE9 4NMX 4OV6
CREDO 2P4E 2PMW 2QTW 2W2M 2W2N 2W2O 2W2P 2W2Q 2XTJ 3BPS 3GCW 3GCX 3H42 3M0C 3P5B 3P5C 3SQO 4K8R 4NE9 4NMX 4OV6
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