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

oclacitinib

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Cross-References

ID SourceID
PubMed CID44631938
CHEMBL ID2103874
SCHEMBL ID261679
SCHEMBL ID261673
SCHEMBL ID22406314
SCHEMBL ID22406313
SCHEMBL ID19273287
SCHEMBL ID19229712
MeSH IDM0593865

Synonyms (58)

Synonym
oclacitinib (usan)
D10141
1208319-26-9
99gs5xtb51 ,
cyclohexanemethanesulfonamide, n-methyl-4-(methyl-7h-pyrrolo(2,3-d)pyrimidin-4- ylamino)-, trans-
n-methyl(trans-4-(methyl-7h-pyrrolo(2,3-d)pyrimidin-4-ylamino)cyclohexyl) methanesulfonamide
oclacitinib
oclacitinib [usan:inn]
jaki
pf-03394197
pf-03394197, jaki
unii-99gs5xtb51
pf 03394197
CHEMBL2103874
jak-i
oclacitinib [usan]
oclacitinib [green book]
cyclohexanemethanesulfonamide, n-methyl-4-(methyl-7h-pyrrolo(2,3-d)pyrimidin-4-ylamino)-, trans-
oclacitinib [mi]
n-methyl(trans-4-(methyl(7h-pyrrolo(2,3-d)pyrimidin-4-yl)amino)cyclohexyl)methanesulfonamide
oclacitinib [inn]
CS-3277
HY-13577
SCHEMBL261679
SCHEMBL261673
pf-03394197(oclacitinib)
gtpl9696
apoquel (veterinary use)
AC-32992
SCHEMBL22406314
SCHEMBL22406313
n-methyl-1-((1r,4r)-4-(methyl(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclohexyl)methanesulfonamide
AKOS026750309
n-methyl-1-(trans-4-(methyl(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclohexyl)methanesulfonamide
pf03394197
bdbm185700
us9161939, 1a
AKOS027439963
n-methyl-1-[(1r,4r)-4-[methyl({7h-pyrrolo[2,3-d]pyrimidin-4-yl})amino]cyclohexyl]methanesulfonamide
mfcd25976611
NCGC00390707-03
SCHEMBL19273287
SCHEMBL19229712
pf 03394197;pf03394197;oclacitinib
BCP07898
oclacitinib,pf-03394197
EX-A1602
AS-17051
DTXSID501016299 ,
AMY19409
NCGC00390707-01
Q27272209
n-methyl-1-[4-[methyl(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclohexyl]methanesulfonamide
NCGC00390707-08
N11414
A927519
SY070791
n-methyl-1-[trans-4-[methyl(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclohexyl]methanesulfonamide

Research Excerpts

Overview

Oclacitinib is a Janus kinase (JK)1 inhibitor that has been shown to be effective and safe for the treatment of allergic dermatitis in dogs. Oclac itinib controls itch and inflammation in allergic disease via the inhibition of the JAK/STAT pathway.

