Compounds > MK-8353
Page last updated: 2024-11-13

MK-8353

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Description

MK-8353: ERK inhibitor used in oncology [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

MK-8353 : A member of the class of indazoles that is 1H-indazole substituted by a 6-(propan-2-yloxy)pyridin-3-yl group at position 3 and by a {[(3S)-3-(methylsulfanyl)-1-(2-{4-[4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl]-3,6-dihydropyridin-1(2H)-yl}-2-oxoethyl)pyrrolidin-3-yl]carbonyl}amino group at position 5. It is a potent and selective inhibitor of ERK1 and ERK2 in vitro (IC50 values of 23.0 nM and 8.8 nM, respectively). The drug is being developed by Merck Sharp & Dohme and is currently in clinical development for the treatment of advanced/metastatic solid tumors. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID58282870
CHEMBL ID4213970
CHEBI ID167664
SCHEMBL ID10236331

Synonyms (29)

Synonym
mk8353
mk-8353
(3s)-3-(methylsulfanyl)-1-(2-{4-[4-(1-methyl-1h-1,2,4-triazol-3-yl)phenyl]-3,6-dihydropyridin-1(2h)-yl}-2-oxoethyl)-n-{3-[6-(propan-2-yloxy)pyridin-3-yl]-1h-indazol-5-yl}pyrrolidine-3-carboxamide
CHEBI:167664
1184173-73-6
sch-900353
sch900353
mk 8353
S8701
SCHEMBL10236331
HY-111407
CS-0040548
(s)-n-(3-(6-isopropoxypyridin-3-yl)-1h-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1h-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2h)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide
ZB1630
(s)-n-(3-(6-isopropoxypyridin-3-yl)-1h-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1h-1,2,4-triazol-3-yl)phenyl)-5,6-dihydropyridin-1(2h)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide
BS-14448
(3s)-3-(methylsulfanyl)-1-(2-{4-[4-(1-methyl-1h-1,2,4-triazol-3-yl)phenyl]-3,6-dihydropyridin-1(2h)-yl}-2-oxoethyl)-n-(3-{6-[(propan-2-yl)oxy]pyridin-3-yl}-1h-indazol-5-yl)pyrrolidine-3-carboxamide
gtpl9974
(3s)-3-methylsulfanyl-1-[2-[4-[4-(1-methyl-1,2,4-triazol-3-yl)phenyl]-3,6-dihydro-2h-pyridin-1-yl]-2-oxoethyl]-n-[3-(6-propan-2-yloxypyridin-3-yl)-1h-indazol-5-yl]pyrrolidine-3-carboxamide
nsc-818002
nsc818002
D80532
mk-8353;sch900353
mk-8353 (sch900353)
AKOS037648529
EX-A3191
CHEMBL4213970 ,
bdbm50458803
AC-35897

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"We have developed an orally bioavailable ERK inhibitor, MK-8353; conducted preclinical studies to demonstrate activity, pharmacodynamic endpoints, dosing, and schedule; completed a study in healthy volunteers (P07652); and subsequently performed a phase I clinical trial in patients with advanced solid tumors (MK-8353-001)."( Development of MK-8353, an orally administered ERK1/2 inhibitor, in patients with advanced solid tumors.
Adjei, AA; Bishop, WR; Carr, D; Chun, P; Cooper, A; Dayananth, P; Deng, Y; Flaherty, KT; Fong, PC; Hwu, WJ; Kirschmeier, P; Long, BJ; Miselis, NR; Moreno, BH; Moschos, SJ; Ramanathan, RK; Ribas, A; Robert, L; Rubin, EH; Rubino, J; Rush, TS; Samatar, AA; Schiller, J; Shapira-Frommer, R; Shipps, GW; Sullivan, RJ; Tawbi, HA; Zhang, D, 2018)		1.08
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitorAn EC 2.7.11.* (protein-serine/threonine kinase) inhibitor that interferes with the action of mitogen-activated protein kinase (EC 2.7.11.24).
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
apoptosis inducerAny substance that induces the process of apoptosis (programmed cell death) in multi-celled organisms.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (10)

ClassDescription
indazoles
triazolesAn azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.
dihydropyridine
pyridinesAny organonitrogen heterocyclic compound based on a pyridine skeleton and its substituted derivatives.
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
secondary carboxamideA carboxamide resulting from the formal condensation of a carboxylic acid with a primary amine; formula RC(=O)NHR(1).
pyrrolidinecarboxamide
N-alkylpyrrolidine
methyl sulfideAny aliphatic sulfide in which at least one of the organyl groups attached to the sulfur is a methyl group.
tertiary carboxamideA carboxamide resulting from the formal condensation of a carboxylic acid with a secondary amine; formula RC(=O)NHR(1)R(2).
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (17)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)3.35000.00011.753610.0000AID1385278; AID1385279
Cytochrome P450 2C8Homo sapiens (human)IC50 (µMol)4.25000.00081.88487.9000AID1385298; AID1385299
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)5.00000.00002.800510.0000AID1385300; AID1385301
Mitogen-activated protein kinase 3 Homo sapiens (human)IC50 (µMol)0.02000.00253.09269.5820AID1385274
Mitogen-activated protein kinase 1Homo sapiens (human)IC50 (µMol)0.00700.00031.68789.2000AID1385275
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Caspase-1Homo sapiens (human)Activity0.18500.18500.18500.1850AID1385302
Caspase-14Homo sapiens (human)Activity0.18500.18500.18500.1850AID1385302
Caspase-3Homo sapiens (human)Activity0.18500.18500.18500.1850AID1385302
Caspase-2Homo sapiens (human)Activity0.18500.18500.18500.1850AID1385302
Caspase-4Homo sapiens (human)Activity0.18500.18500.18500.1850AID1385302
Caspase-5Homo sapiens (human)Activity0.18500.18500.18500.1850AID1385302
Caspase-7Homo sapiens (human)Activity0.18500.18500.18500.1850AID1385302
Caspase-9Homo sapiens (human)Activity0.18500.18500.18500.1850AID1385302
Caspase-6Homo sapiens (human)Activity0.18500.18500.18500.1850AID1385302
Caspase-8Homo sapiens (human)Activity0.18500.18500.18500.1850AID1385302
Inactive caspase-12Homo sapiens (human)Activity0.18500.18500.18500.1850AID1385302
Caspase-10Homo sapiens (human)Activity0.18500.18500.18500.1850AID1385302
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (228)

Processvia Protein(s)Taxonomy
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
lipid hydroxylationCytochrome P450 2C8Homo sapiens (human)
organic acid metabolic processCytochrome P450 2C8Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C8Homo sapiens (human)
steroid metabolic processCytochrome P450 2C8Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C8Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C8Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C8Homo sapiens (human)
retinol metabolic processCytochrome P450 2C8Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 2C8Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C8Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C8Homo sapiens (human)
oxidative demethylationCytochrome P450 2C8Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C8Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
positive regulation of macrophage chemotaxisMitogen-activated protein kinase 3 Homo sapiens (human)
