The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28686445 |
39 |
Discovery and Optimization of Chromeno[2,3-c]pyrrol-9(2H)-ones as Novel Selective and Orally Bioavailable Phosphodiesterase 5 Inhibitors for the Treatment of Pulmonary Arterial Hypertension. |
Sun Yat-Sen University |
| 28359790 |
110 |
Design, synthesis and optimization of 7-substituted-pyrazolo[4,3-b]pyridine ALK5 (activin receptor-like kinase 5) inhibitors. |
Takeda California |
| 28274629 |
76 |
Effects of 6-paradol, an unsaturated ketone from gingers, on cytochrome P450-mediated drug metabolism. |
Hanyang University |
| 28230986 |
7 |
Design, Synthesis, and Evaluation of a Novel Series of Oxadiazine Gamma Secretase Modulators for Familial Alzheimer's Disease. |
Forum Pharmaceuticals |
| 28212021 |
111 |
Discovery and Development of 1-[(2-Bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole Dimesylate Monohydrate (SUVN-502): A Novel, Potent, Selective and Orally Active Serotonin 6 (5-HT |
Suven Life Sciences |
| 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 |
| 28337332 |
41 |
BMS-933043, a Selectivea7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia. |
Bristol-Myers Squibb |
| 28337324 |
14 |
Discovery of GBT440, an Orally Bioavailable R-State Stabilizer of Sickle Cell Hemoglobin. |
Global Blood Therapeutics |
| 28003141 |
65 |
Identification and optimization of a novel series of indoleamine 2,3-dioxygenase inhibitors. |
Bristol-Myers Squibb Research and Development |
| 28169164 |
19 |
Structure-based design and SAR development of 5,6-dihydroimidazolo[1,5-f]pteridine derivatives as novel Polo-like kinase-1 inhibitors. |
Takeda California |
| 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 |
| 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 |
| 27579727 |
33 |
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
Janssen Pharmaceutica |
| 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 |
| 27660692 |
70 |
Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-¿ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate. |
Infinity Pharmaceuticals |
| 27326332 |
66 |
Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARa Selective Agonist. |
Bristol-Myers Squibb |
| 26914985 |
124 |
Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. |
Boehringer Ingelheim Rcv |
| 27190604 |
26 |
Discovery of Potent, Orally Bioavailable Inhibitors of Human Cytomegalovirus. |
Boehringer Ingelheim (Canada) |
| 26985323 |
5 |
Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors. |
Merck Research Laboratories |
| 26985314 |
23 |
Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain Aß Reduction in Rodents. |
Bristol-Myers Squibb |
| 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 |
| 27020304 |
31 |
Identification and biological activity of 6-alkyl-substituted 3-methyl-pyridine-2-carbonyl amino dimethyl-benzoic acid EP4 antagonists. |
Eli Lilly |
| 27055941 |
19 |
Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1). |
Bristol-Myers Squibb Research and Development |
| 26709102 |
142 |
Discovery of Vibegron: A Potent and Selectiveß3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder. |
Merck Research Laboratories |
| 26764191 |
38 |
Discovery of potent aryl-substituted 3-[(3-methylpyridine-2-carbonyl) amino]-2,4-dimethyl-benzoic acid EP4 antagonists with improved pharmacokinetic profile. |
Eli Lilly |
| 26509551 |
31 |
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases. |
Pfizer |
| 26363868 |
10 |
3-Nitrotriazole-based piperazides as potent antitrypanosomal agents. |
Northshore University Healthsystem |
| 25978966 |
65 |
Development of a novel class of potent and selective FIXa inhibitors. |
Merck Research Laboratories |
| 26313252 |
22 |
Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
Astrazeneca |
| 26288692 |
37 |
Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer. |
Bristol-Myers Squibb Research and Development |
| 26191360 |
99 |
Discovery of a Potent and Selective ROMK Inhibitor with Pharmacokinetic Properties Suitable for Preclinical Evaluation. |
Merck Research Laboratories |
| 26225459 |
48 |
Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile). |
Heptares Therapeutics |
| 26191364 |
10 |
Dimeric Macrocyclic Antagonists of Inhibitor of Apoptosis Proteins for the Treatment of Cancer. |
Bristol-Myers Squibb Research |
| 26105194 |
24 |