ExcerptReferenceRelevance
"Oclacitinib is a Janus kinase (JK)1 inhibitor that has been shown to be effective and safe for the treatment of allergic dermatitis in dogs. "( A pharmacokinetic study of oclacitinib maleate in six cats.
Carrasco, I; Cristòfol, C; Ferrer, L; Puigdemont, A, 2020)		2.3
"Oclacitinib is an effective systemic therapy for dogs with atopic dermatitis (AD). "( Efficacy and safety of 0.0584% hydrocortisone aceponate topical spray and systemic oclacitinib combination therapy in dogs with atopic dermatitis: a randomized, double-blinded, placebo-controlled trial.
Fukamachi, T; Hisano, T; Imanishi, I; Iyori, K; Kanda, S; Momiyama, S; Motegi, T; Nishiyama, S; Taguchi, N; Takahashi, J, 2021)		2.29
"Oclacitinib is a synthetic janus kinase-1 (JAK1) inhibitor, that selectively inhibits cytokines involved in inflammation and pruritus."( Use of oclacitinib as antipruritic drug during sarcoptic mange infestation treatment.
Cornegliani, L; Guidi, E; Vercelli, A, 2020)		1.73
"Oclacitinib is a selective Janus kinase inhibitor for the treatment of canine allergic pruritus and atopic dermatitis in dogs. "( The frequency of urinary tract infection and subclinical bacteriuria in dogs with allergic dermatitis treated with oclacitinib: a prospective study.
Moore, AR; Rosychuk, RAW; Schissler, JR; Simpson, AC, 2017)		2.11
"Oclacitinib (OCL) is a novel immunosuppressive agent approved for dogs that controls itch and inflammation in allergic disease via the inhibition of the JAK/STAT pathway. "( Oclacitinib depletes canine CD4
Jaroszewski, JJ; Jasiecka-Mikołajczyk, A; Maślanka, T, 2018)		3.37
"Oclacitinib is a Janus kinase inhibitor used to control pruritus and skin lesions in canine allergic skin disease; its effect on canine T cells is not well-characterized."( Immunomodulatory in vitro effects of oclacitinib on canine T-cell proliferation and cytokine production.
Banovic, F; Barber, JP; Gogal, RM; Gordon, H; Tarigo, J, 2019)		2.23
"Oclacitinib is a Janus-kinase inhibitor that decreases interleukin-31-induced pruritus in cats. "( A double-blinded, randomized, methylprednisolone-controlled study on the efficacy of oclacitinib in the management of pruritus in cats with nonflea nonfood-induced hypersensitivity dermatitis.
Matricoti, I; Noli, C; Schievano, C, 2019)		2.18
"Oclacitinib is a generally well-tolerated, veterinary-approved, nonselective JAKinib that has therapeutic potential as an immunosuppressant."( The role of oclacitinib in the management of ischaemic dermatopathy in four dogs.
Levy, BJ; Linder, KE; Olivry, T, 2019)		1.61
"Oclacitinib is a Janus kinase (JAK) 1 enzyme inhibitor and blocks JAK1-dependent cytokines and is used to control pruritus. "( A blinded, randomized, placebo-controlled trial of the safety of oclacitinib in cats.
Alves, MSR; Campos, DR; da Veiga, CCP; de Souza, MSG; Fernandes, JI; Lopes, NL; Machado, MA; Merlo, A; Scott, FB, 2019)		2.19
"Oclacitinib is a Janus kinase inhibitor that decreases pruritus and lesions in allergic dogs. "( Oclacitinib in feline nonflea-, nonfood-induced hypersensitivity dermatitis: results of a small prospective pilot study of client-owned cats.
Borio, S; Colombo, S; Noli, C; Ortalda, C, 2015)		3.3

Treatment

Oclacitinib treatment on cAD-affected dogs shifted the composition of microbiota towards that in healthy dogs. The latter brought it much closer to healthy microbiota, particularly in the gut.

ExcerptReferenceRelevance
"Oclacitinib treatment significantly reduced pVAS and CADESI-04 scores, by 51% and 86.7%, respectively. "( Immunomodulatory effect of long-term oclacitinib maleate therapy in dogs with atopic dermatitis.
Coura, FM; da Costa-Val, AP; da Silveira-Lemos, D; De Caro Martins, G; de Oliveira Melo-Junior, OA; Diamantino, GML; Giunchetti, RC; Melo, MM; Nogueira, MM, 2022)		2.44
"Oclacitinib treatment on cAD-affected dogs shifted the composition of microbiota towards that in healthy dogs, and the latter brought it much closer to healthy microbiota, particularly in the gut."( A comprehensive analysis of gut and skin microbiota in canine atopic dermatitis in Shiba Inu dogs.
Busch, H; Hirose, M; Ibrahim, SM; Künstner, A; Lenfers, T; Nishifuji, K; Olbrich, M; Osumi, T; Shimazaki, Y; Thomsen, M; Watson, A; Wohlers, I, 2023)		1.63
"Oclacitinib treatment was then initiated at the dosage of 0.4-0.7 mg/kg twice daily, along with a tapering regimen of oral prednisolone."( The role of oclacitinib in the management of ischaemic dermatopathy in four dogs.
Levy, BJ; Linder, KE; Olivry, T, 2019)		1.61
"Treatment with oclacitinib maleate (Apoquel®, Zoetis; 0.46-0.5 mg/kg po, bid) resulted in rapid and complete resolution of the pruritus with subsequent improvement in demeanor and fur regrowth."( TREATMENT SUCCESS IN THREE ANDEAN BEARS (TREMARCTOS ORNATUS) WITH ALOPECIA SYNDROME USING OCLACITINIB MALEATE (APOQUEL®).
Cosgrove, SB; Drake, GJ; Guézénec, M; Kolter, L; Leclerc, A; Lécu, A; Lemberger, K; López, J; Magnone, W; Nicolau, A; Nuttall, T; Pin, D; Potier, R, 2017)		1.02

Toxicity

Oclacitinib is safe and effective for treating dogs with pruritus associated with allergic and atopic dermatitis, based on randomized clinical trials of up to 4 months duration. Three times as many adverse events attributed to gastrointestinal signs were reported in the ciclosporin group compared with the oclac itinib group.

