The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28557458 |
16 |
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 |
| 27789138 |
355 |
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors. |
Abbvie Bioresearch Center |
| 28004573 |
82 |
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 |
| 28088086 |
5 |
Design and synthesis of new RAF kinase-inhibiting antiproliferative quinoline derivatives. Part 2: Diarylurea derivatives. |
University of Sharjah |
| 28280261 |
84 |
Non-kinase targets of protein kinase inhibitors. |
The University of Sydney |
| 27816515 |
143 |
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors. |
Merck |
| 27777009 |
11 |
Design, synthesis and activity of novel sorafenib analogues bearing chalcone unit. |
Jiangxi Science & Technology Normal University |
| 27288186 |
29 |
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 |
| 27246618 |
73 |
GSK114: A selective inhibitor for elucidating the biological role of TNNI3K. |
Glaxosmithkline |
| 27010810 |
24 |
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
Oribase Pharma |
| 26852623 |
2 |
Natural Products as Sources of New Drugs from 1981 to 2014. |
Nih Special Volunteer |
| 27089211 |
38 |
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors. |
Zhejiang University |
| 27155899 |
30 |
Design and synthesis of N-(4-aminopyridin-2-yl)amides as B-Raf(V600E) inhibitors. |
Jilin University |
| 27085672 |
151 |
Purinylpyridinylamino-based DFG-in/aC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling. |
Amgen |
| 26724730 |
12 |
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 |
| 26810260 |
3 |
Discovery of highly selective CRAF inhibitors, 3-carboxamido-2H-indazole-6-arylamide: In silico FBLD design, synthesis and evaluation. |
Hanyang University |
| 26804230 |
48 |
Optimization of tetrahydronaphthalene inhibitors of Raf with selectivity over hERG. |
Takeda Pharmaceutical |
| 26739779 |
15 |
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 |
| 26762835 |
342 |
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 |
| 26396681 |
58 |
Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma. |
Novartis Institutes For Biomedical Research |
| 26318998 |
1 |
Probing a 3,4'-bis-guanidinium diaryl derivative as an allosteric inhibitor of the Ras pathway. |
Trinity College |
| 26318067 |
34 |
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors. |
Hanyang University |
| 26355916 |
106 |
Identification of Purines and 7-Deazapurines as Potent and Selective Type I Inhibitors of Troponin I-Interacting Kinase (TNNI3K). |
Glaxosmithkline |
| 25662701 |
23 |
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 |
| 25007344 |
73 |
Optimization of potent DFG-in inhibitors of platelet derived growth factor receptorß (PDGF-Rß) guided by water thermodynamics. |
Christian-Albrechts-University of Kiel |
| 25965804 |
80 |
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 |
| 26005534 |
158 |
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors. |
Genomics Institute of The Novartis Research Foundation |
| 26005530 |
20 |
N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors. |
Guangzhou Institutes of Biomedicine and Health |
| 25835317 |
63 |
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 |
| 25611072 |
20 |
Structural investigation of B-Raf paradox breaker and inducer inhibitors. |
Umr Cnrs-Universit£ |
| 25587754 |
146 |
Discovery of 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK). |
Amgen |
| 25461318 |
8 |
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 |
| 25086238 |
13 |
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives containing diaryl urea moiety as potent antitumor agents. |
Shenyang Pharmaceutical University |
| 24878193 |
8 |
Design, synthesis and biological evaluation of benzyl 2-(1H-imidazole-1-yl) pyrimidine analogues as selective and potent Raf inhibitors. |
Hanyang University |
| 25462267 |
39 |
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 |
| 25440879 |
13 |
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives possessing diaryl semicarbazone scaffolds as potent antitumor agents. |
Shenyang Pharmaceutical University |
| 25313996 |
91 |
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase. |
Merck Research Laboratories |
| 25267006 |
1 |
Design, synthesis and biological evaluation of novel 5-phenyl-1H-pyrazole derivatives as potential BRAF(V600E) inhibitors. |
Nanjing University |
| 25221654 |
39 |
Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors. |
