Compounds > delgocitinib
Page last updated: 2024-11-13

delgocitinib

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Description

delgocitinib: a Janus kinase inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

delgocitinib : A pyrrolopyrimidine that is 7H-pyrrolo[2,3-d]pyrimidine substituted by a (3S,4R)-1-(cyanoacetyl)-3-methyl-1,6-diazaspiro[3.4]octan-6-yl group at position 4. It is a pan-Janus kinase (JAK) inhibitor and is approved for treatment of atopic dermatitis (AD) in Japan. [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 CID50914062
CHEMBL ID4297507
CHEBI ID167600
SCHEMBL ID12547007

Synonyms (45)

Synonym
1263774-59-9
delgocitinibum
3-[(3s,4r)-3-methyl-6-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile
corectim
leo 124249
CHEBI:167600
leo-124249a
leo 124249a
jte-052
jte-052a
leo-124249
delgocitinib
FHX ,
SCHEMBL12547007
gtpl9619
jte052
ent-60
corectim (tn)
CS-0031558
D11046
HY-109053
delgocitinib (jan/usan)
delgocitinib [inn]
1,6-diazaspiro(3.4)octane-1-propanenitrile, 3-methyl-.beta.-oxo-6-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-, (3s,4r)-
delgocitinib [who-dd]
delgocitinib [jan]
3-[(3s,4r)-3-methyl-7-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1,7-diazaspiro[3.4]octan-1-yl]-3-oxidanylidene-propanenitrile
1,6-diazaspiro(3.4)octane-1-propanenitrile, 3-methyl-beta-oxo-6-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-, (3s,4r)-
delgocitinib [usan]
9l0q8kk220 ,
3-((3s,4r)-3-methyl-6-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-1,6-diazaspiro(3.4)octan-1-yl)-3-oxopropanenitrile
unii-9l0q8kk220
leo-124249;jte-052
AT24880
CHEMBL4297507
3-[(3s,4r)-3-methyl-7-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1,7-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile
A936874
3-((3s,4r)-3-methyl-6-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl)-3-oxopropanenitrile
MS-24514
bdbm50545650
EX-A5577
BD178539
DTXSID401336933
3-[(3s,4r)-3-methyl-6-{7h-pyrrolo[2,3-d]pyrimidin-4-yl}-1,6-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile
AKOS040741622

Research Excerpts

Overview

Delgocitinib is a pan-Janus kinase/JAK inhibitor that broadly blocks pro-inflammatory cytokines. It has been effective in other inflammatory skin conditions.

ExcerptReferenceRelevance
"Delgocitinib ointment is a newly approved topical medication for the treatment of atopic dermatitis (AD). "( Delgocitinib in atopic dermatitis.
Ho, J; Molin, S, 2021)		3.51
"Delgocitinib is a pan-Janus kinase/JAK inhibitor that broadly blocks pro-inflammatory cytokines and has been effective in other inflammatory skin conditions."( A phase 2a randomized vehicle-controlled multi-center study of the safety and efficacy of delgocitinib in subjects with moderate-to-severe alopecia areata.
Colavincenzo, M; Del Duca, E; Estrada, Y; Florek, AG; Glickman, JW; Guttman-Yassky, E; Hagstrom, EL; Hashim, P; Ibler, E; Mikhaylov, D; Nia, J; Paller, AS; Posligua, AL; Rangel, SM; Singer, GK, 2023)		1.85

Toxicity

ExcerptReferenceRelevance
" JTE-052 ointment at doses up to 3% was safe and well tolerated."( Efficacy and safety of topical JTE-052, a Janus kinase inhibitor, in Japanese adult patients with moderate-to-severe atopic dermatitis: a phase II, multicentre, randomized, vehicle-controlled clinical study.
Igarashi, A; Nagata, T; Nakagawa, H; Nemoto, O, 2018)		0.48
" JTE-052 ointments of 1% and 3% were generally safe and well tolerated in both populations."( Phase 1 studies to assess the safety, tolerability and pharmacokinetics of JTE-052 (a novel Janus kinase inhibitor) ointment in Japanese healthy volunteers and patients with atopic dermatitis.
Nagata, T; Nakagawa, H; Nemoto, O; Ninomiya, N; Yamada, H, 2018)		0.48
" The incidence of adverse events was similar with delgocitinib and vehicle; none led to discontinuation of delgocitinib."( Efficacy and safety of topical delgocitinib in patients with chronic hand eczema: data from a randomized, double-blind, vehicle-controlled phase IIa study.
Bauer, A; Elsner, P; Mahler, V; Molin, S; Nielsen, TSS; Worm, M, 2020)		1.1
" Safety end-points included the incidence and severity of adverse events (AEs)."( Long-term safety and efficacy of delgocitinib ointment, a topical Janus kinase inhibitor, in adult patients with atopic dermatitis.
Igarashi, A; Kaino, H; Murata, R; Nagata, T; Nakagawa, H; Nemoto, O; Saeki, H, 2020)		0.84
" The secondary endpoint included safety profile by reported adverse events."( A phase 2a randomized vehicle-controlled multi-center study of the safety and efficacy of delgocitinib in subjects with moderate-to-severe alopecia areata.
Colavincenzo, M; Del Duca, E; Estrada, Y; Florek, AG; Glickman, JW; Guttman-Yassky, E; Hagstrom, EL; Hashim, P; Ibler, E; Mikhaylov, D; Nia, J; Paller, AS; Posligua, AL; Rangel, SM; Singer, GK, 2023)		1.13

Dosage Studied

ExcerptRelevanceReference
"In this trial, delgocitinib cream showed a dose-response relationship in terms of efficacy and was well tolerated."( The pan-JAK inhibitor delgocitinib in a cream formulation demonstrates dose response in chronic hand eczema in a 16-week randomized phase IIb trial.
Agner, T; Bauer, A; Ehst, B; Korn, S; Resen, K; Schliemann, S; Shi, VY; Thyssen, JP; Tillmann, S; Worm, M, 2022)		1.39
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitorAn EC 2.7.10.* (protein-tyrosine kinase) inhibitor that specifically blocks the action of non-specific protein-tyrosine kinase (EC 2.7.10.2).
anti-inflammatory drugA substance that reduces or suppresses inflammation.
antipsoriaticA drug used to treat psoriasis.
antiseborrheicA drug or agent applied to the skin to control seborrhea or seborrheic dermatitis.
[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 (6)

