Page last updated: 2024-09-05

sb 203580 and vx-745

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

Compound Research Comparison

Studies
(sb 203580)
Trials
(sb 203580)
Recent Studies (post-2010)
(sb 203580)
Studies
(vx-745)
Trials
(vx-745)
Recent Studies (post-2010) (vx-745)
3,48941,13758135

Protein Interaction Comparison

ProteinTaxonomysb 203580 (IC50)vx-745 (IC50)
Mitogen-activated protein kinase 13Homo sapiens (human)0.0577
Bile salt export pumpHomo sapiens (human)10
Tyrosine-protein kinase ABL1Homo sapiens (human)1
Cytochrome P450 3A4Homo sapiens (human)0.0008
Platelet-derived growth factor receptor betaHomo sapiens (human)1
Adenosine receptor A3Homo sapiens (human)8.547
Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)1
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)8.547
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)0.029
Mu-type opioid receptorRattus norvegicus (Norway rat)0.0008
Tyrosine-protein kinase ABL2Homo sapiens (human)1
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)8.547
Mitogen-activated protein kinase 14 Mus musculus (house mouse)0.0442
Mitogen-activated protein kinase 12Homo sapiens (human)0.0577
Sodium-dependent dopamine transporter Homo sapiens (human)8.098
Mitogen-activated protein kinase 11Homo sapiens (human)0.2462
Mitogen-activated protein kinase 14Homo sapiens (human)0.4028

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 sb 203580 and vx-745

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 sb 203580 and vx-745

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