Target Information
Target General Infomation | |||||
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Target ID |
T65864
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Former ID |
TTDC00201
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Target Name |
Mitogen-activated protein kinase 14
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Gene Name |
MAPK14
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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
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Target Type |
Clinical Trial
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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] | |||||
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Coronary artery disease [ICD9: 410-414, 429.2; ICD10: I20-I25] | |||||
Diabetic retinopathy [ICD9: 250.5; ICD10: H36, E10.3, E11.3, E13.3] | |||||
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25] | |||||
Inflammatory bowel disease [ICD9: 555, 556; ICD10: K50, K51] | |||||
Inflammatory disorder [ICD code not available] | |||||
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
Psoriasis [ICD9: 696; ICD10: L40] | |||||
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06] | |||||
Rheumatold arthritis; Coronary artery disease [ICD9: 410-414, 429.2, 710-719, 714; ICD10: I20-I25, M00-M25, 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.
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BioChemical Class |
Kinase
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Target Validation |
T65864
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UniProt ID | |||||
EC Number |
EC 2.7.11.24
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Sequence |
MSQERPTFYRQELNKTIWEVPERYQNLSPVGSGAYGSVCAAFDTKTGLRVAVKKLSRPFQ
SIIHAKRTYRELRLLKHMKHENVIGLLDVFTPARSLEEFNDVYLVTHLMGADLNNIVKCQ KLTDDHVQFLIYQILRGLKYIHSADIIHRDLKPSNLAVNEDCELKILDFGLARHTDDEMT GYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLTGRTLFPGTDHIDQLKLILRLVG TPGAELLKKISSESARNYIQSLTQMPKMNFANVFIGANPLAVDLLEKMLVLDSDKRITAA QALAHAYFAQYHDPDDEPVADPYDQSFESRDLLIDEWKSLTYDEVISFVPPPLDQEEMES |
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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 521505 | ClinicalTrials.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 521518 | ClinicalTrials.gov (NCT00038766) CNI-1493 for Treatment of Moderate to Severe Crohn's Disease. U.S. National Institutes of Health. | ||||
Ref 521803 | ClinicalTrials.gov (NCT00291902) A Pharmacokinetic Study Of SB-681323 In Subjects With Coronary Heart Disease Undergoing Percutaneous Intervention. U.S. National Institutes of Health. | ||||
Ref 530740 | Comparative 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 537274 | Efficacy, 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 546259 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007147) | ||||
Ref 546408 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007964) | ||||
Ref 546829 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010505) | ||||
Ref 546871 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010787) | ||||
Ref 547031 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012315) | ||||
Ref 547528 | 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 547702 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018538) | ||||
Ref 525872 | Biochem J. 2000 Oct 1;351(Pt 1):95-105.Specificity and mechanism of action of some commonly used protein kinase inhibitors. | ||||
Ref 526355 | J Med Chem. 2002 Jun 20;45(13):2733-40.From imidazoles to pyrimidines: new inhibitors of cytokine release. | ||||
Ref 526530 | Bioorg Med Chem Lett. 2003 Feb 10;13(3):347-50.Imidazopyrimidines, potent inhibitors of p38 MAP kinase. | ||||
Ref 526668 | J 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 526904 | J 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 527229 | Bioorg 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 527230 | Bioorg Med Chem Lett. 2004 Nov 1;14(21):5389-94.Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase. | ||||
Ref 527308 | J Med Chem. 2004 Dec 2;47(25):6239-47.Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. | ||||
Ref 527421 | J Med Chem. 2005 Feb 10;48(3):710-22.Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors. | ||||
Ref 527722 | Bioorg 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 527732 | Bioorg 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 527737 | J 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 527747 | Bioorg 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 527836 | Bioorg 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 528056 | J 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 528108 | J 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 528429 | J 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 528490 | J 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 529522 | Bioorg 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 529552 | Bioorg 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 529583 | Bioorg 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 530497 | Bioorg 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 530550 | J Med Chem. 2010 Mar 25;53(6):2345-53.Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders. | ||||
Ref 530740 | Comparative 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 530753 | Bioorg 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 530812 | Bioorg 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 531380 | 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. | ||||
Ref 531881 | Novel triazolopyridylbenzamides as potent and selective p38alpha inhibitors. Bioorg Med Chem Lett. 2012 May 15;22(10):3431-6. | ||||
Ref 533170 | p38 MAP Kinase Inhibition Reduces Propionibacterium acnes-Induced Inflammation in Vitro. Dermatol Ther (Heidelb). 2015 Mar;5(1):53-66. | ||||
Ref 535215 | The 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 535310 | Involvement of p38 mitogen-activated protein kinase followed by chemokine expression in crescentic glomerulonephritis. Am J Kidney Dis. 2001 Dec;38(6):1169-77. | ||||
Ref 535631 | From extracellular to intracellular targets, inhibiting MAP kinases in treatment of Crohn's disease. Ann N Y Acad Sci. 2002 Nov;973:349-58. | ||||
Ref 535798 | Prevention 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 535852 | Inhibition 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 536549 | Privileged structures: a useful concept for the rational design of new lead drug candidates. Mini Rev Med Chem. 2007 Nov;7(11):1108-19. | ||||
Ref 537274 | Efficacy, 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. |
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