ExcerptReferenceRelevance
"In this study, oclacitinib provided rapid, effective and safe control of pruritus associated with allergic dermatitis, with owners and veterinarians noting substantial improvements in pruritus and dermatitis VAS scores."( Efficacy and safety of oclacitinib for the control of pruritus and associated skin lesions in dogs with canine allergic dermatitis.
Boucher, JF; Cleaver, DM; Cosgrove, SB; Follis, SL; Harfst, JA; King, VL; Martin, DD; Stegemann, MR; Walsh, KF; Wren, JA, 2013)		1.05
"Oclacitinib provided rapid, effective and safe control of AD, with substantial improvement in VAS and CADESI-02 scores."( A blinded, randomized, placebo-controlled trial of the efficacy and safety of the Janus kinase inhibitor oclacitinib (Apoquel®) in client-owned dogs with atopic dermatitis.
Cleaver, DM; Cosgrove, SB; Follis, SI; King, VI; Stegemann, MR; Tena, JK; Walsh, KF; Wren, JA, 2013)		2.05
"Ciclosporin is approved for the treatment of atopic dermatitis (AD) in dogs and has been shown to be safe and effective."( A blinded, randomized clinical trial comparing the efficacy and safety of oclacitinib and ciclosporin for the control of atopic dermatitis in client-owned dogs.
Cosgrove, SB; Davis, KR; King, VL; Little, PR; Stegemann, MR, 2015)		0.65
" Three times as many adverse events attributed to gastrointestinal signs were reported in the ciclosporin group compared with the oclacitinib group."( A blinded, randomized clinical trial comparing the efficacy and safety of oclacitinib and ciclosporin for the control of atopic dermatitis in client-owned dogs.
Cosgrove, SB; Davis, KR; King, VL; Little, PR; Stegemann, MR, 2015)		0.85
"Oclacitinib is safe and effective for treating dogs with pruritus associated with allergic and atopic dermatitis, based on randomized clinical trials of up to 4 months duration."( Long-term compassionate use of oclacitinib in dogs with atopic and allergic skin disease: safety, efficacy and quality of life.
Cleaver, DM; Cosgrove, SB; Daniels, AE; Gilmer, AR; King, VL; Stegemann, MR; Wren, JA, 2015)		2.15
"Results indicated that oclacitinib was safe and efficacious for long-term use and improved the quality of life for dogs in this study."( Long-term compassionate use of oclacitinib in dogs with atopic and allergic skin disease: safety, efficacy and quality of life.
Cleaver, DM; Cosgrove, SB; Daniels, AE; Gilmer, AR; King, VL; Stegemann, MR; Wren, JA, 2015)		1.01
" Oclacitinib maleate was well tolerated during the study and few adverse events were observed in treated cats."( A blinded, randomized, placebo-controlled trial of the safety of oclacitinib in cats.
Alves, MSR; Campos, DR; da Veiga, CCP; de Souza, MSG; Fernandes, JI; Lopes, NL; Machado, MA; Merlo, A; Scott, FB, 2019)		1.66
"Oclacitinib maleate was well tolerated by cats at 1 mg/kg and 2 mg/kg and appeared to be safe for this species when administered orally twice daily for 28 days."( A blinded, randomized, placebo-controlled trial of the safety of oclacitinib in cats.
Alves, MSR; Campos, DR; da Veiga, CCP; de Souza, MSG; Fernandes, JI; Lopes, NL; Machado, MA; Merlo, A; Scott, FB, 2019)		2.19

Pharmacokinetics

The pharmacokinetic parameters of oclacitinib in the cat are similar to those described for the dog, although absorption and elimination are somewhat faster and variability between individuals is somewhat greater. The prandial state of dogs did not significantly affect the rate or extent of absorption when dosed orally.

