The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28591512 |
114 |
Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines. |
Glaxosmithkline |
| 28230986 |
7 |
Design, Synthesis, and Evaluation of a Novel Series of Oxadiazine Gamma Secretase Modulators for Familial Alzheimer's Disease. |
Forum Pharmaceuticals |
| 28038328 |
17 |
Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3). |
East China University of Science and Technology |
| 28072531 |
120 |
Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension. |
Arena Pharmaceuticals |
| 28111141 |
58 |
The design and synthesis of novel spirocyclic heterocyclic sulfone ROMK inhibitors as diuretics. |
Merck |
| 28089699 |
63 |
Investigation of piperazine benzamides as humanß |
Merck |
| 28337320 |
21 |
Discovery and Assessment of Atropisomers of (±)-Lesinurad. |
Wuxi Apptec |
| 28523106 |
1 |
Discovery of Fluorine-Containing Benzoxazinyl-oxazolidinones for the Treatment of Multidrug Resistant Tuberculosis. |
Peking Union Medical College and Chinese Academy of Medical Sciences |
| 28254166 |
81 |
Discovery of novel BTK inhibitors with carboxylic acids. |
Merck |
| 28151659 |
89 |
Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases. |
Queen Mary University of London |
| 28064141 |
12 |
Methoxylated 2'-hydroxychalcones as antiparasitic hit compounds. |
University of Modena and Reggio Emilia |
| 28523109 |
79 |
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4. |
Glaxosmithkline |
| 28185720 |
42 |
Discovery of phenyl acetamides as potent and selective GPR119 agonists. |
Merck |
| 27958732 |
93 |
Design and Synthesis of a New Series of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes asa7 Nicotinic Receptor Agonists. 1. Development of Pharmacophore and Early Structure-Activity Relationship. |
Bristol-Myers Squibb |
| 27855359 |
15 |
Discovery of benzimidazole derivatives as modulators of mitochondrial function: A potential treatment for Alzheimer's disease. |
Korea Institute of Science and Technology |
| 27914948 |
36 |
Triazolopyridine ethers as potent, orally active mGlu |
Bristol-Myers Squibb |
| 27517811 |
12 |
Synthesis and T-type calcium channel-blocking effects of aryl(1,5-disubstituted-pyrazol-3-yl)methyl sulfonamides for neuropathic pain treatment. |
Korea Institute of Science & Technology (Kist) |
| 27769670 |
5 |
Bis(N-amidinohydrazones) and N-(amidino)-N'-aryl-bishydrazones: New classes of antibacterial/antifungal agents. |
University of Kentucky |
| 28105289 |
51 |
Development of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes] asa7 Nicotinic Receptor Agonists. |
Bristol-Myers Squibb Research and Development |
| 27866818 |
84 |
The discovery of quinoline based single-ligand human H |
Glaxosmithkline |
| 27836401 |
57 |
Novel bicyclo[3.1.0]hexane analogs as antagonists of metabotropic glutamate 2/3 receptors for the treatment of depression. |
Eli Lilly |
| 27815121 |
132 |
Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects. |
Merck |
| 27994755 |
18 |
Carboxamide Spleen Tyrosine Kinase (Syk) Inhibitors: Leveraging Ground State Interactions To Accelerate Optimization. |
Merck |
| 27994747 |
66 |
Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes. |
Merck |
| 27994738 |
50 |
Sulfonamides as Selective Na |
Amgen |
| 27994728 |
23 |
Pyrazole Inhibitors of GluN2B NMDA Receptor Subunit. |
Dart Neuroscience |
| 27789141 |
58 |
II. Discovery of a novel series of CXCR3 antagonists with a beta amino acid core. |
Sanofi |
| 27780638 |
65 |
5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents. |
University of Washington |
| 27769623 |
21 |
Metabolism-based structure optimization: Discovery of a potent and orally available tyrosine kinase ALK inhibitor bearing the tetracyclic benzo[b]carbazolone core. |
Ocean University of China |
| 27769621 |
109 |
Discovery of imidazopyridazines as potent Pim-1/2 kinase inhibitors. |
Amgen |
