168 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet?-cells from apoptosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
East China Normal University
Discovery of novel anti-angiogenesis agents. Part 6: Multi-targeted RTK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Xi'An Jiaotong University
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck
The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
St. John'S University
Structural modifications at the 6-position of thieno[2,3-d]pyrimidines and their effects on potency at FLT3 for treatment of acute myeloid leukemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Yonsei University
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Southeast University
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Shenyang Pharmaceutical University
Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Icahn School of Medicine At Mount Sinai
Optimization of potent DFG-in inhibitors of platelet derived growth factor receptorß (PDGF-Rß) guided by water thermodynamics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Christian-Albrechts-University of Kiel
Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astellas Pharma
Discovery of orally active anticancer candidate CFI-400945 derived from biologically promising spirooxindoles: success and challenges.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Zhengzhou University
The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Takeda Pharmaceutical
Trimeric hemibastadin congener from the marine sponge Ianthella basta.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Heinrich-Heine University
Synthesis and optimization of substituted furo[2,3-d]-pyrimidin-4-amines and 7H-pyrrolo[2,3-d]pyrimidin-4-amines as ACK1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
3D QSAR studies on a series of potent and high selective inhibitors for three kinases of RTK family.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Dalian University
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Takeda Pharmaceutical
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Takeda Pharmaceutical
Multitargeted drug development: Discovery and profiling of dihydroxy substituted 1-aza-9-oxafluorenes as lead compounds targeting Alzheimer disease relevant kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Martin-Luther-University Halle-Wittenberg
Design and synthesis of pyrrolo[3,2-d]pyrimidine HER2/EGFR dual inhibitors: improvement of the physicochemical and pharmacokinetic profiles for potent in vivo anti-tumor efficacy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Takeda Pharmaceutical
Design and synthesis of pyrrolo[3,2-d]pyrimidine human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors: exploration of novel back-pocket binders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Takeda Pharmaceutical
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Discovery of loperamide as an antagonist of angiopoietin1 and angiopoietin2 by virtual screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Zhejiang Gongshang University
Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Cephalon
Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
National Cancer Institute-Bethesda
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Harvard Medical School
Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Novel 2,3-dihydro-1,4-benzoxazines as potent and orally bioavailable inhibitors of tumor-driven angiogenesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Oxford
TIE-2/VEGF-R2 SAR and in vitro activity of C3-acyl dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole analogs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Cephalon
Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Pharma
Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Westf£Lische Wilhelms-Universit£T M£Nster
VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Kentucky
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Shenyang Pharmaceutical University
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ansaris
Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Takeda Pharmaceutical
Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institute For Biomedical Research
Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ariad Pharmaceuticals
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
Discovery and selectivity-profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Martin-Luther-University Halle-Wittenberg
Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Design, synthesis, and evaluation of 5-methyl-4-phenoxy-5H-pyrrolo[3,2-d]pyrimidine derivatives: novel VEGFR2 kinase inhibitors binding to inactive kinase conformation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Takeda Pharmaceutical
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ambit Biosciences
Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Center For Molecular Medicine of The Austrian Academy of Sciences
Rational design of inhibitors that bind to inactive kinase conformations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Research Foundation
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institute of Biomedical Research
Analysis of kinase inhibitor selectivity using a thermodynamics-based partition index.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
8-THP-DHI analogs as potent Type I dual TIE-2/VEGF-R2 receptor tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Cephalon
Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Cgi Pharmaceuticals
Novel thienopyrimidine and thiazolopyrimidine kinase inhibitors with activity against Tie-2 in vitro and in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
Labeled 3-aryl-4-indolylmaleimide derivatives and their potential as angiogenic PET biomarkers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Hadassah Hebrew University Hospital
2-{3-[4-(Alkylsulfinyl)phenyl]-1-benzofuran-5-yl}-5-methyl-1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta with good brain permeability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Takeda Pharmaceutical
Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
N-substituted 2'-(aminoaryl)benzothiazoles as kinase inhibitors: hit identification and scaffold hopping.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
4Sc
Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Search for inhibitors of bacterial and human protein kinases among derivatives of diazepines[1,4] annelated with maleimide and indole cycles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Institute of General Genetics
Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Discovery of imidazole vinyl pyrimidines as a novel class of kinase inhibitors which inhibit Tie-2 and are orally bioavailable.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eberhard-Karls University
Design, synthesis and characterization of N9/N7-substituted 6-aminopurines as VEGF-R and EGF-R inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eberhard-Karls University
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Genomics Institute of The Novartis Research Foundation
Design and synthesis of dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole oximes as potent dual inhibitors of TIE-2 and VEGF-R2 receptor tyrosine kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Cephalon
Entry into a new class of protein kinase inhibitors by pseudo ring design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
Optimization of triarylimidazoles for Tie2: influence of conformation on potency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
1,2,3-Thiadiazole substituted pyrazolones as potent KDR/VEGFR-2 kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Cephalon
