Page last updated: 2024-09-05

vx-745 and sb 203580

vx-745 has been researched along with sb 203580 in 17 studies

Compound Research Comparison

Studies
(vx-745)
Trials
(vx-745)
Recent Studies (post-2010)
(vx-745)
Studies
(sb 203580)
Trials
(sb 203580)
Recent Studies (post-2010) (sb 203580)
581353,48941,137

Protein Interaction Comparison

ProteinTaxonomyvx-745 (IC50)sb 203580 (IC50)
Citron Rho-interacting kinaseHomo sapiens (human)1
Cyclin-G-associated kinaseHomo sapiens (human)0.4133
Mitogen-activated protein kinase 13Homo sapiens (human)0.2329
Mitogen-activated protein kinase 2Pneumocystis carinii0.105
Receptor-interacting serine/threonine-protein kinase 2Homo sapiens (human)1.0359
RAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)0.7575
Cytochrome P450 1A2Homo sapiens (human)2
Tyrosine-protein kinase LckHomo sapiens (human)3.45
Neutrophil elastaseHomo sapiens (human)0.025
Cytochrome P450 3A4Homo sapiens (human)0.062
Cytochrome P450 2D6Homo sapiens (human)2
TyrosinaseMus musculus (house mouse)0.034
Cholesteryl ester transfer proteinHomo sapiens (human)0.04
Cytochrome P450 2C9 Homo sapiens (human)1
Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)5
Serine/threonine-protein kinase B-rafHomo sapiens (human)1
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)0.36
Prostaglandin G/H synthase 1Homo sapiens (human)2
Thromboxane-A synthase Homo sapiens (human)0.494
Adenosine receptor A2aHomo sapiens (human)6.068
Ephrin type-B receptor 2Homo sapiens (human)7.8
Adenosine receptor A1Homo sapiens (human)2.95
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)0.01
Delta-type opioid receptorMus musculus (house mouse)0.02
Cytochrome P450 2C19Homo sapiens (human)0.8
TGF-beta receptor type-1Homo sapiens (human)6
Mitogen-activated protein kinase 9Homo sapiens (human)0.9517
Mitogen-activated protein kinase 14 Mus musculus (house mouse)0.056
Casein kinase I isoform deltaHomo sapiens (human)0.4147
Casein kinase I isoform epsilonHomo sapiens (human)1
Mitogen-activated protein kinase 12Homo sapiens (human)0.2329
Mitogen-activated protein kinase 10Homo sapiens (human)0.6933
Mitogen-activated protein kinase 1Rattus norvegicus (Norway rat)0.048
Myotonin-protein kinaseHomo sapiens (human)1
Mitogen-activated protein kinase 11Homo sapiens (human)0.2646
Mitogen-activated protein kinase 14Homo sapiens (human)0.39
P2X purinoceptor 7Homo sapiens (human)5
Serine/threonine-protein kinase 36Homo sapiens (human)1
Serine/threonine-protein kinase NLKHomo sapiens (human)1
TRAF2 and NCK-interacting protein kinaseHomo sapiens (human)1

Research

Studies (17)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's8 (47.06)29.6817
2010's9 (52.94)24.3611
2020's0 (0.00)2.80