ClassDescription
pyrrolopyrimidine
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
nitrileA compound having the structure RC#N; thus a C-substituted derivative of hydrocyanic acid, HC#N. In systematic nomenclature, the suffix nitrile denotes the triply bound #N atom, not the carbon atom attached to it.
azaspiro compoundAn azaspiro compound is a spiro compound in which at least one of the cyclic components is a nitrogen heterocyle.
tertiary carboxamideA carboxamide resulting from the formal condensation of a carboxylic acid with a secondary amine; formula RC(=O)NHR(1)R(2).
N-acylazetidine
[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 (5)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Tyrosine-protein kinase JAK2Homo sapiens (human)IC50 (µMol)0.07450.00010.372210.0000AID1668978; AID1668981; AID1668982; AID1668983; AID1668984; AID1875944
Tyrosine-protein kinase LckHomo sapiens (human)IC50 (µMol)5.80000.00021.317310.0000AID1668969
Tyrosine-protein kinase JAK1Homo sapiens (human)IC50 (µMol)0.02030.00030.23787.3000AID1668977; AID1668980; AID1668981; AID1668982; AID1668986; AID1875947
Non-receptor tyrosine-protein kinase TYK2Homo sapiens (human)IC50 (µMol)0.05330.00020.29504.1000AID1668979; AID1668983; AID1668986
Tyrosine-protein kinase JAK3Homo sapiens (human)IC50 (µMol)0.02200.00010.41937.9200AID1668968; AID1668980; AID1875945
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (144)

Processvia Protein(s)Taxonomy
positive regulation of platelet aggregationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of platelet activationTyrosine-protein kinase JAK2Homo sapiens (human)
response to antibioticTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of SMAD protein signal transductionTyrosine-protein kinase JAK2Homo sapiens (human)
microglial cell activationTyrosine-protein kinase JAK2Homo sapiens (human)
adaptive immune responseTyrosine-protein kinase JAK2Homo sapiens (human)
chromatin remodelingTyrosine-protein kinase JAK2Homo sapiens (human)
transcription by RNA polymerase IITyrosine-protein kinase JAK2Homo sapiens (human)
protein phosphorylationTyrosine-protein kinase JAK2Homo sapiens (human)
apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
immune responseTyrosine-protein kinase JAK2Homo sapiens (human)
signal transductionTyrosine-protein kinase JAK2Homo sapiens (human)
enzyme-linked receptor protein signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
G protein-coupled receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationTyrosine-protein kinase JAK2Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK2Homo sapiens (human)
tyrosine phosphorylation of STAT proteinTyrosine-protein kinase JAK2Homo sapiens (human)
mesoderm developmentTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of cell population proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to oxidative stressTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of cardiac muscle cell apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cell-substrate adhesionTyrosine-protein kinase JAK2Homo sapiens (human)
response to amineTyrosine-protein kinase JAK2Homo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase JAK2Homo sapiens (human)
cytokine-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of cell-cell adhesionTyrosine-protein kinase JAK2Homo sapiens (human)
actin filament polymerizationTyrosine-protein kinase JAK2Homo sapiens (human)
cell differentiationTyrosine-protein kinase JAK2Homo sapiens (human)
erythrocyte differentiationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cell migrationTyrosine-protein kinase JAK2Homo sapiens (human)
axon regenerationTyrosine-protein kinase JAK2Homo sapiens (human)
intracellular mineralocorticoid receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of insulin secretionTyrosine-protein kinase JAK2Homo sapiens (human)
response to lipopolysaccharideTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of type II interferon productionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of interleukin-1 beta productionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of interleukin-17 productionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of tumor necrosis factor productionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of natural killer cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
response to hydroperoxideTyrosine-protein kinase JAK2Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
symbiont-induced defense-related programmed cell deathTyrosine-protein kinase JAK2Homo sapiens (human)
response to tumor necrosis factorTyrosine-protein kinase JAK2Homo sapiens (human)
post-embryonic hemopoiesisTyrosine-protein kinase JAK2Homo sapiens (human)
intracellular signal transductionTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-12-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
cellular response to interleukin-3Tyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-5-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
collagen-activated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-3-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
granulocyte-macrophage colony-stimulating factor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of T cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of protein import into nucleusTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinTyrosine-protein kinase JAK2Homo sapiens (human)
activation of Janus kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of DNA bindingTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of MAPK cascadeTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of neuron apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
post-translational protein modificationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of MHC class II biosynthetic processTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of nitric oxide biosynthetic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cell differentiationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IITyrosine-protein kinase JAK2Homo sapiens (human)
regulation of receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK2Homo sapiens (human)
protein autophosphorylationTyrosine-protein kinase JAK2Homo sapiens (human)
platelet-derived growth factor receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of inflammatory responseTyrosine-protein kinase JAK2Homo sapiens (human)
modulation of chemical synaptic transmissionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of NK T cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionTyrosine-protein kinase JAK2Homo sapiens (human)
type II interferon-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
growth hormone receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
growth hormone receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of growth hormone receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
mammary gland epithelium developmentTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-6-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of leukocyte proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
response to interleukin-12Tyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-35-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
cellular response to lipopolysaccharideTyrosine-protein kinase JAK2Homo sapiens (human)
cellular response to dexamethasone stimulusTyrosine-protein kinase JAK2Homo sapiens (human)
extrinsic apoptotic signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
cellular response to virusTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cold-induced thermogenesisTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of growth factor dependent skeletal muscle satellite cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of epithelial cell apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of postsynapse to nucleus signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of signaling receptor activityTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of T-helper 17 type immune responseTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of apoptotic signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