positive regulation of macrophage proliferationMitogen-activated protein kinase 3 Homo sapiens (human)
MAPK cascadeMitogen-activated protein kinase 3 Homo sapiens (human)
DNA-templated transcriptionMitogen-activated protein kinase 3 Homo sapiens (human)
protein phosphorylationMitogen-activated protein kinase 3 Homo sapiens (human)
apoptotic processMitogen-activated protein kinase 3 Homo sapiens (human)
insulin receptor signaling pathwayMitogen-activated protein kinase 3 Homo sapiens (human)
Schwann cell developmentMitogen-activated protein kinase 3 Homo sapiens (human)
phosphorylationMitogen-activated protein kinase 3 Homo sapiens (human)
sensory perception of painMitogen-activated protein kinase 3 Homo sapiens (human)
regulation of ossificationMitogen-activated protein kinase 3 Homo sapiens (human)
BMP signaling pathwayMitogen-activated protein kinase 3 Homo sapiens (human)
regulation of cellular pHMitogen-activated protein kinase 3 Homo sapiens (human)
thyroid gland developmentMitogen-activated protein kinase 3 Homo sapiens (human)
positive regulation of cyclase activityMitogen-activated protein kinase 3 Homo sapiens (human)
lipopolysaccharide-mediated signaling pathwayMitogen-activated protein kinase 3 Homo sapiens (human)
positive regulation of telomere maintenance via telomeraseMitogen-activated protein kinase 3 Homo sapiens (human)
regulation of stress-activated MAPK cascadeMitogen-activated protein kinase 3 Homo sapiens (human)
cellular response to amino acid starvationMitogen-activated protein kinase 3 Homo sapiens (human)
cellular response to reactive oxygen speciesMitogen-activated protein kinase 3 Homo sapiens (human)
peptidyl-tyrosine autophosphorylationMitogen-activated protein kinase 3 Homo sapiens (human)
ERBB2-ERBB3 signaling pathwayMitogen-activated protein kinase 3 Homo sapiens (human)
outer ear morphogenesisMitogen-activated protein kinase 3 Homo sapiens (human)
myelinationMitogen-activated protein kinase 3 Homo sapiens (human)
signal transduction in response to DNA damageMitogen-activated protein kinase 3 Homo sapiens (human)
response to exogenous dsRNAMitogen-activated protein kinase 3 Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIMitogen-activated protein kinase 3 Homo sapiens (human)
insulin-like growth factor receptor signaling pathwayMitogen-activated protein kinase 3 Homo sapiens (human)
thymus developmentMitogen-activated protein kinase 3 Homo sapiens (human)
modulation of chemical synaptic transmissionMitogen-activated protein kinase 3 Homo sapiens (human)
cartilage developmentMitogen-activated protein kinase 3 Homo sapiens (human)
stress-activated MAPK cascadeMitogen-activated protein kinase 3 Homo sapiens (human)
regulation of cytoskeleton organizationMitogen-activated protein kinase 3 Homo sapiens (human)
positive regulation of telomerase activityMitogen-activated protein kinase 3 Homo sapiens (human)
Bergmann glial cell differentiationMitogen-activated protein kinase 3 Homo sapiens (human)
face developmentMitogen-activated protein kinase 3 Homo sapiens (human)
lung morphogenesisMitogen-activated protein kinase 3 Homo sapiens (human)
trachea formationMitogen-activated protein kinase 3 Homo sapiens (human)
cardiac neural crest cell development involved in heart developmentMitogen-activated protein kinase 3 Homo sapiens (human)
ERK1 and ERK2 cascadeMitogen-activated protein kinase 3 Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeMitogen-activated protein kinase 3 Homo sapiens (human)
interleukin-1-mediated signaling pathwayMitogen-activated protein kinase 3 Homo sapiens (human)
response to epidermal growth factorMitogen-activated protein kinase 3 Homo sapiens (human)
cellular response to mechanical stimulusMitogen-activated protein kinase 3 Homo sapiens (human)
cellular response to cadmium ionMitogen-activated protein kinase 3 Homo sapiens (human)
cellular response to tumor necrosis factorMitogen-activated protein kinase 3 Homo sapiens (human)
caveolin-mediated endocytosisMitogen-activated protein kinase 3 Homo sapiens (human)
regulation of Golgi inheritanceMitogen-activated protein kinase 3 Homo sapiens (human)
xenophagyMitogen-activated protein kinase 3 Homo sapiens (human)
negative regulation of TORC1 signalingMitogen-activated protein kinase 3 Homo sapiens (human)
positive regulation of telomere cappingMitogen-activated protein kinase 3 Homo sapiens (human)
positive regulation of xenophagyMitogen-activated protein kinase 3 Homo sapiens (human)
regulation of early endosome to late endosome transportMitogen-activated protein kinase 3 Homo sapiens (human)
intracellular signal transductionMitogen-activated protein kinase 3 Homo sapiens (human)
positive regulation of macrophage chemotaxisMitogen-activated protein kinase 1Homo sapiens (human)
positive regulation of macrophage proliferationMitogen-activated protein kinase 1Homo sapiens (human)
regulation of transcription by RNA polymerase IIMitogen-activated protein kinase 1Homo sapiens (human)
protein phosphorylationMitogen-activated protein kinase 1Homo sapiens (human)
apoptotic processMitogen-activated protein kinase 1Homo sapiens (human)
chemotaxisMitogen-activated protein kinase 1Homo sapiens (human)
DNA damage responseMitogen-activated protein kinase 1Homo sapiens (human)
signal transductionMitogen-activated protein kinase 1Homo sapiens (human)
chemical synaptic transmissionMitogen-activated protein kinase 1Homo sapiens (human)
learning or memoryMitogen-activated protein kinase 1Homo sapiens (human)
insulin receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
positive regulation of peptidyl-threonine phosphorylationMitogen-activated protein kinase 1Homo sapiens (human)
Schwann cell developmentMitogen-activated protein kinase 1Homo sapiens (human)
peptidyl-serine phosphorylationMitogen-activated protein kinase 1Homo sapiens (human)
peptidyl-threonine phosphorylationMitogen-activated protein kinase 1Homo sapiens (human)
cytosine metabolic processMitogen-activated protein kinase 1Homo sapiens (human)
regulation of ossificationMitogen-activated protein kinase 1Homo sapiens (human)
androgen receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
regulation of cellular pHMitogen-activated protein kinase 1Homo sapiens (human)
thyroid gland developmentMitogen-activated protein kinase 1Homo sapiens (human)
regulation of protein stabilityMitogen-activated protein kinase 1Homo sapiens (human)
lipopolysaccharide-mediated signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
positive regulation of telomere maintenance via telomeraseMitogen-activated protein kinase 1Homo sapiens (human)
regulation of stress-activated MAPK cascadeMitogen-activated protein kinase 1Homo sapiens (human)