ExcerptReferenceRelevance
" The prandial state of dogs did not significantly affect the rate or extent of absorption of oclacitinib maleate when dosed orally, as demonstrated by the lack of significant differences in pharmacokinetic parameters between the oral fasted and oral fed treatment groups."( The pharmacokinetics of oclacitinib maleate, a Janus kinase inhibitor, in the dog.
Boucher, JF; Collard, WT; Fielder, AF; Hummel, BD; King, VL; Malpas, PB; Mullins, MA; Stegemann, MR, 2014)		0.93
" Its use in cats has been limited by the absence of pharmacokinetic data."( A pharmacokinetic study of oclacitinib maleate in six cats.
Carrasco, I; Cristòfol, C; Ferrer, L; Puigdemont, A, 2020)		0.86
"To determine the pharmacokinetic parameters of oclacitinib in cats after oral and intravenous administration."( A pharmacokinetic study of oclacitinib maleate in six cats.
Carrasco, I; Cristòfol, C; Ferrer, L; Puigdemont, A, 2020)		1.11
"The pharmacokinetic parameters of oclacitinib in the cat are similar to those described for the dog, although absorption and elimination are somewhat faster and variability between individuals is somewhat greater."( A pharmacokinetic study of oclacitinib maleate in six cats.
Carrasco, I; Cristòfol, C; Ferrer, L; Puigdemont, A, 2020)		1.13

Bioavailability

ExcerptReferenceRelevance
" The absolute bioavailability study used a crossover design with 10 dogs."( The pharmacokinetics of oclacitinib maleate, a Janus kinase inhibitor, in the dog.
Boucher, JF; Collard, WT; Fielder, AF; Hummel, BD; King, VL; Malpas, PB; Mullins, MA; Stegemann, MR, 2014)		0.71
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51

Dosage Studied

The combination of PCSO-524 and oclacitinib may help to alleviate the rebound effect that occurs when tapering down the dosage. There was no association identified between daily maintenance dosage of oclAcitonib and odds of malignancy or benign skin masses for dogs in the exposed group.

