Target Information

Target General Infomation
Target ID
T65864
Former ID
TTDC00201
Target Name
Mitogen-activated protein kinase 14
Gene Name
MAPK14
Synonyms
CRK1; CSAID binding protein; CSBP; Cytokine suppressive anti-inflammatory drug binding protein; MAP kinase MXI2; MAP kinase p38; MAP kinase p38alpha; MAX-interacting protein 2; Mitogen-activated protein kinase p38; Mitogen-activated protein kinase p38 alpha; P38 Mitogen-activatedprotein kinase alpha; P38 mitogen activatedprotein kinase; SAPK2A; MAPK14
Target Type
Clinical Trial
Disease Acute lung injury; Acute respiratory distress syndrome [ICD9: 518.5, 518.82; ICD10: J80]
Acute coronary syndrome [ICD9: 444; ICD10: I74]
Arthritis [ICD9: 710-719; ICD10: M00-M25]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Coronary artery disease [ICD9: 410-414, 429.2; ICD10: I20-I25]
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47]
Diabetic retinopathy [ICD9: 250.5; ICD10: H36, E10.3, E11.3, E13.3]
Inflammatory bowel disease [ICD9: 555, 556; ICD10: K50, K51]
Inflammatory disorder [ICD code not available]
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Psoriasis [ICD9: 696; ICD10: L40]
Rheumatold arthritis; Coronary artery disease [ICD9: 410-414, 429.2, 710-719, 714; ICD10: I20-I25, M00-M25, M05-M06]
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06]
Function
Responds to activation by environmental stress, pro- inflammatory cytokines and lipopolysaccharide (lps) by phosphorylating a number of transcription factors, such as elk-1 and atf2 and several downstream kinases, such asmapkapk2 and mapkapk5.
BioChemical Class
Kinase
Target Validation
T65864
UniProt ID
Q16539
EC Number
EC 2.7.11.24
Sequence
MSQERPTFYRQELNKTIWEVPERYQNLSPVGSGAYGSVCAAFDTKTGLRVAVKKLSRPFQ
SIIHAKRTYRELRLLKHMKHENVIGLLDVFTPARSLEEFNDVYLVTHLMGADLNNIVKCQ
KLTDDHVQFLIYQILRGLKYIHSADIIHRDLKPSNLAVNEDCELKILDFGLARHTDDEMT
GYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLTGRTLFPGTDHIDQLKLILRLVG
TPGAELLKKISSESARNYIQSLTQMPKMNFANVFIGANPLAVDLLEKMLVLDSDKRITAA
QALAHAYFAQYHDPDDEPVADPYDQSFESRDLLIDEWKSLTYDEVISFVPPPLDQEEMES
Drugs and Mode of Action
Drug(s) Losmapimod Drug Info Phase 3 Acute coronary syndrome [542778], [548217]
VX-702 Drug Info Phase 2a Rheumatold arthritis; Coronary artery disease [536651], [541308]
CI-1040 Drug Info Phase 2 Discovery agent [521505], [541019]
CNI-1493 Drug Info Phase 2 Inflammatory bowel disease [521518]
Dilmapimod Drug Info Phase 2 Acute lung injury; Acute respiratory distress syndrome [521803], [542759]
VX-702 Drug Info Phase 2 Coronary artery disease [530740], [537274], [541308]
GSK610677 Drug Info Phase 1 Chronic obstructive pulmonary disease [548758]
VX-702 Drug Info Phase 1 Inflammatory disorder [536651], [541308]
FR167653 Drug Info Preclinical Discovery agent [546408]
PAMAPIMOD Drug Info Discontinued in Phase 2 Rheumatoid arthritis [547702]
R-1487 Drug Info Discontinued in Phase 1 Rheumatoid arthritis [547528]
SB 235699 Drug Info Discontinued in Phase 1 Psoriasis [547031]
SB-242235 Drug Info Discontinued in Phase 1 Arthritis [546871]
SB 203580 Drug Info Terminated Discovery agent [540732], [546259]
SB220025 Drug Info Terminated Arthritis [541295], [546829]
Inhibitor (5-amino-1-phenyl-1H-pyrazol-4-yl)phenylmethanone Drug Info [528056]
2-Chlorophenol Drug Info [551393]
3-(1-NAPHTHYLMETHOXY)PYRIDIN-2-AMINE Drug Info [551374]
3-(Benzyloxy)Pyridin-2-Amine Drug Info [551393]
4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole Drug Info [527308]
4-(2-Ethyl-4-m-tolyl-thiazol-5-yl)-pyridine Drug Info [527737]
4-PHENOXY-N-(PYRIDIN-2-YLMETHYL)BENZAMIDE Drug Info [551374]
4-Phenylsulfanyl-7H-pyrrolo[2,3-d]pyrimidine Drug Info [527421]
