The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28249207 |
78 |
Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet?-cells from apoptosis. |
East China Normal University |
28268139 |
25 |
Discovery of new Syk inhibitors through structure-based virtual screening. |
Second Military Medical University |
27789138 |
355 |
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors. |
Abbvie Bioresearch Center |
27839918 |
28 |
Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK). |
Takeda California |
27771180 |
49 |
Identification of 4-(2-furanyl)pyrimidin-2-amines as Janus kinase 2 inhibitors. |
Central China Normal University |
27994755 |
18 |
Carboxamide Spleen Tyrosine Kinase (Syk) Inhibitors: Leveraging Ground State Interactions To Accelerate Optimization. |
Merck |
27288183 |
130 |
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors. |
Southeast University |
27003761 |
120 |
Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor. |
Nerviano Medical Sciences |
26951753 |
336 |
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors. |
Novartis Institutes For Biomedical Research |
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 |
26384287 |
65 |
Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors. |
Kangwon National University |
26342867 |
52 |
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors. |
Sichuan University |
26320624 |
45 |
Orally bioavailable Syk inhibitors with activity in a rat PK/PD model. |
Novartis Institutes For Biomedical Research |
26318067 |
34 |
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors. |
Hanyang University |
26222319 |
192 |
Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy. |
Nerviano Medical Sciences |
26071372 |
89 |
Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3. |
Astellas Pharma |
26005534 |
158 |
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors. |
Genomics Institute of The Novartis Research Foundation |
25633741 |
67 |
Discovery and profiling of a selective and efficacious Syk inhibitor. |
Novartis Institutes For Biomedical Research |
25625541 |
58 |
Overcoming mutagenicity and ion channel activity: optimization of selective spleen tyrosine kinase inhibitors. |
Merck |
25743214 |
12 |
LEADOPT: an automatic tool for structure-based lead optimization, and its application in structural optimizations of VEGFR2 and SYK inhibitors. |
Sichuan University |
25872982 |
57 |
Application of cultured human mast cells (CHMC) for the design and structure-activity relationship of IgE-mediated mast cell activation inhibitors. |
Amarit Bioscience |
25827523 |
275 |
Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors. |
Vertex Pharmaceuticals |
24980703 |
296 |
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors. |
Nerviano Medical Sciences |
25589930 |
62 |
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation. |
Lexicon Pharmaceuticals |
25479567 |
50 |
Recent advances in the discovery of small molecule inhibitors of interleukin-1 receptor-associated kinase 4 (IRAK4) as a therapeutic target for inflammation and oncology disorders. |
Nimbus Discovery |
25409491 |
83 |
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. |
Zhejiang University |
25369270 |
93 |
Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634. |
Galapagos |
24139169 |
175 |
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases. |
Nerviano Medical Sciences |
24779514 |
128 |
Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase. |
Gilead Sciences |
24726806 |
108 |
Syk inhibitors with high potency in presence of blood. |
Novartis Institutes For Biomedical Research |
24900823 |
6 |
Phenyl carboxamide analogues as spleen tyrosine kinase (syk) inhibitors. |
Dart Neuroscience |
24520947 |
87 |
Using ovality to predict nonmutagenic, orally efficacious pyridazine amides as cell specific spleen tyrosine kinase inhibitors. |
Hoffmann-La Roche |
24569110 |
11 |
Discovery of dual ZAP70 and Syk kinases inhibitors by docking into a rare C-helix-out conformation of Syk. |
University of Zurich |
24389511 |
25 |
Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors. |
Zhejiang University |
23993776 |
17 |
Discovery of ZAP70 inhibitors by high-throughput docking into a conformation of its kinase domain generated by molecular dynamics. |
University of Zurich |
24100158 |
148 |
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90). |
Nerviano Medical Sciences |
24044867 |
86 |
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
Califia Bio |
23917087 |
32 |
Inhibitors of switch kinase 'spleen tyrosine kinase' in inflammation and immune-mediated disorders: a review. |
Punjabi University |
23742252 |
81 |
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase |
Genomics Institute of The Novartis Research Foundation |
23350847 |
