Page last updated: 2024-09-03

gefitinib and imatinib

gefitinib has been researched along with imatinib in 28 studies

Compound Research Comparison

Studies
(gefitinib)
Trials
(gefitinib)
Recent Studies (post-2010)
(gefitinib)
Studies
(imatinib)
Trials
(imatinib)
Recent Studies (post-2010) (imatinib)
5,2315662,9192360157

Protein Interaction Comparison

ProteinTaxonomygefitinib (IC50)imatinib (IC50)
Chain A, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE ABLMus musculus (house mouse)0.1
Aurora kinase AHomo sapiens (human)4.3
Solute carrier family 22 member 2Homo sapiens (human)4.2
Bile salt export pumpHomo sapiens (human)10
Tyrosine-protein kinase ABL1Homo sapiens (human)0.6804
Tyrosine-protein kinase ABL1Mus musculus (house mouse)0.3704
Proto-oncogene tyrosine-protein kinase SrcGallus gallus (chicken)2.784
Epidermal growth factor receptorHomo sapiens (human)0.0001
Carbonic anhydrase 2Homo sapiens (human)0.372
Receptor tyrosine-protein kinase erbB-2Homo sapiens (human)0.0001
Platelet-derived growth factor receptor betaMus musculus (house mouse)0.3
Tyrosine-protein kinase LckHomo sapiens (human)0.2667
Cyclin-dependent kinase 1Homo sapiens (human)4.3
Macrophage colony-stimulating factor 1 receptorHomo sapiens (human)0.8417
Tyrosine-protein kinase LynHomo sapiens (human)0.22
ATP-dependent translocase ABCB1Homo sapiens (human)5.0229
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)0.4
Hepatocyte growth factor receptorHomo sapiens (human)0.0216
Platelet-derived growth factor receptor betaHomo sapiens (human)0.285
Dihydrofolate reductaseEscherichia coli K-120.372
Mast/stem cell growth factor receptor KitHomo sapiens (human)1.2682
Breakpoint cluster region proteinHomo sapiens (human)0.5032
Solute carrier family 2, facilitated glucose transporter member 4Mus musculus (house mouse)0.473
Dipeptidyl peptidase 4Rattus norvegicus (Norway rat)5
Ribosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)0.175
Platelet-derived growth factor receptor alphaHomo sapiens (human)0.1516
Thromboxane-A synthase Homo sapiens (human)0.198
Cyclin-dependent kinase 2Homo sapiens (human)3.318
Histamine H2 receptorHomo sapiens (human)1.963
Platelet-derived growth factor receptor alpha Mus musculus (house mouse)0.3
5-hydroxytryptamine receptor 2AHomo sapiens (human)1.891
Sodium-dependent serotonin transporterHomo sapiens (human)1.402
Receptor-type tyrosine-protein kinase FLT3Homo sapiens (human)0.131
Tyrosine-protein kinase ABL2Homo sapiens (human)0.156
Tyrosine-protein kinase SYKHomo sapiens (human)5
Serine/threonine-protein kinase PLK1Homo sapiens (human)4.3
Platelet-derived growth factor receptor betaRattus norvegicus (Norway rat)0.162
Epithelial discoidin domain-containing receptor 1Homo sapiens (human)0.2964
Discoidin domain-containing receptor 2Homo sapiens (human)0.457
Leucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)8.3
Multidrug and toxin extrusion protein 2Homo sapiens (human)1.625
Multidrug and toxin extrusion protein 1Homo sapiens (human)0.1467
Aurora kinase BHomo sapiens (human)4.3
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)2.9096
Aurora kinase CHomo sapiens (human)4.3

Research

Studies (28)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's6 (21.43)29.6817
2010's18 (64.29)24.3611
2020's4 (14.29)2.80