ExcerptRelevanceReference
" The prandial state of dogs did not significantly affect the rate or extent of absorption of oclacitinib maleate when dosed orally, as demonstrated by the lack of significant differences in pharmacokinetic parameters between the oral fasted and oral fed treatment groups."( The pharmacokinetics of oclacitinib maleate, a Janus kinase inhibitor, in the dog.
Boucher, JF; Collard, WT; Fielder, AF; Hummel, BD; King, VL; Malpas, PB; Mullins, MA; Stegemann, MR, 2014)		0.93
" Dogs received oclacitinib at labelled dosing for an intended period of 180-230 days with a follow-up urinalysis and urine culture performed regardless of urinary tract signs."( The frequency of urinary tract infection and subclinical bacteriuria in dogs with allergic dermatitis treated with oclacitinib: a prospective study.
Moore, AR; Rosychuk, RAW; Schissler, JR; Simpson, AC, 2017)		1.02
" Remission was maintained in two dogs with lower doses or dosing frequencies of oclacitinib, whereas the two others required persistent twice daily administration of this JAKinib."( The role of oclacitinib in the management of ischaemic dermatopathy in four dogs.
Levy, BJ; Linder, KE; Olivry, T, 2019)		1.12
"Further larger-scale studies are warranted to investigate optimal strain(s), dosing and duration of probiotic supplementation as an adjunctive strategy in management of canine atopic dermatitis."( Pilot evaluation of Enterococcus faecium SF68 as adjunctive therapy for oclacitinib-responsive adult atopic dermatitis in dogs.
Griffin, C; Rosenkrantz, W; Yamazaki, C, 2019)		0.75
" Larger doses and/or shorter dosing intervals would be recommended in cats to achieve similar blood concentrations to those in dogs."( A pharmacokinetic study of oclacitinib maleate in six cats.
Carrasco, I; Cristòfol, C; Ferrer, L; Puigdemont, A, 2020)		0.86
" Les doses plus importantes et/ou les intervalles de dosage pourraient être recommandés chez le chat pour atteindre les concentrations sanguines semblables à celles du chien."( A pharmacokinetic study of oclacitinib maleate in six cats.
Carrasco, I; Cristòfol, C; Ferrer, L; Puigdemont, A, 2020)		0.86
" Results for cumulative incidences of malignancies and other variables were compared between groups, and the effect of daily maintenance dosage of oclacitinib on cumulative incidences of malignancies and other skin masses was evaluated within the exposed group."( Age- and breed-matched retrospective cohort study of malignancies and benign skin masses in 660 dogs with allergic dermatitis treated long-term with versus without oclacitinib.
Angus, JC; Edginton, HD; Lancellotti, BA; Rosenkrantz, WS, 2020)		0.95
" There was no association identified between daily maintenance dosage of oclacitinib and odds of malignancy or benign skin masses for dogs in the exposed group."( Age- and breed-matched retrospective cohort study of malignancies and benign skin masses in 660 dogs with allergic dermatitis treated long-term with versus without oclacitinib.
Angus, JC; Edginton, HD; Lancellotti, BA; Rosenkrantz, WS, 2020)		0.99
" Le surnageant des lignées cellulaires a été évalué pour la présence de 11 cytokines [IL-2, -6, -7, -8, -10, -15 et -18, et MCP-1, facteur de stimulation des colonies de granulocytes-macrophages ( GM-CSF), l'interféron (IFN)γ et le facteur de nécrose tumorale (TNF)α] par dosage immuno-enzymatique (ELISA)."( Cytokine production and the effects of oclacitinib in three canine mast cell tumour cell lines.
de Mello Souza, CH; Hwang, B; Shiomitsu, K, 2022)		0.99
" Les concentrations sériques d'IL-10 et de TGF-β1 ont été mesurées par dosage immuno-enzymatique."( Long-term effects of ciclosporin and oclacitinib on mediators of tolerance, regulatory T-cells, IL-10 and TGF-β, in dogs with atopic dermatitis.
Bizikova, P; Herrmann, I; Holmes, J; Mamo, LB; Mohammed, JP; Murphy, KM, 2023)		1.18
"The combination of PCSO-524 and oclacitinib may help to alleviate the rebound effect that occurs when tapering down the dosage of oclacitinib, as compared to using oclacitinib alone for the management of cAD."( A randomised, double-blinded, controlled trial to determine the efficacy of combined therapy of oclacitinib and marine oil extract PCSO-524 in dogs with atopic dermatitis.
Fukamachi, T; Hisano, T; Hsiao, YH; Imanishi, I; Iyori, K; Kusakabe, M; Nishiyama, T; Taguchi, N, 2023)		1.41
"This retrospective study evaluates in which group of dogs [oclacitinib (OC) or azathioprine (AZ)] remission of pemphigus foliaceus (PF) was more effectively achieved with matched induction dosing of glucocorticoids; it further evaluates which group had a higher glucocorticoid-sparing effect."( The use of oclacitinib compared to azathioprine in the management of canine pemphigus foliaceus: A retrospective analysis.
Bidot, WA; Griffin, CE; Hernandez-Bures, A; Rosenkrantz, WS, 2023)		1.54
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency18.99910.01237.983543.2770AID1645841
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency35.48130.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Tyrosine-protein kinase JAK2Homo sapiens (human)IC50 (µMol)0.01800.00010.372210.0000AID1639175
Tyrosine-protein kinase JAK1Homo sapiens (human)IC50 (µMol)0.01000.00030.23787.3000AID1639174
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (110)

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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (21)

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)
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)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (7)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1639175Inhibition of human recombinant JAK2 (808 to 1132 residues) by Z-Lyte assay2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
The impact of binding site waters on the activity/selectivity trade-off of Janus kinase 2 (JAK2) inhibitors.
AID1639174Inhibition of human recombinant JAK1 (852 to 1142 residues) by Z-Lyte assay2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
The impact of binding site waters on the activity/selectivity trade-off of Janus kinase 2 (JAK2) inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (69)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's33 (47.83)24.3611
2020's36 (52.17)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 43.37

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 Index43.37 (24.57)
Research Supply Index4.45 (2.92)
Research Growth Index4.74 (4.65)
Search Engine Demand Index128.80 (26.88)
Search Engine Supply Index3.97 (0.95)