| 27736063 |
34 |
Design, Synthesis, and Pharmacological Evaluation of 2-(2,5-Dimethyl-5,6,7,8-tetrahydroquinolin-8-yl)-N-aryl Propanamides as Novel Smoothened (Smo) Antagonists. |
University of Chinese Academy of Sciences |
| 27564532 |
3 |
Discovery of a Potent Acyclic, Tripeptidic, Acyl Sulfonamide Inhibitor of Hepatitis C Virus NS3 Protease as a Back-up to Asunaprevir with the Potential for Once-Daily Dosing. |
Bristol-Myers Squibb Research and Development |
| 27933954 |
122 |
Discovery of [5-Amino-1-(2-methyl-3H-benzimidazol-5-yl)pyrazol-4-yl]-(1H-indol-2-yl)methanone (CH5183284/Debio 1347), An Orally Available and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor. |
Chugai Pharmaceutical |
| 27709945 |
62 |
Design, Synthesis, and Biological Evaluation of Novel Tetrahydroprotoberberine Derivatives (THPBs) as Selectivea |
Chinese Academy of Sciences |
| 27690432 |
75 |
Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986). |
Charles River Discovery Research Services |
| 27637151 |
35 |
Discovery of novel 2',4'-dimethyl-[4,5'-bithiazol]-2-yl amino derivatives as orally bioavailable TRPV4 antagonists for the treatment of pain: Part 1. |
Shionogi |
| 27583770 |
82 |
Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locke |
Bristol-Myers Squibb Research and Development |
| 27548392 |
76 |
Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor. |
Janssen Research and Development |
| 27527804 |
109 |
Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK). |
Teva Branded Pharmaceutical Products R & D |
| 27660692 |
70 |
Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-¿ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate. |
Infinity Pharmaceuticals |
| 27634196 |
60 |
Discovery of novel 2',4'-dimethyl-[4,5'-bithiazol]-2-yl amino derivatives as orally bioavailable TRPV4 antagonists for the treatment of pain: Part 2. |
Shionogi |
| 27564135 |
499 |
1,2,4-Triazolyl 5-Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists. |
Aptuit |
| 27502700 |
36 |
Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension. |
Novartis Institutes of Biomedical Research (Nibr) |
| 27326332 |
66 |
Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARa Selective Agonist. |
Bristol-Myers Squibb |
| 27078757 |
121 |
Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2-(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor-1 Receptor (IGF-1R). |
Astrazeneca |
| 27096048 |
80 |
Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders. |
Peking Union Medical College and Chinese Academy of Medical Sciences |
| 27256912 |
36 |
Discovery of hydroxyl 1,2-diphenylethanamine analogs as potent cholesterol ester transfer protein inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
| 27190600 |
48 |
Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
Merck Research Laboratories |
| 26999509 |
7 |
Discovery of Potent Benzofuran-Derived Diapophytoene Desaturase (CrtN) Inhibitors with Enhanced Oral Bioavailability for the Treatment of Methicillin-Resistant Staphylococcus aureus (MRSA) Infections. |
East China University of Science and Technology |
| 27096041 |
27 |
Core Replacements in a Potent Series of VEGFR-2 Inhibitors and Their Impact on Potency, Solubility, and hERG. |
Novartis Institutes For Biomedical Research |
| 27038498 |
33 |
Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine. |
Gilead Sciences |
| 26985319 |
36 |
Potent and Selective CK2 Kinase Inhibitors with Effects on Wnt Pathway Signaling in Vivo. |
Astrazeneca |
| 27229618 |
30 |
Novel free fatty acid receptor 1 (GPR40) agonists based on 1,3,4-thiadiazole-2-carboxamide scaffold. |
Saint Petersburg State University |
| 27173799 |
97 |
Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics. |
Shanghai Institute of Materia Medica |
| 27106708 |
130 |
The discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors. |
Merck Research Laboratories |
| 27003636 |
