Target Information

Target General Infomation
Target ID
T34624
Former ID
TTDR00365
Target Name
Stress kinase p38
Synonyms
MAP kinase p38; Mitogen-activated protein kinase p38; P38 MAP kinase; P38 MAPK; Stress-activated protein kinase
Target Type
Clinical Trial
Disease Asthma [ICD10: J45]
Atherosclerosis; Psoriasis [ICD9:414.0, 440, 696; ICD10: I70, L40]
Chronic obstructive pulmonary disease; Asthma [ICD9: 490-492, 493, 494-496; ICD10: J40-J44, J47, J45]
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25]
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06]
BioChemical Class
Kinase
EC Number
EC 2.7.1.37
Drugs and Mode of Action
Drug(s) AZD7624 Drug Info Phase 2 Chronic obstructive pulmonary disease [524912]
BMS-582949 Drug Info Phase 2 Atherosclerosis; Psoriasis [522211], [542780]
GSK2269557 Drug Info Phase 2 Chronic obstructive pulmonary disease; Asthma [525290]
TAK-715 Drug Info Phase 2 Rheumatoid arthritis [522447]
LY-2228820 Drug Info Phase 1/2 Cancer [524019], [542875]
AVE-9940 Drug Info Discontinued in Phase 1 Rheumatoid arthritis [548220]
AZD-6703 Drug Info Discontinued in Phase 1 Rheumatoid arthritis [542667], [548025]
SB-281832 Drug Info Discontinued in Phase 1 Asthma [547451]
TA-5493 Drug Info Discontinued in Phase 1 Inflammatory disease [548178]
AMG-548 Drug Info Terminated Inflammatory disease [547846]
Inhibitor AMG-548 Drug Info [527639]
AVE-9940 Drug Info [550183]
AZD-6703 Drug Info [531914]
AZD7624 Drug Info [533111]
BMS-582949 Drug Info [532303]
GSK2269557 Drug Info [531958]
LY-2228820 Drug Info [542875]
SB-281832 Drug Info [526851]
TA-5493 Drug Info [550897]
TAK-715 Drug Info [531443]
References
Ref 522211ClinicalTrials.gov (NCT00605735) PoC in Rheumatoid Arthritis With Methotrexate. U.S. National Institutes of Health.
Ref 522447ClinicalTrials.gov (NCT00760864) Safety and Efficacy of TAK-715 in Subjects With Rheumatoid Arthritis. U.S. National Institutes of Health.
Ref 524019ClinicalTrials.gov (NCT01663857) A Study of LY2228820 for Recurrent Ovarian Cancer. U.S. National Institutes of Health.
Ref 524912ClinicalTrials.gov (NCT02238483) A Phase IIa Study to Investigate the Efficacy and Safety of AZD7624 in Chronic Obstructive Pulmonary Disease (COPD) Patients While on Maintenance Therapy. U.S. National Institutes of Health.
Ref 525290ClinicalTrials.gov (NCT02522299) A Study to Evaluate the Safety, Efficacy and Changes in Induced Sputum and Blood Biomarkers Following Daily Repeat Doses of Inhaled GSK2269557 in Chronic Obstructive Pulmonary Disease (COPD) Subjects With Acute Exacerbation.
Ref 542667(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: 7687).
Ref 542780(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: 7838).
Ref 542875(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: 7959).
Ref 547451Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016500)
Ref 547846Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019881)
Ref 548025Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021256)
Ref 548178Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022792)
Ref 548220Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023206)
Ref 526851p38 MAPK inhibitors ameliorate target organ damage in hypertension: Part 1. p38 MAPK-dependent endothelial dysfunction and hypertension. J Pharmacol Exp Ther. 2003 Dec;307(3):932-8. Epub 2003 Oct 15.
Ref 527639p38 MAP kinase inhibitors: many are made, but few are chosen. Curr Opin Drug Discov Devel. 2005 Jul;8(4):421-30.
Ref 531443Inhibition of Wnt/beta-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Idelta/?. Chem Biol. 2011 Apr 22;18(4):485-94.
Ref 531914The discovery of N-cyclopropyl-4-methyl-3-[6-(4-methylpiperazin-1-yl)-4-oxoquinazolin-3(4H)-yl]benzamide (AZD6703), a clinical p38alpha MAP kinase inhibitor for the treatment of inflammatory diseases. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3879-83.
Ref 531958Evaluation of WO2012032067 and WO2012055846: two selective PI3Kdelta inhibitors, which is GSK-2269557. Expert Opin Ther Pat. 2012 Aug;22(8):965-70.
Ref 532303Synthesis and evaluation of carbamoylmethylene linked prodrugs of BMS-582949, a clinical p38alpha inhibitor. Bioorg Med Chem Lett. 2013 May 15;23(10):3028-33.
Ref 533111Investigational p38 inhibitors for the treatment of chronic obstructive pulmonary disease. Expert Opin Investig Drugs. 2015 Mar;24(3):383-92.
Ref 542875(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: 7959).
Ref 550183US patent application no. 2008,0119,498, Therapeutic agent for pruritus comprising p38 map kinase inhibitor as the active ingredient.
Ref 550897US patent application no. 2008,0269,123, Methods for treating polycystic kidney disease (pkd) or other cyst forming diseases.

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