300 articles for thisTarget
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Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers.
Novartis Institutes For Biomedical Research
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.
Abbvie Bioresearch Center
Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen.
The Institute of Cancer Research
Design and synthesis of new RAF kinase-inhibiting antiproliferative quinoline derivatives. Part 2: Diarylurea derivatives.
University of Sharjah
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.
Merck
Design, synthesis and activity of novel sorafenib analogues bearing chalcone unit.
Jiangxi Science & Technology Normal University
Discovery of 3-benzyl-1,3-benzoxazine-2,4-dione analogues as allosteric mitogen-activated kinase kinase (MEK) inhibitors and anti-enterovirus 71 (EV71) agents.
Peking University Health Science Center
GSK114: A selective inhibitor for elucidating the biological role of TNNI3K.
Glaxosmithkline
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.
Oribase Pharma
Design, biological evaluation and 3D QSAR studies of novel dioxin-containing triaryl pyrazoline derivatives as potential B-Raf inhibitors.
Nanjing University
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.
Zhejiang University
Design and synthesis of N-(4-aminopyridin-2-yl)amides as B-Raf(V600E) inhibitors.
Jilin University
Purinylpyridinylamino-based DFG-in/aC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling.
Amgen
Design and synthesis of new imidazo[1,2-a]pyridine and imidazo[1,2-a]pyrazine derivatives with antiproliferative activity against melanoma cells.
Semmelweis University
Discovery of highly selective CRAF inhibitors, 3-carboxamido-2H-indazole-6-arylamide: In silico FBLD design, synthesis and evaluation.
Hanyang University
Optimization of tetrahydronaphthalene inhibitors of Raf with selectivity over hERG.
Takeda Pharmaceutical
Discovery of EBI-907: A highly potent and orally active B-Raf(V600E) inhibitor for the treatment of melanoma and associated cancers.
Shanghai Hengrui Pharmaceutical
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).
Icahn School of Medicine At Mount Sinai
Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.
Novartis Institutes For Biomedical Research
Probing a 3,4'-bis-guanidinium diaryl derivative as an allosteric inhibitor of the Ras pathway.
Trinity College
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.
Hanyang University
Identification of Purines and 7-Deazapurines as Potent and Selective Type I Inhibitors of Troponin I-Interacting Kinase (TNNI3K).
Glaxosmithkline
Synthesis and biological evaluation of 3-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-4-(indol-3-yl)-maleimides as potent, selective GSK-3ß inhibitors and neuroprotective agents.
Zhejiang University
Optimization of potent DFG-in inhibitors of platelet derived growth factor receptorß (PDGF-Rß) guided by water thermodynamics.
Christian-Albrechts-University of Kiel
Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.
Eli Lilly
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.
Genomics Institute of The Novartis Research Foundation
N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors.
Guangzhou Institutes of Biomedicine and Health
Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer.
Sichuan University
Structural investigation of B-Raf paradox breaker and inducer inhibitors.
Umr Cnrs-Universit£
Discovery of 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK).
Amgen
Design, synthesis and evaluation of novel 2-(1H-imidazol-2-yl) pyridine Sorafenib derivatives as potential BRAF inhibitors and anti-tumor agents.
China Pharmaceutical University
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives containing diaryl urea moiety as potent antitumor agents.
Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of benzyl 2-(1H-imidazole-1-yl) pyrimidine analogues as selective and potent Raf inhibitors.
Hanyang University
Design, synthesis and biological evaluation of bis-aryl ureas and amides based on 2-amino-3-purinylpyridine scaffold as DFG-out B-Raf kinase inhibitors.
China Pharmaceutical University
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives possessing diaryl semicarbazone scaffolds as potent antitumor agents.
Shenyang Pharmaceutical University
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.
Merck Research Laboratories
Design, synthesis and biological evaluation of novel 5-phenyl-1H-pyrazole derivatives as potential BRAF(V600E) inhibitors.
Nanjing University
Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors.
Novartis Institutes For Biomedical Research
Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: optimization of in vitro potencies and pharmacokinetic properties.
Development Center For Biotechnology
Design, synthesis and evaluation of novel diaryl urea derivatives as potential antitumor agents.
Peking Union Medical College
Recent progress in the identification of BRAF inhibitors as anti-cancer agents.
Cairo University
Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives.
Takeda Pharmaceutical
Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors.
