General Information of DTT (ID: TTQBR95)

DTT Name Stress-activated protein kinase 2a (p38 alpha) DTT Info
Gene Name MAPK14

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Investigative Drug(s)
1 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ozagrel DMIGKA1 Xerophthalmia 5B55.Y Phase 4 [1]
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4 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Losmapimod DMIL37Z Acute coronary syndrome BA41 Phase 3 [1]
VX-702 DMKJDR6 Coronary artery disease BA80 Phase 2a [2]
Dilmapimod DMBYJ92 Acute lung injury NB32.3 Phase 2 [1]
VX-745 DMJAEG6 Alzheimer disease 8A20 Phase 2 [3]
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6 Patented Agent(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
PMID25991433-Compound-A1 DM89LF0 N. A. N. A. Patented [4]
PMID25991433-Compound-F2 DM37VIQ N. A. N. A. Patented [4]
PMID25991433-Compound-L1 DM2135Y N. A. N. A. Patented [4]
PMID25991433-Compound-L2 DM58UO9 N. A. N. A. Patented [4]
PMID25991433-Compound-L3 DM3LWUR N. A. N. A. Patented [4]
PMID25991433-Compound-O2 DMTROIQ N. A. N. A. Patented [4]
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⏷ Show the Full List of 6 Patented Agent(s)
8 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
PAMAPIMOD DM9SYUT Rheumatoid arthritis FA20 Discontinued in Phase 2 [5]
FR167653 DM69OR8 Chronic obstructive pulmonary disease CA22 Discontinued in Phase 1 [6]
R-1487 DM7WPI0 Rheumatoid arthritis FA20 Discontinued in Phase 1 [7]
SB 235699 DMNH8XU Psoriasis vulgaris EA90 Discontinued in Phase 1 [3]
SB-242235 DMKSFL0 Arthritis FA20 Discontinued in Phase 1 [8]
SB 203580 DMAET6F N. A. N. A. Terminated [9]
SB220025 DMSBUET Arthritis FA20 Terminated [10]
SC-102 DM1MQ6Z Solid tumour/cancer 2A00-2F9Z Terminated [11]
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⏷ Show the Full List of 8 Discontinued Drug(s)
56 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
(5-amino-1-phenyl-1H-pyrazol-4-yl)phenylmethanone DMF0YJ3 Discovery agent N.A. Investigative [12]
2-Chlorophenol DM2E3X5 Discovery agent N.A. Investigative [10]
3-(1-NAPHTHYLMETHOXY)PYRIDIN-2-AMINE DMXMBEF Discovery agent N.A. Investigative [11]
3-(Benzyloxy)Pyridin-2-Amine DM35VEI Discovery agent N.A. Investigative [10]
4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole DMN9YOB Discovery agent N.A. Investigative [13]
4-(2-Ethyl-4-m-tolyl-thiazol-5-yl)-pyridine DMFJW2E Discovery agent N.A. Investigative [14]
4-PHENOXY-N-(PYRIDIN-2-YLMETHYL)BENZAMIDE DMIPQTW Discovery agent N.A. Investigative [11]
4-Phenylsulfanyl-7H-pyrrolo[2,3-d]pyrimidine DMHANXD Discovery agent N.A. Investigative [15]
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol DMSKJ1X Discovery agent N.A. Investigative [16]
6-(4-Fluoro-phenylsulfanyl)-9H-purine DM5JWEY Discovery agent N.A. Investigative [15]
6-Benzylsulfanyl-9H-purine DMI7FNZ Discovery agent N.A. Investigative [15]
6-o-tolylquinazolin-2-amine DM4TX9O Discovery agent N.A. Investigative [17]
6-Phenylsulfanyl-9H-purine DMZ76NQ Discovery agent N.A. Investigative [15]
9-(4-Fluoro-benzyl)-6-phenylsulfanyl-9H-purine DMW2NY9 Discovery agent N.A. Investigative [15]
9-Benzyl-6-(4-fluoro-phenylsulfanyl)-9H-purine DM8Q0D9 Discovery agent N.A. Investigative [15]
9-Benzyl-6-phenylsulfanyl-9H-purine DMNCL5G Discovery agent N.A. Investigative [15]
B-Octylglucoside DMMO75G Discovery agent N.A. Investigative [10]
Bisindolylmaleimide-I DMOQJZC Discovery agent N.A. Investigative [18]
CI-1040 DMF3DZX Discovery agent N.A. Investigative [18]
Dihydro-quinolinone DM9UK6D Discovery agent N.A. Investigative [19]
DP-802 DMARTC2 Inflammation 1A00-CA43.1 Investigative [20]
GSK-280 DM325YR Inflammation 1A00-CA43.1 Investigative [20]
GW-788388 DMIBUW5 Solid tumour/cancer 2A00-2F9Z Investigative [21]
IN-1130 DM3YJXF Discovery agent N.A. Investigative [22]
IN-1166 DMMS6D3 Discovery agent N.A. Investigative [22]
KN-62 DMLZ89P Discovery agent N.A. Investigative [18]
KT-5720 DM9J50F Discovery agent N.A. Investigative [18]
L-779450 DM51B74 Discovery agent N.A. Investigative [23]
ML-3163 DM3S5UC Discovery agent N.A. Investigative [24]
ML-3375 DMXJY6W Discovery agent N.A. Investigative [25]
ML-3403 DMTQWI8 Discovery agent N.A. Investigative [25]
N-(3-(trifluoromethoxy)benzyl)-4-phenoxybenzamide DM6UC8Y Discovery agent N.A. Investigative [26]
N-(3-(trifluoromethyl)benzyl)-4-phenoxybenzamide DMSMRF9 Discovery agent N.A. Investigative [26]
N-(4-(trifluoromethyl)benzyl)-4-phenoxybenzamide DMZ0V8O Discovery agent N.A. Investigative [26]
N-(4-fluorobenzyl)-N-(pyridin-4-yl)-2-naphthamide DMP1ICB Discovery agent N.A. Investigative [27]
N-(4-methyl-benzyl)-4-phenoxy-benzamide DMZX2BH Discovery agent N.A. Investigative [26]
Oxindole 94 DMPFD6Y Pain MG30-MG3Z Investigative [28]
PD-0166326 DMD2CG9 Discovery agent N.A. Investigative [29]
PD-0173956 DM8RW92 Discovery agent N.A. Investigative [29]
PHA-666859 DMHQ6KT Diabetic retinopathy 9B71.0 Investigative [20]
Phenyl-(3-phenyl-1H-indazol-6-yl)-amine DMDCTNU Discovery agent N.A. Investigative [30]
PMID22521646C12 DMYQDXO Discovery agent N.A. Investigative [31]
RO-316233 DMAGLPW Discovery agent N.A. Investigative [18]
Ro-3201195 DM9GXYV Discovery agent N.A. Investigative [32]
Ro31-8220 DMDJLF0 Discovery agent N.A. Investigative [18]
RWJ-68354 DMNLVRS Discovery agent N.A. Investigative [33]
SB-216995 DMOH9TA Discovery agent N.A. Investigative [19]
SB-218655 DMJKE4M Discovery agent N.A. Investigative [19]
SB-227931 DMO1WI8 Discovery agent N.A. Investigative [34]
Small molecule 34 DMWJ70Q Discovery agent N.A. Investigative [10]
STAUROSPORINONE DMU2H4K Discovery agent N.A. Investigative [18]
Talmapimod DMMTSL2 Discovery agent N.A. Investigative [35]
Triazolopyridine DM1F2K0 Discovery agent N.A. Investigative [11]
Tyrphostin ag-1478 DM87ZIH Discovery agent N.A. Investigative [36]
UCB-1277763 DMFUE43 Inflammation 1A00-CA43.1 Investigative [20]
ZM-336372 DMD5JYQ Discovery agent N.A. Investigative [37]
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⏷ Show the Full List of 56 Investigative Drug(s)
Molecule Interaction Atlas