169 |
Pyrrolopyrazines as selective spleen tyrosine kinase inhibitors. |
Hoffmann-La Roche |
23362959 |
72 |
Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and in vivo. |
Sichuan University |
21903390 |
79 |
Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
Glaxosmithkline |
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 |
23151054 |
15 |
Rational design of highly selective spleen tyrosine kinase inhibitors. |
Hoffmann-La Roche |
22257213 |
98 |
Discovery and development of spleen tyrosine kinase (SYK) inhibitors. |
Rigel |
22695126 |
98 |
Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases. |
Abbott Laboratories |
22452518 |
22 |
Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo. |
Sichuan University |
22372864 |
25 |
Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases. |
Hanmi Research Center |
24900264 |
106 |
The Discovery of VX-745: A Novel and Selective p38a Kinase Inhibitor. |
TBA |
22464456 |
27 |
X-ray crystallographic structure-based design of selective thienopyrazole inhibitors for interleukin-2-inducible tyrosine kinase. |
Sanofi Us |
15975507 |
13 |
Features of selective kinase inhibitors. |
University of California San Francisco |
20138514 |
93 |
3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta. |
Vertex Pharmaceuticals |
19716697 |
110 |
The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II. |
Boehringer Ingelheim Pharmaceuticals |
18183025 |
12060 |
A quantitative analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
19394223 |
50 |
Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase. |
Glaxosmithkline |
19397322 |
58 |
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
National Cancer Institute-Bethesda |
18823784 |
38 |
Structure-activity relationship studies of imidazo[1,2-c]pyrimidine derivatives as potent and orally effective Syk family kinases inhibitors. |
Kissei Pharmaceutical |
18359226 |
50 |
Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors. |
Bristol-Myers Squibb Research and Development |
18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University of Oxford |
18024135 |
1 |
A photoswitchable ITAM peptidomimetic: synthesis and real time surface plasmon resonance (SPR) analysis of the effects of cis-trans isomerization on binding. |
Utrecht University |
17997320 |
29 |
Novel pyrazolo[1,5-a]pyrimidines as c-Src kinase inhibitors that reduce IKr channel blockade. |
Kissei Pharmaceutical |
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 |
17095233 |
45 |
Synthesis and c-Src inhibitory activity of imidazo[1,5-a]pyrazine derivatives as an agent for treatment of acute ischemic stroke. |
Kissei Pharmaceutical |
16876403 |
85 |
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure. |
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories |
12657254 |
10 |
Amino propynyl benzoic acid building block in rigid spacers of divalent ligands binding to the Syk SH2 domains with equally high affinity as the natural ligand. |
Utrecht University |
12617920 |
41 |
Discovery of novel and selective IKK-beta serine-threonine protein kinase inhibitors. Part 1. |
Kyoto 619-0216 |
12941345 |
42 |
Potent small molecule inhibitors of spleen tyrosine kinase (Syk). |
Aventis Pharmaceuticals |
22310227 |
89 |
5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors. |
Glaxosmithkline |
16249345 |
25 |
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580. |
Glaxosmithkline |
22136433 |
67 |
7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes. |
Ludwig-Maximilians University of Munich |
22014550 |
337 |
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
Ansaris |
21981714 |
48 |
Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer. |
Genentech |
22014755 |
36 |
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells. |
Hanyang University |
21999461 |
90 |
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase. |
RhôNe-Poulenc Rorer |
22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
21936542 |
143 |
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. |
Novartis Institute For Biomedical Research |
21699136 |
16 |
Selectivity of kinase inhibitor fragments. |
Glaxosmithkline |
21705217 |
60 |
Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors. |
Bristol-Myers Squibb |
21620699 |
51 |
Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors. |
Pfizer |
21470862 |
110 |
NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor. |
Nerviano Medical Sciences |
21341675 |
266 |
Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors. |
Glaxosmithkline |
24900229 |
41 |
Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery. |
TBA |
21035336 |
42 |
5-amino-pyrazoles as potent and selective p38a inhibitors. |
Bristol-Myers Squibb Research and Development |
20873740 |
111 |
