Page last updated: 2024-09-05

sb 203580 and birb 796

sb 203580 has been researched along with birb 796 in 25 studies

Compound Research Comparison

Studies
(sb 203580)
Trials
(sb 203580)
Recent Studies (post-2010)
(sb 203580)
Studies
(birb 796)
Trials
(birb 796)
Recent Studies (post-2010) (birb 796)
3,48941,137137580

Protein Interaction Comparison

ProteinTaxonomysb 203580 (IC50)birb 796 (IC50)
Mitogen-activated protein kinase 13Homo sapiens (human)0.1057
Mitogen-activated protein kinase kinase kinase 7Homo sapiens (human)0.9
Receptor-interacting serine/threonine-protein kinase 2Homo sapiens (human)10
Serine/threonine-protein kinase 10Homo sapiens (human)1
Mitogen-activated protein kinase kinase kinase kinase 4Homo sapiens (human)1
Epidermal growth factor receptorHomo sapiens (human)3.8
RAF proto-oncogene serine/threonine-protein kinaseHomo sapiens (human)1.4
High affinity nerve growth factor receptorHomo sapiens (human)0.58
Heat shock protein beta-1Homo sapiens (human)0.058
Protein kinase C beta typeHomo sapiens (human)6.9
Tyrosine-protein kinase LckHomo sapiens (human)2.1
Tyrosine-protein kinase YesHomo sapiens (human)8.9
Tyrosine-protein kinase LynHomo sapiens (human)0.96
Proto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)0.515
Tyrosine-protein kinase HCKHomo sapiens (human)1.7
Platelet-derived growth factor receptor betaHomo sapiens (human)6.2
Tyrosine-protein kinase FgrHomo sapiens (human)8.5
Mast/stem cell growth factor receptor KitHomo sapiens (human)1
Serine/threonine-protein kinase B-rafHomo sapiens (human)0.0834
Vascular endothelial growth factor receptor 1 Homo sapiens (human)0.625
Ephrin type-A receptor 1Homo sapiens (human)0.63
Fibroblast growth factor receptor 4Homo sapiens (human)7
Mitogen-activated protein kinase 1Homo sapiens (human)9.2
Ephrin type-A receptor 2Homo sapiens (human)0.16
Ephrin type-A receptor 3Homo sapiens (human)1.1
Ephrin type-A receptor 8Homo sapiens (human)1
Ephrin type-B receptor 2Homo sapiens (human)0.58
Tyrosine-protein kinase receptor Tie-1Homo sapiens (human)1
Vascular endothelial growth factor receptor 3Homo sapiens (human)0.27
Vascular endothelial growth factor receptor 2Homo sapiens (human)0.34
Tyrosine-protein kinase FRKHomo sapiens (human)1
Mitogen-activated protein kinase 8Homo sapiens (human)1
Mitogen-activated protein kinase 9Homo sapiens (human)0.2989
Cyclin-dependent kinase 8Homo sapiens (human)1
Glycogen synthase kinase-3 betaHomo sapiens (human)1.06
Tyrosine-protein kinase BlkHomo sapiens (human)1
Mitogen-activated protein kinase 12Homo sapiens (human)0.2298
Mitogen-activated protein kinase 10Homo sapiens (human)1.2
Ephrin type-B receptor 3Homo sapiens (human)9.4
Ephrin type-A receptor 5Homo sapiens (human)0.09
Ephrin type-B receptor 4Homo sapiens (human)0.9
Ephrin type-B receptor 1Homo sapiens (human)0.11
Ephrin type-A receptor 4Homo sapiens (human)0.07
Cyclin-dependent-like kinase 5 Homo sapiens (human)1
Angiopoietin-1 receptorHomo sapiens (human)0.5125
Focal adhesion kinase 1Homo sapiens (human)2
Protein kinase C delta typeHomo sapiens (human)1.9
Epithelial discoidin domain-containing receptor 1Homo sapiens (human)1
Protein-tyrosine kinase 2-betaHomo sapiens (human)0.7
Ephrin type-A receptor 7Homo sapiens (human)1
TGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)0.9
Mitogen-activated protein kinase 11Homo sapiens (human)0.256
NT-3 growth factor receptorHomo sapiens (human)1
Mitogen-activated protein kinase 14Homo sapiens (human)0.0674
BDNF/NT-3 growth factors receptorHomo sapiens (human)0.525
Discoidin domain-containing receptor 2Homo sapiens (human)0.2707
Misshapen-like kinase 1Homo sapiens (human)0.04
STE20-like serine/threonine-protein kinase Homo sapiens (human)1
Mitogen-activated protein kinase kinase kinase 20Homo sapiens (human)1
TRAF2 and NCK-interacting protein kinaseHomo sapiens (human)1
Serine/threonine-protein kinase MRCK betaHomo sapiens (human)1