Zhejiang University
Design, synthesis, and evaluation of novel VEGFR2 kinase inhibitors: discovery of [1,2,4]triazolo[1,5-a]pyridine derivatives with slow dissociation kinetics.
Takeda Pharmaceutical
Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor.
Takeda Pharmaceutical
Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.
Takeda Pharmaceutical
Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors.
Astrazeneca
The discovery of potent and selective 4-aminothienopyridines as B-Raf kinase inhibitors.
Glaxosmithkline
Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors.
Takeda Pharmaceutical
Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors.
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.
Takeda Pharmaceutical
Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.
Cellzome
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.
Takeda Pharmaceutical
Design, synthesis and biological evaluation ofß-carboline derivatives as novel inhibitors targeting B-Raf kinase.
China Pharmaceutical University
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.
Takeda Pharmaceutical
Potent and selective aminopyrimidine-based B-Raf inhibitors with favorable physicochemical and pharmacokinetic properties.
Genentech
Synthesis, biological evaluation and 3D-QSAR studies of novel 4,5-dihydro-1H-pyrazole niacinamide derivatives as BRAF inhibitors.
Nanjing University
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.
Ambit Biosciences
Tri- and tetrasubstituted pyrazole derivates: regioisomerism switches activity from p38MAP kinase to important cancer kinases.
Islamic University of Gaza
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.
Harvard Medical School
Dual binding site inhibitors of B-RAF kinase.
Johnson & Johnson Pharmaceutical Research & Development
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.
Amgen
The identification of potent and selective imidazole-based inhibitors of B-Raf kinase.
Glaxosmithkline
Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors.
Westf£Lische Wilhelms-Universit£T M£Nster
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.
Glaxosmithkline
Structure-based de novo design and biochemical evaluation of novel BRAF kinase inhibitors.
Sejong University
Structure-based design of isoindoline-1,3-diones and 2,3-dihydrophthalazine-1,4-diones as novel B-Raf inhibitors.
Pfizer
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.
Takeda Pharmaceutical
Identification of novel BRAF kinase inhibitors with structure-based virtual screening.
Sejong University
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.
Ariad Pharmaceuticals
Discovery and optimization of pyrazoline compounds as B-Raf inhibitors.
Millennium Pharmaceuticals
Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.
Millennium Pharmaceuticals
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.
TBA
Identification of potent ITK inhibitors through focused compound library design including structural information.
Nycomed
Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.
Pfizer
Switch control pocket inhibitors of p38-MAP kinase. Durable type II inhibitors that do not require binding into the canonical ATP hinge region.
Deciphera Pharmaceuticals
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.
Takeda Pharmaceutical
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
Rational design of inhibitors that bind to inactive kinase conformations.
Novartis Research Foundation
The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796.
The University of Arizona
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.
Wyeth Research
5-Substituted [1]pyrindine derivatives with antiproliferative activity.
University of Paris
Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.
Wyeth Research
BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.
The Institute of Cancer Research
Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.
Wyeth Research
Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors.
Boehringer Ingelheim Pharmaceuticals
Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4.
Wyeth Research
4-Anilino-7-alkenylquinoline-3-carbonitriles as potent MEK1 kinase inhibitors.
Wyeth Research
Competitive Kinase Enrichment Proteomics Reveals that Abemaciclib Inhibits GSK3β and Activates WNT Signaling.
University of North Carolina at Chapel Hill
Small molecule inhibitor screen identifies synergistic activity of the bromodomain inhibitor CPI203 and bortezomib in drug resistant myeloma.
Knight Cancer Institute
In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494).
AbbVie Bioresearch Center
CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients.
Mayo Clinic
Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2).
Harvard Medical School
Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine.
Eli Lilly and Company
Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition.
Genentech, Inc and Exelixis
Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036.
Tufts Medical Center
Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase.
GlaxoSmithKline
LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2.
Eli Lilly and Company
Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein.
The Scripps Research Institute
BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo.
Boehringer Ingelheim Austria GmbH
Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885.
GlaxoSmithKline
NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family.
Johann Wolfgang Goethe University
Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours.
AbbVie
The mystery of titan hunter: Rationalized striking of the MAPK pathway via Newly synthesized 6-Indolylpyridone-3-Carbonitrile derivatives.
Tanta University
Quinazoline-based VEGFR-2 inhibitors as potential anti-angiogenic agents: A contemporary perspective of SAR and molecular docking studies.
