| Drug General Information |
| Drug ID |
D04YHW
|
| Former ID |
DIB009978
|
| Drug Name |
R-1487
|
| Drug Type |
Small molecular drug
|
| Indication |
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10:M05-M06]
|
Discontinued in Phase 1 |
[1]
|
|---|
| Company |
Roche Holding AG
|
| Structure |
|
Download
2D MOL
3D MOL
|
| Formula |
C19H18F2N4O3
|
| Canonical SMILES |
c12c(cc(c(=O)n2C)Oc2c(cc(cc2)F)F)cnc(n1)NC1CCOCC1
|
| PubChem Compound ID |
|
| Target and Pathway |
| Target(s) |
Mitogen-activated protein kinase 14 |
Target Info |
Inhibitor |
[2]
|
|---|
|
KEGG Pathway
|
MAPK signaling pathway
|
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Rap1 signaling pathway
|
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FoxO signaling pathway
|
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Sphingolipid signaling pathway
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Adrenergic signaling in cardiomyocytes
|
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VEGF signaling pathway
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Osteoclast differentiation
|
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Signaling pathways regulating pluripotency of stem cells
|
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Platelet activation
|
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Toll-like receptor signaling pathway
|
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NOD-like receptor signaling pathway
|
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RIG-I-like receptor signaling pathway
|
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T cell receptor signaling pathway
|
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Fc epsilon RI signaling pathway
|
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TNF signaling pathway
|
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Leukocyte transendothelial migration
|
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Neurotrophin signaling pathway
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Retrograde endocannabinoid signaling
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Dopaminergic synapse
|
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Inflammatory mediator regulation of TRP channels
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GnRH signaling pathway
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Progesterone-mediated oocyte maturation
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Prolactin signaling pathway
|
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Amyotrophic lateral sclerosis (ALS)
|
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Epithelial cell signaling in Helicobacter pylori infection
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Shigellosis
|
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Salmonella infection
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Pertussis
|
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Leishmaniasis
|
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Chagas disease (American trypanosomiasis)
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Toxoplasmosis
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Tuberculosis
|
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Hepatitis C
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Influenza A
|
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Epstein-Barr virus infection
|
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Proteoglycans in cancer
|
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NetPath Pathway
|
IL5 Signaling Pathway
|
|
FSH Signaling Pathway
|
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TCR Signaling Pathway
|
|
PANTHER Pathway
|
Alzheimer disease-amyloid secretase pathway
|
|
Angiogenesis
|
|
B cell activation
|
|
EGF receptor signaling pathway
|
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FGF signaling pathway
|
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Interferon-gamma signaling pathway
|
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Oxidative stress response
|
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Parkinson disease
|
|
TGF-beta signaling pathway
|
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Toll receptor signaling pathway
|
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VEGF signaling pathway
|
|
Ras Pathway
|
|
p53 pathway feedback loops 2
|
|
p38 MAPK pathway
|
|
CCKR signaling map ST
|
|
Pathway Interaction Database
|
Endothelins
|
|
BCR signaling pathway
|
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p73 transcription factor network
|
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p38 MAPK signaling pathway
|
|
Atypical NF-kappaB pathway
|
|
IL4-mediated signaling events
|
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CD40/CD40L signaling
|
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IL12-mediated signaling events
|
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Regulation of p38-alpha and p38-beta
|
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CDC42 signaling events
|
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Angiopoietin receptor Tie2-mediated signaling
|
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FAS (CD95) signaling pathway
|
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Thromboxane A2 receptor signaling
|
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Role of Calcineurin-dependent NFAT signaling in lymphocytes
|
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Glucocorticoid receptor regulatory network
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IL2-mediated signaling events
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Rapid glucocorticoid signaling
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Regulation of Androgen receptor activity
|
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ATF-2 transcription factor network
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IL6-mediated signaling events
|
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p38 signaling mediated by MAPKAP kinases
|
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Retinoic acid receptors-mediated signaling
|
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CXCR3-mediated signaling events
|
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Signaling mediated by p38-alpha and p38-beta
|
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EPO signaling pathway
|
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Signaling events mediated by VEGFR1 and VEGFR2
|
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p53 pathway
|
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S1P2 pathway
|
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Trk receptor signaling mediated by the MAPK pathway
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VEGFR3 signaling in lymphatic endothelium
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FGF signaling pathway
|
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RAC1 signaling pathway
|
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Regulation of retinoblastoma protein
|
|
PathWhiz Pathway
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Fc Epsilon Receptor I Signaling in Mast Cells
|
|
Reactome
|
NOD1/2 Signaling Pathway
|
|
p38MAPK events
|
|
ERK/MAPK targets
|
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Activation of PPARGC1A (PGC-1alpha) by phosphorylation
|
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Oxidative Stress Induced Senescence
|
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CDO in myogenesis
|
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DSCAM interactions
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ADP signalling through P2Y purinoceptor 1
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Platelet sensitization by LDL
|
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VEGFA-VEGFR2 Pathway
|
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activated TAK1 mediates p38 MAPK activation
|
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Activation of the AP-1 family of transcription factors
|
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KSRP (KHSRP) binds and destabilizes mRNA
|
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WikiPathways
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Toll-like receptor signaling pathway
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Monoamine Transport
|
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Serotonin HTR1 Group and FOS Pathway
|
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TCR Signaling Pathway
|
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Senescence and Autophagy in Cancer
|
|
Interferon type I signaling pathways
|
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Insulin Signaling
|
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EGF/EGFR Signaling Pathway
|
|
MAPK Cascade
|
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Oxidative Stress
|
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p38 MAPK Signaling Pathway
|
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IL-4 Signaling Pathway
|
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MAPK Signaling Pathway
|
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TGF beta Signaling Pathway
|
|
Kit receptor signaling pathway
|
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Cardiac Hypertrophic Response
|
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MAP kinase activation in TLR cascade
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Regulation of mRNA Stability by Proteins that Bind AU-rich Elements
|
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Nanoparticle-mediated activation of receptor signaling
|
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Structural Pathway of Interleukin 1 (IL-1)
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JAK/STAT
|
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Amyotrophic lateral sclerosis (ALS)
|
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Alpha 6 Beta 4 signaling pathway
|
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Cardiac Progenitor Differentiation
|
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BDNF signaling pathway
|
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Integrated Pancreatic Cancer Pathway
|
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Oncostatin M Signaling Pathway
|
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Parkinsons Disease Pathway
|
|
Corticotropin-releasing hormone
|
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AGE/RAGE pathway
|
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B Cell Receptor Signaling Pathway
|
|
Prostate Cancer
|
|
TSLP Signaling Pathway
|
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TWEAK Signaling Pathway
|
|
FSH signaling pathway
|
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Leptin signaling pathway
|
|
RANKL/RANK Signaling Pathway
|
|
miR-targeted genes in muscle cell - TarBase
|
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miR-targeted genes in lymphocytes - TarBase
|
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miR-targeted genes in leukocytes - TarBase
|
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miR-targeted genes in epithelium - TarBase
|
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IL-1 signaling pathway
|
|
Signal amplification
|
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Platelet homeostasis
|
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NGF signalling via TRKA from the plasma membrane
|
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Myogenesis
|
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DSCAM interactions
|
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MicroRNAs in cardiomyocyte hypertrophy
|
|
Angiogenesis
|
|
Physiological and Pathological Hypertrophy of the Heart
|
|
Regulation of toll-like receptor signaling pathway
|
| References |
| REF 1 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017105) |
|---|
| REF 2 | Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors of p38alpha mitogen-activated protein kinase. J Med Chem. 2011 Apr 14;54(7):2255-65. |
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