protein phosphorylationTyrosine-protein kinase LckHomo sapiens (human)
intracellular zinc ion homeostasisTyrosine-protein kinase LckHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processTyrosine-protein kinase LckHomo sapiens (human)
response to xenobiotic stimulusTyrosine-protein kinase LckHomo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase LckHomo sapiens (human)
hemopoiesisTyrosine-protein kinase LckHomo sapiens (human)
platelet activationTyrosine-protein kinase LckHomo sapiens (human)
T cell differentiationTyrosine-protein kinase LckHomo sapiens (human)
T cell costimulationTyrosine-protein kinase LckHomo sapiens (human)
positive regulation of heterotypic cell-cell adhesionTyrosine-protein kinase LckHomo sapiens (human)
intracellular signal transductionTyrosine-protein kinase LckHomo sapiens (human)
peptidyl-tyrosine autophosphorylationTyrosine-protein kinase LckHomo sapiens (human)
Fc-gamma receptor signaling pathwayTyrosine-protein kinase LckHomo sapiens (human)
T cell receptor signaling pathwayTyrosine-protein kinase LckHomo sapiens (human)
positive regulation of T cell receptor signaling pathwayTyrosine-protein kinase LckHomo sapiens (human)
positive regulation of T cell activationTyrosine-protein kinase LckHomo sapiens (human)
leukocyte migrationTyrosine-protein kinase LckHomo sapiens (human)
release of sequestered calcium ion into cytosolTyrosine-protein kinase LckHomo sapiens (human)
regulation of lymphocyte activationTyrosine-protein kinase LckHomo sapiens (human)
positive regulation of leukocyte cell-cell adhesionTyrosine-protein kinase LckHomo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayTyrosine-protein kinase LckHomo sapiens (human)
innate immune responseTyrosine-protein kinase LckHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayTyrosine-protein kinase LckHomo sapiens (human)
B cell receptor signaling pathwayTyrosine-protein kinase LckHomo sapiens (human)
response to antibioticTyrosine-protein kinase JAK1Homo sapiens (human)
protein phosphorylationTyrosine-protein kinase JAK1Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK1Homo sapiens (human)
cytokine-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
positive regulation of homotypic cell-cell adhesionTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-15-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-4-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-2-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-9-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-11-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
type III interferon-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
type II interferon-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
type I interferon-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-6-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
T-helper 17 cell lineage commitmentTyrosine-protein kinase JAK1Homo sapiens (human)
cellular response to virusTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-10-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
protein localization to cell-cell junctionTyrosine-protein kinase JAK1Homo sapiens (human)
positive regulation of protein localization to nucleusTyrosine-protein kinase JAK1Homo sapiens (human)
positive regulation of sprouting angiogenesisTyrosine-protein kinase JAK1Homo sapiens (human)
intracellular signal transductionTyrosine-protein kinase JAK1Homo sapiens (human)
tyrosine phosphorylation of STAT proteinTyrosine-protein kinase JAK1Homo sapiens (human)
cell differentiationTyrosine-protein kinase JAK1Homo sapiens (human)
growth hormone receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK1Homo sapiens (human)
protein phosphorylationNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
immune responseNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
cytokine-mediated signaling pathwayNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
positive regulation of type II interferon productionNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
positive regulation of interleukin-17 productionNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
positive regulation of natural killer cell proliferationNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
interleukin-12-mediated signaling pathwayNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
type III interferon-mediated signaling pathwayNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
positive regulation of T cell proliferationNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STATNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
positive regulation of NK T cell proliferationNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
type II interferon-mediated signaling pathwayNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
type I interferon-mediated signaling pathwayNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
cellular response to virusNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
interleukin-10-mediated signaling pathwayNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
positive regulation of protein localization to nucleusNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
positive regulation of T-helper 17 type immune responseNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
intracellular signal transductionNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
cell differentiationNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
growth hormone receptor signaling pathway via JAK-STATNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
adaptive immune responseTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of dendritic cell cytokine productionTyrosine-protein kinase JAK3Homo sapiens (human)
protein phosphorylationTyrosine-protein kinase JAK3Homo sapiens (human)
enzyme-linked receptor protein signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
tyrosine phosphorylation of STAT proteinTyrosine-protein kinase JAK3Homo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase JAK3Homo sapiens (human)
B cell differentiationTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of interleukin-10 productionTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of interleukin-12 productionTyrosine-protein kinase JAK3Homo sapiens (human)
intracellular signal transductionTyrosine-protein kinase JAK3Homo sapiens (human)
interleukin-15-mediated signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
interleukin-4-mediated signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
interleukin-2-mediated signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
interleukin-9-mediated signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
T cell homeostasisTyrosine-protein kinase JAK3Homo sapiens (human)
innate immune responseTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of FasL productionTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of T-helper 1 cell differentiationTyrosine-protein kinase JAK3Homo sapiens (human)
regulation of receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of T cell activationTyrosine-protein kinase JAK3Homo sapiens (human)
growth hormone receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK3Homo sapiens (human)
regulation of T cell apoptotic processTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of thymocyte apoptotic processTyrosine-protein kinase JAK3Homo sapiens (human)
response to interleukin-2Tyrosine-protein kinase JAK3Homo sapiens (human)
response to interleukin-4Tyrosine-protein kinase JAK3Homo sapiens (human)
response to interleukin-15Tyrosine-protein kinase JAK3Homo sapiens (human)
response to interleukin-9Tyrosine-protein kinase JAK3Homo sapiens (human)
regulation of apoptotic processTyrosine-protein kinase JAK3Homo sapiens (human)
cell differentiationTyrosine-protein kinase JAK3Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK3Homo sapiens (human)
cytokine-mediated signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (31)