mammary gland epithelial cell proliferationMitogen-activated protein kinase 1Homo sapiens (human)
cellular response to amino acid starvationMitogen-activated protein kinase 1Homo sapiens (human)
cellular response to reactive oxygen speciesMitogen-activated protein kinase 1Homo sapiens (human)
response to nicotineMitogen-activated protein kinase 1Homo sapiens (human)
ERBB signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
ERBB2-ERBB3 signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
outer ear morphogenesisMitogen-activated protein kinase 1Homo sapiens (human)
myelinationMitogen-activated protein kinase 1Homo sapiens (human)
response to exogenous dsRNAMitogen-activated protein kinase 1Homo sapiens (human)
steroid hormone mediated signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
negative regulation of cell differentiationMitogen-activated protein kinase 1Homo sapiens (human)
insulin-like growth factor receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
thymus developmentMitogen-activated protein kinase 1Homo sapiens (human)
progesterone receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
T cell receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
B cell receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
stress-activated MAPK cascadeMitogen-activated protein kinase 1Homo sapiens (human)
regulation of cytoskeleton organizationMitogen-activated protein kinase 1Homo sapiens (human)
positive regulation of telomerase activityMitogen-activated protein kinase 1Homo sapiens (human)
Bergmann glial cell differentiationMitogen-activated protein kinase 1Homo sapiens (human)
long-term synaptic potentiationMitogen-activated protein kinase 1Homo sapiens (human)
face developmentMitogen-activated protein kinase 1Homo sapiens (human)
lung morphogenesisMitogen-activated protein kinase 1Homo sapiens (human)
trachea formationMitogen-activated protein kinase 1Homo sapiens (human)
labyrinthine layer blood vessel developmentMitogen-activated protein kinase 1Homo sapiens (human)
cardiac neural crest cell development involved in heart developmentMitogen-activated protein kinase 1Homo sapiens (human)
ERK1 and ERK2 cascadeMitogen-activated protein kinase 1Homo sapiens (human)
response to epidermal growth factorMitogen-activated protein kinase 1Homo sapiens (human)
cellular response to cadmium ionMitogen-activated protein kinase 1Homo sapiens (human)
cellular response to tumor necrosis factorMitogen-activated protein kinase 1Homo sapiens (human)
caveolin-mediated endocytosisMitogen-activated protein kinase 1Homo sapiens (human)
regulation of Golgi inheritanceMitogen-activated protein kinase 1Homo sapiens (human)
positive regulation of telomere cappingMitogen-activated protein kinase 1Homo sapiens (human)
regulation of early endosome to late endosome transportMitogen-activated protein kinase 1Homo sapiens (human)
cell surface receptor signaling pathwayMitogen-activated protein kinase 1Homo sapiens (human)
intracellular signal transductionMitogen-activated protein kinase 1Homo sapiens (human)
cellular response to organic substanceCaspase-1Homo sapiens (human)
pattern recognition receptor signaling pathwayCaspase-1Homo sapiens (human)
proteolysisCaspase-1Homo sapiens (human)
apoptotic processCaspase-1Homo sapiens (human)
signal transductionCaspase-1Homo sapiens (human)
osmosensory signaling pathwayCaspase-1Homo sapiens (human)
protein autoprocessingCaspase-1Homo sapiens (human)
positive regulation of interleukin-1 beta productionCaspase-1Homo sapiens (human)
positive regulation of interleukin-18 productionCaspase-1Homo sapiens (human)
defense response to bacteriumCaspase-1Homo sapiens (human)
regulation of apoptotic processCaspase-1Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionCaspase-1Homo sapiens (human)
positive regulation of cysteine-type endopeptidase activity involved in apoptotic processCaspase-1Homo sapiens (human)
icosanoid biosynthetic processCaspase-1Homo sapiens (human)
regulation of inflammatory responseCaspase-1Homo sapiens (human)
positive regulation of inflammatory responseCaspase-1Homo sapiens (human)
protein maturationCaspase-1Homo sapiens (human)
defense response to virusCaspase-1Homo sapiens (human)
pyroptosisCaspase-1Homo sapiens (human)
cellular response to lipopolysaccharideCaspase-1Homo sapiens (human)
cellular response to mechanical stimulusCaspase-1Homo sapiens (human)
cellular response to type II interferonCaspase-1Homo sapiens (human)
cytokine precursor processingCaspase-1Homo sapiens (human)
signaling receptor ligand precursor processingCaspase-1Homo sapiens (human)
AIM2 inflammasome complex assemblyCaspase-1Homo sapiens (human)
positive regulation of tumor necrosis factor-mediated signaling pathwayCaspase-1Homo sapiens (human)
proteolysisCaspase-14Homo sapiens (human)
epidermis developmentCaspase-14Homo sapiens (human)
keratinizationCaspase-14Homo sapiens (human)
cornificationCaspase-14Homo sapiens (human)
positive regulation of neuron apoptotic processCaspase-14Homo sapiens (human)
neurotrophin TRK receptor signaling pathwayCaspase-3Homo sapiens (human)
luteolysisCaspase-3Homo sapiens (human)
response to hypoxiaCaspase-3Homo sapiens (human)
B cell homeostasisCaspase-3Homo sapiens (human)
negative regulation of cytokine productionCaspase-3Homo sapiens (human)
proteolysisCaspase-3Homo sapiens (human)
apoptotic processCaspase-3Homo sapiens (human)
DNA damage responseCaspase-3Homo sapiens (human)
axonal fasciculationCaspase-3Homo sapiens (human)
heart developmentCaspase-3Homo sapiens (human)
sensory perception of soundCaspase-3Homo sapiens (human)
learning or memoryCaspase-3Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to osmotic stressCaspase-3Homo sapiens (human)
response to xenobiotic stimulusCaspase-3Homo sapiens (human)
response to UVCaspase-3Homo sapiens (human)
response to woundingCaspase-3Homo sapiens (human)
response to glucoseCaspase-3Homo sapiens (human)
response to X-rayCaspase-3Homo sapiens (human)
regulation of macroautophagyCaspase-3Homo sapiens (human)
protein processingCaspase-3Homo sapiens (human)
hippocampus developmentCaspase-3Homo sapiens (human)
protein catabolic processCaspase-3Homo sapiens (human)
erythrocyte differentiationCaspase-3Homo sapiens (human)
platelet formationCaspase-3Homo sapiens (human)
negative regulation of B cell proliferationCaspase-3Homo sapiens (human)
regulation of protein stabilityCaspase-3Homo sapiens (human)
response to cobalt ionCaspase-3Homo sapiens (human)
response to estradiolCaspase-3Homo sapiens (human)
response to lipopolysaccharideCaspase-3Homo sapiens (human)
glial cell apoptotic processCaspase-3Homo sapiens (human)
response to tumor necrosis factorCaspase-3Homo sapiens (human)
response to nicotineCaspase-3Homo sapiens (human)