Authors

AuthorsStudies
Hegedus, T; Kéri, G; Német, K; Orfi, L; Ozvegy-Laczka, C; Sarkadi, B; Schuetz, JD; Ujhelly, O; Váradi, A; Várady, G1
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
Knight, ZA; Shokat, KM1
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
Lombardo, F; Obach, RS; Waters, NJ1
Bikker, JA; Brooijmans, N; Mansour, TS; Wissner, A1
Müller, H; Pick, A; Wiese, M1
Benfenati, E; Raska, I; Toropov, AA; Toropova, AP1
Morphy, R1
Doak, AK; Prusiner, SB; Shoichet, BK; Wille, H1
Afshari, CA; Eschenberg, M; Hamadeh, HK; Lee, PH; Lightfoot-Dunn, R; Morgan, RE; Qualls, CW; Ramachandran, B; Trauner, M; van Staden, CJ1
Hajduk, PJ; Johnson, EF; Kifle, L; Merta, PJ; Metz, JT; Soni, NB1
Russu, WA; Shallal, HM1
Dubey, PK; Pal, M; Piedrafita, FJ; Rajitha, C; Sunku, V; Veeramaneni, VR1
Ciceri, P; Davis, MI; Herrgard, S; Hocker, M; Hunt, JP; Pallares, G; Treiber, DK; Wodicka, LM; Zarrinkar, PP1
Al-Mazaideh, GM; Erdmann, F; Göllner, C; Rohe, A; Schmidt, M; Sippl, W; Wichapong, K1
Davis, MI; Khan, J; Li, SQ; Patel, PR; Shen, M; Sun, H; Thomas, CJ1
Afshari, CA; Chen, Y; Dunn, RT; Hamadeh, HK; Kalanzi, J; Kalyanaraman, N; Morgan, RE; van Staden, CJ1
Aleo, MD; Bonin, PD; Luo, Y; Potter, DM; Swiss, R; Will, Y1
Bullock, AN; Canning, P; Choi, S; Cuny, GD; Mohedas, AH; Sanvitale, CE; Wang, Y; Xing, X; Yu, PB1
Chen, M; Hu, C; Suzuki, A; Thakkar, S; Tong, W; Yu, K1
Chen, ZS; Korlipara, V; Lei, Z; Romu, AA; Zhou, B1
Aiche, S; Bassermann, F; Becker, W; Canevari, G; Casale, E; Depaolini, SR; Ehrlich, HC; Felder, ER; Feuchtinger, A; Garz, AK; Gohlke, BO; Götze, K; Greif, PA; Hahne, H; Heinzlmeir, S; Helm, D; Huenges, J; Jeremias, I; Kayser, G; Klaeger, S; Koch, H; Koenig, PA; Kramer, K; Kuster, B; Médard, G; Meng, C; Petzoldt, S; Polzer, H; Preissner, R; Qiao, H; Reinecke, M; Reiter, K; Rueckert, L; Ruland, J; Ruprecht, B; Schlegl, J; Schmidt, T; Schneider, S; Schoof, M; Spiekermann, K; Tõnisson, N; Vick, B; Vooder, T; Walch, A; Wilhelm, M; Wu, Z; Zecha, J; Zolg, DP1
Bandarage, UK; Cao, J; Gao, H; Green, J; Jacobs, MD; Marhefka, C1
Ding, K; Lu, X; Smaill, JB1
Caballero, E; García-Cárceles, J; Gil, C; Martínez, A1
Delabio, LC; Dutra, JP; Hembecker, M; Kita, DH; Moure, VR; Pereira, GDS; Scheiffer, G; Valdameri, G; Zattoni, IF1
Benfodda, Z; Duvauchelle, V; Meffre, P1

Reviews

7 review(s) available for gefitinib and imatinib

ArticleYear
Features of selective kinase inhibitors.
    Chemistry & biology, 2005, Volume: 12, Issue:6

    Topics: Animals; Drug Evaluation, Preclinical; Humans; Phosphoric Monoester Hydrolases; Protein Kinase Inhibitors; Substrate Specificity

2005
Selectively nonselective kinase inhibition: striking the right balance.
    Journal of medicinal chemistry, 2010, Feb-25, Volume: 53, Issue:4

    Topics: Animals; Antineoplastic Agents; Drug Design; Drug Discovery; Humans; Protein Binding; Protein Kinase Inhibitors; Structure-Activity Relationship

2010
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
    Drug discovery today, 2016, Volume: 21, Issue:4

    Topics: Chemical and Drug Induced Liver Injury; Databases, Factual; Drug Labeling; Humans; Pharmaceutical Preparations; Risk

2016
Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.
    Journal of medicinal chemistry, 2020, 10-08, Volume: 63, Issue:19

    Topics: Chemistry, Pharmaceutical; Humans; Point Mutation; Protein Kinase Inhibitors

2020
Kinase Inhibitors as Underexplored Antiviral Agents.
    Journal of medicinal chemistry, 2022, 01-27, Volume: 65, Issue:2

    Topics: Animals; Antiviral Agents; Drug Repositioning; Humans; Protein Kinase Inhibitors; Virus Diseases; Viruses

2022
Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators.
    European journal of medicinal chemistry, 2022, Jul-05, Volume: 237

    Topics: Antineoplastic Agents; ATP Binding Cassette Transporter, Subfamily G, Member 2; Breast Neoplasms; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Female; Humans; Neoplasm Proteins; Neoplastic Stem Cells

2022
Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery.
    European journal of medicinal chemistry, 2022, Aug-05, Volume: 238

    Topics: Antifungal Agents; Chemistry, Pharmaceutical; Drug Discovery; Structure-Activity Relationship; Thiophenes

2022

Other Studies

21 other study(ies) available for gefitinib and imatinib

ArticleYear
High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter.
    Molecular pharmacology, 2004, Volume: 65, Issue:6

    Topics: Adenosine Triphosphatases; Animals; Cell Line; Cell Membrane; Drug Resistance, Multiple; Enzyme Inhibitors; HL-60 Cells; Humans; Insecta; Protein-Tyrosine Kinases