Processvia Protein(s)Taxonomy
protein kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
signaling receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
growth hormone receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-12 receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
protein bindingTyrosine-protein kinase JAK2Homo sapiens (human)
ATP bindingTyrosine-protein kinase JAK2Homo sapiens (human)
protein kinase bindingTyrosine-protein kinase JAK2Homo sapiens (human)
heme bindingTyrosine-protein kinase JAK2Homo sapiens (human)
type 1 angiotensin receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
acetylcholine receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
histone H3Y41 kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
SH2 domain bindingTyrosine-protein kinase JAK2Homo sapiens (human)
histone bindingTyrosine-protein kinase JAK2Homo sapiens (human)
identical protein bindingTyrosine-protein kinase JAK2Homo sapiens (human)
phosphatidylinositol 3-kinase bindingTyrosine-protein kinase JAK2Homo sapiens (human)
insulin receptor substrate bindingTyrosine-protein kinase JAK2Homo sapiens (human)
metal ion bindingTyrosine-protein kinase JAK2Homo sapiens (human)
peptide hormone receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
phosphotyrosine residue bindingTyrosine-protein kinase LckHomo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase LckHomo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase LckHomo sapiens (human)
protein serine/threonine phosphatase activityTyrosine-protein kinase LckHomo sapiens (human)
protein bindingTyrosine-protein kinase LckHomo sapiens (human)
ATP bindingTyrosine-protein kinase LckHomo sapiens (human)
phospholipase activator activityTyrosine-protein kinase LckHomo sapiens (human)
protein kinase bindingTyrosine-protein kinase LckHomo sapiens (human)
protein phosphatase bindingTyrosine-protein kinase LckHomo sapiens (human)
SH2 domain bindingTyrosine-protein kinase LckHomo sapiens (human)
T cell receptor bindingTyrosine-protein kinase LckHomo sapiens (human)
CD4 receptor bindingTyrosine-protein kinase LckHomo sapiens (human)
CD8 receptor bindingTyrosine-protein kinase LckHomo sapiens (human)
identical protein bindingTyrosine-protein kinase LckHomo sapiens (human)
phospholipase bindingTyrosine-protein kinase LckHomo sapiens (human)
phosphatidylinositol 3-kinase bindingTyrosine-protein kinase LckHomo sapiens (human)
ATPase bindingTyrosine-protein kinase LckHomo sapiens (human)
signaling receptor bindingTyrosine-protein kinase LckHomo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase JAK1Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase JAK1Homo sapiens (human)
growth hormone receptor bindingTyrosine-protein kinase JAK1Homo sapiens (human)
protein bindingTyrosine-protein kinase JAK1Homo sapiens (human)
ATP bindingTyrosine-protein kinase JAK1Homo sapiens (human)
protein phosphatase bindingTyrosine-protein kinase JAK1Homo sapiens (human)
ubiquitin protein ligase bindingTyrosine-protein kinase JAK1Homo sapiens (human)
CCR5 chemokine receptor bindingTyrosine-protein kinase JAK1Homo sapiens (human)
metal ion bindingTyrosine-protein kinase JAK1Homo sapiens (human)
protein tyrosine kinase activityNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activityNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
growth hormone receptor bindingNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
protein bindingNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
ATP bindingNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
type 1 angiotensin receptor bindingNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase JAK3Homo sapiens (human)
protein bindingTyrosine-protein kinase JAK3Homo sapiens (human)
ATP bindingTyrosine-protein kinase JAK3Homo sapiens (human)
protein phosphatase bindingTyrosine-protein kinase JAK3Homo sapiens (human)
growth hormone receptor bindingTyrosine-protein kinase JAK3Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase JAK3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
extrinsic component of plasma membraneTyrosine-protein kinase JAK2Homo sapiens (human)
extrinsic component of cytoplasmic side of plasma membraneTyrosine-protein kinase JAK2Homo sapiens (human)
nucleusTyrosine-protein kinase JAK2Homo sapiens (human)
nucleoplasmTyrosine-protein kinase JAK2Homo sapiens (human)
cytoplasmTyrosine-protein kinase JAK2Homo sapiens (human)
cytosolTyrosine-protein kinase JAK2Homo sapiens (human)
cytoskeletonTyrosine-protein kinase JAK2Homo sapiens (human)
plasma membraneTyrosine-protein kinase JAK2Homo sapiens (human)
caveolaTyrosine-protein kinase JAK2Homo sapiens (human)
focal adhesionTyrosine-protein kinase JAK2Homo sapiens (human)
granulocyte macrophage colony-stimulating factor receptor complexTyrosine-protein kinase JAK2Homo sapiens (human)
endosome lumenTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-12 receptor complexTyrosine-protein kinase JAK2Homo sapiens (human)
membrane raftTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-23 receptor complexTyrosine-protein kinase JAK2Homo sapiens (human)
postsynapseTyrosine-protein kinase JAK2Homo sapiens (human)
glutamatergic synapseTyrosine-protein kinase JAK2Homo sapiens (human)
euchromatinTyrosine-protein kinase JAK2Homo sapiens (human)
cytosolTyrosine-protein kinase JAK2Homo sapiens (human)
pericentriolar materialTyrosine-protein kinase LckHomo sapiens (human)
immunological synapseTyrosine-protein kinase LckHomo sapiens (human)
cytosolTyrosine-protein kinase LckHomo sapiens (human)
plasma membraneTyrosine-protein kinase LckHomo sapiens (human)
membrane raftTyrosine-protein kinase LckHomo sapiens (human)
extracellular exosomeTyrosine-protein kinase LckHomo sapiens (human)
plasma membraneTyrosine-protein kinase LckHomo sapiens (human)
cytoplasmTyrosine-protein kinase JAK1Homo sapiens (human)
plasma membraneTyrosine-protein kinase JAK1Homo sapiens (human)
cytoplasmic side of plasma membraneTyrosine-protein kinase JAK1Homo sapiens (human)
extrinsic component of cytoplasmic side of plasma membraneTyrosine-protein kinase JAK1Homo sapiens (human)
nucleusTyrosine-protein kinase JAK1Homo sapiens (human)
cytoplasmTyrosine-protein kinase JAK1Homo sapiens (human)
endosomeTyrosine-protein kinase JAK1Homo sapiens (human)
cytosolTyrosine-protein kinase JAK1Homo sapiens (human)
cytoskeletonTyrosine-protein kinase JAK1Homo sapiens (human)
focal adhesionTyrosine-protein kinase JAK1Homo sapiens (human)
cytosolTyrosine-protein kinase JAK1Homo sapiens (human)
plasma membraneNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
cytoplasmic side of plasma membraneNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
extrinsic component of plasma membraneNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
extrinsic component of cytoplasmic side of plasma membraneNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
nucleusNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
cytoplasmNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
cytosolNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
cytoskeletonNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
plasma membraneNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
interleukin-12 receptor complexNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
extracellular exosomeNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
interleukin-23 receptor complexNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
cytosolNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
extrinsic component of plasma membraneTyrosine-protein kinase JAK3Homo sapiens (human)
extrinsic component of cytoplasmic side of plasma membraneTyrosine-protein kinase JAK3Homo sapiens (human)
endosomeTyrosine-protein kinase JAK3Homo sapiens (human)
cytosolTyrosine-protein kinase JAK3Homo sapiens (human)
cytoskeletonTyrosine-protein kinase JAK3Homo sapiens (human)
plasma membraneTyrosine-protein kinase JAK3Homo sapiens (human)
cytosolTyrosine-protein kinase JAK3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (58)

