ChEMBL logo

ChEMBL

spacer
ChEMBL Statistics
  Loading Statistics...
spacer

Target Report Card

Target Name and Classification

Target ID CHEMBL3776
Target Type SINGLE PROTEIN
Preferred Name Caspase-8
Synonyms Apoptotic cysteine protease | Apoptotic protease Mch-5 | CAP4 | CASP-8 | CASP8 | Caspase-8 subunit p10 | Caspase-8 subunit p18 | Caspase-8 | FADD-homologous ICE/ced-3-like protease | FADD-like ICE | FLICE | ICE-like apoptotic protease 5 | MACH | MCH5 | MORT1-associated ced-3 homolog
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > protease > cysteine protease > cysteine protease cd clan > cysteine protease c14 family

Target Components

Component Description Relationship Accession
Caspase-8 SINGLE PROTEIN Q14790

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL3831289 Caspase PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL2105721 NIVOCASAN Caspase-8 inhibitor 2 PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000064012
Ensembl ENSG00000064012
GO Cellular Component GO:0005654 (nucleoplasm)
GO:0005737 (cytoplasm)
GO:0005739 (mitochondrion)
GO:0005741 (mitochondrial outer membrane)
GO:0005815 (microtubule organizing center)
GO:0005829 (cytosol)
GO:0005856 (cytoskeleton)
GO:0031264 (death-inducing signaling complex)
GO:0031265 (CD95 death-inducing signaling complex)
GO:0043005 (neuron projection)
GO:0043234 (protein complex)
GO:0044297 (cell body)
GO:0045121 (membrane raft)
GO:0097342 (ripoptosome)
GO Molecular Function GO:0004197 (cysteine-type endopeptidase activity)
GO:0005123 (death receptor binding)
GO:0005164 (tumor necrosis factor receptor binding)
GO:0005515 (protein binding)
GO:0008233 (peptidase activity)
GO:0008234 (cysteine-type peptidase activity)
GO:0016787 (hydrolase activity)
GO:0031625 (ubiquitin protein ligase binding)
GO:0032403 (protein complex binding)
GO:0035877 (death effector domain binding)
GO:0042802 (identical protein binding)
GO:0097110 (scaffold protein binding)
GO:0097153 (cysteine-type endopeptidase activity involved in apoptotic process)
GO:0097199 (cysteine-type endopeptidase activity involved in apoptotic signaling pathway)
GO Biological Process GO:0006508 (proteolysis)
GO:0006915 (apoptotic process)
GO:0006919 (activation of cysteine-type endopeptidase activity involved in apoptotic process)
GO:0006921 (cellular component disassembly involved in execution phase of apoptosis)
GO:0007166 (cell surface receptor signaling pathway)
GO:0009409 (response to cold)
GO:0010803 (regulation of tumor necrosis factor-mediated signaling pathway)
GO:0010939 (regulation of necrotic cell death)
GO:0016032 (viral process)
GO:0030101 (natural killer cell activation)
GO:0030225 (macrophage differentiation)
GO:0032025 (response to cobalt ion)
GO:0032355 (response to estradiol)
GO:0032496 (response to lipopolysaccharide)
GO:0034612 (response to tumor necrosis factor)
GO:0035666 (TRIF-dependent toll-like receptor signaling pathway)
GO:0036462 (TRAIL-activated apoptotic signaling pathway)
GO:0039650 (suppression by virus of host cysteine-type endopeptidase activity involved in apoptotic process)
GO:0042110 (T cell activation)
GO:0042113 (B cell activation)
GO:0042981 (regulation of apoptotic process)
GO:0043123 (positive regulation of I-kappaB kinase/NF-kappaB signaling)
GO:0043124 (negative regulation of I-kappaB kinase/NF-kappaB signaling)
GO:0045471 (response to ethanol)
GO:0045651 (positive regulation of macrophage differentiation)
GO:0045862 (positive regulation of proteolysis)
GO:0046677 (response to antibiotic)
GO:0051291 (protein heterooligomerization)
GO:0051603 (proteolysis involved in cellular protein catabolic process)
GO:0060715 (syncytiotrophoblast cell differentiation involved in labyrinthine layer development)
GO:0070423 (nucleotide-binding oligomerization domain containing signaling pathway)
GO:0071260 (cellular response to mechanical stimulus)
GO:0071407 (cellular response to organic cyclic compound)
GO:0071550 (death-inducing signaling complex assembly)
GO:0097190 (apoptotic signaling pathway)
GO:0097191 (extrinsic apoptotic signaling pathway)
GO:0097194 (execution phase of apoptosis)
GO:0097202 (activation of cysteine-type endopeptidase activity)
GO:0097296 (activation of cysteine-type endopeptidase activity involved in apoptotic signaling pathway)
GO:1900740 (positive regulation of protein insertion into mitochondrial membrane involved in apoptotic signaling pathway)
GO:1902041 (regulation of extrinsic apoptotic signaling pathway via death domain receptors)
GO:1902042 (negative regulation of extrinsic apoptotic signaling pathway via death domain receptors)
Wikipedia Caspase_8