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol Drug Info [528490]
4-[3-(4-FLUOROPHENYL)-1H-PYRAZOL-4-YL]PYRIDINE Drug Info [551374]
6-(4-Fluoro-phenylsulfanyl)-9H-purine Drug Info [527421]
6-Benzylsulfanyl-9H-purine Drug Info [527421]
6-o-tolylquinazolin-2-amine Drug Info [528429]
6-Phenylsulfanyl-9H-purine Drug Info [527421]
9-(4-Fluoro-benzyl)-6-phenylsulfanyl-9H-purine Drug Info [527421]
9-Benzyl-6-(4-fluoro-phenylsulfanyl)-9H-purine Drug Info [527421]
9-Benzyl-6-phenylsulfanyl-9H-purine Drug Info [527421]
B-Octylglucoside Drug Info [551393]
BISINDOLYLMALEIMIDE IX Drug Info [525872]
CI-1040 Drug Info [525872]
CNI-1493 Drug Info [535631]
compound 12 Drug Info [531881]
Dihydro-quinolinone Drug Info [530753]
Dilmapimod Drug Info [550963]
DP-802 Drug Info [543431]
FR167653 Drug Info [535310], [535798]
GF-109203 Drug Info [525872]
GSK-280 Drug Info [543431]
GSK610677 Drug Info [550963]
GW-788388 Drug Info [528108]
IN-1130 Drug Info [529552]
IN-1166 Drug Info [529552]
KN-62 Drug Info [525872]
KT-5720 Drug Info [525872]
L-779450 Drug Info [527836]
Losmapimod Drug Info [550963]
ML-3163 Drug Info [526355]
ML-3375 Drug Info [526668]
ML-3403 Drug Info [526668]
N-(3-(trifluoromethoxy)benzyl)-4-phenoxybenzamide Drug Info [527747]
N-(3-(trifluoromethyl)benzyl)-4-phenoxybenzamide Drug Info [527747]
N-(4-(trifluoromethyl)benzyl)-4-phenoxybenzamide Drug Info [527747]
N-(4-fluorobenzyl)-N-(pyridin-4-yl)-2-naphthamide Drug Info [530812]
N-(4-methyl-benzyl)-4-phenoxy-benzamide Drug Info [527747]
P38 MAP kinase alpha inhibitors Drug Info [543431]
PAMAPIMOD Drug Info [530550]
PD-0166326 Drug Info [530497]
PD-0173956 Drug Info [530497]
PHA-666859 Drug Info [543431]
Phenyl-(3-phenyl-1H-indazol-6-yl)-amine Drug Info [527722]
R-1487 Drug Info [531380]
RO-316233 Drug Info [525872]
Ro-3201195 Drug Info [529522]
RWJ-68354 Drug Info [526530]
SB 202190 Drug Info [535852]
SB 203580 Drug Info [535215], [536549]
SB 235699 Drug Info [535353]
SB-216995 Drug Info [530753]
SB-218655 Drug Info [530753]
SB-227931 Drug Info [527732]
SB-242235 Drug Info [529583]
SB220025 Drug Info [551393]
Small molecule 34 Drug Info [551393]
STAUROSPORINONE Drug Info [525872]
Triazolopyridine Drug Info [551374]
TYRPHOSTIN AG-1478 Drug Info [527230]
UCB-1277763 Drug Info [543431]
Vertex 745 (VX745) Drug Info [535353]
VK-19911 Drug Info [526904]
ZM-336372 Drug Info [527229]
Modulator Talmapimod Drug Info [533170]
VX-702 Drug Info [530740], [537274]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway MAPK signaling pathway
Rap1 signaling pathway
FoxO signaling pathway
Sphingolipid signaling pathway
Adrenergic signaling in cardiomyocytes
VEGF signaling pathway
Osteoclast differentiation
Signaling pathways regulating pluripotency of stem cells
Platelet activation
Toll-like receptor signaling pathway
NOD-like receptor signaling pathway
RIG-I-like receptor signaling pathway
T cell receptor signaling pathway
Fc epsilon RI signaling pathway
TNF signaling pathway
Leukocyte transendothelial migration
Neurotrophin signaling pathway
Retrograde endocannabinoid signaling
Dopaminergic synapse
Inflammatory mediator regulation of TRP channels
GnRH signaling pathway
Progesterone-mediated oocyte maturation
Prolactin signaling pathway
Amyotrophic lateral sclerosis (ALS)
Epithelial cell signaling in Helicobacter pylori infection
Shigellosis
Salmonella infection
Pertussis
Leishmaniasis
Chagas disease (American trypanosomiasis)
Toxoplasmosis
Tuberculosis
Hepatitis C
Influenza A
Epstein-Barr virus infection
Proteoglycans in cancer
NetPath Pathway IL5 Signaling Pathway
FSH Signaling Pathway
TCR Signaling Pathway
PANTHER Pathway Alzheimer disease-amyloid secretase pathway
Angiogenesis