Assay IDTitleYearJournalArticle
AID1668982Inhibition of JAK1/JAK2 in human A549 assessed as reduction in IL31-induced Stat3 phosphorylation preincubated for 30 mins followed by IL31 stimulation and measured after 15 mins2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668987Lipophilicity, logD of the compound at pH 72020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668994Protein binding in rat2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1669018Cmax in rat at 10 mg/kg, po2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668970Inhibition of IL2-induced human T cell proliferation preincubated for 30 mins followed by IL2 stimulation and measured after 3 days by [3H]thymidine incorporation based scintillation counting method2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668997Metabolic stability in rat liver microsomes incubated for 60 mins2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668993Protein binding in human2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1875945Inhibition of JAK 3 (unknown origin)2022Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.
AID1668969Inhibition of N-terminal His6-tagged recombinant full-length human Lck using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1669014MRT in rat at 1 mg/kg, iv2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1669009Terminal half life in dog at 0.3 mg/kg, iv2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668977Inhibition of N-terminal GST-fused human JAK1 (850 to 1154 residues) expressed in baculovirus expression system using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1669015MRT in dog at 0.3 mg/kg, iv2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668979Inhibition of N-terminal GST-fused human TyK2 (871 to end residues) expressed in baculovirus expression system using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1669008Terminal half life in rat at 1 mg/kg, iv2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668992Solubility of the compound in FeSSIF2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668968Inhibition of human JAK3 (780 to end residues) expressed in baculovirus infected Sf9 cells using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668999Metabolic stability in human hepatocytes incubated for 60 mins2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668976Clearance in monkey at 0.1 mg/kg, iv2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668981Inhibition of JAK1/JAK2 in human PBMC assessed as reduction in IL6-induced Stat3 phosphorylation in CD3- CD4+ cells preincubated for 30 mins followed by IL6 stimulation and measured after 15 mins2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668996Protein binding in monkey2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668983Inhibition of JAK2/Tyk2 in human PBMC assessed as reduction in IL-23-induced Stat3 phosphorylation in CD3+CD4+ cells preincubated for 30 mins followed by IL-23 stimulation and measured after 15 mins2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1669005Anti-dermatitis activity in BN rat model of 2,4-dinitrochlorobenzene induced chronic dermatitis assessed as suppression of ear swelling at 10 mg/kg, po administered once daily from day 1 to day 21 relative to control2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668985Selectivity ratio of IC50 for JAK2 in human PBMC to IC50 for JAK1/JAK2 in human A549 cells2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668998Metabolic stability in dog liver microsomes incubated for 60 mins2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1669020Oral bioavailability in rat at 10 mg/kg2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668989Solubility of the compound in human Caco2 cells2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668995Protein binding in dog2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668990Solubility of the compound in PBS buffer2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1669013Volume of distribution at steady state in dog at 0.3 mg/kg, iv2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1669017Tmax in dog at 1 mg/kg, po2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668978Inhibition of N-terminal GST-fused human JAK2 (880 to end residues) expressed in baculovirus infected Sf21 cells using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668980Inhibition of JAK1/JAK3 in human PBMC assessed as reduction in IL2-induced Stat5 phosphorylation in CD3+CD4+ cells preincubated for 30 mins followed by IL2 stimulation and measured after 15 mins2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1669003Antiarthritic activity in po dosed Lewis rat model of adjuvant-induced arthritis assessed as reduction in paw swelling administered once daily from day 1 to day 28 by plethysmometer analysis2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1669010Total clearance in rat at 1 mg/kg, iv2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1669016Tmax in rat at 10 mg/kg, po2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1669000Metabolic stability in rat hepatocytes incubated for 60 mins2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1669007Anti-dermatitis activity in BN rat model of 2,4-dinitrochlorobenzene induced chronic dermatitis assessed as suppression of ear swelling administered topically as ointment thrice daily from day 1 to day 21 relative to control2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668986Inhibition of JAK1/Tyk2 in human PBMC assessed as reduction in INFalpha-induced Stat1 phosphorylation in CD3+CD4+ cells preincubated for 30 mins followed by INFalpha stimulation and measured after 15 mins2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1669006Anti-dermatitis activity in BN rat model of 2,4-dinitrochlorobenzene induced chronic dermatitis assessed as suppression of ear swelling administered topically as ointment once daily from day 1 to day 212020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668988Apparent permeability in human Caco2 cells2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1875947Inhibition of JAK 1 (unknown origin)2022Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.
AID1669019Cmax in dog at 1 mg/kg, po2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668991Solubility of the compound in FaSSIF2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668975Metabolic stability in monkey liver microsomes incubated for 60 mins2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1669002Metabolic stability in monkey hepatocytes incubated for 60 mins2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1875944Inhibition of JAK 2 (unknown origin)2022Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.
AID1669012Volume of distribution at steady state in rat at 1 mg/kg, iv2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1669004Antiarthritic activity in dosed Lewis rat model of adjuvant-induced arthritis assessed as reduction in paw swelling at 30 mg/kg, po administered once daily from day 1 to day 28 by plethysmometer analysis relative to control2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1669011Total clearance in dog at 0.3 mg/kg, iv2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668974Metabolic stability in human liver microsomes incubated for 60 mins2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1668984Inhibition of JAK2 in human PBMC assessed as reduction in GM-CSF-induced Stat5 phosphorylation in CD3- CD4+ cells preincubated for 30 mins followed by GM-CSF stimulation and measured after 15 mins2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1669021Oral bioavailability in dog at 1 mg/kg2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1669001Metabolic stability in dog hepatocytes incubated for 60 mins2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
AID1345714Human Janus kinase 2 (Janus kinase (JakA) family)2015Inflammation research : official journal of the European Histamine Research Society ... [et al.], Jan, Volume: 64, Issue:1
Pharmacological properties of JTE-052: a novel potent JAK inhibitor that suppresses various inflammatory responses in vitro and in vivo.
AID1345872Human tyrosine kinase 2 (Janus kinase (JakA) family)2015Inflammation research : official journal of the European Histamine Research Society ... [et al.], Jan, Volume: 64, Issue:1
Pharmacological properties of JTE-052: a novel potent JAK inhibitor that suppresses various inflammatory responses in vitro and in vivo.
AID1345744Human Janus kinase 3 (Janus kinase (JakA) family)2015Inflammation research : official journal of the European Histamine Research Society ... [et al.], Jan, Volume: 64, Issue:1
Pharmacological properties of JTE-052: a novel potent JAK inhibitor that suppresses various inflammatory responses in vitro and in vivo.
AID1345757Human Janus kinase 1 (Janus kinase (JakA) family)2015Inflammation research : official journal of the European Histamine Research Society ... [et al.], Jan, Volume: 64, Issue:1
Pharmacological properties of JTE-052: a novel potent JAK inhibitor that suppresses various inflammatory responses in vitro and in vivo.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (31)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's8 (25.81)24.3611
2020's23 (74.19)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 48.84