Novartis Institutes For Biomedical Research |
| 24858546 |
46 |
Guanidinium-based derivatives: searching for new kinase inhibitors. |
Trinity College |
| 24773549 |
20 |
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 |
| 24675135 |
4 |
Design, synthesis and evaluation of novel diaryl urea derivatives as potential antitumor agents. |
Peking Union Medical College & Chinese Academy of Medical Sciences |
| 24424304 |
10 |
Recent progress in the identification of BRAF inhibitors as anti-cancer agents. |
Cairo University |
| 23906342 |
14 |
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 |
| 24389511 |
25 |
Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors. |
Zhejiang University |
| 23755884 |
23 |
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 |
| 23623674 |
1 |
Synthetic approaches to the 2011 new drugs. |
Shenogen Pharma Group |
| 23498918 |
41 |
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 |
| 23490150 |
48 |
Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors. |
Takeda Pharmaceutical |
| 23398453 |
4 |
Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors. |
Astrazeneca |
| 23218715 |
36 |
The discovery of potent and selective 4-aminothienopyridines as B-Raf kinase inhibitors. |
Glaxosmithkline |
| 22537109 |
25 |
Identification of a novel family of BRAF(V600E) inhibitors. |
University of Pennsylvania |
| 19303774 |
87 |
1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3. |
Glaxosmithkline |
| 23147077 |
23 |
Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors. |
Takeda Pharmaceutical |
| 23123015 |
22 |
Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors. |
Takeda Pharmaceutical |
| 22883026 |
34 |
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 |
| 22726925 |
216 |
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 |
| 22808911 |
18 |
Conformation-specific effects of Raf kinase inhibitors. |
Takeda California |
| 22980219 |
55 |
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 |
| 22704238 |
18 |
Design, synthesis and biological evaluation ofß-carboline derivatives as novel inhibitors targeting B-Raf kinase. |
China Pharmaceutical University |
| 22439974 |
79 |
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 |
| 22335519 |
3 |
Potent and selective aminopyrimidine-based B-Raf inhibitors with favorable physicochemical and pharmacokinetic properties. |
Genentech |
| 22583669 |
1 |
Synthesis, biological evaluation and 3D-QSAR studies of novel 4,5-dihydro-1H-pyrazole niacinamide derivatives as BRAF inhibitors. |
Nanjing University |
| 22168626 |
32 |
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 |
| 22185282 |
32 |
Tri- and tetrasubstituted pyrazole derivates: regioisomerism switches activity from p38MAP kinase to important cancer kinases. |
Islamic University of Gaza |
| 15975507 |
13 |
Features of selective kinase inhibitors. |
University of California San Francisco |
| 18183025 |
12060 |
A quantitative analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
| 17850214 |
99 |
The selectivity of protein kinase inhibitors: a further update. |
University of Dundee |
| 18662874 |
20 |
Knowledge-based design of 7-azaindoles as selective B-Raf inhibitors. |
Glaxosmithkline |
| 18077425 |
197 |
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
Harvard Medical School |
| 18434146 |
28 |
Dual binding site inhibitors of B-RAF kinase. |
Johnson & Johnson Pharmaceutical Research & Development |
| 18278858 |
93 |
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 |
| 16260133 |
43 |
The identification of potent and selective imidazole-based inhibitors of B-Raf kinase. |
Glaxosmithkline |
| 22377675 |
44 |
Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors. |
Westf£Lische Wilhelms-Universit£T M£Nster |
| 16249345 |
25 |
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580. |
Glaxosmithkline |
| 22222036 |
9 |
Small molecule inhibitors of BRAF in clinical trials. |
The Institute of Cancer Research |
| 22196123 |
23 |
Structure-based de novo design and biochemical evaluation of novel BRAF kinase inhibitors. |
Sejong University |
| 22137342 |
26 |
Discovery and optimization of thieno[2,3-d]pyrimidines as B-Raf inhibitors. |
Celgene |
| 22024030 |
22 |
Structure-based design of isoindoline-1,3-diones and 2,3-dihydrophthalazine-1,4-diones as novel B-Raf inhibitors. |
Pfizer |
| 22003817 |
71 |
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 |
| 22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
| 21873050 |
6 |
Identification of novel BRAF kinase inhibitors with structure-based virtual screening. |