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding. |
Nerviano Medical Sciences |
19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
19039322 |
50 |
Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
Center For Molecular Medicine of The Austrian Academy of Sciences |
16783341 |
34 |
Rational design of inhibitors that bind to inactive kinase conformations. |
Novartis Research Foundation |
20050669 |
61 |
Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer. |
Genentech |
19879134 |
94 |
Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4. |
Cgi Pharmaceuticals |
20141146 |
234 |
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors. |
Nerviano Medical Sciences |
19926477 |
100 |
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization. |
Abbott Laboratories |
19427203 |
28 |
Synthetic staurosporines via a ring closing metathesis strategy as potent JAK3 inhibitors and modulators of allergic responses. |
Johnson & Johnson Pharmaceutical Research & Development |
19414255 |
58 |
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase. |
Vertex Pharmaceuticals |
19285393 |
90 |
Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors. |
Glaxosmithkline |
19254842 |
141 |
Pharmacophore modeling study based on known spleen tyrosine kinase inhibitors together with virtual screening for identifying novel inhibitors. |
Sichuan University |
18938080 |
102 |
Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK). |
Vertex Pharmaceuticals |
18799313 |
20 |
Identification of novel protein kinase CK1 delta (CK1delta) inhibitors through structure-based virtual screening. |
Università |
17827009 |
116 |
Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors. |
Tanabe Research Laboratories Usa |
16970394 |
147 |
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity. |
Amgen |
16789733 |
41 |
Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
16682193 |
62 |
Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
16216497 |
67 |
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection. |
Abbott Bioresearch Center |
15711537 |
653 |
A small molecule-kinase interaction map for clinical kinase inhibitors. |
Ambit Biosciences |
15566298 |
34 |
The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase. |
Bristol-Myers Squibb |
15317463 |
16 |
Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15225718 |
35 |
Synthesis and structure-activity relationships of novel IKK-beta inhibitors. Part 3: Orally active anti-inflammatory agents. |
Kyoto 619-0216 |
12672234 |
64 |
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase. |
Boehringer Ingelheim Pharmaceuticals |
12668002 |
57 |
Discovery and SAR of novel Naphthyridines as potent inhibitors of spleen tyrosine kinase (SYK). |
Boehringer Ingelheim Pharmaceuticals |
12139450 |
29 |
Discovery of 2-phenylamino-imidazo[4,5-h]isoquinolin-9-ones: a new class of inhibitors of lck kinase. |
Boehringer Ingelheim Pharmaceuticals |
12086485 |
10 |
Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
Boehringer Ingelheim Pharmaceuticals |
11741491 |
12 |
Design and synthesis of non-peptidic inhibitors for the Syk C-terminal SH2 domain based on structure-based in-silico screening. |
Waseda University |
32433887 |
62 |
Discovery of Highly Selective Inhibitors of Calmodulin-Dependent Kinases That Restore Insulin Sensitivity in the Diet-Induced Obesity |
University of Nottingham |
11462983 |
50 |
Design, synthesis, and biological evaluation of a series of lavendustin A analogues that inhibit EGFR and Syk tyrosine kinases, as well as tubulin polymerization. |
Purdue University |
32292564 |
138 |
Efficacy and Tolerability of Pyrazolo[1,5- |
The Genomics Institute of The Novartis Research Foundation |
32292557 |
119 |
Discovery of Lanraplenib (GS-9876): A Once-Daily Spleen Tyrosine Kinase Inhibitor for Autoimmune Diseases. |
Gilead Sciences |
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 |
27429068 |
54 |
Evolution of a Novel, Orally Bioavailable Series of PI3K? Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
Glaxosmithkline R&D |
27578246 |
158 |
Optimisation of a novel series of potent and orally bioavailable azanaphthyridine SYK inhibitors. |
Glaxosmithkline R&D |
10571165 |
30 |
Nonpeptidic SH2 inhibitors of the tyrosine kinase ZAP-70. |
Ariad Pharmaceuticals |
30532965 |
81 |
Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase ? through a Deconstruction and Regrowth Approach. |
Glaxosmithkline R&D |
31693351 |
473 |
Discovery of 4 |
TBA |
9871562 |
2 |
1-Methoxy-agroclavine from Penicillium sp. WC75209, a novel inhibitor of the Lck tyrosine kinase. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
31074988 |
95 |