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index48.84 (24.57)
Research Supply Index3.74 (2.92)
Research Growth Index4.82 (4.65)
Search Engine Demand Index77.12 (26.88)
Search Engine Supply Index2.10 (0.95)

This Compound (48.84)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials10 (32.26%)5.53%
Reviews4 (12.90%)6.00%
Case Studies4 (12.90%)4.05%
Observational0 (0.00%)0.25%
Other13 (41.94%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
carbamates
[no description available]		3.4110amino-acid anion
croton oil
[no description available]		2.1310N-acyl-hexosamine
bisindolylmaleimide iv
[no description available]		2.4110indoles;
maleimides
leflunomide
Leflunomide: An isoxazole derivative that inhibits dihydroorotate dehydrogenase, the fourth enzyme in the pyrimidine biosynthetic pathway. It is used an immunosuppressive agent in the treatment of RHEUMATOID ARTHRITIS and PSORIATIC ARTHRITIS.. leflunomide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-methyl-1,2-oxazole-4-carboxylic acid with the anilino group of 4-(trifluoromethyl)aniline. The prodrug of teriflunomide.		2.4110(trifluoromethyl)benzenes;
isoxazoles;
monocarboxylic acid amide		antineoplastic agent;
antiparasitic agent;
EC 1.3.98.1 [dihydroorotate oxidase (fumarate)] inhibitor;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
hepatotoxic agent;
immunosuppressive agent;
non-steroidal anti-inflammatory drug;
prodrug;
pyrimidine synthesis inhibitor;
tyrosine kinase inhibitor
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one: specific inhibitor of phosphatidylinositol 3-kinase; structure in first source		2.4110chromones;
morpholines;
organochlorine compound		autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector
olomoucine
olomoucine: inhibits protein P34CDC2. olomoucine : A 9H-purine that is substituted by a (2-hydroxyethyl)nitrilo, benzylnitrilo and a methyl group at positions 2,6 and 9, respectively. It is a cyclin-dependent kinase inhibitor.		2.41102,6-diaminopurines;
ethanolamines		EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
tyrphostin a9
[no description available]		2.4110alkylbenzenegeroprotector
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		10.23258pyrrole;
secondary amine
imatinib mesylate
imatinib methanesulfonate : A methanesulfonate (mesylate) salt that is the monomesylate salt of imatinib. Used for treatment of chronic myelogenous leukemia and gastrointestinal stromal tumours.		2.4110methanesulfonate saltanticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor
gefitinib
[no description available]		2.4110aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
epidermal growth factor receptor antagonist
lestaurtinib
[no description available]		2.4110indolocarbazole
methotrexate
[no description available]		2.1710dicarboxylic acid;
monocarboxylic acid amide;
pteridines		abortifacient;
antimetabolite;
antineoplastic agent;
antirheumatic drug;
dermatologic drug;
DNA synthesis inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
immunosuppressive agent
canertinib
[no description available]		2.4110monochlorobenzenes;
morpholines;
organofluorine compound;
quinazolines		antineoplastic agent;
tyrosine kinase inhibitor
cyc 202
seliciclib : 2,6-Diaminopurine carrying benzylamino, (2R)-1-hydroxybutan-2-yl and isopropyl substituents at C-6, C-2-N and N-9 respectively. It is an experimental drug candidate in the family of pharmacological cyclin-dependent kinase (CDK) inhibitors.		2.41102,6-diaminopurinesantiviral drug;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
sb 203580
[no description available]		2.4110imidazoles;
monofluorobenzenes;
pyridines;
sulfoxide		EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector;
Hsp90 inhibitor;
neuroprotective agent
erlotinib
[no description available]		2.4110aromatic ether;
quinazolines;
secondary amino compound;
terminal acetylenic compound		antineoplastic agent;
epidermal growth factor receptor antagonist;
protein kinase inhibitor
sorafenib
[no description available]		2.4110(trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
phenylureas;
pyridinecarboxamide		angiogenesis inhibitor;
anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
ferroptosis inducer;
tyrosine kinase inhibitor
pd 166326
PD 166326: a pyrido(2,3-d)pyrimidine src tyrosine kinase inhibitor		2.4110
purvalanol a
6-((3-chloro)anilino)-2-(isopropyl-2-hydroxyethylamino)-9-isopropylpurine: purvalanol A is the (1R)-isomer;		2.4110purvalanol
stilbenes
Stilbenes: Organic compounds that contain 1,2-diphenylethylene as a functional group.. trans-stilbene : The trans-isomer of stilbene.		3.3110stilbene
s 1033
[no description available]		2.4110(trifluoromethyl)benzenes;
imidazoles;
pyridines;
pyrimidines;
secondary amino compound;
secondary carboxamide		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
4-(4-(4-chloro-phenyl)thiazol-2-ylamino)phenol
[no description available]		2.4110substituted aniline
u 0126
U 0126: protein kinase kinase inhibitor; structure in first source		2.4110aryl sulfide;
dinitrile;
enamine;
substituted aniline		antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
osteogenesis regulator;
vasoconstrictor agent
dasatinib
N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source. dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN).		2.41101,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
alsterpaullone
alsterpaullone: structure in first source. alsterpaullone : An organic heterotetracyclic compound that is 1,3-dihydro-2H-1-benzazepin-2-one which shares its 4-5 bond with the 3-2 bond of 5-nitro-1H-indole.		2.4110C-nitro compound;
caprolactams;
organic heterotetracyclic compound		anti-HIV-1 agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
EC 2.7.11.26 (tau-protein kinase) inhibitor
genistein
[no description available]		2.41107-hydroxyisoflavonesantineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
geroprotector;
human urinary metabolite;
phytoestrogen;
plant metabolite;
tyrosine kinase inhibitor
rottlerin
rottlerin: an angiogenesis inhibitor; an inhibitor of protein kinase Cdelta (PKCdelta) and calmodulin kinase III; RN refers to (E)-isomer; do not confuse this chalcone with an anthraquinone that is also called rottlerin (RN 481-72-1);. rottlerin : A chromenol that is 2,2-dimethyl-2H-chromene substituted by hydroxy groups at positions 5 and 7, a 3-acetyl-2,4,6-trihydroxy-5-methylbenzyl group at position 6 and a (1E)-3-oxo-1-phenylprop-1-en-3-yl group at position 8. A potassium channel opener, it is isolated from Mallotus philippensis.		2.4110aromatic ketone;
benzenetriol;
chromenol;
enone;
methyl ketone		anti-allergic agent;
antihypertensive agent;
antineoplastic agent;
apoptosis inducer;
K-ATP channel agonist;
metabolite
alvocidib
alvocidib: structure given in first source. alvocidib : A synthetic dihydroxyflavone that is 5,7-dihydroxyflavone which is substituted by a 3-hydroxy-1-methylpiperidin-4-yl group at position 8 and by a chlorine at the 2' position (the (-)-3S,4R stereoisomer). A cyclin-dependent kinase 9 (CDK9) inhibitor, it has been studied for the treatment of acute myeloid leukaemia, arthritis and atherosclerotic plaque formation.		2.4110dihydroxyflavone;
hydroxypiperidine;
monochlorobenzenes;
tertiary amino compound		antineoplastic agent;
antirheumatic drug;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
3-[6-[4-(trifluoromethoxy)anilino]-4-pyrimidinyl]benzamide
[no description available]		2.4110pyrimidines
bosutinib
4-((2,4-dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methyl-1-piperazinyl)propoxy)-3-quinolinecarbonitrile: a Src kinase inhibitor; structure in first source		2.4110aminoquinoline;
aromatic ether;
dichlorobenzene;
N-methylpiperazine;
nitrile;
tertiary amino compound		antineoplastic agent;
tyrosine kinase inhibitor
su 11248
[no description available]		2.4110monocarboxylic acid amide;