Design, synthesis and evaluation of MCH receptor 1 antagonists--Part III: Discovery of pre-clinical development candidate BI 186908. |
Boehringer Ingelheim Pharma |
| 26091726 |
41 |
Discovery and characterization of a potent and selective EP4 receptor antagonist. |
Eli Lilly |
| 22328583 |
132 |
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. |
Pfizer |
| 25953512 |
74 |
Discovery of (1R,2S)-2-{[(2,4-Dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide (E2006): A Potent and Efficacious Oral Orexin Receptor Antagonist. |
Eisai |
| 26087021 |
94 |
Novel Octahydropyrrolo[3,4-c]pyrroles Are Selective Orexin-2 Antagonists: SAR Leading to a Clinical Candidate. |
TBA |
| 26005524 |
147 |
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes. |
Merck Research Laboratories |
| 25879485 |
60 |
Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
Seragon Pharmaceuticals |
| 21289076 |
2 |
Reevaluation of the microsomal metabolism of montelukast: major contribution by CYP2C8 at clinically relevant concentrations. |
University of Helsinki |
| 23118326 |
5 |
Clinical pharmacokinetics, metabolism, and drug-drug interaction of carfilzomib. |
Onyx Pharmaceuticals |
| 22496391 |
40 |
Characterization of the in vitro and in vivo metabolism and disposition and cytochrome P450 inhibition/induction profile of saxagliptin in human. |
Bristol-Myers Squibb Research |
| 22645092 |
15 |
Selective mechanism-based inactivation of CYP3A4 by CYP3cide (PF-04981517) and its utility as an in vitro tool for delineating the relative roles of CYP3A4 versus CYP3A5 in the metabolism of drugs. |
Pfizer |
| 22930276 |
25 |
Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors. |
Amgen |
| 23132334 |
28 |
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor. |
Glaxosmithkline |
| 25781223 |
96 |
Utilizing structures of CYP2D6 and BACE1 complexes to reduce risk of drug-drug interactions with a novel series of centrally efficacious BACE1 inhibitors. |
The Scripps Research Institute |
| 25415535 |
118 |
Inhibitors of c-Jun N-terminal kinases: an update. |
Eberhard Karls Universit£T T£Bingen |
| 25050169 |
52 |
Optimization of 1,2,4-Triazolopyridines as Inhibitors of Human 11ß-Hydroxysteroid Dehydrogenase Type 1 (11ß-HSD-1). |
Bristol-Myers Squibb |
| 24980053 |
153 |
Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists. |
Bristol-Myers Squibb |
| 25556092 |
85 |
Selective CB2 receptor agonists. Part 2: Structure-activity relationship studies and optimization of proline-based compounds. |
Boehringer Ingelheim Pharma |
| 25453808 |
101 |
Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors. |
Bristol-Myers Squibb |
| 25330343 |
49 |
Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro. |
Translational Research Institute |
| 25310383 |
50 |
Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
Novartis Institutes For Biomedical Research |
| 25179681 |
81 |
Design, synthesis, and structure-activity and structure-pharmacokinetic relationship studies of novel [6,6,5] tricyclic fused oxazolidinones leading to the discovery of a potent, selective, and orally bioavailable FXa inhibitor. |
Chinese Academy of Sciences |
| 24900876 |
56 |
Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction. |
Astrazeneca |
| 24900838 |
30 |
Delayed and Prolonged Histone Hyperacetylation with a Selective HDAC1/HDAC2 Inhibitor. |
Merck Research Laboratories |
| 24685542 |
67 |
Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases. |
Bristol-Myers Squibb Research and Development |
| 24428186 |
10 |
Design, synthesis, and pharmacological evaluation of a novel series of pyridopyrazine-1,6-dione¿-secretase modulators. |
Pfizer |
| 24530032 |
65 |
Structure-based optimization of cyclopropyl urea derivatives as potent soluble epoxide hydrolase inhibitors for potential decrease of renal injury without hypotensive action. |
Dainippon Sumitomo Pharma |
| 24900630 |
16 |
Synthesis and in vitro and in vivo pharmacological evaluation of new 4-aminoquinoline-based compounds. |
University of Cape Town |
| 24252545 |
12 |
Discovery of an irreversible HCV NS5B polymerase inhibitor. |
Merck Research Laboratories |
| 24900593 |
45 |
Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development. |
Glaxosmithkline |
| 24090135 |
201 |
Design of substituted imidazolidinylpiperidinylbenzoic acids as chemokine receptor 5 antagonists: potent inhibitors of R5 HIV-1 replication. |