51 |
Synthesis and Biological Evaluation of Novels1 Receptor Ligands for Treating Neuropathic Pain: 6-Hydroxypyridazinones. |
Huazhong University of Science and Technology |
| 26985317 |
20 |
Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5. |
Bristol-Myers Squibb Research & Development |
| 26985314 |
23 |
Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain Aß Reduction in Rodents. |
Bristol-Myers Squibb |
| 26985309 |
8 |
Astemizole Derivatives as Fluorescent Probes for hERG Potassium Channel Imaging. |
Shandong University |
| 27117428 |
50 |
1-Sulfonyl-6-Piperazinyl-7-Azaindoles as potent and pseudo-selective 5-HT6 receptor antagonists. |
Selvita |
| 26937601 |
55 |
Structure-Based Design of an Iminoheterocyclicß-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aß in Nonhuman Primates. |
Merck Research Laboratories |
| 26924461 |
45 |
Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series. |
Bristol-Myers Squibb Research and Development |
| 27117261 |
31 |
Amine-free melanin-concentrating hormone receptor 1 antagonists: Novel non-basic 1-(2H-indazole-5-yl)pyridin-2(1H)-one derivatives and mitigation of mutagenicity in Ames test. |
Takeda Pharmaceutical |
| 27017115 |
77 |
Differentiation of ROMK potency from hERG potency in the phenacetyl piperazine series through heterocycle incorporation. |
Merck Research Laboratories |
| 26876931 |
36 |
Optimization of N'-(arylsulfonyl)pyrazoline-1-carboxamidines by exploiting a novel interaction site in the 5-HT6 antagonistic binding pocket. |
Abbott Healthcare Products |
| 26756222 |
70 |
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants. |
Pfizer |
| 26951750 |
59 |
Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors. |
Novartis Institutes For Biomedical Research |
| 26923695 |
43 |
Novel 2,4-diaminopyrimidines bearing tetrahydronaphthalenyl moiety against anaplastic lymphoma kinase (ALK): Synthesis, in vitro, ex vivo, and in vivo efficacy studies. |
Chungbuk National University |
| 27055939 |
2 |
Novel tricyclics (e.g., GSK945237) as potent inhibitors of bacterial type IIA topoisomerases. |
Glaxosmithkline |
| 26852363 |
72 |
Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore. |
Merck |
| 26951894 |
376 |
1,2,4-Triazolyl octahydropyrrolo[2,3-b]pyrroles: A new series of potent and selective dopamine D3 receptor antagonists. |
Aptuit |
| 26898814 |
154 |
SAR exploration at the C-3 position of tetrahydro-ß-carboline sstr3 antagonists. |
Merck Research Laboratories |
| 26819673 |
55 |
Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat. |
Astrazeneca |
| 26900657 |
1 |
New direct inhibitors of InhA with antimycobacterial activity based on a tetrahydropyran scaffold. |
University of Ljubljana |
| 26935940 |
23 |
Emerging targets and new small molecule therapies in Parkinson's disease treatment. |
School of Medicine of University of Electronic Science and Technology of China |
| 26751273 |
92 |
Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses. |
Glaxosmithkline |
| 26736071 |
79 |
Melanin-Concentrating Hormone Receptor 1 Antagonists Lacking an Aliphatic Amine: Synthesis and Structure-Activity Relationships of Novel 1-(Imidazo[1,2-a]pyridin-6-yl)pyridin-2(1H)-one Derivatives. |
Takeda Pharmaceutical |
| 26713112 |
36 |
Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety. |
Genentech |
| 26704965 |
229 |
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models. |
University of Illinois At Chicago |
| 26700945 |
68 |
Structure-Based Discovery of Novel and Selective 5-Hydroxytryptamine 2B Receptor Antagonists for the Treatment of Irritable Bowel Syndrome. |
National Institute of Biological Sciences, Beijing |
| 26709102 |
142 |
Discovery of Vibegron: A Potent and Selectiveß3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder. |
Merck Research Laboratories |
| 26804230 |
48 |
Optimization of tetrahydronaphthalene inhibitors of Raf with selectivity over hERG. |