B cell activation
EGF receptor signaling pathway
FGF signaling pathway
Interferon-gamma signaling pathway
Oxidative stress response
Parkinson disease
TGF-beta signaling pathway
Toll receptor signaling pathway
VEGF signaling pathway
Ras Pathway
p53 pathway feedback loops 2
p38 MAPK pathway
CCKR signaling map ST
Pathway Interaction Database Endothelins
BCR signaling pathway
p73 transcription factor network
p38 MAPK signaling pathway
Atypical NF-kappaB pathway
IL4-mediated signaling events
CD40/CD40L signaling
IL12-mediated signaling events
Regulation of p38-alpha and p38-beta
CDC42 signaling events
Angiopoietin receptor Tie2-mediated signaling
FAS (CD95) signaling pathway
Thromboxane A2 receptor signaling
Role of Calcineurin-dependent NFAT signaling in lymphocytes
Glucocorticoid receptor regulatory network
IL2-mediated signaling events
Rapid glucocorticoid signaling
Regulation of Androgen receptor activity
ATF-2 transcription factor network
IL6-mediated signaling events
p38 signaling mediated by MAPKAP kinases
Retinoic acid receptors-mediated signaling
CXCR3-mediated signaling events
Signaling mediated by p38-alpha and p38-beta
EPO signaling pathway
Signaling events mediated by VEGFR1 and VEGFR2
p53 pathway
S1P2 pathway
Trk receptor signaling mediated by the MAPK pathway
VEGFR3 signaling in lymphatic endothelium
FGF signaling pathway
RAC1 signaling pathway
Regulation of retinoblastoma protein
PathWhiz Pathway Fc Epsilon Receptor I Signaling in Mast Cells
Reactome NOD1/2 Signaling Pathway
p38MAPK events
ERK/MAPK targets
Activation of PPARGC1A (PGC-1alpha) by phosphorylation
Oxidative Stress Induced Senescence
CDO in myogenesis
DSCAM interactions
ADP signalling through P2Y purinoceptor 1
Platelet sensitization by LDL
VEGFA-VEGFR2 Pathway
activated TAK1 mediates p38 MAPK activation
Activation of the AP-1 family of transcription factors
KSRP (KHSRP) binds and destabilizes mRNA
WikiPathways Toll-like receptor signaling pathway
Monoamine Transport
Serotonin HTR1 Group and FOS Pathway
TCR Signaling Pathway
Senescence and Autophagy in Cancer
Interferon type I signaling pathways
Insulin Signaling
EGF/EGFR Signaling Pathway
MAPK Cascade
Oxidative Stress
p38 MAPK Signaling Pathway
IL-4 Signaling Pathway
MAPK Signaling Pathway
TGF beta Signaling Pathway
Kit receptor signaling pathway
Cardiac Hypertrophic Response
MAP kinase activation in TLR cascade
Regulation of mRNA Stability by Proteins that Bind AU-rich Elements
Nanoparticle-mediated activation of receptor signaling
Structural Pathway of Interleukin 1 (IL-1)
JAK/STAT
Amyotrophic lateral sclerosis (ALS)
Alpha 6 Beta 4 signaling pathway
Cardiac Progenitor Differentiation
BDNF signaling pathway
Integrated Pancreatic Cancer Pathway
Oncostatin M Signaling Pathway
Parkinsons Disease Pathway
Corticotropin-releasing hormone
AGE/RAGE pathway
B Cell Receptor Signaling Pathway
Prostate Cancer
TSLP Signaling Pathway
TWEAK Signaling Pathway
FSH signaling pathway
Leptin signaling pathway
RANKL/RANK Signaling Pathway
miR-targeted genes in muscle cell - TarBase
miR-targeted genes in lymphocytes - TarBase
miR-targeted genes in leukocytes - TarBase
miR-targeted genes in epithelium - TarBase
IL-1 signaling pathway
Signal amplification
Platelet homeostasis
NGF signalling via TRKA from the plasma membrane
Myogenesis
DSCAM interactions
MicroRNAs in cardiomyocyte hypertrophy
Angiogenesis
Physiological and Pathological Hypertrophy of the Heart
Regulation of toll-like receptor signaling pathway
References
Ref 521505ClinicalTrials.gov (NCT00033384) CI-1040 in Treating Patients With Advanced Breast, Colon, Pancreatic, or Non-Small Cell Lung Cancer. U.S. National Institutes of Health.