Sejong University |
| 21561767 |
48 |
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant. |
Ariad Pharmaceuticals |
| 21536432 |
54 |
Non-oxime pyrazole based inhibitors of B-Raf kinase. |
Array Biopharma |
| 20634068 |
2 |
Discovery and optimization of pyrazoline compounds as B-Raf inhibitors. |
Millennium Pharmaceuticals |
| 21341678 |
49 |
Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors. |
Millennium Pharmaceuticals |
| 24900231 |
22 |
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway. |
TBA |
| 20965724 |
57 |
Identification of potent ITK inhibitors through focused compound library design including structural information. |
Nycomed |
| 20961062 |
42 |
Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity. |
Pfizer |
| 20800479 |
33 |
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 |
| 20833055 |
44 |
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 |
| 19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
| 16783341 |
34 |
Rational design of inhibitors that bind to inactive kinase conformations. |
Novartis Research Foundation |
| 20621496 |
31 |
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 |
| 20307980 |
22 |
B-Raf kinase inhibitors: hit enrichment through scaffold hopping. |
Wyeth Research |
| 19884006 |
47 |
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors. |
Wyeth Research |
| 19969400 |
4 |
5-Substituted [1]pyrindine derivatives with antiproliferative activity. |
University of Paris |
| 19864136 |
45 |
Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors. |
Wyeth Research |
| 19854649 |
49 |
Discovery of highly potent and selective type I B-Raf kinase inhibitors. |
Wyeth Research |
| 20148563 |
42 |
BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring. |
The Institute of Cancer Research |
| 19875283 |
41 |
Novel pyrazolopyrimidines as highly potent B-Raf inhibitors. |
Wyeth Research |
| 19362830 |
47 |
Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors. |
Wyeth Research |
| 19356929 |
17 |
Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors. |
Boehringer Ingelheim Pharmaceuticals |
| 19317452 |
155 |
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 |
| 18815050 |
34 |
4-Anilino-7-alkenylquinoline-3-carbonitriles as potent MEK1 kinase inhibitors. |
Wyeth Research |
| 17574417 |
98 |
SAR of a novel 'Anthranilamide Like' series of VEGFR-2, multi protein kinase inhibitors for the treatment of cancer. |
Bayer Research Center |
| 16392826 |
68 |
Novel inhibitors of B-RAF based on a disubstituted pyrazine scaffold. Generation of a nanomolar lead. |
Institute of Cancer Research |
| 15317461 |
53 |
Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors. |
Glaxosmithkline |
| 32340792 |
16 |
Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting |
National Research Centre (Nrc Id: 60014618) |
| 32305182 |
48 |
Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
Shenyang Pharmaceutical University |
| 31757666 |
314 |
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors. |
Merck |
| 27491711 |
422 |
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties. |
Merck And |
| 30660499 |
42 |
Discovery of highly potent V600E-B-RAF kinase inhibitors: Molecular modeling study. |
University of Sharjah |
| 31789518 |
11 |
Urea Derivatives in Modern Drug Discovery and Medicinal Chemistry. |
Purdue University |
| 31284081 |
60 |
Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors. |
National Research Centre |
| 31053508 |
34 |
Discovery of novel phenoxybenzamide analogues as Raf/HDAC dual inhibitors. |
China Pharmaceutical University |
| 30977659 |
35 |
Design and Synthesis of Type-IV Inhibitors of BRAF Kinase That Block Dimerization and Overcome Paradoxical MEK/ERK Activation. |
University of South Carolina |
| 31693351 |
473 |
Discovery of 4 |
TBA |
| 31312411 |
15 |
Rigidification Dramatically Improves Inhibitor Selectivity for RAF Kinases. |
University of Southern California |
| 31252305 |
18 |
Light-controlled inhibition of BRAFV600E kinase. |
University Medical Center Groningen |
| 32223235 |
12 |
Discovery of Selective Small Molecule Degraders of BRAF-V600E. |
Cullgen |
| 31244114 |
56 |
Design, Synthesis, and Structure-Activity Relationships of 1,2,3-Triazole Benzenesulfonamides as New Selective Leucine-Zipper and Sterile-? Motif Kinase (ZAK) Inhibitors. |
Jinan University |
| 31059256 |
28 |
Design and Discovery of |
Novartis Institutes For Biomedical Research |
| 30630714 |
33 |