Tehran University of Medical Sciences
Synthesis and evaluation of dihydrofuro[2,3-b]pyridine derivatives as potent IRAK4 inhibitors.
Soochow University
Targeting HSP90 for Cancer Therapy: Current Progress and Emerging Prospects.
Sichuan University
Advances in dual-targeting inhibitors of HDAC6 for cancer treatment.
Guizhou Medical University
Hydroxamic acid hybrids: Histone deacetylase inhibitors with anticancer therapeutic potency.
Shandong University
Design, Synthesis, and Biological Evaluation of 5-Amino-4-fluoro-1H-benzo[d]imidazole-6-carboxamide Derivatives as Novel and Potential MEK/RAF Complex Inhibitors Based on the "Clamp" Strategy.
Sichuan University
Non-kinase off-target inhibitory activities of clinically-relevant kinase inhibitors.
Purdue University
Identification of the Clinical Candidate PF-07284890 (ARRY-461), a Highly Potent and Brain Penetrant BRAF Inhibitor for the Treatment of Cancer.
Enliven Therapeutics
Synthesis of a new series of 4-pyrazolylquinolinones with apoptotic antiproliferative effects as dual EGFR/BRAFV600E inhibitors.
Princess Nourah bint Abdulrahman University
The Discovery of Exarafenib (KIN-2787): Overcoming the Challenges of Pan-RAF Kinase Inhibition.
Kinnate Biopharma
Pyrrole-containing hybrids as potential anticancer agents: An insight into current developments and structure-activity relationships.
Jiangxi Science & Technology Normal University
The mechanism of UNC-51-like kinase 1 and the applications of small molecule modulators in cancer treatment.
Shenyang Pharmaceutical University
Recent advances and future directions on small molecule VEGFR inhibitors in oncological conditions.
Taipei Medical University
Design, synthesis and characterisation of a novel type II B-RAF paradox breaker inhibitor.
University of Orleans
Application and synthesis of thiazole ring in clinically approved drugs.
Zhengzhou University
SAR of a novel 'Anthranilamide Like' series of VEGFR-2, multi protein kinase inhibitors for the treatment of cancer.
Bayer Research Center
Discovery of a Dual Tubulin and Neuropilin-1 (NRP1) Inhibitor with Potent In Vivo Anti-Tumor Activity via Pharmacophore-based Docking Screening, Structure Optimization, and Biological Evaluation.
China Pharmaceutical University
The Hitchhiker's Guide to Deep Learning Driven Generative Chemistry.
Insilico Medicine Hong Kong
Identification of novel piperazine-tethered phthalazines as selective CDK1 inhibitors endowed with in vitro anticancer activity toward the pancreatic cancer.
Kafrelsheikh University
Rational Design of Covalent Kinase Inhibitors by an Integrated Computational Workflow (Kin-Cov).
Jinan University
A decade of approved first-in-class small molecule orphan drugs: Achievements, challenges and perspectives.
China Pharmaceutical University
Design, synthesis, broad-spectrum antiproliferative activity, and kinase inhibitory effect of triarylpyrazole derivatives possessing arylamides or arylureas moieties.
Korea Institute of Science and Technology
Dual-target kinase drug design: Current strategies and future directions in cancer therapy.
Sichuan University
From Hit Seeking to Magic Bullets: The Successful Union of Epigenetic and Fragment Based Drug Discovery (EPIDD + FBDD).
University of S£O Paulo
Molecular hybrids: A five-year survey on structures of multiple targeted hybrids of protein kinase inhibitors for cancer therapy.
Al-Azhar University
Small-Molecule Drug Discovery in Triple Negative Breast Cancer: Current Situation and Future Directions.
Sichuan University
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
Menoufia University
Discovery of a potent and highly selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase: Structural activity relationship and antitumor activity both in vitro and in vivo.
Sichuan University
Structure-Based and Knowledge-Informed Design of B-Raf Inhibitors Devoid of Deleterious PXR Binding.
Cnrs
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.
University of Arkansas For Medical Sciences
Novel inhibitors of B-RAF based on a disubstituted pyrazine scaffold. Generation of a nanomolar lead.
Institute of Cancer Research
Discovery of novel spiro compound as RAF kinase inhibitor with in vitro potency against KRAS mutant cancer.