Ref 521518ClinicalTrials.gov (NCT00038766) CNI-1493 for Treatment of Moderate to Severe Crohn's Disease. U.S. National Institutes of Health.
Ref 521803ClinicalTrials.gov (NCT00291902) A Pharmacokinetic Study Of SB-681323 In Subjects With Coronary Heart Disease Undergoing Percutaneous Intervention. U.S. National Institutes of Health.
Ref 530740Comparative renal excretion of VX-702, a novel p38 MAPK inhibitor, and methotrexate in the perfused rat kidney model. Drug Dev Ind Pharm. 2010 Mar;36(3):315-22.
Ref 536651Emerging drugs for rheumatoid arthritis. Expert Opin Emerg Drugs. 2008 Mar;13(1):175-96.
Ref 537274Efficacy, pharmacodynamics, and safety of VX-702, a novel p38 MAPK inhibitor, in rheumatoid arthritis: results of two randomized, double-blind, placebo-controlled clinical studies. Arthritis Rheum. 2009 May;60(5):1232-41.
Ref 540732(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5269).
Ref 541019(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5676).
Ref 541295(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6038).
Ref 541308(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6059).
Ref 542759(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7815).
Ref 542778(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7835).
Ref 546259Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007147)
Ref 546408Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007964)
Ref 546829Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010505)
Ref 546871Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010787)
Ref 547031Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012315)
Ref 547528Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017105)
Ref 547702Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018538)
Ref 548217Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023191)
Ref 548758Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028430)
Ref 525872Biochem J. 2000 Oct 1;351(Pt 1):95-105.Specificity and mechanism of action of some commonly used protein kinase inhibitors.
Ref 526355J Med Chem. 2002 Jun 20;45(13):2733-40.From imidazoles to pyrimidines: new inhibitors of cytokine release.
Ref 526530Bioorg Med Chem Lett. 2003 Feb 10;13(3):347-50.Imidazopyrimidines, potent inhibitors of p38 MAP kinase.
Ref 526668J Med Chem. 2003 Jul 17;46(15):3230-44.Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes.
Ref 526904J Med Chem. 2003 Dec 18;46(26):5651-62.Synthesis and structure-activity relationship of aminobenzophenones. A novel class of p38 MAP kinase inhibitors with high antiinflammatory activity.
Ref 527229Bioorg Med Chem Lett. 2004 Nov 1;14(21):5383-7.A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis.
Ref 527230Bioorg Med Chem Lett. 2004 Nov 1;14(21):5389-94.Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase.
Ref 527308J Med Chem. 2004 Dec 2;47(25):6239-47.Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole.
Ref 527421J Med Chem. 2005 Feb 10;48(3):710-22.Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors.
Ref 527722Bioorg Med Chem Lett. 2005 Nov 15;15(22):5095-9.Design and synthesis of 6-anilinoindazoles as selective inhibitors of c-Jun N-terminal kinase-3.
Ref 527732Bioorg Med Chem Lett. 2005 Nov 1;15(21):4666-70.The neuroprotective action of JNK3 inhibitors based on the 6,7-dihydro-5H-pyrrolo[1,2-a]imidazole scaffold.
Ref 527737J Med Chem. 2005 Sep 22;48(19):5966-79.Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent.
Ref 527747Bioorg Med Chem Lett. 2005 Dec 1;15(23):5274-9. Epub 2005 Sep 19.Two classes of p38alpha MAP kinase inhibitors having a common diphenylether core but exhibiting divergent binding modes.