Takeda Pharmaceutical |
| 26652717 |
96 |
Discovery and Characterization of (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one (BMN 673, Talazoparib), a Novel, Highly Potent, and Orally Efficacious Poly(ADP-ribose) Polymerase-1/2 Inhibitor, as an Anticancer Agent. |
Biomarin Pharmaceutical |
| 26761776 |
62 |
Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent. |
Sungkyunkwan University |
| 26747393 |
4 |
Discovery and preclinical evaluation of potent, orally bioavailable, metabolically stable cyclopropylindolobenzazepine acylsulfonamides as thumb site 1 inhibitors of the hepatitis c virus NS5B RNA-dependent, RNA polymerase. |
Bristol-Myers Squibb Pharmaceutical Research and Development |
| 26653180 |
61 |
Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors. |
Eli Lilly |
| 26640981 |
3 |
Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials? |
University of Belgrade |
| 26684851 |
86 |
Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia. |
Janssen Pharmaceutica |
| | 29 |
Synthesis and structure-activity relationships of novel 3′-Hty-substituted pneumocandins |
TBA |
| 28209465 |
124 |
Identification of highly potent and selective PI3K? inhibitors. |
Bristol-Myers Squibb |
| 29461823 |
2 |
Development of (6 R)-2-Nitro-6-[4-(trifluoromethoxy)phenoxy]-6,7-dihydro-5 H-imidazo[2,1- b][1,3]oxazine (DNDI-8219): A New Lead for Visceral Leishmaniasis. |
University of Auckland |
| 29457982 |
80 |
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. |
Genentech |
| 29283260 |
113 |
Targeting Acidic Mammalian chitinase Is Effective in Animal Model of Asthma. |
Oncoarendi Therapeutics |
| 28994286 |
2 |
Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
Crystal Pharmatech |
| 28415011 |
54 |
Design and synthesis of novel xanthine derivatives as potent and selective A |
Advinus Therapeutics |
| 28892629 |
74 |
Development of (4-Cyanophenyl)glycine Derivatives as Reversible Inhibitors of Lysine Specific Demethylase 1. |
University of Manchester |
| 28873303 |
1 |
Discovery of Novel Macrocyclic Hedgehog Pathway Inhibitors Acting by Suppressing the Gli-Mediated Transcription. |
Shanghai Institute of Materia Medica (Simm) |
| 28408226 |
51 |
Discovery of novel aminobenzisoxazole derivatives as orally available factor IXa inhibitors. |
Mochida Pharmaceutical |
| 28385504 |
52 |
The discovery of tetrahydropyridine analogs as hNav1.7 selective inhibitors for analgesia. |
Wuxi Apptec (Shanghai) |
| 28385503 |
19 |
Novel small molecule guanidine Sigma1 inhibitors for advanced prostate cancer. |
Drexel University College of Medicine |
| 28574690 |
98 |
Design, Multicomponent Synthesis, and Anticancer Activity of a Focused Histone Deacetylase (HDAC) Inhibitor Library with Peptoid-Based Cap Groups. |
Heinrich-Heine-Universit£T D£Sseldorf |
| 28541707 |
119 |
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase? (PI3K?) Inhibitor for the Treatment of Immunological Disorders. |
Bristol-Myers Squibb |
| 28537728 |
43 |
Antimalarial Inhibitors Targeting Serine Hydroxymethyltransferase (SHMT) with in Vivo Efficacy and Analysis of their Binding Mode Based on X-ray Cocrystal Structures. |
Eth Zurich |
| 28498658 |
47 |
Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design. |
Pfizer |
| 28489379 |
165 |
Hydroxy-Substituted Heteroarylpiperazines: Novel Scaffolds for?-Arrestin-Biased D |
Friedrich-Alexander University Erlangen-Nuernberg |
| 28430437 |
19 |
Discovery of a Hepatitis C Virus NS5B Replicase Palm Site Allosteric Inhibitor (BMS-929075) Advanced to Phase 1 Clinical Studies. |
Bristol-Myers Squibb Research and Development |
| 28418664 |
32 |
Selective I |
Bristol-Myers Squibb |
| 28347666 |
45 |
Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3K?/? inhibitors for the treatment of PTEN-deficient tumours. |
Astrazeneca |
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