References

1 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
2 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.
3 Pharmacological inhibitors of MAPK pathways. Trends Pharmacol Sci. 2002 Jan;23(1):40-5.
4 c-Jun N-terminal kinase inhibitors: a patent review (2010 - 2014).Expert Opin Ther Pat. 2015;25(8):849-72.
5 Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders. J Med Chem. 2010 Mar 25;53(6):2345-53.
6 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.
7 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.
8 Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4433-7.
9 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.
10 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
11 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
12 Discovery of S-[5-amino-1-(4-fluorophenyl)-1H-pyrazol-4-yl]-[3-(2,3-dihydroxypropoxy)phenyl]methanone (RO3201195), an orally bioavailable and highl... J Med Chem. 2006 Mar 9;49(5):1562-75.
13 Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. J Med Chem. 2004 Dec 2;47(25):6239-47.
14 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 (T... J Med Chem. 2005 Sep 22;48(19):5966-79.
15 Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors. J Med Chem. 2005 Feb 10;48(3):710-22.
16 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006 Nov 2;49(22):6500-9.
17 Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity. J Med Chem. 2006 Sep 21;49(19):5671-86.
18 Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.
19 In silico search for multi-target anti-inflammatories in Chinese herbs and formulas. Bioorg Med Chem. 2010 Mar 15;18(6):2204-2218.
20 URL: 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).
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 orall... J Med Chem. 2006 Apr 6;49(7):2210-21.
22 Synthesis and biological evaluation of trisubstituted imidazole derivatives as inhibitors of p38alpha mitogen-activated protein kinase. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4006-10.
23 The identification of potent and selective imidazole-based inhibitors of B-Raf kinase. Bioorg Med Chem Lett. 2006 Jan 15;16(2):378-81.
24 From imidazoles to pyrimidines: new inhibitors of cytokine release. J Med Chem. 2002 Jun 20;45(13):2733-40.
25 Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. J Med Chem. 2003 Jul 17;46(15):3230-44.
26 Two classes of p38alpha MAP kinase inhibitors having a common diphenylether core but exhibiting divergent binding modes. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5274-9.
27 Amide-based inhibitors of p38alpha MAP kinase. Part 2: design, synthesis and SAR of potent N-pyrimidyl amides. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2560-3.
28 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.
29 Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6872-6.
30 Design and synthesis of 6-anilinoindazoles as selective inhibitors of c-Jun N-terminal kinase-3. Bioorg Med Chem Lett. 2005 Nov 15;15(22):5095-9.
31 Novel triazolopyridylbenzamides as potent and selective p38alpha inhibitors. Bioorg Med Chem Lett. 2012 May 15;22(10):3431-6.
32 Microwave-assisted synthesis of 5-aminopyrazol-4-yl ketones and the p38(MAPK) inhibitor RO3201195 for study in Werner syndrome cells. Bioorg Med Chem Lett. 2008 Jul 1;18(13):3745-8.
33 Imidazopyrimidines, potent inhibitors of p38 MAP kinase. Bioorg Med Chem Lett. 2003 Feb 10;13(3):347-50.
34 The neuroprotective action of JNK3 inhibitors based on the 6,7-dihydro-5H-pyrrolo[1,2-a]imidazole scaffold. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4666-70.
35 Mitogen-activated protein kinases in innate immunity.Nat Rev Immunol.2013 Sep;13(9):679-92.
36 Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase. Bioorg Med Chem Lett. 2004 Nov 1;14(21):5389-94.
37 A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis. Bioorg Med Chem Lett. 2004 Nov 1;14(21):5383-7.