Ref 527836Bioorg Med Chem Lett. 2006 Jan 15;16(2):378-81. Epub 2005 Nov 2.The identification of potent and selective imidazole-based inhibitors of B-Raf kinase.
Ref 528056J Med Chem. 2006 Mar 9;49(5):1562-75.Discovery of S-[5-amino-1-(4-fluorophenyl)-1H-pyrazol-4-yl]-[3-(2,3-dihydroxypropoxy)phenyl]methanone (RO3201195), an orally bioavailable and highly selective inhibitor of p38 MAP kinase.
Ref 528108J Med Chem. 2006 Apr 6;49(7):2210-21.Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
Ref 528429J Med Chem. 2006 Sep 21;49(19):5671-86.Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.
Ref 528490J Med Chem. 2006 Nov 2;49(22):6500-9.4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
Ref 529522Bioorg Med Chem Lett. 2008 Jul 1;18(13):3745-8. Epub 2008 May 16.Microwave-assisted synthesis of 5-aminopyrazol-4-yl ketones and the p38(MAPK) inhibitor RO3201195 for study in Werner syndrome cells.
Ref 529552Bioorg Med Chem Lett. 2008 Jul 15;18(14):4006-10. Epub 2008 Jun 6.Synthesis and biological evaluation of trisubstituted imidazole derivatives as inhibitors of p38alpha mitogen-activated protein kinase.
Ref 529583Bioorg Med Chem Lett. 2008 Aug 1;18(15):4433-7. Epub 2008 Jun 12.Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.
Ref 530497Bioorg Med Chem Lett. 2009 Dec 15;19(24):6872-6. Epub 2009 Oct 23.Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors.
Ref 530550J Med Chem. 2010 Mar 25;53(6):2345-53.Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
Ref 530740Comparative renal excretion of VX-702, a novel p38 MAPK inhibitor, and methotrexate in the perfused rat kidney model. Drug Dev Ind Pharm. 2010 Mar;36(3):315-22.
Ref 530753Bioorg Med Chem. 2010 Mar 15;18(6):2204-18. Epub 2010 Feb 8.In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.
Ref 530812Bioorg Med Chem Lett. 2010 Apr 15;20(8):2560-3. Epub 2010 Mar 2.Amide-based inhibitors of p38alpha MAP kinase. Part 2: design, synthesis and SAR of potent N-pyrimidyl amides.
Ref 531380Discovery 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.
Ref 531881Novel triazolopyridylbenzamides as potent and selective p38alpha inhibitors. Bioorg Med Chem Lett. 2012 May 15;22(10):3431-6.
Ref 533170p38 MAP Kinase Inhibition Reduces Propionibacterium acnes-Induced Inflammation in Vitro. Dermatol Ther (Heidelb). 2015 Mar;5(1):53-66.
Ref 535215The p38 mitogen-activated protein kinase pathway plays a critical role in thrombin-induced endothelial chemokine production and leukocyte recruitment. Blood. 2001 Aug 1;98(3):667-73.
Ref 535310Involvement of p38 mitogen-activated protein kinase followed by chemokine expression in crescentic glomerulonephritis. Am J Kidney Dis. 2001 Dec;38(6):1169-77.
Ref 535353Pharmacological inhibitors of MAPK pathways. Trends Pharmacol Sci. 2002 Jan;23(1):40-5.
Ref 535631From extracellular to intracellular targets, inhibiting MAP kinases in treatment of Crohn's disease. Ann N Y Acad Sci. 2002 Nov;973:349-58.
Ref 535798Prevention of the onset and progression of collagen-induced arthritis in rats by the potent p38 mitogen-activated protein kinase inhibitor FR167653. Arthritis Rheum. 2003 Sep;48(9):2670-81.
Ref 535852Inhibition of p38 MAPK decreases myocardial TNF-alpha expression and improves myocardial function and survival in endotoxemia. Cardiovasc Res. 2003 Oct 1;59(4):893-900.
Ref 536549Privileged structures: a useful concept for the rational design of new lead drug candidates. Mini Rev Med Chem. 2007 Nov;7(11):1108-19.
Ref 537274Efficacy, pharmacodynamics, and safety of VX-702, a novel p38 MAPK inhibitor, in rheumatoid arthritis: results of two randomized, double-blind, placebo-controlled clinical studies. Arthritis Rheum. 2009 May;60(5):1232-41.
Ref 543431(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1499).
Ref 550963Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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