response to hydrogen peroxideCaspase-3Homo sapiens (human)
T cell homeostasisCaspase-3Homo sapiens (human)
response to amino acidCaspase-3Homo sapiens (human)
fibroblast apoptotic processCaspase-3Homo sapiens (human)
cell fate commitmentCaspase-3Homo sapiens (human)
negative regulation of cell cycleCaspase-3Homo sapiens (human)
negative regulation of activated T cell proliferationCaspase-3Homo sapiens (human)
striated muscle cell differentiationCaspase-3Homo sapiens (human)
response to glucocorticoidCaspase-3Homo sapiens (human)
neuron apoptotic processCaspase-3Homo sapiens (human)
protein maturationCaspase-3Homo sapiens (human)
anterior neural tube closureCaspase-3Homo sapiens (human)
pyroptosisCaspase-3Homo sapiens (human)
leukocyte apoptotic processCaspase-3Homo sapiens (human)
cellular response to staurosporineCaspase-3Homo sapiens (human)
apoptotic signaling pathwayCaspase-3Homo sapiens (human)
intrinsic apoptotic signaling pathwayCaspase-3Homo sapiens (human)
execution phase of apoptosisCaspase-3Homo sapiens (human)
positive regulation of pyroptosisCaspase-3Homo sapiens (human)
positive regulation of amyloid-beta formationCaspase-3Homo sapiens (human)
epithelial cell apoptotic processCaspase-3Homo sapiens (human)
keratinocyte differentiationCaspase-3Homo sapiens (human)
positive regulation of neuron apoptotic processCaspase-3Homo sapiens (human)
neuron differentiationCaspase-3Homo sapiens (human)
luteolysisCaspase-2Homo sapiens (human)
neural retina developmentCaspase-2Homo sapiens (human)
apoptotic processCaspase-2Homo sapiens (human)
DNA damage responseCaspase-2Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCaspase-2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageCaspase-2Homo sapiens (human)
protein processingCaspase-2Homo sapiens (human)
ectopic germ cell programmed cell deathCaspase-2Homo sapiens (human)
positive regulation of apoptotic processCaspase-2Homo sapiens (human)
negative regulation of apoptotic processCaspase-2Homo sapiens (human)
cellular response to mechanical stimulusCaspase-2Homo sapiens (human)
apoptotic signaling pathwayCaspase-2Homo sapiens (human)
execution phase of apoptosisCaspase-2Homo sapiens (human)
positive regulation of apoptotic signaling pathwayCaspase-2Homo sapiens (human)
extrinsic apoptotic signaling pathway in absence of ligandCaspase-2Homo sapiens (human)
positive regulation of neuron apoptotic processCaspase-2Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processCaspase-2Homo sapiens (human)
proteolysisCaspase-4Homo sapiens (human)
inflammatory responseCaspase-4Homo sapiens (human)
protein autoprocessingCaspase-4Homo sapiens (human)
defense response to bacteriumCaspase-4Homo sapiens (human)
innate immune responseCaspase-4Homo sapiens (human)
regulation of inflammatory responseCaspase-4Homo sapiens (human)
positive regulation of inflammatory responseCaspase-4Homo sapiens (human)
defense response to Gram-positive bacteriumCaspase-4Homo sapiens (human)
protein maturationCaspase-4Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCaspase-4Homo sapiens (human)
pyroptosisCaspase-4Homo sapiens (human)
intrinsic apoptotic signaling pathwayCaspase-4Homo sapiens (human)
non-canonical inflammasome complex assemblyCaspase-4Homo sapiens (human)
positive regulation of tumor necrosis factor-mediated signaling pathwayCaspase-4Homo sapiens (human)
cellular response to amyloid-betaCaspase-4Homo sapiens (human)
positive regulation of interleukin-18-mediated signaling pathwayCaspase-4Homo sapiens (human)
apoptotic processCaspase-4Homo sapiens (human)
positive regulation of neuron apoptotic processCaspase-4Homo sapiens (human)
proteolysisCaspase-5Homo sapiens (human)
substantia nigra developmentCaspase-5Homo sapiens (human)
protein maturationCaspase-5Homo sapiens (human)
cellular response to mechanical stimulusCaspase-5Homo sapiens (human)
positive regulation of neuron apoptotic processCaspase-5Homo sapiens (human)
apoptotic processCaspase-5Homo sapiens (human)
positive regulation of inflammatory responseCaspase-5Homo sapiens (human)
proteolysisCaspase-7Homo sapiens (human)
apoptotic processCaspase-7Homo sapiens (human)
heart developmentCaspase-7Homo sapiens (human)
response to UVCaspase-7Homo sapiens (human)
protein processingCaspase-7Homo sapiens (human)
protein catabolic processCaspase-7Homo sapiens (human)
defense response to bacteriumCaspase-7Homo sapiens (human)
fibroblast apoptotic processCaspase-7Homo sapiens (human)
striated muscle cell differentiationCaspase-7Homo sapiens (human)
neuron apoptotic processCaspase-7Homo sapiens (human)
protein maturationCaspase-7Homo sapiens (human)
lymphocyte apoptotic processCaspase-7Homo sapiens (human)
cellular response to lipopolysaccharideCaspase-7Homo sapiens (human)
cellular response to staurosporineCaspase-7Homo sapiens (human)
execution phase of apoptosisCaspase-7Homo sapiens (human)
positive regulation of plasma membrane repairCaspase-7Homo sapiens (human)
positive regulation of neuron apoptotic processCaspase-7Homo sapiens (human)
response to hypoxiaCaspase-9Homo sapiens (human)
kidney developmentCaspase-9Homo sapiens (human)
response to ischemiaCaspase-9Homo sapiens (human)
apoptotic processCaspase-9Homo sapiens (human)
DNA damage responseCaspase-9Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageCaspase-9Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic process by cytochrome cCaspase-9Homo sapiens (human)
protein processingCaspase-9Homo sapiens (human)
platelet formationCaspase-9Homo sapiens (human)
response to cobalt ionCaspase-9Homo sapiens (human)
response to estradiolCaspase-9Homo sapiens (human)
response to lipopolysaccharideCaspase-9Homo sapiens (human)
glial cell apoptotic processCaspase-9Homo sapiens (human)
cellular response to UVCaspase-9Homo sapiens (human)
signal transduction in response to DNA damageCaspase-9Homo sapiens (human)
positive regulation of apoptotic processCaspase-9Homo sapiens (human)
fibroblast apoptotic processCaspase-9Homo sapiens (human)
neuron apoptotic processCaspase-9Homo sapiens (human)
protein maturationCaspase-9Homo sapiens (human)
cellular response to dexamethasone stimulusCaspase-9Homo sapiens (human)
leukocyte apoptotic processCaspase-9Homo sapiens (human)
intrinsic apoptotic signaling pathwayCaspase-9Homo sapiens (human)
epithelial cell apoptotic processCaspase-9Homo sapiens (human)
positive regulation of neuron apoptotic processCaspase-9Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processCaspase-9Homo sapiens (human)
activation of innate immune responseCaspase-6Homo sapiens (human)
proteolysisCaspase-6Homo sapiens (human)
apoptotic processCaspase-6Homo sapiens (human)
protein autoprocessingCaspase-6Homo sapiens (human)