Target Cross References - Protein

canSAR Q14790
CGD Caspase 8 defiency
Human Protein Atlas ENSG00000064012
IntAct Q14790
Guide to Pharmacology 1624
Open Targets ENSG00000064012
PharmGKB PA26092
Reactome R-HSA-111465 (Apoptotic cleavage of cellular proteins.)
R-HSA-140534 (Ligand-dependent caspase activation.)
R-HSA-168638 (NOD1/2 Signaling Pathway.)
R-HSA-2562578 (TRIF-mediated programmed cell death.)
R-HSA-264870 (Caspase-mediated cleavage of cytoskeletal proteins.)
R-HSA-3371378 (Regulation by c-FLIP.)
R-HSA-5213460 (RIPK1-mediated regulated necrosis.)
R-HSA-5218900 (CASP8 activity is inhibited.)
R-HSA-5357786 (TNFR1-induced proapoptotic signaling.)
R-HSA-5357905 (Regulation of TNFR1 signaling.)
R-HSA-5660668 (CLEC7A/inflammasome pathway.)
R-HSA-5675482 (Regulation of necroptotic cell death.)
R-HSA-69416 (Dimerization of procaspase-8.)
R-HSA-75108 (Activation, myristolyation of BID and translocation to mitochondria.)
R-HSA-75153 (Apoptotic execution phase.)
R-HSA-75157 (FasL/ CD95L signaling.)
R-HSA-75158 (TRAIL signaling.)
R-HSA-933543 (NF-kB activation through FADD/RIP-1 pathway mediated by caspase-8 and -10.)
UniProt O14676 Q14790 Q14791 Q14792 Q14793 Q14794 Q14795 Q14796 Q15780 Q15806 Q53TT5 Q8TDI1 Q8TDI2 Q8TDI3 Q8TDI4 Q8TDI5 Q96T22 Q9C0K4 Q9UQ81

Target Cross References - Domain

InterPro IPR001309 (Pept_C14_p20.)
IPR001875 (DED_dom.)
IPR002138 (Pept_C14_p10.)
IPR011029 (DEATH-like_dom.)
IPR015917 (Pept_C14A.)
IPR016129 (Caspase_his_AS.)
IPR029030 (Caspase-like_dom.)
IPR033139 (Caspase_cys_AS.)
Pfam PF01335 (DED)

Target Cross References - Structure

PDBe 1F9E 1I4E 1QDU 1QTN 2C2Z 2FUN 2Y1L 3H11 3KJN 3KJQ 4JJ7 4PRZ 4PS1 4ZBW 5JQE
CREDO 1F9E 1I4E 1QDU 1QTN 2C2Z 2FUN 2Y1L 3H11 3KJN 3KJQ 4JJ7 4PRZ 4PS1 4ZBW 5JQE
spacer
spacer