Research

Studies (25)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's10 (40.00)29.6817
2010's15 (60.00)24.3611
2020's0 (0.00)2.80

Authors

AuthorsStudies
Breitfelder, S; Cirillo, P; Gilmore, T; Graham, AG; Hickey, E; Klaus, B; Madwed, J; Moriak, M; Moss, N; Pargellis, C; Pav, S; Proto, A; Regan, J; Swinamer, A; Tong, L; Torcellini, C1
Capolino, A; Cirillo, PF; Gilmore, T; Graham, AG; Hickey, E; Kroe, RR; Madwed, J; Moriak, M; Moss, N; Nelson, R; Pargellis, CA; Regan, J; Swinamer, A; Torcellini, C; Tsang, M1
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
Ahrens, GM; Hering, JS; Karcher, SC; Laufer, SA; Niess, R1
Alessi, DR; Arthur, JS; Bain, J; Cohen, P; Elliott, M; Hastie, CJ; Klevernic, I; McLauchlan, H; Plater, L; Shpiro, N1
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
Domeyer, DM; Hauser, DR; Kinkel, K; Laufer, SA; Liedtke, AJ1
Groebe, D; Hajduk, PJ; Kifle, L; Merta, PJ; Sarris, K; Sun, C; Swann, SL1
Boman, E; Ceide, SC; Chang, CD; Dahl, R; Dalesandro, D; Delaet, NG; Erb, E; Ernst, JT; Gibbs, A; Kahl, J; Kessler, L; Kucharski, J; Larson, CJ; Lum, C; Lundström, J; Miller, S; Montalban, AG; Nakanishi, H; Roberts, E; Saiah, E; Sullivan, R; Urban, J; Wang, Z1
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
Bauer, SM; Boeckler, FM; Fischer, S; Grütter, C; Koeberle, SC; Laufer, SA; Mayer-Wrangowski, SC; Niess, R; Rauh, D; Storch, K; Wentsch, HK; Zimmermann, M1
Davis, MI; Khan, J; Li, SQ; Patel, PR; Shen, M; Sun, H; Thomas, CJ1
Bhat, R; Canan, S; Chojnowski, A; Goldberg, R; Hawryluk, N; Khetani, V; Kreiss, T; Mortensen, D; Prorok, M; Rotella, DP; Siekierka, JJ; Tummalapalli, SR; Zeldis, J1
Anderson, WF; Arancio, O; Chico, LW; Minasov, G; Pelletier, JC; Roy, SM; Van Eldik, LJ; Watterson, DM1
Gagnon, AI; Jia, Y; Quinn, CM; Talanian, R1
Kok, JJ; Loomans, EE; Nelissen, RL; van der Lee, MM; Zaman, GJ1
Brown, A; Foxwell, BM; Page, TH; Ray, KP; Timms, EM1
Aoki, T; Arai, T; Hayashi, S; Hirokawa, H; Inoue, H; Kainoh, M; Kawai, H; Koga, Y; Meguro, H; Ohno, M; Oshida, K; Suyama, K1
Falck, D; Giera, M; Honing, M; Kool, J; Niessen, WM; Rahimi Pirkolachachi, F1
Chang, G; Li, Y; Lu, K; Ye, L; Zhang, D; Zhang, P1
Hirose, E; Ishimaru, Y; Narahara, S; Sakamoto, A; Sugiuchi, H; Yamaguchi, R; Yamaguchi, Y; Yamamoto, T1
Dastidar, SG; Diwan, M; Najmi, AK; Singh, RK1

Reviews

1 review(s) available for sb 203580 and birb 796

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

Other Studies

24 other study(ies) available for sb 203580 and birb 796

ArticleYear
Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.
    Journal of medicinal chemistry, 2002, Jul-04, Volume: 45, Issue:14

    Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Binding, Competitive; Cell Line; Chromatography, High Pressure Liquid; Crystallography, X-Ray; Enzyme Inhibitors; Female; Fluorescence; Humans; Lipopolysaccharides; Mice; Mice, Inbred BALB C; Mitogen-Activated Protein Kinases; Models, Molecular; Naphthalenes; p38 Mitogen-Activated Protein Kinases; Protein Binding; Pyrazoles; Structure-Activity Relationship; Tumor Necrosis Factor-alpha; Urea