pyrroles		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
immunomodulator;
neuroprotective agent;
vascular endothelial growth factor receptor antagonist
palbociclib
[no description available]		2.4110aminopyridine;
aromatic ketone;
cyclopentanes;
piperidines;
pyridopyrimidine;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
viroxime
[no description available]		2.4110
everolimus
[no description available]		2.4110cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
primary alcohol;
secondary alcohol		anticoronaviral agent;
antineoplastic agent;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
pd 184352
2-(2-chloro-4-iodophenylamino)-N-cyclopropylmethoxy-3,4-difluorobenzamide: inhibits MAP kinase kinase; structure in first source		2.4110aminobenzoic acid
bibx 1382bs
BIBX 1382BS: an ErbB receptor kinase inhibitor; no further information available 4/2001		2.4110substituted aniline
vacuolin-1
vacuolin-1: inhibits Ca2-dependent lysosomal exocytosis		2.4110
pd 0325901
mirdametinib: has antineoplastic activity; appears to be a MEK inhibitor. PD 0325901 : A hydroxamic acid ester that is benzhydroxamic acid (N-hydroxybenzamide) in which the hydroxamic acid group has been converted to the corresponding 2,3-dihydroxypropyl ester and in which the benzene ring has been substituted at position 2 by a (2-fluoro-4-iodophenyl)amino group and at positions 3 and 4 by fluorines (the R enantiomer).		2.4110difluorobenzene;
hydroxamic acid ester;
monofluorobenzenes;
organoiodine compound;
propane-1,2-diols;
secondary amino compound		antineoplastic agent;
EC 2.7.12.2 (mitogen-activated protein kinase kinase) inhibitor
midostaurin
midostaurin : An organic heterooctacyclic compound that is the N-benzoyl derivative of staurosporine.		2.4110benzamides;
gamma-lactam;
indolocarbazole;
organic heterooctacyclic compound		antineoplastic agent;
EC 2.7.11.13 (protein kinase C) inhibitor
tofacitinib
tofacitinib : A pyrrolopyrimidine that is pyrrolo[2,3-d]pyrimidine substituted at position 4 by an N-methyl,N-(1-cyanoacetyl-4-methylpiperidin-3-yl)amino moiety. Used as its citrate salt to treat moderately to severely active rheumatoid arthritis.		4.8140N-acylpiperidine;
nitrile;
pyrrolopyrimidine;
tertiary amino compound		antirheumatic drug;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
osu 03012
OSU 03012: a PDK-1 inhibitor; structure in first source		2.4110antibiotic antifungal drug;
aromatic amide;
glycine derivative;
organofluorine compound;
phenanthrenes;
pyrazoles		antineoplastic agent;
apoptosis inducer;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor
bx795
BX795: structure in first source		2.4110ureas
azd 6244
AZD 6244: a MEK inhibitor		2.4110benzimidazoles;
bromobenzenes;
hydroxamic acid ester;
monochlorobenzenes;
organofluorine compound;
secondary amino compound		anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
a 443654
A 443654: an Akt kinase inhibitor; structure in first source		2.4110indoles
apilimod
[no description available]		2.4110
pik 75
PIK 75: structure in first source		2.4110
saracatinib
[no description available]		2.4110aromatic ether;
benzodioxoles;
diether;
N-methylpiperazine;
organochlorine compound;
oxanes;
quinazolines;
secondary amino compound		anticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
autophagy inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
radiosensitizing agent
regorafenib
[no description available]		2.4110(trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
phenylureas;
pyridinecarboxamide		antineoplastic agent;
hepatotoxic agent;
tyrosine kinase inhibitor
bi 2536
[no description available]		2.4110
crizotinib
Crizotinib: A piperidine and aminopyridine derivative that acts as an inhibitor of RECEPTOR PROTEIN-TYROSINE KINASES, including ANAPLASTIC LYMPHOMA KINASE (ALK) and HEPATOCYTE GROWTH FACTOR RECEPTOR (HGFR; c-Met). It is used in the treatment of NON-SMALL CELL LUNG CANCER.. crizotinib : A 3-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)pyrazol-4-yl]pyridin-2-amine that has R configuration at the chiral centre. The active enantiomer, it acts as a kinase inhibitor and is used for the treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC)		2.41103-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)pyrazol-4-yl]pyridin-2-amineantineoplastic agent;
biomarker;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
trametinib
[no description available]		2.4110acetamides;
aromatic amine;
cyclopropanes;
organofluorine compound;
organoiodine compound;
pyridopyrimidine;
ring assembly		anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector
pha 767491
PHA 767491: a Cdc7 inhibitor; structure in first source		2.4110pyrrolopyridine
dactolisib
dactolisib: antineoplastic agent that inhibits both phosphatidylinositol 3-kinase and mTOR. dactolisib : An imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 4-(1-cyanoisopropyl)phenyl group and at position 8 by a quinolin-3-yl group. A dual PI3K/mTOR inhibitor used in cancer treatment.		2.4110imidazoquinoline;
nitrile;
quinolines;
ring assembly;
ureas		antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor
3-(4-chlorophenyl)-adamantane-1-carboxylic acid (pyridin-4-ylmethyl)amide
[no description available]		2.4110organochlorine compound
azd8330
[no description available]		2.4110pyridinecarboxamide
fedratinib
fedratinib: a selective small-molecule inhibitor of JAK2		2.4110sulfonamide
14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene
14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene: has antineoplastic activity; also inhibits Fms-like tyrosine kinase-3; structure in first source		2.4110
pci 32765
ibrutinib: a Btk protein inhibitor. ibrutinib : A member of the class of acrylamides that is (3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine in which the piperidine nitrogen is replaced by an acryloyl group. A selective and covalent inhibitor of the enzyme Bruton's tyrosine kinase, it is used for treatment of B-cell malignancies.		2.4110acrylamides;
aromatic amine;
aromatic ether;
N-acylpiperidine;
pyrazolopyrimidine;
tertiary carboxamide		antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
mk 2206
MK 2206: a protein kinase inhibitor and antineoplastic agent		2.4110organic heterotricyclic compoundEC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide
N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide: a Janus kinase 1 and Janus kinase 2 inhibitor; structure in first source. momelotinib : A benzamide obtained by formal condensation of the carboxy group of 4-{2-[4-(morpholin-4-yl)anilino]pyrimidin-4-yl}benzoic acid with the primary amino group of aminoacetonitrile. It is an ATP-competitive JAK1/JAK2 inhibitor with IC50 of 11 nM and 18 nM, respectively. Used for the treatment of patients with intermediate- or high-risk myelofibrosis.		2.4110aminopyrimidine;
benzamides;
morpholines;
nitrile;
secondary amino compound;
tertiary amino compound		anti-anaemic agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
incb-018424
[no description available]		3.8620nitrile;
pyrazoles;
pyrrolopyrimidine		antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
fit-039
FIT-039: CDK9 inhibitor; structure in first source		2.4110
azd2014
vistusertib: potent and selective dual mTORC1 and mTORC2 inhibitor; structure in first source		2.4110
bay 869766
[no description available]		2.4110
baricitinib
[no description available]		3.8620azetidines;
nitrile;
pyrazoles;
pyrrolopyrimidine;
sulfonamide		anti-inflammatory agent;
antirheumatic drug;
antiviral agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
immunosuppressive agent
piperidines
Piperidines: A family of hexahydropyridines.		4.2720
an2728