This Compound (43.37)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials16 (23.19%)5.53%
Reviews3 (4.35%)6.00%
Case Studies10 (14.49%)4.05%
Observational0 (0.00%)0.25%
Other40 (57.97%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
azathioprine
Azathioprine: An immunosuppressive agent used in combination with cyclophosphamide and hydroxychloroquine in the treatment of rheumatoid arthritis. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance has been listed as a known carcinogen. (Merck Index, 11th ed). azathioprine : A thiopurine that is 6-mercaptopurine in which the mercapto hydrogen is replaced by a 1-methyl-4-nitroimidazol-5-yl group. It is a prodrug for mercaptopurine and is used as an immunosuppressant, prescribed for the treatment of inflammatory conditions and after organ transplantation and also for treatment of Crohn's didease and MS.		7.920aryl sulfide;
C-nitro compound;
imidazoles;
thiopurine		antimetabolite;
antineoplastic agent;
carcinogenic agent;
DNA synthesis inhibitor;
hepatotoxic agent;
immunosuppressive agent;
prodrug
chloroquine
Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.		2.1110aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
ketoconazole
1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.		2.1110dichlorobenzene;
dioxolane;
ether;
imidazoles;
N-acylpiperazine;
N-arylpiperazine
ketotifen
Ketotifen: A cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. It has been proposed for the treatment of asthma, rhinitis, skin allergies, and anaphylaxis.. ketotifen : An organic heterotricyclic compound that is 4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one which is substituted at position 4 by a 1-methylpiperidin-4-ylidene group. A blocker of histamine H1 receptors with a stabilising action on mast cells, it is used (usually as its hydrogen fumarate salt) for the treatment of asthma, where it may take several weeks to exert its full effect.		2.1110cyclic ketone;
olefinic compound;
organic heterotricyclic compound;
organosulfur heterocyclic compound;
piperidines;
tertiary amino compound		anti-asthmatic drug;
H1-receptor antagonist
potassium iodide
Potassium Iodide: An inorganic compound that is used as a source of iodine in thyrotoxic crisis and in the preparation of thyrotoxic patients for thyroidectomy. (From Dorland, 27th ed). potassium iodide : A metal iodide salt with a K(+) counterion. It is a scavenger of hydroxyl radicals.		2.610potassium saltexpectorant;
radical scavenger
prednisolone
Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.. prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone.		5.766311beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antineoplastic agent;
drug metabolite;
environmental contaminant;
immunosuppressive agent;
xenobiotic
methylprednisolone
Methylprednisolone: A PREDNISOLONE derivative with similar anti-inflammatory action.. 6alpha-methylprednisolone : The 6alpha-stereoisomer of 6-methylprednisolone.		8.59116-methylprednisolone;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antiemetic;
environmental contaminant;
neuroprotective agent;
xenobiotic
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.		6.0440pyrrole;
secondary amine
isoxazoles
Isoxazoles: Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions.. isoxazole : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing three carbon atoms and an oxygen and nitrogen atom adjacent to each other. It is the parent of the class of isoxazoles.. isoxazoles : Oxazoles in which the N and O atoms are adjacent.		2.1110isoxazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
toluene 2,4-diisocyanate
Toluene 2,4-Diisocyanate: Skin irritant and allergen used in the manufacture of polyurethane foams and other elastomers.. toluene 2,4-diisocyanate : A toluene meta-diisocyanate in which the isocyanato groups are at positions 2 and 4 relative to the methyl group on the benzene ring.		2.1110toluene meta-diisocyanateallergen;
hapten
hydrocortisone aceponate
hydrocortisone aceponate: RN given refers to (11beta)-isomers; structure given in first source		8.711corticosteroid hormone
maleic acid
maleic acid: RN given refers to parent cpd(Z)-isomer which is maleic acid; all RR's given refer to (Z)-isomer; (E)-isomer is fumaric acid. maleic acid : A butenedioic acid in which the double bond has cis- (Z)-configuration.		2.4110butenedioic acidalgal metabolite;
mouse metabolite;
plant metabolite
tacrolimus
Tacrolimus: A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.. tacrolimus (anhydrous) : A macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis.		8.5911macrolide lactambacterial metabolite;