2002
Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796).
    Journal of medicinal chemistry, 2003, Oct-23, Volume: 46, Issue:22

    Topics: Animals; Cell Line; Crystallography, X-Ray; Enzyme Inhibitors; Enzyme-Linked Immunosorbent Assay; Heating; Humans; In Vitro Techniques; Ligands; Lipopolysaccharides; Mice; Mitogen-Activated Protein Kinase 14; Mitogen-Activated Protein Kinases; Naphthalenes; Protein Binding; Protein Denaturation; Pyrazoles; Structure-Activity Relationship; Tumor Necrosis Factor-alpha; Urea

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
Design, synthesis, and biological evaluation of phenylamino-substituted 6,11-dihydro-dibenzo[b,e]oxepin-11-ones and dibenzo[a,d]cycloheptan-5-ones: novel p38 MAP kinase inhibitors.
    Journal of medicinal chemistry, 2006, Dec-28, Volume: 49, Issue:26

    Topics: Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Drug Design; Humans; Molecular Structure; Oxepins; p38 Mitogen-Activated Protein Kinases; Protein Kinase Inhibitors; Structure-Activity Relationship

2006
The selectivity of protein kinase inhibitors: a further update.
    The Biochemical journal, 2007, Dec-15, Volume: 408, Issue:3

    Topics: Amino Acid Sequence; Animals; Cell Line; Drug Design; Enzyme Activation; Humans; Mitogen-Activated Protein Kinases; Phosphorylation; Protein Kinase Inhibitors; Recombinant Proteins; Spodoptera

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
Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region.
    Journal of medicinal chemistry, 2008, Jul-24, Volume: 51, Issue:14

    Topics: Drug Design; Humans; Imidazoles; Molecular Mimicry; p38 Mitogen-Activated Protein Kinases; Protein Kinase Inhibitors; Structure-Activity Relationship

2008
Biochemical and biophysical characterization of unique switch pocket inhibitors of p38α.
    Bioorganic & medicinal chemistry letters, 2010, Oct-01, Volume: 20, Issue:19

    Topics: Adenosine Triphosphate; Binding Sites; Computer Simulation; Crystallography, X-Ray; Fluorescence Resonance Energy Transfer; Kinetics; Mitogen-Activated Protein Kinase 14; Protein Binding; Protein Kinase Inhibitors; Protein Structure, Tertiary; Structure-Activity Relationship

2010
Optimization of alpha-ketoamide based p38 inhibitors through modifications to the region that binds to the allosteric site.
    Bioorganic & medicinal chemistry letters, 2010, Aug-15, Volume: 20, Issue:16

    Topics: Administration, Oral; Allosteric Site; Amides; Animals; Anti-Inflammatory Agents, Non-Steroidal; Binding Sites; Cell Line; Computer Simulation; Humans; p38 Mitogen-Activated Protein Kinases; Protein Binding; Protein Kinase Inhibitors; Rats; Structure-Activity Relationship

2010
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
Dibenzosuberones as p38 mitogen-activated protein kinase inhibitors with low ATP competitiveness and outstanding whole blood activity.
    Journal of medicinal chemistry, 2013, Jan-10, Volume: 56, Issue:1

    Topics: Adenosine Triphosphate; Animals; Anti-Inflammatory Agents, Non-Steroidal; Binding Sites; Dibenzocycloheptenes; Hydrophobic and Hydrophilic Interactions; Lipopolysaccharides; Models, Molecular; p38 Mitogen-Activated Protein Kinases; Protein Binding; Solubility; Structure-Activity Relationship; Tumor Necrosis Factor-alpha

2013
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
Discovery of a Stress-Activated Protein Kinase Inhibitor for Lymphatic Filariasis.
    ACS medicinal chemistry letters, 2018, Mar-08, Volume: 9, Issue:3

    Topics:

2018
Homogeneous time-resolved fluorescence and its applications for kinase assays in drug discovery.
    Analytical biochemistry, 2006, Sep-15, Volume: 356, Issue:2

    Topics: Adenosine Triphosphate; Catalysis; Dose-Response Relationship, Drug; Fluorescence Resonance Energy Transfer; Imidazoles; Kinetics; Naphthalenes; Phosphotransferases; Pyrazoles; Pyridines; Reproducibility of Results; Time Factors

2006
Enzyme fragment complementation binding assay for p38alpha mitogen-activated protein kinase to study the binding kinetics of enzyme inhibitors.
    Assay and drug development technologies, 2006, Volume: 4, Issue:4