epithelial cell differentiationCaspase-6Homo sapiens (human)
positive regulation of apoptotic processCaspase-6Homo sapiens (human)
regulation of programmed cell deathCaspase-6Homo sapiens (human)
positive regulation of necroptotic processCaspase-6Homo sapiens (human)
pyroptosisCaspase-6Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCaspase-6Homo sapiens (human)
cellular response to staurosporineCaspase-6Homo sapiens (human)
execution phase of apoptosisCaspase-6Homo sapiens (human)
hepatocyte apoptotic processCaspase-6Homo sapiens (human)
positive regulation of neuron apoptotic processCaspase-6Homo sapiens (human)
angiogenesisCaspase-8Homo sapiens (human)
regulation of cytokine productionCaspase-8Homo sapiens (human)
proteolysisCaspase-8Homo sapiens (human)
apoptotic processCaspase-8Homo sapiens (human)
heart developmentCaspase-8Homo sapiens (human)
regulation of tumor necrosis factor-mediated signaling pathwayCaspase-8Homo sapiens (human)
natural killer cell activationCaspase-8Homo sapiens (human)
macrophage differentiationCaspase-8Homo sapiens (human)
positive regulation of cell migrationCaspase-8Homo sapiens (human)
response to cobalt ionCaspase-8Homo sapiens (human)
response to estradiolCaspase-8Homo sapiens (human)
response to lipopolysaccharideCaspase-8Homo sapiens (human)
positive regulation of interleukin-1 beta productionCaspase-8Homo sapiens (human)
response to tumor necrosis factorCaspase-8Homo sapiens (human)
TRAIL-activated apoptotic signaling pathwayCaspase-8Homo sapiens (human)
T cell activationCaspase-8Homo sapiens (human)
B cell activationCaspase-8Homo sapiens (human)
positive regulation of apoptotic processCaspase-8Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionCaspase-8Homo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionCaspase-8Homo sapiens (human)
regulation of innate immune responseCaspase-8Homo sapiens (human)
response to ethanolCaspase-8Homo sapiens (human)
positive regulation of macrophage differentiationCaspase-8Homo sapiens (human)
positive regulation of proteolysisCaspase-8Homo sapiens (human)
proteolysis involved in protein catabolic processCaspase-8Homo sapiens (human)
protein maturationCaspase-8Homo sapiens (human)
negative regulation of necroptotic processCaspase-8Homo sapiens (human)
syncytiotrophoblast cell differentiation involved in labyrinthine layer developmentCaspase-8Homo sapiens (human)
pyroptosisCaspase-8Homo sapiens (human)
cellular response to mechanical stimulusCaspase-8Homo sapiens (human)
cellular response to organic cyclic compoundCaspase-8Homo sapiens (human)
apoptotic signaling pathwayCaspase-8Homo sapiens (human)
extrinsic apoptotic signaling pathwayCaspase-8Homo sapiens (human)
execution phase of apoptosisCaspase-8Homo sapiens (human)
activation of cysteine-type endopeptidase activityCaspase-8Homo sapiens (human)
self proteolysisCaspase-8Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processCaspase-8Homo sapiens (human)
extrinsic apoptotic signaling pathway via death domain receptorsCaspase-8Homo sapiens (human)
positive regulation of neuron apoptotic processCaspase-8Homo sapiens (human)
proteolysisInactive caspase-12Homo sapiens (human)
apoptotic processInactive caspase-12Homo sapiens (human)
positive regulation of neuron apoptotic processInactive caspase-12Homo sapiens (human)
positive regulation of inflammatory responseInactive caspase-12Homo sapiens (human)
proteolysisCaspase-10Homo sapiens (human)
apoptotic processCaspase-10Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionCaspase-10Homo sapiens (human)
protein maturationCaspase-10Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processCaspase-10Homo sapiens (human)
macrophage differentiationCaspase-10Homo sapiens (human)
extrinsic apoptotic signaling pathway via death domain receptorsCaspase-10Homo sapiens (human)
positive regulation of neuron apoptotic processCaspase-10Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (69)

Processvia Protein(s)Taxonomy
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2C8Homo sapiens (human)
iron ion bindingCytochrome P450 2C8Homo sapiens (human)
protein bindingCytochrome P450 2C8Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C8Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 2C8Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C8Homo sapiens (human)
aromatase activityCytochrome P450 2C8Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 2C8Homo sapiens (human)
heme bindingCytochrome P450 2C8Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C8Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
phosphotyrosine residue bindingMitogen-activated protein kinase 3 Homo sapiens (human)
protein serine/threonine kinase activityMitogen-activated protein kinase 3 Homo sapiens (human)
MAP kinase activityMitogen-activated protein kinase 3 Homo sapiens (human)
protein bindingMitogen-activated protein kinase 3 Homo sapiens (human)
ATP bindingMitogen-activated protein kinase 3 Homo sapiens (human)
phosphatase bindingMitogen-activated protein kinase 3 Homo sapiens (human)
identical protein bindingMitogen-activated protein kinase 3 Homo sapiens (human)
protein serine kinase activityMitogen-activated protein kinase 3 Homo sapiens (human)
DNA-binding transcription factor bindingMitogen-activated protein kinase 3 Homo sapiens (human)
phosphotyrosine residue bindingMitogen-activated protein kinase 1Homo sapiens (human)
DNA bindingMitogen-activated protein kinase 1Homo sapiens (human)
protein serine/threonine kinase activityMitogen-activated protein kinase 1Homo sapiens (human)
MAP kinase activityMitogen-activated protein kinase 1Homo sapiens (human)
protein bindingMitogen-activated protein kinase 1Homo sapiens (human)
ATP bindingMitogen-activated protein kinase 1Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityMitogen-activated protein kinase 1Homo sapiens (human)
phosphatase bindingMitogen-activated protein kinase 1Homo sapiens (human)
identical protein bindingMitogen-activated protein kinase 1Homo sapiens (human)
protein serine kinase activityMitogen-activated protein kinase 1Homo sapiens (human)
endopeptidase activityCaspase-1Homo sapiens (human)
cysteine-type endopeptidase activityCaspase-1Homo sapiens (human)
protein bindingCaspase-1Homo sapiens (human)
cysteine-type endopeptidase activator activity involved in apoptotic processCaspase-1Homo sapiens (human)
kinase bindingCaspase-1Homo sapiens (human)
cytokine bindingCaspase-1Homo sapiens (human)
identical protein bindingCaspase-1Homo sapiens (human)
CARD domain bindingCaspase-1Homo sapiens (human)
caspase bindingCaspase-1Homo sapiens (human)
cysteine-type endopeptidase activityCaspase-14Homo sapiens (human)
protein bindingCaspase-14Homo sapiens (human)