Eternity Bioscience
Discovery of 6,7-dihydro-5H-pyrrolo[3,4-d] pyrimidine derivatives as a new class of ATR inhibitors.
Sichuan University
The overview of Mitogen-activated extracellular signal-regulated kinase (MEK)-based dual inhibitor in the treatment of cancers.
Zhengzhou University
Isoxazole derivatives as anticancer agent: A review on synthetic strategies, mechanism of action and SAR studies.
Central University of Punjab
Evaluation of imidazo[2,1-b]thiazole-based anticancer agents in one decade (2011-2020): Current status and future prospects.
University of Sharjah
Identification of the Benzoimidazole Compound as a Selective FLT3 Inhibitor by Cell-Based High-Throughput Screening of a Diversity Library.
Sun Yat-Sen University Cancer Center
Discovery of spiro amide SHR902275: A potent, selective, and efficacious RAF inhibitor targeting RAS mutant cancers.
Eternity Bioscience
Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.
Glaxosmithkline
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3
Genentech
Identification of Diarylurea Inhibitors of the Cardiac-Specific Kinase TNNI3K by Designing Selectivity Against VEGFR2, p38α, and B-Raf.
Glaxosmithkline
Discovery, Synthesis, and Evaluation of Highly Selective Vascular Endothelial Growth Factor Receptor 3 (VEGFR3) Inhibitor for the Potential Treatment of Metastatic Triple-Negative Breast Cancer.
West China Hospital of Sichuan University
Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors.
Korea Institute of Science and Technology
Discovery of a Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase with Oral Anti-Inflammatory Activity.
Janssen Research & Development
Design and synthesis of 1H-pyrazolo[3,4-b]pyridines targeting mitogen-activated protein kinase kinase 4 (MKK4) - A promising target for liver regeneration.
Eberhard Karls Universit£T
Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity.
Korea Institute of Science & Technology (Kist)
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.
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.
Sichuan University
Design, synthesis, biological evaluation, and docking studies of novel (imidazol-5-yl)pyrimidine-based derivatives as dual BRAF
Korea Institute of Science & Technology (Kist)
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.
National Research Centre
Modification of imidazothiazole derivatives gives promising activity in B-Raf kinase enzyme inhibition; synthesis, in vitro studies and molecular docking.
University of Science & Technology (Ust)
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a Pyridopyridazinone pan-RAF Kinase Inhibitor.
Genentech
2-Anilinoquinoline based arylamides as broad spectrum anticancer agents with B-RAF
Korea Institute of Science & Technology (Kist)
Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer.
Zhuhai Campus of Zunyi Medical University
Identification of BRaf-Sparing Amino-Thienopyrimidines with Potent IRE1α Inhibitory Activity.
Paraza Pharma
Anticancer profile of newly synthesized BRAF inhibitors possess 5-(pyrimidin-4-yl)imidazo[2,1-b]thiazole scaffold.
National Research Centre (Nrc)
Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting
National Research Centre (Nrc Id: 60014618)
Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity.
Shenyang Pharmaceutical University
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.
Merck
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.
Merck And
Discovery of highly potent V600E-B-RAF kinase inhibitors: Molecular modeling study.
University of Sharjah
Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors.
National Research Centre
Discovery of novel phenoxybenzamide analogues as Raf/HDAC dual inhibitors.
China Pharmaceutical University
Design and Synthesis of Type-IV Inhibitors of BRAF Kinase That Block Dimerization and Overcome Paradoxical MEK/ERK Activation.
University of South Carolina
Rigidification Dramatically Improves Inhibitor Selectivity for RAF Kinases.
University of Southern California
Design, Synthesis, and Structure-Activity Relationships of 1,2,3-Triazole Benzenesulfonamides as New Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors.
Jinan University
Design, synthesis, and in vitro evaluation of N-(3-(3-alkyl-1H-pyrazol-5-yl) phenyl)-aryl amide for selective RAF inhibition.
Hanyang University
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.
University of South China
Discovery of potent Pan-Raf inhibitors with increased solubility to overcome drug resistance.
China Pharmaceutical University
Privileged Structures and Polypharmacology within and between Protein Families.
The Institute of Cancer Research
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.
University of Florida
Discovery of a potent p38α/MAPK14 kinase inhibitor: Synthesis, in vitro/in vivo biological evaluation, and docking studies.