Authors

AuthorsStudies
Becker, JW; Cameron, PM; Fitzgerald, CE; O'Keefe, SJ; Patel, SB; Pikounis, VB; Scapin, G; Zaller, D1
Atteridge, CE; Azimioara, MD; Benedetti, MG; Biggs, WH; Carter, TA; Ciceri, P; Edeen, PT; Fabian, MA; Floyd, M; Ford, JM; Galvin, M; Gerlach, JL; Grotzfeld, RM; Herrgard, S; Insko, DE; Insko, MA; Lai, AG; Lélias, JM; Lockhart, DJ; Mehta, SA; Milanov, ZV; Patel, HK; Treiber, DK; Velasco, AM; Wodicka, LM; Zarrinkar, PP1
Bookland, RG; Brugel, TA; Clark, MP; De, B; Golebiowski, A; Hsieh, LC; Janusz, MJ; Laufersweiler, MJ; Laughlin, SK; Maier, J; Mekel, MJ; Sabat, M; Vanrens, JC; Walter, RL1
Bagley, MC; Davis, T; Dix, MC; Kipling, D; Rokicki, MJ1
Atteridge, CE; Campbell, BT; Chan, KW; Ciceri, P; Davis, MI; Edeen, PT; Faraoni, R; Floyd, M; Gallant, P; Herrgard, S; Hunt, JP; Karaman, MW; Lockhart, DJ; Milanov, ZV; Morrison, MJ; Pallares, G; Patel, HK; Pritchard, S; Treiber, DK; Wodicka, LM; Zarrinkar, PP1
Boman, E; Ceide, SC; Chang, CD; Dahl, R; Dalesandro, D; Delaet, NG; Erb, E; Ernst, JT; Gibbs, A; Kahl, J; Kessler, L; Larson, CJ; Lundström, J; Miller, S; Montalban, AG; Nakanishi, H; Roberts, E; Saiah, E; Sullivan, R; Wang, Z1
Alvira, E; Benson, AG; Blevis-Bal, R; Boehm, TL; Christie, L; Devadas, B; Devraj, RV; Durley, RC; Hepperle, M; Hickory, BS; Hitchcock, J; Jerome, KD; Kurumbail, R; Madsen, HM; Marrufo, LD; Monahan, JB; Naing, W; Owen, TJ; Promo, MA; Rucker, PV; Selness, SR; Shieh, H; Walker, JK; Xing, L1
Hajduk, PJ; Johnson, EF; Kifle, L; Merta, PJ; Metz, JT; Soni, NB1
Russu, WA; Shallal, HM1
Ciceri, P; Davis, MI; Herrgard, S; Hocker, M; Hunt, JP; Pallares, G; Treiber, DK; Wodicka, LM; Zarrinkar, PP1
Davis, MI; Khan, J; Li, SQ; Patel, PR; Shen, M; Sun, H; Thomas, CJ1
Bellon, SF; Bemis, GW; Chen, G; Cochran, JE; Duffy, JP; Evindar, G; Ford, PJ; Galullo, VP; Gao, H; Germann, UA; Green, J; Harrington, EM; Huang, C; Jones, P; Murcko, MA; Pazhanisamy, S; Salituro, FG; Su, MS; Taslimi, P; Wang, YM; Wilson, KP1
Anderson, WF; Arancio, O; Chico, LW; Minasov, G; Pelletier, JC; Roy, SM; Van Eldik, LJ; Watterson, DM1
Laufer, S; Wagner, G1
Azevedo, R; de Vlieg, J; Kazemier, B; Oubrie, A; Raaijmakers, H; van Zeeland, M1
Arthur, JS; Aubareda, A; Batty, IH; Boothby, M; Crowe, J; Dean, JL; Gaestel, M; Gray, A; Lee, K; Leslie, NR; McGuire, VA; Monk, CE; O'Keefe, SJ; Ronkina, N; Santos, SG; Schwermann, J1
Dastidar, SG; Diwan, M; Najmi, AK; Singh, RK1

Reviews

2 review(s) available for vx-745 and sb 203580

ArticleYear
A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.
    Journal of medicinal chemistry, 2019, 06-13, Volume: 62, Issue:11

    Topics: Animals; Brain; Cognitive Dysfunction; Humans; Inflammation; Nervous System Diseases; p38 Mitogen-Activated Protein Kinases; Protein Kinase Inhibitors

2019
Small molecular anti-cytokine agents.
    Medicinal research reviews, 2006, Volume: 26, Issue:1

    Topics: ADAM Proteins; ADAM17 Protein; Animals; Caspase Inhibitors; Cytochrome P-450 Enzyme Inhibitors; Cytokines; Humans; Hydroxamic Acids; Imidazoles; Matrix Metalloproteinase Inhibitors; Oligopeptides; p38 Mitogen-Activated Protein Kinases; Protein Kinase Inhibitors; Pyridazines; Pyridines; Pyrimidines; Quinazolines; Structure-Activity Relationship; Succinates; Thiazoles; Tumor Necrosis Factor-alpha; Urea