protease bindingCaspase-3Homo sapiens (human)
aspartic-type endopeptidase activityCaspase-3Homo sapiens (human)
cysteine-type endopeptidase activityCaspase-3Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase inhibitor activityCaspase-3Homo sapiens (human)
death receptor bindingCaspase-3Homo sapiens (human)
protein bindingCaspase-3Homo sapiens (human)
peptidase activityCaspase-3Homo sapiens (human)
phospholipase A2 activator activityCaspase-3Homo sapiens (human)
protein-containing complex bindingCaspase-3Homo sapiens (human)
cysteine-type endopeptidase activity involved in apoptotic processCaspase-3Homo sapiens (human)
cysteine-type endopeptidase activity involved in apoptotic signaling pathwayCaspase-3Homo sapiens (human)
cysteine-type endopeptidase activity involved in execution phase of apoptosisCaspase-3Homo sapiens (human)
enzyme activator activityCaspase-3Homo sapiens (human)
cysteine-type endopeptidase activityCaspase-2Homo sapiens (human)
protein bindingCaspase-2Homo sapiens (human)
enzyme bindingCaspase-2Homo sapiens (human)
protein domain specific bindingCaspase-2Homo sapiens (human)
identical protein bindingCaspase-2Homo sapiens (human)
cysteine-type endopeptidase activity involved in execution phase of apoptosisCaspase-2Homo sapiens (human)
cysteine-type endopeptidase activity involved in apoptotic signaling pathwayCaspase-2Homo sapiens (human)
lipopolysaccharide bindingCaspase-4Homo sapiens (human)
cysteine-type endopeptidase activityCaspase-4Homo sapiens (human)
protein bindingCaspase-4Homo sapiens (human)
lipid bindingCaspase-4Homo sapiens (human)
CARD domain bindingCaspase-4Homo sapiens (human)
cysteine-type endopeptidase activity involved in apoptotic processCaspase-4Homo sapiens (human)
cysteine-type endopeptidase activityCaspase-5Homo sapiens (human)
protein bindingCaspase-5Homo sapiens (human)
cysteine-type peptidase activityCaspase-5Homo sapiens (human)
cysteine-type endopeptidase activity involved in apoptotic processCaspase-5Homo sapiens (human)
RNA bindingCaspase-7Homo sapiens (human)
aspartic-type endopeptidase activityCaspase-7Homo sapiens (human)
cysteine-type endopeptidase activityCaspase-7Homo sapiens (human)
protein bindingCaspase-7Homo sapiens (human)
peptidase activityCaspase-7Homo sapiens (human)
cysteine-type peptidase activityCaspase-7Homo sapiens (human)
cysteine-type endopeptidase activity involved in apoptotic processCaspase-7Homo sapiens (human)
cysteine-type endopeptidase activity involved in execution phase of apoptosisCaspase-7Homo sapiens (human)
cysteine-type endopeptidase activityCaspase-9Homo sapiens (human)
protein bindingCaspase-9Homo sapiens (human)
enzyme activator activityCaspase-9Homo sapiens (human)
peptidase activityCaspase-9Homo sapiens (human)
SH3 domain bindingCaspase-9Homo sapiens (human)
protein kinase bindingCaspase-9Homo sapiens (human)
cysteine-type endopeptidase activity involved in apoptotic processCaspase-9Homo sapiens (human)
cysteine-type endopeptidase activity involved in apoptotic signaling pathwayCaspase-9Homo sapiens (human)
cysteine-type endopeptidase activityCaspase-6Homo sapiens (human)
protein bindingCaspase-6Homo sapiens (human)
cysteine-type peptidase activityCaspase-6Homo sapiens (human)
identical protein bindingCaspase-6Homo sapiens (human)
cysteine-type endopeptidase activity involved in apoptotic processCaspase-6Homo sapiens (human)
cysteine-type endopeptidase activity involved in execution phase of apoptosisCaspase-6Homo sapiens (human)
cysteine-type endopeptidase activityCaspase-8Homo sapiens (human)
death receptor bindingCaspase-8Homo sapiens (human)
tumor necrosis factor receptor bindingCaspase-8Homo sapiens (human)
protein bindingCaspase-8Homo sapiens (human)
peptidase activityCaspase-8Homo sapiens (human)
cysteine-type peptidase activityCaspase-8Homo sapiens (human)
ubiquitin protein ligase bindingCaspase-8Homo sapiens (human)
death effector domain bindingCaspase-8Homo sapiens (human)
identical protein bindingCaspase-8Homo sapiens (human)
protein-containing complex bindingCaspase-8Homo sapiens (human)
scaffold protein bindingCaspase-8Homo sapiens (human)
cysteine-type endopeptidase activity involved in apoptotic processCaspase-8Homo sapiens (human)
cysteine-type endopeptidase activity involved in apoptotic signaling pathwayCaspase-8Homo sapiens (human)
cysteine-type endopeptidase activity involved in apoptotic processInactive caspase-12Homo sapiens (human)
cysteine-type endopeptidase activityInactive caspase-12Homo sapiens (human)
cysteine-type endopeptidase activityCaspase-10Homo sapiens (human)
protein bindingCaspase-10Homo sapiens (human)
ubiquitin protein ligase bindingCaspase-10Homo sapiens (human)
death effector domain bindingCaspase-10Homo sapiens (human)
cysteine-type endopeptidase activity involved in apoptotic processCaspase-10Homo sapiens (human)
cysteine-type endopeptidase activity involved in apoptotic signaling pathwayCaspase-10Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (48)

Processvia Protein(s)Taxonomy
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C8Homo sapiens (human)
plasma membraneCytochrome P450 2C8Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C8Homo sapiens (human)
cytoplasmCytochrome P450 2C8Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C8Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
nucleusMitogen-activated protein kinase 3 Homo sapiens (human)
nuclear envelopeMitogen-activated protein kinase 3 Homo sapiens (human)
nucleoplasmMitogen-activated protein kinase 3 Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 3 Homo sapiens (human)
mitochondrionMitogen-activated protein kinase 3 Homo sapiens (human)
early endosomeMitogen-activated protein kinase 3 Homo sapiens (human)
late endosomeMitogen-activated protein kinase 3 Homo sapiens (human)
endoplasmic reticulum lumenMitogen-activated protein kinase 3 Homo sapiens (human)
Golgi apparatusMitogen-activated protein kinase 3 Homo sapiens (human)
cytosolMitogen-activated protein kinase 3 Homo sapiens (human)
cytoskeletonMitogen-activated protein kinase 3 Homo sapiens (human)
plasma membraneMitogen-activated protein kinase 3 Homo sapiens (human)
caveolaMitogen-activated protein kinase 3 Homo sapiens (human)
focal adhesionMitogen-activated protein kinase 3 Homo sapiens (human)
pseudopodiumMitogen-activated protein kinase 3 Homo sapiens (human)
glutamatergic synapseMitogen-activated protein kinase 3 Homo sapiens (human)
nucleusMitogen-activated protein kinase 3 Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 3 Homo sapiens (human)
extracellular regionMitogen-activated protein kinase 1Homo sapiens (human)
nucleusMitogen-activated protein kinase 1Homo sapiens (human)