Sanofi |
| 23973211 |
145 |
Fragment-based discovery of focal adhesion kinase inhibitors. |
Merck |
| 23896611 |
16 |
Tetrazole-based deoxyamodiaquines: synthesis, ADME/PK profiling and pharmacological evaluation as potential antimalarial agents. |
University of Cape Town |
| 23808489 |
11 |
2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways. |
Merck Research Laboratories |
| 23664879 |
73 |
Discovery of 1-(1,3,5-triazin-2-yl)piperidine-4-carboxamides as inhibitors of soluble epoxide hydrolase. |
Glaxosmithkline |
| 23200256 |
54 |
Discovery of N-[[1-[2-(tert-butylcarbamoylamino)ethyl]-4-(hydroxymethyl)-4-piperidyl]methyl]-3,5-dichloro-benzamide as a selective T-type calcium channel (Cav3.2) inhibitor. |
Astrazeneca |
| 16248836 |
154 |
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity. |
F. Hoffmann-La Roche |
| 22651823 |
57 |
Diazine indole acetic acids as potent, selective, and orally bioavailable antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases. |
Pfizer |
| 22533986 |
181 |
Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors. |
Arqule |
| 22409598 |
28 |
Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks. |
Pfizer |
| 22924734 |
87 |
Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the treatment of |
Pfizer |
| 22784008 |
100 |
Synthesis and biological evaluation of the 1-arylpyrazole class ofs(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862). |
Esteve |
| 22708876 |
106 |
Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-ß-alanine (MK-0893) for the treatment of type II diabetes. |
Merck Research Laboratories |
| 22548342 |
210 |
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors. |
Exelixis |
| 22938786 |
86 |
Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
Dainippon Sumitomo Pharma |
| 22185670 |
73 |
Oxadiazoles in medicinal chemistry. |
Astrazeneca |
| 24900436 |
18 |
Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened. |
TBA |
| 22328963 |
4 |
Discovery of a Potent HIV Integrase Inhibitor that Leads to a Prodrug with Significant anti-HIV Activity. |
TBA |
| 24900359 |
31 |
Optimization of the Central Core of Indolinone-Acetic Acid-Based CRTH2 (DP2) Receptor Antagonists. |
TBA |
| 22542012 |
155 |
The design, synthesis, and biological evaluation of PIM kinase inhibitors. |
Exelixis |
| 24900284 |
129 |
Discovery of a Novel Series of CRTH2 (DP2) Receptor Antagonists Devoid of Carboxylic Acids. |
TBA |
| 22239545 |
287 |
Ligand-based design of a potent and selective inhibitor of cytochrome P450 2C19. |
Amgen |
| 22361135 |
29 |
Indolyl and dihydroindolyl N-glycinamides as potent and in vivo active NPY5 antagonists. |
Lundbeck Research Usa |
| 21438541 |
45 |
Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difluoropropyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyr |
Pfizer |
| 21316976 |
62 |
17,20-lyase inhibitors. Part 4: design, synthesis and structure-activity relationships of naphthylmethylimidazole derivatives as novel 17,20-lyase inhibitors. |
Takeda Pharmaceutical |
| 19284751 |
26 |
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable"back-up" compound for N-tert-butyl isoquine. |
University of Liverpool |
| 18462007 |
7 |
Selective inhibition of aromatase by a dihydroisocoumarin from Xyris pterygoblephara. |
Universidade Federal De Minas Gerais |
| 17630726 |
32 |
Naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone: a potent, orally bioavailable human CB1/CB2 dual agonist with antihyperalgesic properties and restricted central nervous system penetration. |
Novartis Institutes For Biomedical Research |
| 17201408 |
91 |
Synthesis and biological evaluation of quinoline salicylic acids as P-selectin antagonists. |
Wyeth Research |
| 22070604 |
150 |
Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor¿ (PPAR¿) modulators. |
Merck Research Laboratories |
| 21978946 |
45 |
Discovery of orteronel (TAK-700), a naphthylmethylimidazole derivative, as a highly selective 17,20-lyase inhibitor with potential utility in the treatment of prostate cancer. |
Takeda Pharmaceutical |
| 21865048 |
29 |
2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727): a potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivation of CYP3A. |
Dainippon Sumitomo Pharma |
| 21411321 |
28 |
Design, synthesis and structure-activity relationships of (indo-3-yl) heterocyclic derivatives as agonists of the CB1 receptor. Discovery of a clinical candidate. |