University of Sharjah
Synthesis, in vitro antiproliferative activity, and kinase inhibitory effects of pyrazole-containing diarylureas and diarylamides.
University of Sharjah
Design and synthesis of new potent anticancer benzothiazole amides and ureas featuring pyridylamide moiety and possessing dual B-Raf(V600E) and C-Raf kinase inhibitory activities.
Korea Institute of Science & Technology (Kist)
Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase.
Array Biopharma
Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer.
Shanghai Pharmaceuticals Holding
Identification and synthesis of N-(thiophen-2-yl) benzamide derivatives as BRAF(V600E) inhibitors.
Central South University
Potent BRAF kinase inhibitors based on 2,4,5-trisubstituted imidazole with naphthyl and benzothiophene 4-substituents.
The Institute of Cancer Research
A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.
Northwestern University
Structural modifications of a 3-methoxy-2-aminopyridine compound to reduce potential for mutagenicity and time-dependent drug-drug interaction.
Pfizer
Pyrazolopyridine inhibitors of B-Raf(V600E). Part 4: rational design and kinase selectivity profile of cell potent type II inhibitors.
Array Biopharma
Combining pharmacophore, docking and substructure search approaches to identify and optimize novel B-RafV600E inhibitors.
Chinese Academy of Sciences
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 2. Synthesis and characterization of a novel imide-type prodrug for improving oral absorption.
Takeda Pharmaceutical
Potent and selective pyrazolo[1,5-a]pyrimidine based inhibitors of B-Raf(V600E) kinase with favorable physicochemical and pharmacokinetic properties.
Array Biopharma
The discovery of potent and selective pyridopyrimidin-7-one based inhibitors of B-RafV600E kinase.
Array Biopharma
Design, synthesis and biological evaluation of novel (E)-α-benzylsulfonyl chalcone derivatives as potential BRAF inhibitors.
Nanjing University
Design and synthesis of 6,6-fused heterocyclic amides as raf kinase inhibitors.
Novartis Institutes For Biomedical Research
Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors.
Array Biopharma
Pyrazolopyridine inhibitors of B-Raf(V600E). Part 3: an increase in aqueous solubility via the disruption of crystal packing.
Array Biopharma
Pyrazolopyridine inhibitors of B-RafV600E. Part 2: structure-activity relationships.
Arraybiopharma
Novel tricyclic pyrazole BRAF inhibitors with imidazole or furan central scaffolds.
The Institute of Cancer Research
Novel hinge binder improves activity and pharmacokinetic properties of BRAF inhibitors.
The Institute of Cancer Research
Development of novel, highly potent inhibitors of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF): increasing cellular potency through optimization of a distal heteroaromatic group.
The Institute of Cancer Research
Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines.
Korea Institute of Science and Technology
Bioactive metabolites from the endophytic fungus Stemphylium globuliferum isolated from Mentha pulegium.
Heinrich-Heine-Universitat
Novel potent BRAF inhibitors: toward 1 nM compounds through optimization of the central phenyl ring.
The Institute of Cancer Research
Cytotoxic metabolites from the fungal endophyte Alternaria sp. and their subsequent detection in its host plant Polygonum senegalense.
Heinrich-Heine-Universit£T
Recent advances of RAF (rapidly accelerated fibrosarcoma) inhibitors as anti-cancer agents.
University of Science & Technology (Ust)
Synthesis, anticancer activity and molecular modeling studies of 1,2,4-triazole derivatives as EGFR inhibitors.
Nahda University
Design and biological evaluation of novel triaryl pyrazoline derivatives with dioxane moiety for selective BRAF
Nanjing University
Isolation, Characterization, and Structure-Activity Relationship Analysis of Abietane Diterpenoids from Callicarpa bodinieri as Spleen Tyrosine Kinase Inhibitors.
Yunnan University
Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure-Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept.
Institute of Cancer Research
N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[d]thiazol-2-yl)cyclopropanecarboxamide (TAK632) Promotes Inhibition of BRAF through the Induction of Inhibited Dimers.
University of Pennsylvania
Design, synthesis and anticancer evaluation of novel spirobenzo[h]chromene and spirochromane derivatives with dual EGFR and B-RAF inhibitory activities.
Beni-Suef University
Effects of rigidity on the selectivity of protein kinase inhibitors.