immunosuppressive agent
bay 11-7082
(E)-3-tosylacrylonitrile : A nitrile that is acrylonitrile in which the hydrogen located beta,trans to the cyano group is replaced by a tosyl group. It is an inhibitor of cytokine-induced IkappaB-alpha phosphorylation in cells.		2.610nitrile;
sulfone		apoptosis inducer;
EC 2.7.11.10 (IkappaB kinase) inhibitor;
EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor;
non-steroidal anti-inflammatory drug;
platelet aggregation inhibitor
norketotifen
norketotifen: Ketotifen is an antimalarial prodrug of norketotifen with blood schizonticidal and liver-stage efficacy; structure in first source		2.1110organosulfur heterocyclic compound
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.		6.0440N-acylpiperidine;
nitrile;
pyrrolopyrimidine;
tertiary amino compound		antirheumatic drug;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
incb-018424
[no description available]		5.8530nitrile;
pyrazoles;
pyrrolopyrimidine		antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
afoxolaner
afoxolaner: an oral, chewable insecticide-acaricide to control fleas and ticks in dogs		2.1110
baricitinib
[no description available]		5.5520azetidines;
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.		6.0440
mobic
Meloxicam: A benzothiazine and thiazole derivative that acts as a NSAID and cyclooxygenase-2 (COX-2) inhibitor. It is used in the treatment of RHEUMATOID ARTHRITIS; OSTEOARTHRITIS; and ANKYLOSING SPONDYLITIS.. meloxicam : A benzothiazine that is piroxicam in which the pyridin-2-yl group is replaced by a 5-methyl-1,3-thiazol-2-yl group. A non-steroidal anti-inflammatory drug and selective inhibitor of COX-2, it is used particularly for the management of rheumatoid arthritis.		2.41101,3-thiazoles;
benzothiazine;
monocarboxylic acid amide		analgesic;
antirheumatic drug;
cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
transforming growth factor beta
Transforming Growth Factor beta: A factor synthesized in a wide variety of tissues. It acts synergistically with TGF-alpha in inducing phenotypic transformation and can also act as a negative autocrine growth factor. TGF-beta has a potential role in embryonal development, cellular differentiation, hormone secretion, and immune function. TGF-beta is found mostly as homodimer forms of separate gene products TGF-beta1, TGF-beta2 or TGF-beta3. Heterodimers composed of TGF-beta1 and 2 (TGF-beta1.2) or of TGF-beta2 and 3 (TGF-beta2.3) have been isolated. The TGF-beta proteins are synthesized as precursor proteins.		2.610
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).		10.5672
ConditionIndicatedRelationship StrengthStudiesTrials
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.8330
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Eczema, Atopic
[description not available]		013.013911
Canine Diseases
[description not available]		010.494613
Cat Diseases
Diseases of the domestic cat (Felis catus or F. domesticus). This term does not include diseases of the so-called big cats such as CHEETAHS; LIONS; tigers, cougars, panthers, leopards, and other Felidae for which the heading CARNIVORA is used.		04.961
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.		013.013911
Pemphigus Foliaceus
[description not available]		03.1130
Pemphigus
Group of chronic blistering diseases characterized histologically by ACANTHOLYSIS and blister formation within the EPIDERMIS.		03.1130
Allergic Reaction
[description not available]		04.8132
Hypersensitivity
Altered reactivity to an antigen, which can result in pathologic reactions upon subsequent exposure to that particular antigen.		09.8132
Itching
[description not available]		07.39148
Pruritus
An intense itching sensation that produces the urge to rub or scratch the skin to obtain relief.		07.39148
Toxoplasmosis, Animal
Acquired infection of non-human animals by organisms of the genus TOXOPLASMA.		02.4110
Lupus Erythematosus, Cutaneous, Subacute
[description not available]		02.610
Lupus Erythematosus, Chronic Cutaneous
[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
Lupus Erythematosus, Discoid
A chronic form of cutaneous lupus erythematosus (LUPUS ERYTHEMATOSUS, CUTANEOUS) in which the skin lesions mimic those of the systemic form but in which systemic signs are rare. It is characterized by the presence of discoid skin plaques showing varying degrees of edema, erythema, scaliness, follicular plugging, and skin atrophy. Lesions are surrounded by an elevated erythematous border. The condition typically involves the face and scalp, but widespread dissemination may occur.		02.610
Skin Ulcer