Merck Research Laboratories |
| 21147532 |
82 |
Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core. |
Merck Research Laboratories |
| 19029327 |
7 |
In vitro and in vivo studies to characterize the clearance mechanism and potential cytochrome P450 interactions of anidulafungin. |
Pfizer |
| 21036042 |
7 |
Azaindole N-methyl hydroxamic acids as HIV-1 integrase inhibitors-II. The impact of physicochemical properties on ADME and PK. |
Pfizer |
| 20942471 |
79 |
First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis. |
Genkyotex |
| 20797855 |
63 |
PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor. |
Pfizer |
| 20452209 |
64 |
Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A. |
Merck Research Laboratories |
| 20423086 |
93 |
Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity. |
Merck Research Laboratories |
| 20223663 |
100 |
2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability. |
Wyeth Research |
| 20218621 |
131 |
Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic acid (BMS-687453). |
Bristol-Myers Squibb |
| 20184326 |
40 |
Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
Merck Research Laboratories |
| 19682899 |
211 |
Discovery of 3,3-disubstituted piperidine-derived trisubstituted ureas as highly potent soluble epoxide hydrolase inhibitors. |
Merck Research Laboratories |
| 19541481 |
57 |
Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors. |
Bristol-Myers Squibb |
| 19719241 |
55 |
Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists. |
Wyeth Research |
| 19537798 |
22 |
Identification of an orally active opioid receptor-like 1 (ORL1) receptor antagonist 4-{3-[(2R)-2,3-dihydroxypropyl]-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl}-1-[(1S,3S,4R)-spiro[bicyclo[2.2.1]heptane-2,1'-cyclopropan]-3-ylmethyl]piperidine as clinical candidate. |
Tsukuba Research Institute |
| 19209845 |
12 |
Discovery of (R)-6-cyclopentyl-6-(2-(2,6-diethylpyridin-4-yl)ethyl)-3-((5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)methyl)-4-hydroxy-5,6-dihydropyran-2-one (PF-00868554) as a potent and orally available hepatitis C virus polymerase inhibitor. |
Pfizer |
| 19222165 |
36 |
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century. |
University of Liverpool |
| 19447613 |
9 |
Nocathiacin analogs: Synthesis and antibacterial activity of novel water-soluble amides. |
Merck Research Laboratories |
| 19354254 |
24 |
Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists. |
Merck Research Laboratories |
| 19320488 |
171 |
1-Sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonists for the treatment of obesity. |
Merck Research Laboratories |
| 19309152 |
81 |
Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats. |
Merck Research Laboratories |
| 18477506 |
7 |
Tetrahydro anthranilic acid as a surrogate for anthranilic acid: application to the discovery of potent niacin receptor agonists. |
Merck Research Laboratories |
| 17705360 |
76 |
Structure-based optimization of protein tyrosine phosphatase 1B inhibitors: from the active site to the second phosphotyrosine binding site. |
Wyeth Research |
| 17399990 |
45 |
In vitro activity of novel dual action MDR anthranilamide modulators with inhibitory activity on CYP-450 (Part 2). |
Université |
| 16495056 |
23 |
Design and synthesis of selective, high-affinity inhibitors of human cytochrome P450 2J2. |
Universite Paris 5 René |
| 11606127 |
96 |
Synthesis of sulfaphenazole derivatives and their use as inhibitors and tools for comparing the active sites of human liver cytochromes P450 of the 2C subfamily. |
Université |
| 32089426 |
35 |
3,3-Difluoro-3,4,5,6-tetrahydropyridin-2-amines: Potent and permeable BACE-1 inhibitors. |
Janssen Research & Development |
| 32945812 |
79 |
Discovery of Vixotrigine: A Novel Use-Dependent Sodium Channel Blocker for the Treatment of Trigeminal Neuralgia. |
Convergence Pharmaceuticals |
| 32787083 |
172 |
Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma. |
Ontario Institute For Cancer Research |
| 32334912 |
130 |
Discovery and optimization of new oxadiazole substituted thiazole ROR?t inverse agonists through a bioisosteric amide replacement approach. |
Phenex Pharmaceuticals |
| 32336498 |
324 |
Optimization and biological evaluation of thiazole-bis-amide inverse agonists of ROR?t. |