Design, synthesis, and in vitro evaluation of N-(3-(3-alkyl-1H-pyrazol-5-yl) phenyl)-aryl amide for selective RAF inhibition. |
Hanyang University |
| 30600149 |
35 |
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton. |
University of South China |
| 30529543 |
57 |
Discovery of potent Pan-Raf inhibitors with increased solubility to overcome drug resistance. |
China Pharmaceutical University |
| 30613326 |
32 |
Privileged Structures and Polypharmacology within and between Protein Families. |
The Institute of Cancer Research |
| 30384048 |
365 |
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 |
| 31520926 |
28 |
Discovery of a potent p38?/MAPK14 kinase inhibitor: Synthesis, in vitro/in vivo biological evaluation, and docking studies. |
University of Sharjah |
| 30006168 |
1 |
Synthesis, in vitro antiproliferative activity, and kinase inhibitory effects of pyrazole-containing diarylureas and diarylamides. |
University of Sharjah |
| 27017549 |
15 |
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) |
| 24675381 |
47 |
Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase. |
Array Biopharma |
| 31200237 |
95 |
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 |
| 24042006 |
78 |
Imidazo[4,5-b]pyridine inhibitors of B-Raf kinase. |
Array Biopharma |
| 23489628 |
6 |
Identification and synthesis of N-(thiophen-2-yl) benzamide derivatives as BRAF(V600E) inhibitors. |
Central South University |
| 23376011 |
37 |
Potent BRAF kinase inhibitors based on 2,4,5-trisubstituted imidazole with naphthyl and benzothiophene 4-substituents. |
The Institute of Cancer Research |
| 30978288 |
113 |
A Selective and Brain Penetrant p38?MAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
Northwestern University |
| 23116892 |
1 |
Structural modifications of a 3-methoxy-2-aminopyridine compound to reduce potential for mutagenicity and time-dependent drug-drug interaction. |
Pfizer |
| 22954737 |
28 |
Pyrazolopyridine inhibitors of B-Raf(V600E). Part 4: rational design and kinase selectivity profile of cell potent type II inhibitors. |
Array Biopharma |
| 22858139 |
25 |
Combining pharmacophore, docking and substructure search approaches to identify and optimize novel B-RafV600E inhibitors. |
Chinese Academy of Sciences |
| 22763369 |
1 |
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 |
| 22196124 |
48 |
Potent and selective pyrazolo[1,5-a]pyrimidine based inhibitors of B-Raf(V600E) kinase with favorable physicochemical and pharmacokinetic properties. |
Array Biopharma |
| 22534450 |
36 |
The discovery of potent and selective pyridopyrimidin-7-one based inhibitors of B-RafV600E kinase. |
Array Biopharma |
| 22361686 |
3 |
Design, synthesis and biological evaluation of novel (E)-?-benzylsulfonyl chalcone derivatives as potential BRAF inhibitors. |
Nanjing University |
| 22264479 |
56 |
Design and synthesis of 6,6-fused heterocyclic amides as raf kinase inhibitors. |
Novartis Institutes For Biomedical Research |
| 24900315 |
42 |
Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors. |
Array Biopharma |
| 22209462 |
16 |
Pyrazolopyridine inhibitors of B-Raf(V600E). Part 3: an increase in aqueous solubility via the disruption of crystal packing. |
Array Biopharma |
| 21807507 |
55 |
4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors. |
Ambit Biosciences |
| 21802293 |
69 |
Pyrazolopyridine inhibitors of B-RafV600E. Part 2: structure-activity relationships. |
Arraybiopharma |
| 20667740 |
32 |
Novel tricyclic pyrazole BRAF inhibitors with imidazole or furan central scaffolds. |
The Institute of Cancer Research |
| 20597484 |
170 |
Novel hinge binder improves activity and pharmacokinetic properties of BRAF inhibitors. |
The Institute of Cancer Research |
| 20199087 |
91 |
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 |
| 20149658 |
1 |
Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines. |
Korea Institute of Science and Technology |
| 19271717 |
96 |
Bioactive metabolites from the endophytic fungus Stemphylium globuliferum isolated from Mentha pulegium. |
Heinrich-Heine-Universitat |
| 19473026 |
80 |
Novel potent BRAF inhibitors: toward 1 nM compounds through optimization of the central phenyl ring. |
The Institute of Cancer Research |
| 18494522 |
244 |
Cytotoxic metabolites from the fungal endophyte Alternaria sp. and their subsequent detection in its host plant Polygonum senegalense. |
Heinrich-Heine-Universit£T |
| 30216849 |
18 |
Recent advances of RAF (rapidly accelerated fibrosarcoma) inhibitors as anti-cancer agents. |
University of Science & Technology (Ust) |
