Page last updated: 2024-09-04

birb 796 and sb 203580

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

Compound Research Comparison

Studies
(birb 796)
Trials
(birb 796)
Recent Studies (post-2010)
(birb 796)
Studies
(sb 203580)
Trials
(sb 203580)
Recent Studies (post-2010) (sb 203580)
1375803,48941,137

Protein Interaction Comparison

ProteinTaxonomybirb 796 (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 (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 birb 796 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

Other Studies

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

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