Discovery of thienopyridines as Src-family selective Lck inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Bioresearch Center
Profile and molecular modeling of 3-(indole-3-yl)-4-(3,4,5-trimethoxyphenyl)-1 H-pyrrole-2,5-dione (1) as a highly selective VEGF-R2/3 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eberhard-Karls University
Design and effective synthesis of novel templates, 3,7-diphenyl-4-amino-thieno and furo-[3,2-c]pyridines as protein kinase inhibitors and in vitro evaluation targeting angiogenetic kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Targegen
Novel C-3 N-urea, amide, and carbamate dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole analogs as potent TIE-2 and VEGF-R2 dual inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Cephalon
1,4-Dihydroindeno[1,2-c]pyrazoles as novel multitargeted receptor tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Discovery of the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Jinan University
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Arkansas For Medical Sciences
Structure-Based Design of Selective Salt-Inducible Kinase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Johann Wolfgang Goethe University
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Bioresearch Center
2-Hydroxy-4,6-diamino-[1,3,5]triazines: a novel class of VEGF-R2 (KDR) tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Johnson & Johnson Pharmaceutical Research and Development
A small molecule-kinase interaction map for clinical kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ambit Biosciences
Discovery of 3-Aminopyrazole Derivatives as New Potent and Orally Bioavailable AXL Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Jinan University
A-420983: a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Bioresearch Center
A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clin![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Cephalon
Development of natural product-derived receptor tyrosine kinase inhibitors based on conservation of protein domain fold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Institut FüR Molekulare Physiologie
Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sichuan University/Collaborative Innovation Center of Biotherapy
From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sichuan University
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Beijing Normal University
Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sun Yat-Sen University
Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Bioresearch Center
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Research Laboratories
Discovery of 1,6-naphthyridinone-based MET kinase inhibitor bearing quinoline moiety as promising antitumor drug candidate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
China Pharmaceutical University
Novel 5,6-disubstituted pyrrolo[2,3-d]pyrimidine derivatives as broad spectrum antiproliferative agents: Synthesis, cell based assays, kinase profile and molecular docking study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Korea Institute of Science and Technology
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck And
Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck II.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Basf Bioresearch
Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Basf Bioresearch
Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Japan Tobacco
Discovery of novel anti-angiogenesis agents. Part 9: Multiplex inhibitors suppressing compensatory activations of RTKs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
The First Affiliated Hospital of Xi'An Jiaotong University
Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
National Research Centre
Synthesis and biological evaluation of new MET inhibitors with 1,6-naphthyridinone scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Central China Normal University
Synthesis and evaluation of thieno[3,2-d]pyrimidine derivatives as novel FMS inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chung-Ang University
Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Southeast University
Discovery of novel anti-angiogenesis agents. Part 10: Multi-target inhibitors of VEGFR-2, Tie-2 and EphB4 incorporated with 1,2,3-triazol.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Xi'An Jiaotong University
Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Arkansas For Medical Sciences
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Florida
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Takeda Pharmaceutical
A Selective and Brain Penetrant p38?MAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Northwestern University
Bioactive metabolites from the endophytic fungus Stemphylium globuliferum isolated from Mentha pulegium.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Heinrich-Heine-Universitat
Cytotoxic metabolites from the fungal endophyte Alternaria sp. and their subsequent detection in its host plant Polygonum senegalense.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Heinrich-Heine-Universit£T
Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sichuan University/Collaborative Innovation Center of Biotherapy
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Jinan University
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Korea Institute of Science & Technology (Kist)
Discovery of novel anti-angiogenesis agents. Part 8: Diaryl thiourea bearing 1H-indazole-3-amine as multi-target RTKs inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Xi'An Jiaotong University
Discovery of novel anti-angiogenesis agents. Part 7: Multitarget inhibitors of VEGFR-2, TIE-2 and EphB4.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Xi'An Jiaotong University
Structure-based design, synthesis, and evaluation of 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel c-Met inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
China Pharmaceutical University
Small molecules inhibit STAT3 activation, autophagy, and cancer cell anchorage-independent growth.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Indiana University School of Medicine
Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
Chromone containing sulfonamides as potent carbonic anhydrase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Ondokuz Mayis University
Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Aimst University
Plant-derived flavones as inhibitors of aurora B kinase and their quantitative structure-activity relationships.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Konkuk University
In vitro and in vivo pharmacological characterization of BM-613 [N-n-pentyl-N'-[2-(4'-methylphenylamino)-5-nitrobenzenesulfonyl]urea], a novel dual thromboxane synthase inhibitor and thromboxane receptor antagonist.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
University of Li&Eagrove;Ge
Functional calcitonin gene-related peptide subtype 2 receptors in porcine coronary arteries are identified as calcitonin gene-related peptide subtype 1 receptors by radioligand binding and reverse transcription-polymerase chain reaction.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Creighton University
High throughput receptor-based virtual screening under ZINC database, synthesis, and biological evaluation of ketol-acid reductoisomerase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Nankai University
Design and synthesis of novel 2-amino-5-hydroxyindole derivatives that inhibit human 5-lipoxygenase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Friedrich Alexander University Erlangen
Discovery of potent 3,5-diphenyl-1,2,4-oxadiazole sphingosine-1-phosphate-1 (S1P1) receptor agonists with exceptional selectivity against S1P2 and S1P3.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Merck Research Laboratories