2006

Other Studies

15 other study(ies) available for vx-745 and sb 203580

ArticleYear
Structural basis for p38alpha MAP kinase quinazolinone and pyridol-pyrimidine inhibitor specificity.
    Nature structural biology, 2003, Volume: 10, Issue:9

    Topics: Amino Acid Sequence; Animals; Cloning, Molecular; Enzyme Inhibitors; Glycine; Imidazoles; Inhibitory Concentration 50; Kinetics; Mice; Mitogen-Activated Protein Kinase 14; Mitogen-Activated Protein Kinases; Models, Chemical; Models, Molecular; Molecular Sequence Data; Mutation; Peptides; Protein Binding; Protein Isoforms; Protein Structure, Tertiary; Pyridazines; Pyridines; Pyrimidines; Quinazolines; Sequence Homology, Amino Acid

2003
A small molecule-kinase interaction map for clinical kinase inhibitors.
    Nature biotechnology, 2005, Volume: 23, Issue:3

    Topics: Benzamides; Drug Design; Escherichia coli; Escherichia coli Proteins; Imatinib Mesylate; Microchemistry; Pharmaceutical Preparations; Piperazines; Protein Binding; Protein Interaction Mapping; Protein Kinase Inhibitors; Pyrimidines

2005
The development of novel C-2, C-8, and N-9 trisubstituted purines as inhibitors of TNF-alpha production.
    Bioorganic & medicinal chemistry letters, 2006, Aug-15, Volume: 16, Issue:16

    Topics: Cell Line; Chemistry, Pharmaceutical; Crystallography, X-Ray; Drug Design; Humans; Lipopolysaccharides; Models, Chemical; Models, Molecular; p38 Mitogen-Activated Protein Kinases; Purines; Tumor Necrosis Factor-alpha

2006
Rapid synthesis of VX-745: p38 MAP kinase inhibition in Werner syndrome cells.
    Bioorganic & medicinal chemistry letters, 2007, Sep-15, Volume: 17, Issue:18

    Topics: Blotting, Western; Enzyme-Linked Immunosorbent Assay; p38 Mitogen-Activated Protein Kinases; Protein Kinase Inhibitors; Pyridazines; Pyrimidines; Werner Syndrome

2007
A quantitative analysis of kinase inhibitor selectivity.
    Nature biotechnology, 2008, Volume: 26, Issue:1

    Topics: Binding Sites; Enzyme Activation; Humans; Phosphotransferases; Protein Binding; Protein Interaction Mapping; Protein Kinase Inhibitors; Proteome; Quantitative Structure-Activity Relationship

2008
The design and synthesis of novel alpha-ketoamide-based p38 MAP kinase inhibitors.
    Bioorganic & medicinal chemistry letters, 2008, Mar-15, Volume: 18, Issue:6

    Topics: Adenosine Triphosphate; Allosteric Site; Amides; Animals; Binding Sites; Cells, Cultured; Crystallography, X-Ray; Drug Design; Humans; Lipopolysaccharides; Models, Molecular; Molecular Structure; Monocytes; p38 Mitogen-Activated Protein Kinases; Phosphorylation; Protein Binding; Protein Conformation; Protein Kinase Inhibitors; Rats; Structure-Activity Relationship; Tumor Necrosis Factor-alpha

2008
Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase.
    Bioorganic & medicinal chemistry letters, 2009, Oct-15, Volume: 19, Issue:20

    Topics: Administration, Oral; Animals; Anti-Inflammatory Agents; Binding Sites; Catalytic Domain; Crystallography, X-Ray; Drug Discovery; Humans; JNK Mitogen-Activated Protein Kinases; Male; Microsomes, Liver; p38 Mitogen-Activated Protein Kinases; Protein Kinase Inhibitors; Pyridones; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship

2009
Navigating the kinome.
    Nature chemical biology, 2011, Volume: 7, Issue:4

    Topics: Drug Design; Pharmacogenetics; Protein Kinases; Proteome; Systems Biology

2011
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.
    European journal of medicinal chemistry, 2011, Volume: 46, Issue:6

    Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Discovery; Drug Screening Assays, Antitumor; Humans; Models, Molecular; Molecular Structure; Piperazines; Protein Kinase Inhibitors; Protein Kinases; Pyrimidines; Stereoisomerism; Structure-Activity Relationship

2011
Comprehensive analysis of kinase inhibitor selectivity.
    Nature biotechnology, 2011, Oct-30, Volume: 29, Issue:11

    Topics: Catalysis; Drug Design; Enzyme Stability; High-Throughput Screening Assays; Humans; Protein Binding; Protein Kinase Inhibitors; Protein Kinases; Proteomics; Signal Transduction; Substrate Specificity

2011
Identification of potent Yes1 kinase inhibitors using a library screening approach.
    Bioorganic & medicinal chemistry letters, 2013, Aug-01, Volume: 23, Issue:15

    Topics: Binding Sites; Cell Line; Cell Survival; Drug Design; Humans; Hydrogen Bonding; Molecular Docking Simulation; Protein Kinase Inhibitors; Protein Structure, Tertiary; Proto-Oncogene Proteins c-yes; Small Molecule Libraries; Structure-Activity Relationship

2013
The Discovery of VX-745: A Novel and Selective p38α Kinase Inhibitor.
    ACS medicinal chemistry letters, 2011, Oct-13, Volume: 2, Issue:10

    Topics:

2011
X-ray structure of p38α bound to TAK-715: comparison with three classic inhibitors.
    Acta crystallographica. Section D, Biological crystallography, 2012, Volume: 68, Issue:Pt 8

    Topics: Adenosine Triphosphate; Benzamides; Catalytic Domain; Cloning, Molecular; Crystallization; Crystallography, X-Ray; Humans; Imidazoles; Indoles; Ligands; p38 Mitogen-Activated Protein Kinases; Protein Binding; Protein Conformation; Protein Kinase Inhibitors; Pyridazines; Pyridines; Pyrimidines; Structure-Activity Relationship; Thiazoles

2012
Cross talk between the Akt and p38α pathways in macrophages downstream of Toll-like receptor signaling.
    Molecular and cellular biology, 2013, Volume: 33, Issue:21

    Topics: Animals; Cell Line; Enzyme Activation; Heat-Shock Proteins; Imidazoles; Intracellular Signaling Peptides and Proteins; Lipopolysaccharides; Macrophages; Mice; Mice, Inbred C57BL; Mice, Transgenic; Mitogen-Activated Protein Kinase 14; Molecular Chaperones; Neoplasm Proteins; Phosphatidylinositol Phosphates; Phosphorylation; Protein Processing, Post-Translational; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins c-akt; Pyridazines; Pyridines; Pyrimidines; Receptor Cross-Talk; Signal Transduction; Toll-Like Receptors

2013
Differential effect of p38 and MK2 kinase inhibitors on the inflammatory and toxicity biomarkers in vitro.
    Human & experimental toxicology, 2018, Volume: 37, Issue:5

    Topics: Anti-Inflammatory Agents; Biomarkers; Cell Survival; Cells, Cultured; Cytokines; Hep G2 Cells; Heterocyclic Compounds, 4 or More Rings; Humans; Imidazoles; Inflammation; Intracellular Signaling Peptides and Proteins; Leukocytes, Mononuclear; Lipopolysaccharides; MAP Kinase Kinase 4; Naphthalenes; Nitric Oxide; p38 Mitogen-Activated Protein Kinases; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Pyrazoles; Pyridazines; Pyridines; Pyrimidines; THP-1 Cells; U937 Cells

2018