crisaborole: NSAID, Dermatologic Agent; structure in first source. crisaborole : A member of the class of benzoxaboroles that is 5-hydroxy-1,3-dihydro-2,1-benzoxaborole in which the phenolic hydrogen has been replaced by a 4-cyanophenyl group. A phosphodiesterase 4 inhibitor that is used for treatment of mild to moderate atopic dermatitis in children and adults.		3.3110aromatic ether;
benzoxaborole;
nitrile		antipsoriatic;
non-steroidal anti-inflammatory drug;
phosphodiesterase IV inhibitor
4-(cyclopropylamino)-2-((4-(4-(ethylsulfonyl)piperazin-1-yl)phenyl)amino)pyrimidine-5-carboxamide
4-(cyclopropylamino)-2-((4-(4-(ethylsulfonyl)piperazin-1-yl)phenyl)amino)pyrimidine-5-carboxamide: a protein kinase inhibitor; structure in first source		2.4110
ly2784544
[no description available]		2.4110pyridazines
sb 1518
[no description available]		2.4110
dinaciclib
[no description available]		2.4110pyrazolopyrimidine
gilteritinib
gilteritinib: an FLT3/AXL protein tyrosine kinase inhibitor. gilteritinib : A member of the class of pyrazines that is pyrazine-2-carboxamide which is substituted by {3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}nitrilo, (oxan-4-yl)nitrilo and ethyl groups at positions 3,5 and 6, respectively. It is a potent inhibitor of FLT3 and AXL tyrosine kinase receptors (IC50 = 0.29 nM and 0.73 nM, respectively). Approved by the FDA for the treatment of acute myeloid leukemia in patients who have a FLT3 gene mutation.		2.4110aromatic amine;
monomethoxybenzene;
N-methylpiperazine;
oxanes;
piperidines;
primary carboxamide;
pyrazines;
secondary amino compound		antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
glpg0634
[no description available]		2.4110
incb039110
INCB039110: a JAK1 inhibitor; structure in first source		2.4110
vx-970
berzosertib: an ATR kinase inhibitor		2.4110sulfonamide
ldc4297
LDC4297: a CDK7 inhibitor with antineoplastic activity; structure in first source. LDC4297 : A pyrazolotriazine that is pyrazolo[1,5-a][1,3,5]triazine substituted by a piperidin-3-yloxy group, [2-(1H-pyrazol-1-yl)benzyl]nitrilo group and an isopropyl group at positions 2, 4 and 8 respectively. It is a potent and selective CDK7 inhibitor and exhibits antiviral activity.		2.4110aromatic ether;
piperidines;
pyrazoles;
pyrazolotriazine;
secondary amino compound		antineoplastic agent;
antiviral agent;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
cyclosporine
Cyclosporine: A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. (From Martindale, The Extra Pharmacopoeia, 30th ed).		2.1710
at 9283
[no description available]		2.4110
ag-879
AG-879: structure given in first source		2.4110
hesperadin
[no description available]		2.4110
ConditionIndicatedRelationship StrengthStudiesTrials
Adjuvant Arthritis
[description not available]		02.1110
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.5720
Innate Inflammatory Response
[description not available]		02.8330
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		02.8330
Eczema, Atopic
[description not available]		09.3187
Dermatitis, Atopic
A chronic inflammatory genetically determined disease of the skin marked by increased ability to form reagin (IgE), with increased susceptibility to allergic rhinitis and asthma, and hereditary disposition to a lowered threshold for pruritus. It is manifested by lichenification, excoriation, and crusting, mainly on the flexural surfaces of the elbow and knee. In infants it is known as infantile eczema.		111.3187
2019 Novel Coronavirus Disease
[description not available]		02.4110
Viral Diseases
[description not available]		02.4110
Virus Diseases
A general term for diseases caused by viruses.		02.4110
Dermatitis Medicamentosa
[description not available]		02.3110
Dermatitis, Eczematous
[description not available]		05.9654
Ache
[description not available]		04.8422
Itching
[description not available]		05.9354
Eczema
A pruritic papulovesicular dermatitis occurring as a reaction to many endogenous and exogenous agents (Dorland, 27th ed).		17.9654
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		09.8422
Pruritus
An intense itching sensation that produces the urge to rub or scratch the skin to obtain relief.		010.9354
Alopecia Circumscripta
[description not available]		04.421
Alopecia Areata
Loss of scalp and body hair involving microscopically inflammatory patchy areas.		16.421
Lupus Erythematosus, Cutaneous, Subacute
[description not available]		02.610
Lupus Erythematosus, Cutaneous
A form of lupus erythematosus in which the skin may be the only organ involved or in which skin involvement precedes the spread into other body systems. It has been classified into three forms - acute (= LUPUS ERYTHEMATOSUS, SYSTEMIC with skin lesions), subacute, and chronic (= LUPUS ERYTHEMATOSUS, DISCOID).		02.610
Histiocytosis
General term for the abnormal appearance of histiocytes in the blood. Based on the pathological features of the cells involved rather than on clinical findings, the histiocytic diseases are subdivided into three groups: HISTIOCYTOSIS, LANGERHANS CELL; HISTIOCYTOSIS, NON-LANGERHANS-CELL; and HISTIOCYTIC DISORDERS, MALIGNANT.		07.610
Allergic Contact Dermatitis
[description not available]		04.0221
Dermatitis, Allergic Contact
A contact dermatitis due to allergic sensitization to various substances. These substances subsequently produce inflammatory reactions in the skin of those who have acquired hypersensitivity to them as a result of prior exposure.		04.0221
Hypomelanosis
[description not available]		02.610
Vitiligo
A disorder consisting of areas of macular depigmentation, commonly on extensor aspects of extremities, on the face or neck, and in skin folds. Age of onset is often in young adulthood and the condition tends to progress gradually with lesions enlarging and extending until a quiescent state is reached.		02.8220
Hypopigmentation
A condition caused by a deficiency or a loss of melanin pigmentation in the epidermis, also known as hypomelanosis. Hypopigmentation can be localized or generalized, and may result from genetic defects, trauma, inflammation, or infections.		02.610
Acne
[description not available]		03.6411
Contact Dermatitis
[description not available]		03.6411
Sycosis
[description not available]		03.6411
Nasopharyngitis
Inflammation of the NASOPHARYNX, usually including its mucosa, related lymphoid structure, and glands.		03.6411
Acne Vulgaris
A chronic disorder of the pilosebaceous apparatus associated with an increase in sebum secretion. It is characterized by open comedones (blackheads), closed comedones (whiteheads), and pustular nodules. The cause is unknown, but heredity and age are predisposing factors.		03.6411
Dermatitis, Contact
A type of acute or chronic skin reaction in which sensitivity is manifested by reactivity to materials or substances coming in contact with the skin. It may involve allergic or non-allergic mechanisms.		03.6411
Folliculitis
Inflammation of follicles, primarily hair follicles.		03.6411
Autoimmune Disease
[description not available]		03.1710
Allergic Reaction
[description not available]		03.1710
Autoimmune Diseases
Disorders that are characterized by the production of antibodies that react with host tissues or immune effector cells that are autoreactive to endogenous peptides.		03.1710
Hypersensitivity
Altered reactivity to an antigen, which can result in pathologic reactions upon subsequent exposure to that particular antigen.		03.1710
Blepharitis
Inflammation of the eyelids.		07.3110
Besnier-Boeck Disease
[description not available]		02.3110
Dermatoses
[description not available]		02.3110
Sarcoidosis
An idiopathic systemic inflammatory granulomatous disorder comprised of epithelioid and multinucleated giant cells with little necrosis. It usually invades the lungs with fibrosis and may also involve lymph nodes, skin, liver, spleen, eyes, phalangeal bones, and parotid glands.		07.3110
Skin Diseases
Diseases involving the DERMIS or EPIDERMIS.		02.3110
Dermatitis, Contact, Phototoxic
[description not available]		03.5611