Rational Design of 5-(4-(Isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine (VX-970, M6620): Optimization of Intra- and Intermolecular Polar Interactions of a New Ataxia Telangiectasia Mutated and Rad3-Related (ATR) Kinase Inhibitor. |
Vertex Pharmaceuticals (Europe) |
30987781 |
88 |
Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies. |
Southeast University |
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 |
30340900 |
37 |
Design, synthesis, and biological evaluation of novel aminopyrimidinylisoindolines as AXL kinase inhibitors. |
Korea University |
31526603 |
379 |
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application. |
Takeda Pharmaceutical |
26505898 |
123 |
Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies. |
Novartis Institutes For Biomedical Research |
26509640 |
234 |
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders. |
Abbvie Bioresearch Center |
30249354 |
112 |
Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease. |
Glaxosmithkline R&D |
30082069 |
359 |
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors. |
Vertex Pharmaceuticals |
29945794 |
193 |
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups. |
Vertex Pharmaceuticals |
29198867 |
46 |
Design and synthesis of novel pyrimidine analogs as highly selective, non-covalent BTK inhibitors. |
Carna Biosciences |
29132752 |
3 |
Drug-target interactions that involve the replacement or displacement of magnesium ions. |
Bristol-Myers Squibb Research and Development |
29631132 |
33 |
The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review. |
Shaanxi University of Science & Technology |
29107425 |
90 |
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
Korea Institute of Science & Technology (Kist) |
28259529 |
31 |
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
The Ohio State University |
23230954 |
17 |
Synthesis and biological evaluation of novel series of aminopyrimidine derivatives as urease inhibitors and antimicrobial agents. |
Solapur University |
22233540 |
7 |
Kinetic characterization of a slow-binding inhibitor of Bla2: thiomaltol. |
Baylor University |
21679053 |
22 |
Acetaldehyde-derived modifications on cytosolic human carbonic anhydrases. |
University of Tampere and Tampere University Hospital |
23828198 |
7 |
Key mutations alter the cytochrome P450 BM3 conformational landscape and remove inherent substrate bias. |
University of Manchester |
9933142 |
67 |
Comparisons of hallucinogenic phenylisopropylamine binding affinities at cloned human 5-HT2A, -HT(2B) and 5-HT2C receptors. |
Eli Lilly |
19780074 |
6 |
Development of new and selective Trypanosoma cruzi trans-sialidase inhibitors from sulfonamide chalcones and their derivatives. |
University of British Columbia |
21609408 |
6 |
Pyrone-based inhibitors of metalloproteinase types 2 and 3 may work as conformation-selective inhibitors. |
University of California San Diego |
2531826 |
24 |
[125]I-spectramide: a novel benzamide displaying potent and selective effects at the D2 dopamine receptor. |
Nida Addiction Research Center |
16611214 |
84 |
Synthesis and molecular modelling of novel substituted-4,5-dihydro-(1H)-pyrazole derivatives as potent and highly selective monoamine oxidase-A inhibitors. |
UniversitÀ |
9383449 |
21 |
Structure-activity studies of rapamycin analogs: evidence that the C-7 methoxy group is part of the effector domain and positioned at the FKBP12-FRAP interface. |
Smithkline Beecham Pharmaceuticals |
19338356 |
21 |
Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists. |
Acadia Pharmaceuticals |
17502144 |
89 |
The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-alpha and IKK-beta kinases. |
Gsk |
16107141 |
22 |
Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure. |
Glaxosmithkline |
12704428 |
9 |
Insights into antifolate resistance from malarial DHFR-TS structures. |
Mahidol University |
15588077 |
15 |
Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1). |
Merck Research Laboratories |
15808463 |
35 |
Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors. |
Abbott Laboratories |
16392822 |
87 |
2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]-1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV. |
National Health Research Institutes |
8667360 |
46 |
Tyrphostins. 5. Potent inhibitors of platelet-derived growth factor receptor tyrosine kinase: structure-activity relationships in quinoxalines, quinolines, and indole tyrphostins. |
Hebrew University of Jerusalem |
11462982 |
33 |
Tyrosine kinase inhibitors. 18. 6-Substituted 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as soluble, irreversible inhibitors of the epidermal growth factor receptor. |
University of Auckland |
8558522 |
26 |
2-Sulfonyl-4-chloroanilino moiety: a potent pharmacophore for the anti-human immunodeficiency virus type 1 activity of pyrrolyl aryl sulfones. |
Universita Di Roma |