nucleoplasmMitogen-activated protein kinase 1Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 1Homo sapiens (human)
mitochondrionMitogen-activated protein kinase 1Homo sapiens (human)
early endosomeMitogen-activated protein kinase 1Homo sapiens (human)
late endosomeMitogen-activated protein kinase 1Homo sapiens (human)
endoplasmic reticulum lumenMitogen-activated protein kinase 1Homo sapiens (human)
Golgi apparatusMitogen-activated protein kinase 1Homo sapiens (human)
centrosomeMitogen-activated protein kinase 1Homo sapiens (human)
cytosolMitogen-activated protein kinase 1Homo sapiens (human)
cytoskeletonMitogen-activated protein kinase 1Homo sapiens (human)
plasma membraneMitogen-activated protein kinase 1Homo sapiens (human)
caveolaMitogen-activated protein kinase 1Homo sapiens (human)
focal adhesionMitogen-activated protein kinase 1Homo sapiens (human)
pseudopodiumMitogen-activated protein kinase 1Homo sapiens (human)
azurophil granule lumenMitogen-activated protein kinase 1Homo sapiens (human)
synapseMitogen-activated protein kinase 1Homo sapiens (human)
mitotic spindleMitogen-activated protein kinase 1Homo sapiens (human)
ficolin-1-rich granule lumenMitogen-activated protein kinase 1Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 1Homo sapiens (human)
nucleusMitogen-activated protein kinase 1Homo sapiens (human)
cytoplasmCaspase-1Homo sapiens (human)
cytosolCaspase-1Homo sapiens (human)
nucleolusCaspase-1Homo sapiens (human)
cytoplasmCaspase-1Homo sapiens (human)
cytosolCaspase-1Homo sapiens (human)
microtubuleCaspase-1Homo sapiens (human)
plasma membraneCaspase-1Homo sapiens (human)
canonical inflammasome complexCaspase-1Homo sapiens (human)
NLRP1 inflammasome complexCaspase-1Homo sapiens (human)
NLRP3 inflammasome complexCaspase-1Homo sapiens (human)
AIM2 inflammasome complexCaspase-1Homo sapiens (human)
protein-containing complexCaspase-1Homo sapiens (human)
IPAF inflammasome complexCaspase-1Homo sapiens (human)
protease inhibitor complexCaspase-1Homo sapiens (human)
cornified envelopeCaspase-14Homo sapiens (human)
nucleoplasmCaspase-14Homo sapiens (human)
mitochondrionCaspase-14Homo sapiens (human)
cytosolCaspase-14Homo sapiens (human)
keratin filamentCaspase-14Homo sapiens (human)
nucleusCaspase-14Homo sapiens (human)
cytoplasmCaspase-14Homo sapiens (human)
cytoplasmCaspase-14Homo sapiens (human)
cytosolCaspase-14Homo sapiens (human)
nucleusCaspase-3Homo sapiens (human)
cytoplasmCaspase-3Homo sapiens (human)
nucleusCaspase-3Homo sapiens (human)
nucleoplasmCaspase-3Homo sapiens (human)
cytosolCaspase-3Homo sapiens (human)
neuronal cell bodyCaspase-3Homo sapiens (human)
death-inducing signaling complexCaspase-3Homo sapiens (human)
nucleusCaspase-2Homo sapiens (human)
nucleolusCaspase-2Homo sapiens (human)
cytosolCaspase-2Homo sapiens (human)
endopeptidase complexCaspase-2Homo sapiens (human)
cytoplasmCaspase-2Homo sapiens (human)
cytosolCaspase-4Homo sapiens (human)
extracellular regionCaspase-4Homo sapiens (human)
mitochondrionCaspase-4Homo sapiens (human)
endoplasmic reticulumCaspase-4Homo sapiens (human)
endoplasmic reticulum membraneCaspase-4Homo sapiens (human)
cytosolCaspase-4Homo sapiens (human)
plasma membraneCaspase-4Homo sapiens (human)
protein-containing complexCaspase-4Homo sapiens (human)
non-canonical inflammasome complexCaspase-4Homo sapiens (human)
cytoplasmCaspase-4Homo sapiens (human)
NLRP1 inflammasome complexCaspase-4Homo sapiens (human)
cytosolCaspase-5Homo sapiens (human)
NLRP1 inflammasome complexCaspase-5Homo sapiens (human)
cytoplasmCaspase-5Homo sapiens (human)
extracellular spaceCaspase-7Homo sapiens (human)
nucleusCaspase-7Homo sapiens (human)
cytoplasmCaspase-7Homo sapiens (human)
cytosolCaspase-7Homo sapiens (human)
nucleusCaspase-7Homo sapiens (human)
nucleoplasmCaspase-7Homo sapiens (human)
cytosolCaspase-7Homo sapiens (human)
mitochondrionCaspase-9Homo sapiens (human)
nucleusCaspase-9Homo sapiens (human)
cytosolCaspase-9Homo sapiens (human)
caspase complexCaspase-9Homo sapiens (human)
apoptosomeCaspase-9Homo sapiens (human)
protein-containing complexCaspase-9Homo sapiens (human)
cytosolCaspase-9Homo sapiens (human)
cytoplasmCaspase-9Homo sapiens (human)
nucleusCaspase-6Homo sapiens (human)
nucleoplasmCaspase-6Homo sapiens (human)
cytoplasmCaspase-6Homo sapiens (human)
cytosolCaspase-6Homo sapiens (human)
cytoplasmCaspase-6Homo sapiens (human)
cytoplasmCaspase-8Homo sapiens (human)
nucleoplasmCaspase-8Homo sapiens (human)
mitochondrionCaspase-8Homo sapiens (human)
mitochondrial outer membraneCaspase-8Homo sapiens (human)
cytosolCaspase-8Homo sapiens (human)
cytoskeletonCaspase-8Homo sapiens (human)
lamellipodiumCaspase-8Homo sapiens (human)
cell bodyCaspase-8Homo sapiens (human)
death-inducing signaling complexCaspase-8Homo sapiens (human)
CD95 death-inducing signaling complexCaspase-8Homo sapiens (human)
protein-containing complexCaspase-8Homo sapiens (human)
ripoptosomeCaspase-8Homo sapiens (human)
endoplasmic reticulumInactive caspase-12Homo sapiens (human)
NLRP1 inflammasome complexInactive caspase-12Homo sapiens (human)
cytoplasmInactive caspase-12Homo sapiens (human)
cytosolCaspase-10Homo sapiens (human)
CD95 death-inducing signaling complexCaspase-10Homo sapiens (human)
ripoptosomeCaspase-10Homo sapiens (human)
cytoplasmCaspase-10Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (73)

Assay IDTitleYearJournalArticle
AID1385297Antiproliferative activity against human A2058 cells harboring BRAF V600E/D mutant measured after 4 days
AID1385309Protein binding in mouse plasma at 10 uM
AID1385337Mean residence time in CD1 mouse at 10 mg/kg, iv
AID1385307Protein binding in dog plasma at 10 uM
AID1385316Inhibition of CYP2D6 (unknown origin) preincubated followed by substrate addition
AID1385355Cmax in CD1 mouse at 30 mg/kg, po
AID1385274Inhibition of ERK1 (unknown origin) using peptide substrate measured after 45 mins by IMAP assay
AID1385360Tmax in Sprague-Dawley rat at 10 mg/kg, po
AID1385346Half life in Beagle dog at 3 mg/kg, iv
AID1385285AUC in rat at 10 mg/kg
AID1385368Tmax in monkey at 10 mg/kg, po
AID1385276Antiproliferative activity against human HT-29 cells harboring BRAF V600E/D mutant measured after 4 days
AID1385299Inhibition of CYP2C8 (unknown origin) co-incubated with substrate
AID1385357AUC (0 to infinity) in CD1 mouse at 30 mg/kg, po
AID1385338Clearance in CD1 mouse at 10 mg/kg, iv
AID1385364Tmax in Beagle dog at 30 mg/kg, po
AID1385311Inhibition of ERK1/2 phosphorylation in human A2058 cells after 24 hrs by Western blot analysis
AID1385298Inhibition of CYP2C8 (unknown origin) preincubated followed by substrate addition
AID1385361AUC (0 to infinity) in Sprague-Dawley rat at 10 mg/kg, po
AID1385335AUC (0 to infinity) in CD1 mouse at 10 mg/kg, iv
AID1385354Volume of distribution at steady state in monkey at 1 mg/kg, iv