An ULCER of the skin and underlying tissues.		02.7620
Anal Fistula
[description not available]		07.610
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		02.610
Infection, Postoperative Wound
[description not available]		02.610
Anemia
A reduction in the number of circulating ERYTHROCYTES or in the quantity of HEMOGLOBIN.		07.610
Disbacteriosis
[description not available]		02.610
Dermatoses
[description not available]		07.4670
Erythema Multiforme
A skin and mucous membrane disease characterized by an eruption of macules, papules, nodules, vesicles, and/or bullae with characteristic bull's-eye lesions usually occurring on the dorsal aspect of the hands and forearms.		07.2510
Skin Diseases
Diseases involving the DERMIS or EPIDERMIS.		07.4670
Benign Neoplasms
[description not available]		02.2510
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.		02.2510
Mange, Sarcoptic
[description not available]		02.2510
Scabies
A contagious cutaneous inflammation caused by the bite of the mite SARCOPTES SCABIEI. It is characterized by pruritic papular eruptions and burrows and affects primarily the axillae, elbows, wrists, and genitalia, although it can spread to cover the entire body.		02.2510
Cancer of Skin
[description not available]		02.3110
Cutaneous T-Cell Lymphoma
[description not available]		02.3110
Skin Neoplasms
Tumors or cancer of the SKIN.		02.3110
Lymphoma, T-Cell, Cutaneous
A group of lymphomas exhibiting clonal expansion of malignant T-lymphocytes arrested at varying stages of differentiation as well as malignant infiltration of the skin. MYCOSIS FUNGOIDES; SEZARY SYNDROME; LYMPHOMATOID PAPULOSIS; and PRIMARY CUTANEOUS ANAPLASTIC LARGE CELL LYMPHOMA are the best characterized of these disorders.		02.3110
Blue-Eared Pig Disease
[description not available]		02.1510
Co-infection
[description not available]		02.1510
Haemophilus Infections
Infections with bacteria of the genus HAEMOPHILUS.		02.1510
Asymptomatic Colonization
[description not available]		02.1510
Bacteriuria
The presence of bacteria in the urine which is normally bacteria-free. These bacteria are from the URINARY TRACT and are not contaminants of the surrounding tissues. Bacteriuria can be symptomatic or asymptomatic. Significant bacteriuria is an indicator of urinary tract infection.		07.1510
Urinary Tract Infections
Inflammatory responses of the epithelium of the URINARY TRACT to microbial invasions. They are often bacterial infections with associated BACTERIURIA and PYURIA.		02.1510
Autoimmune Disease
[description not available]		02.5820
Bleb
[description not available]		02.1510
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.		02.5820
Alopecia Cicatrisata
[description not available]		02.1510
Alopecia
Absence of hair from areas where it is normally present.		07.1510
Keratoconjunctivitis Sicca
Drying and inflammation of the conjunctiva as a result of insufficient lacrimal secretion. When found in association with XEROSTOMIA and polyarthritis, it is called SJOGREN'S SYNDROME.		08.5911
Cancer of Liver
[description not available]		02.110
Cancer of Pancreas
[description not available]		02.110
Liver Neoplasms
Tumors or cancer of the LIVER.		02.110
Pancreatic Neoplasms
Tumors or cancer of the PANCREAS. Depending on the types of ISLET CELLS present in the tumors, various hormones can be secreted: GLUCAGON from PANCREATIC ALPHA CELLS; INSULIN from PANCREATIC BETA CELLS; and SOMATOSTATIN from the SOMATOSTATIN-SECRETING CELLS. Most are malignant except the insulin-producing tumors (INSULINOMA).		02.110
Dermatitis
Any inflammation of the skin.		08.4711
Allergic Contact Dermatitis
[description not available]		03.921
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.		03.921
Innate Inflammatory Response
[description not available]		02.1110
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.		02.1110
Aggression
Behavior which may be manifested by destructive and attacking action which is verbal or physical, by covert attitudes of hostility or by obstructionism.		07.1110
Alopecia Circumscripta
[description not available]		06.9640
Palmoplantaris Pustulosis
[description not available]		06.9640
Alopecia Areata
Loss of scalp and body hair involving microscopically inflammatory patchy areas.		06.9640
Psoriasis
A common genetically determined, chronic, inflammatory skin disease characterized by rounded erythematous, dry, scaling patches. The lesions have a predilection for nails, scalp, genitalia, extensor surfaces, and the lumbosacral region. Accelerated epidermopoiesis is considered to be the fundamental pathologic feature in psoriasis.		06.9640
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.		06.9640