University of Southern California
Design and discovery of thioether and nicotinamide containing sorafenib analogues as multikinase inhibitors targeting B-Raf, B-Raf
Yantai University
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?
University of South Australia
Design, synthesis, mechanistic and histopathological studies of small-molecules of novel indole-2-carboxamides and pyrazino[1,2-a]indol-1(2H)-ones as potential anticancer agents effecting the reactive oxygen species production.
Aljouf University
Design, synthesis, and biological evaluation of pyrazole derivatives containing acetamide bond as potential BRAF
Nanjing University
Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins.
Temple University
Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.
Novartis Institutes For Biomedical Research
Design, synthesis and antitumor activity of Novel Sorafenib derivatives bearing pyrazole scaffold.
Jiangxi Science & Technology Normal University
Design, synthesis, biological evaluation and molecular modeling of novel 1H-pyrazolo[3,4-d]pyrimidine derivatives as BRAF
Southern Medical University
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.
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.
Xi'An Jiaotong University
Discovery of novel anti-angiogenesis agents. Part 7: Multitarget inhibitors of VEGFR-2, TIE-2 and EphB4.
Xi'An Jiaotong University
Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors.
University of Macau
Design, synthesis and evaluation of derivatives based on pyrimidine scaffold as potent Pan-Raf inhibitors to overcome resistance.
China Pharmaceutical University
4,6-Diaminopyrimidines as Highly Preferred Troponin I-Interacting Kinase (TNNI3K) Inhibitors.
TBA
INHIBITOR OF PROSTATE SPECIFIC MEMBRANE ANTIGEN AND PHARMACEUTICAL USE THEREOF
Tianjin Hengrui Medicine
NITROGEN-CONTAINING POLYCYCLIC FUSED RING COMPOUND, PHARMACEUTICAL COMPOSITION THEREOF, PREPARATION METHOD THEREFOR, AND USE THEREOF
Applied Pharmaceutical Science
Compounds for inhibiting TNIK and medical uses thereof
Korea Research Institute of Chemical Technology
Substituted carboxamides as inhibitors of WDR5 protein-protein binding
Propellon Therapeutics
Isoquinoline ether compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
Vanderbilt University
Compositions and methods for treating KIT- and PDGFRA-mediated diseases
Blueprint Medicines
2,3-dihydro-isoindole-1-on derivative as BTK kinase suppressant, and pharmaceutical composition including same
Crystalgenomics
Substituted piperidine compounds and their use as orexin receptor modulators
Janssen Pharmaceutica
1-(3-aminopropyl) substituted cyclic amine compounds, preparation method therefor, and pharmaceutical compositions and uses thereof
Shanghai Institute of Material Medica, Chinese Academy of Sciences
Carbonic anhydrase inhibitors: in vitro inhibition of a isoforms (hCA I, hCA II, bCA III, hCA IV) by flavonoids.
Ondokuz Mayis University
Substituted spiro[cycloalkyl-1,3′-indo]-2′(1′H)-one derivatives and their use as P38 mitogen-activated kinase inhibitors
Almirall
Rational Optimization of Drug-Target Residence Time: Insights from Inhibitor Binding to the Staphylococcus aureus FabI Enzyme-Product Complex.
Stony Brook University
26- and 27-Methyl groups of 2-substituted, 19-nor-1a,25-dihydroxylated vitamin D compounds are essential for calcium mobilization in vivo.
University of Wisconsin-Madison
Oxygenation of monoenoic fatty acids by CYP175A1, an orphan cytochrome P450 from Thermus thermophilus HB27.
Tata Institute of Fundamental Research
Dipeptide-derived nitriles containing additional electrophilic sites: potentially irreversible inhibitors of cysteine proteases.
Rheinische Friedrich-Wilhelms-Universitat Bonn
Pharmacological characterization of a novel nonpeptide antagonist radioligand, (+/-)-N-[2-methyl-4-methoxyphenyl]-1-(1-(methoxymethyl) propyl)-6-methyl-1H-1,2,3-triazolo[4,5-c]pyridin-4-amine ([3H]SN003) for corticotropin-releasing factor1 receptors.
Bristol-Myers Squibb Pharmaceuticals Research Institute
Dual-site binding of bivalent 4-aminopyridine- and 4-aminoquinoline-based AChE inhibitors: contribution of the hydrophobic alkylene tether to monomer and dimer affinities.
Hong Kong University of Science and Technology