    Topics: Animals; Cell Line; Cell Line, Tumor; Dose-Response Relationship, Drug; Green Fluorescent Proteins; Humans; Imidazoles; Kinetics; Mitogen-Activated Protein Kinase 14; Molecular Structure; Naphthalenes; Peptide Fragments; Protein Binding; Protein Kinase Inhibitors; Protein Transport; Pyrazoles; Pyridines; Recombinant Fusion Proteins; Structure-Activity Relationship; Surface Plasmon Resonance

2006
Inhibitors of p38 suppress cytokine production in rheumatoid arthritis synovial membranes: does variable inhibition of interleukin-6 production limit effectiveness in vivo?
    Arthritis and rheumatism, 2010, Volume: 62, Issue:11

    Topics: Arthritis, Rheumatoid; Blotting, Western; Cells, Cultured; Cytokines; Enzyme Inhibitors; Enzyme-Linked Immunosorbent Assay; Humans; Imidazoles; Interleukin-6; Macrophages; Monocytes; Naphthalenes; p38 Mitogen-Activated Protein Kinases; Phosphorylation; Pyrazoles; Pyridines; Reverse Transcriptase Polymerase Chain Reaction; Synovial Membrane

2010
Design and synthesis of novel p38α MAP kinase inhibitors: discovery of pyrazole-benzyl ureas bearing 2-molpholinopyrimidine moiety.
    Bioorganic & medicinal chemistry letters, 2012, Aug-01, Volume: 22, Issue:15

    Topics: Administration, Oral; Animals; Binding Sites; Crystallography, X-Ray; Cytochrome P-450 Enzyme System; Drug Design; Drug Evaluation, Preclinical; Humans; Imidazoles; Lipopolysaccharides; Liver; Mice; Mitogen-Activated Protein Kinase 14; Naphthalenes; Protein Kinase Inhibitors; Protein Structure, Tertiary; Pyrazoles; Pyridines; Pyrimidines; Tumor Necrosis Factor-alpha; Urea

2012
Comparison of (bio-)transformation methods for the generation of metabolite-like compound libraries of p38α MAP kinase inhibitors using high-resolution screening.
    Journal of pharmaceutical and biomedical analysis, 2014, Volume: 88

    Topics: Bacillus megaterium; Benzamides; Chemistry, Pharmaceutical; Cytochrome P-450 Enzyme System; High-Throughput Screening Assays; Humans; Hydrogen Peroxide; Imidazoles; Indoles; Light; Liver; Microsomes, Liver; Mitogen-Activated Protein Kinase 14; Naphthalenes; Oxygen; Photochemistry; Piperazines; Protein Kinase Inhibitors; Pyrazoles; Pyridines; Recombinant Proteins; Structure-Activity Relationship; Thiazoles

2014
Protective effects of extendin‑4 on hypoxia/reoxygenation‑induced injury in H9c2 cells.
    Molecular medicine reports, 2015, Volume: 12, Issue:2

    Topics: Adenosine Triphosphate; Animals; Cell Hypoxia; Cell Line; Cell Survival; Creatine Kinase, MB Form; Enzyme-Linked Immunosorbent Assay; Exenatide; Glucose; Glucose Transporter Type 1; Imidazoles; Intercellular Signaling Peptides and Proteins; L-Lactate Dehydrogenase; Mitogen-Activated Protein Kinase 12; Myocytes, Cardiac; Naphthalenes; Peptides; Protective Agents; Proteins; Pyrazoles; Pyridines; Rats; Signal Transduction; Venoms

2015
Mechanism of interleukin-13 production by granulocyte-macrophage colony-stimulating factor-dependent macrophages via protease-activated receptor-2.
    Blood cells, molecules & diseases, 2015, Volume: 55, Issue:1

    Topics: Butadienes; Calcium; Calcium Channel Blockers; Cell Adhesion; Cell Differentiation; Dose-Response Relationship, Drug; Flavonoids; Gallic Acid; Gene Expression Regulation; Granulocyte-Macrophage Colony-Stimulating Factor; Humans; Imidazoles; Interleukin-13; Leukocyte Elastase; Macrophages; Mitogen-Activated Protein Kinase 1; Mitogen-Activated Protein Kinase 3; Monocytes; Naphthalenes; Nitriles; p38 Mitogen-Activated Protein Kinases; Primary Cell Culture; Protein Kinase Inhibitors; Pyrazoles; Pyridines; Receptor, PAR-2; Signal Transduction

2015
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