AID1385365AUC (0 to infinity) in Beagle dog at 30 mg/kg, po
AID1385363Cmax in Beagle dog at 30 mg/kg, po
AID1385351Half life in monkey at 1 mg/kg, iv
AID1385342Mean residence time in Sprague-Dawley rat at 3 mg/kg, iv
AID1385367Cmax in monkey at 10 mg/kg, po
AID1385312Inhibition of ERK1/2 in human A2058 cells assessed as reduction in RSK phosphorylation after 24 hrs by Western blot analysis
AID1385295Inhibition of human ERG at 1 uM by IonWork assay relative to control
AID1385306Protein binding in Sprague-Dawley rat plasma at 10 uM
AID1385314Inhibition of CYP1A2 (unknown origin) preincubated followed by substrate addition
AID1385369AUC (0 to infinity) in monkey at 10 mg/kg, po
AID1385304Apparent permeability across apical to basolateral side in human Caco2 cells
AID1385339Volume of distribution at steady state in CD1 mouse at 10 mg/kg, iv
AID1385305Apparent permeability across basolateral to apical side in human Caco2 cells
AID1385359Cmax in Sprague-Dawley rat at 10 mg/kg, po
AID1385347Mean residence time in Beagle dog at 3 mg/kg, iv
AID1385353Clearance in monkey at 1 mg/kg, iv
AID1385348Clearance in Beagle dog at 3 mg/kg, iv
AID1385280Inhibition of human ERG at 1.5 mg/ml by binding assay relative to control
AID1385358Oral bioavailability in CD1 mouse at 30 mg/kg
AID1385344Volume of distribution at steady state in Sprague-Dawley rat at 3 mg/kg, iv
AID1385310Protein binding in human plasma at 10 uM
AID1385373Antitumor activity against human COLO205 cells xenografted in nude mouse assessed as tumor regression at 60 mg/kg, po bid measured after 28 days relative to control
AID1385318Cardiotoxicity in telemetered guinea pig assessed as changes in QRS interval at 30 to 100 mg/kg
AID1385278Inhibition of CYP3A4 (unknown origin) co-incubated with substrate
AID1385302Activation of caspase (unknown origin)
AID1385340AUC (0 to infinity) in Sprague-Dawley rat at 3 mg/kg, iv
AID1385336Half life in CD1 mouse at 10 mg/kg, iv
AID1385313Inhibition of ERK1/2 phosphorylation in human A2058 cells at 30 nM after 24 hrs by Western blot analysis relative to control
AID1385371Antitumor activity against human COLO205 cells xenografted in nude mouse assessed as tumor growth inhibition at 20 mg/kg, po bid measured after 28 days relative to control
AID1385350AUC (0 to infinity) in monkey at 1 mg/kg, iv
AID1385366Oral bioavailability in Beagle dog at 30 mg/kg
AID1385352Mean residence time in monkey at 1 mg/kg, iv
AID1385277Antiproliferative activity against human COLO205 cells harboring BRAF V600E/D mutant measured after 4 days
AID1385317Cardiotoxicity in telemetered guinea pig assessed as changes in PR interval at 30 to 100 mg/kg
AID1385308Protein binding in monkey plasma at 10 uM
AID1385296Inhibition of human ERG at 10 uM by IonWork assay relative to control
AID1385356Tmax in CD1 mouse at 30 mg/kg, po
AID1385343Clearance in Sprague-Dawley rat at 3 mg/kg, iv
AID1385300Inhibition of CYP2C9 (unknown origin) co-incubated with substrate
AID1385370Oral bioavailability in monkey at 10 mg/kg
AID1385349Volume of distribution at steady state in Beagle dog at 3 mg/kg, iv
AID1385345AUC (0 to infinity) in Beagle dog at 3 mg/kg, iv
AID1385362Oral bioavailability in Sprague-Dawley rat at 10 mg/kg
AID1385303Inhibition of human ERG at 600 nM by voltage clamp method relative to control
AID1385372Antitumor activity against human COLO205 cells xenografted in nude mouse assessed as tumor growth inhibition at 40 mg/kg, po bid measured after 28 days relative to control
AID1385281Inhibition of human ERG at 5 mg/ml by binding assay relative to control
AID1385315Inhibition of CYP2C19 (unknown origin) preincubated followed by substrate addition
AID1385275Inhibition of ERK2 (unknown origin) using peptide substrate measured after 45 mins by IMAP assay
AID1385301Inhibition of CYP2C9 (unknown origin) preincubated followed by substrate addition
AID1385319Cardiotoxicity in telemetered guinea pig assessed as changes in QTc interval at 30 to 100 mg/kg
AID1385341Half life in Sprague-Dawley rat at 3 mg/kg, iv
AID1385279Inhibition of CYP3A4 (unknown origin) preincubated followed by substrate addition
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's3 (60.00)24.3611
2020's2 (40.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.52

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index28.52 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.80 (4.65)
Search Engine Demand Index25.99 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (28.52)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (40.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other3 (60.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
indazoles
Indazoles: A group of heterocyclic aromatic organic compounds consisting of the fusion of BENZENE and PYRAZOLES.		5.2231indazole
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		5.22311,2,3-triazole
azd 6244
AZD 6244: a MEK inhibitor		4.9111benzimidazoles;
bromobenzenes;
hydroxamic acid ester;
monochlorobenzenes;
organofluorine compound;
secondary amino compound		anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
sch772984
[no description available]		2.3110biaryl;
indazoles;
N-acylpiperazine;
N-alkylpyrrolidine;
N-arylpiperazine;
pyridines;
pyrimidines;
pyrrolidinecarboxamide;
secondary carboxamide;
tertiary amino compound;
tertiary carboxamide		analgesic;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
ConditionIndicatedRelationship StrengthStudiesTrials
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.3110
Endotoxemia
A condition characterized by the presence of ENDOTOXINS in the blood. On lysis, the outer cell wall of gram-negative bacteria enters the systemic circulation and initiates a pathophysiologic cascade of pro-inflammatory mediators.		02.3110
Benign Neoplasms
[description not available]		06.0222
Diarrhea
An increased liquidity or decreased consistency of FECES, such as running stool. Fecal consistency is related to the ratio of water-holding capacity of insoluble solids to total water, rather than the amount of water present. Diarrhea is not hyperdefecation or increased fecal weight.		06.0222
Nausea
An unpleasant sensation in the stomach usually accompanied by the urge to vomit. Common causes are early pregnancy, sea and motion sickness, emotional stress, intense pain, food poisoning, and various enteroviruses.		06.0222
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		18.0222
Dermatitis Medicamentosa
[description not available]		04.4811
Lassitude
[description not available]		04.4811
Fatigue
The state of weariness following a period of exertion, mental or physical, characterized by a decreased capacity for work and reduced efficiency to respond to stimuli.		04.4811