2004
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
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
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
    Drug metabolism and disposition: the biological fate of chemicals, 2008, Volume: 36, Issue:7

    Topics: Blood Proteins; Half-Life; Humans; Hydrogen Bonding; Infusions, Intravenous; Pharmacokinetics; Protein Binding

2008
Kinase domain mutations in cancer: implications for small molecule drug design strategies.
    Journal of medicinal chemistry, 2009, Mar-26, Volume: 52, Issue:6

    Topics: Amino Acid Sequence; Antineoplastic Agents; Drug Design; Enzyme Inhibitors; Humans; Molecular Sequence Data; Mutation; Neoplasms; Phosphotransferases; Protein Conformation

2009
Novel lead for potent inhibitors of breast cancer resistance protein (BCRP).
    Bioorganic & medicinal chemistry letters, 2010, Jan-01, Volume: 20, Issue:1

    Topics: ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters; Benzamides; Benzimidazoles; Cell Line, Tumor; Chlorophyll; Humans; Molecular Conformation; Neoplasm Proteins; Phenylurea Compounds; Small Molecule Libraries

2010
QSPR modeling of octanol/water partition coefficient of antineoplastic agents by balance of correlations.
    European journal of medicinal chemistry, 2010, Volume: 45, Issue:4

    Topics: Antineoplastic Agents; Models, Chemical; Octanols; Quantitative Structure-Activity Relationship; Water

2010
Colloid formation by drugs in simulated intestinal fluid.
    Journal of medicinal chemistry, 2010, May-27, Volume: 53, Issue:10

    Topics: Buffers; Chemical Precipitation; Colloids; Intestine, Small; Light; Microscopy, Electron, Transmission; Pharmaceutical Preparations; Scattering, Radiation; Solubility

2010
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
    Toxicological sciences : an official journal of the Society of Toxicology, 2010, Volume: 118, Issue:2

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters; Biological Assay; Biological Transport; Cell Line; Cell Membrane; Chemical and Drug Induced Liver Injury; Cytoplasmic Vesicles; Drug Evaluation, Preclinical; Humans; Liver; Rats; Reproducibility of Results; Spodoptera; Transfection; Xenobiotics

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
Synthesis and pharmacological evaluations of novel 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as a new class of anti-cancer agents.
    European journal of medicinal chemistry, 2011, Volume: 46, Issue:10

    Topics: Antineoplastic Agents; Benzene Derivatives; Cell Line, Tumor; Drug Screening Assays, Antitumor; Humans; Neoplasms; Oxazines; 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
Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay.
    European journal of medicinal chemistry, 2013, Volume: 61

    Topics: Dose-Response Relationship, Drug; Fluorescence Resonance Energy Transfer; Glycolipids; Humans; Membrane Proteins; Models, Molecular; Molecular Structure; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Protein-Tyrosine Kinases; Structure-Activity Relationship

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
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
    Toxicological sciences : an official journal of the Society of Toxicology, 2013, Volume: 136, Issue:1

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters; Biological Transport; Chemical and Drug Induced Liver Injury; Cluster Analysis; Drug-Related Side Effects and Adverse Reactions; Humans; Liver; Male; Multidrug Resistance-Associated Proteins; Pharmacokinetics; Rats; Rats, Sprague-Dawley; Recombinant Proteins; Risk Assessment; Risk Factors; Toxicity Tests

2013
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
    Hepatology (Baltimore, Md.), 2014, Volume: 60, Issue:3

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters; Chemical and Drug Induced Liver Injury; Humans; Male; Mitochondria, Liver; Rats; Rats, Sprague-Dawley; Severity of Illness Index

2014
Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
    Journal of medicinal chemistry, 2014, Oct-09, Volume: 57, Issue:19

    Topics: Activin Receptors, Type I; Aminopyridines; Humans; Mutation; Myositis Ossificans; Phenols; Protein Kinase Inhibitors; Structure-Activity Relationship

2014
Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors.
    Bioorganic & medicinal chemistry letters, 2017, 11-01, Volume: 27, Issue:21

    Topics: Acrylamides; Animals; Cell Line, Tumor; Cell Survival; Drug Design; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Mice; Mutagenesis, Site-Directed; Protein Kinase Inhibitors; Pyrimidines; Structure-Activity Relationship

2017
The target landscape of clinical kinase drugs.
    Science (New York, N.Y.), 2017, 12-01, Volume: 358, Issue:6367

    Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Cytokines; Drug Discovery; fms-Like Tyrosine Kinase 3; Humans; Leukemia, Myeloid, Acute; Lung Neoplasms; Mice; Molecular Targeted Therapy; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proteomics; Xenograft Model Antitumor Assays

2017
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.
    Bioorganic & medicinal chemistry letters, 2018, 08-15, Volume: 28, Issue:15

    Topics: Binding Sites; Crystallography, X-Ray; Drug Design; Models, Molecular; Molecular Structure; Protein Kinase Inhibitors; rho-Associated Kinases; Solubility

2018