| 29940463 |
46 |
Design and biological evaluation of novel triaryl pyrazoline derivatives with dioxane moiety for selective BRAF |
Nanjing University |
| 29578342 |
35 |
Isolation, Characterization, and Structure-Activity Relationship Analysis of Abietane Diterpenoids from Callicarpa bodinieri as Spleen Tyrosine Kinase Inhibitors. |
Yunnan University |
| 30085668 |
41 |
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 |
| 29727562 |
14 |
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 |
| 29549841 |
8 |
Design, synthesis and anticancer evaluation of novel spirobenzo[h]chromene and spirochromane derivatives with dual EGFR and B-RAF inhibitory activities. |
Beni-Suef University |
| 29407977 |
30 |
Effects of rigidity on the selectivity of protein kinase inhibitors. |
University of Southern California |
| 29631788 |
68 |
Design and discovery of thioether and nicotinamide containing sorafenib analogues as multikinase inhibitors targeting B-Raf, B-Raf |
Yantai University |
| 29266937 |
36 |
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy? |
University of South Australia |
| 29461827 |
35 |
Current Insights of BRAF Inhibitors in Cancer. |
Albert Einstein College of Medicine |
| 28505447 |
30 |
Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins. |
Temple University |
| 29107542 |
35 |
Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors. |
Novartis Institutes For Biomedical Research |
| 28927801 |
16 |
Design, synthesis and antitumor activity of Novel Sorafenib derivatives bearing pyrazole scaffold. |
Jiangxi Science & Technology Normal University |
| 29886324 |
28 |
Design, synthesis, biological evaluation and molecular modeling of novel 1H-pyrazolo[3,4-d]pyrimidine derivatives as BRAF |
Southern Medical University |
| 29107425 |
90 |
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
Korea Institute of Science & Technology (Kist) |
| 29032031 |
91 |
Discovery of novel anti-angiogenesis agents. Part 8: Diaryl thiourea bearing 1H-indazole-3-amine as multi-target RTKs inhibitors. |
Xi'An Jiaotong University |
| 29102175 |
91 |
Discovery of novel anti-angiogenesis agents. Part 7: Multitarget inhibitors of VEGFR-2, TIE-2 and EphB4. |
Xi'An Jiaotong University |
| 28586211 |
40 |
Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-? Motif Kinase (ZAK) Inhibitors. |
University of Macau |
| 28242553 |
36 |
Design, synthesis and evaluation of derivatives based on pyrimidine scaffold as potent Pan-Raf inhibitors to overcome resistance. |
China Pharmaceutical University |
| 29561151 |
58 |
4,6-Diaminopyrimidines as Highly Preferred Troponin I-Interacting Kinase (TNNI3K) Inhibitors. |
TBA |
| 21985426 |
27 |
Chromone containing sulfonamides as potent carbonic anhydrase inhibitors. |
Ondokuz Mayis University |
| 15831442 |
46 |
Beneficial effects of a new 20-hydroxyeicosatetraenoic acid synthesis inhibitor, TS-011 [N-(3-chloro-4-morpholin-4-yl) phenyl-N'-hydroxyimido formamide], on hemorrhagic and ischemic stroke. |
Taisho Pharmaceutical |
| 15798001 |
56 |
Inhibitory effect of the 4-aminotetrahydroquinoline derivatives, selective chemoattractant receptor-homologous molecule expressed on T helper 2 cell antagonists, on eosinophil migration induced by prostaglandin D2. |
Kyowa Hakko Kogyo |
| 2904784 |
109 |
Neuroleptic binding to human brain receptors: relation to clinical effects. |
Mayo Clinic |
| 2017157 |
12 |
Regulation of dopamine D2 receptors by sodium and pH. |
Medical Research Service |
| 19549076 |
26 |
Carbonic anhydrase inhibitors: inhibition of cytosolic carbonic anhydrase isozymes II and VII with simple aromatic sulfonamides and some azo dyes. |
Universita Degli Studi Di Firenze |
| 1828505 |
19 |
Characterization and distribution of [125I]epidepride binding to dopamine D2 receptors in basal ganglia and cortex of human brain. |
University of Pennsylvania |
| 19811924 |
23 |
Development of a highly water-soluble peptide-based human neutrophil elastase inhibitor; AE-3763 for treatment of acute organ injury. |
Dainippon Sumitomo Pharma |
| 17949010 |
16 |
Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity. |
Pfizer |
| 15115388 |
36 |
Novel N-arylpyrazolo[3,2-c]-based ligands for the glucocorticoid receptor: receptor binding and in vivo activity. |
Merck Research Laboratories |
| 17915852 |
6 |
Structures of Human Monoamine Oxidase B Complexes with Selective Noncovalent Inhibitors: Safinamide and Coumarin Analogs. |
University of Pavia |
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