Phenex Pharmaceuticals |
| 32551019 |
31 |
Discovery of CPI-1612: A Potent, Selective, and Orally Bioavailable EP300/CBP Histone Acetyltransferase Inhibitor. |
Constellation Pharmaceuticals |
| 32551004 |
32 |
Discovery of BMS-986251: A Clinically Viable, Potent, and Selective ROR?t Inverse Agonist. |
Bristol Myers Squibb |
| 31952960 |
234 |
Discovery of a lead series of potent benzodiazepine 5-HT |
Arena Pharmaceuticals |
| 32452679 |
53 |
Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
Haisco Pharmaceutical Group |
| 32182061 |
5 |
Metabolic and Pharmaceutical Aspects of Fluorinated Compounds. |
Bristol Myers Squibb |
| 32558564 |
16 |
Structure-Based Drug Discovery of |
Sosei Heptares |
| 32502336 |
79 |
Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models. |
Bayer |
| 31898999 |
42 |
Design, synthesis and identification of novel, orally bioavailable non-covalent Nrf2 activators. |
Biogen |
| 32390424 |
9 |
Discovery of the First Vitamin K Analogue as a Potential Treatment of Pharmacoresistant Seizures. |
Ocean University of China |
| 27305487 |
105 |
Discovery of 3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine (ARQ 092): An Orally Bioavailable, Selective, and Potent Allosteric AKT Inhibitor. |
Arqule |
| 27774123 |
37 |
Discovery of AZD2716: A Novel Secreted Phospholipase A |
Astrazeneca |
| 27531604 |
55 |
Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177). |
Bristol-Myers Squibb Research and Development |
| 27460209 |
152 |
Design, synthesis and optimization of novel Alk5 (activin-like kinase 5) inhibitors. |
Takeda California |
| 27432763 |
76 |
Synthesis, structure-activity relationships and biological evaluation of 4,5,6,7-tetrahydropyrazolopyrazines as metabotropic glutamate receptor 5 negative allosteric modulators. |
Sumitomo Dainippon Pharma |
| 27309907 |
164 |
Discovery and Structure-Activity Relationship (SAR) of a Series of Ethanolamine-Based Direct-Acting Agonists of Sphingosine-1-phosphate (S1P1). |
Bristol-Myers Squibb |
| 30707578 |
89 |
Design and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140). |
The Scripps Research Institute |
| 30576906 |
92 |
Novel non-xanthine antagonist of the A |
Bayer Pharmaceuticals |
| 31693857 |
56 |
Development of Robust 17( |
University of Texas Southwestern |
| 31381333 |
302 |
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
TBA |
| 30624919 |
502 |
Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5. |
Recordati |
| 31274313 |
95 |
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633). |
Oric Pharmaceuticals |
| 32369358 |
143 |
Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma. |
University of Toronto |
| 32302132 |
74 |
Design and Characterization of the First Selective and Potent Mechanism-Based Inhibitor of Cytochrome P450 4Z1. |
University of Washington |
| 32031803 |
8 |
Preclinical Optimization of gp120 Entry Antagonists as anti-HIV-1 Agents with Improved Cytotoxicity and ADME Properties through Rational Design, Synthesis, and Antiviral Evaluation. |
Lindsley F. Kimball Research Institute |
| 30869888 |
61 |
Discovery and Early Clinical Development of an Inhibitor of 5-Lipoxygenase Activating Protein (AZD5718) for Treatment of Coronary Artery Disease. |
TBA |
| 30952592 |
206 |
Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC). |
Merck |
| 31288965 |
25 |
Optimization of oxadiazole derivatives with a spirocyclic cyclohexane structure as novel GPR119 agonists. |
Japan Tobacco |
| 31257087 |
243 |
Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as ROR?t inverse agonists. |
Bristol-Myers Squibb |
| 31122869 |
40 |
Design and synthesis of a novel series of cyanoindole derivatives as potent ?-secretase modulators. |
Janssen Research & Development |
| 31023512 |
76 |
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors. |
Sabila Biosciences |
| 32208614 |
7 |
CN128: A New Orally Active Hydroxypyridinone Iron Chelator. |
Zhejiang University |
| 31859507 |
212 |
Discovery of BAY-985, a Highly Selective TBK1/IKK? Inhibitor. |
Bayer |
| 30576602 |
157 |
Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective Na |
Bristol-Myers Squibb Research and Development |
| 30629436 |
66 |
Discovery and Development of N-[4-(1-Cyclobutylpiperidin-4-yloxy)phenyl]-2-(morpholin-4-yl)acetamide Dihydrochloride (SUVN-G3031): A Novel, Potent, Selective, and Orally Active Histamine H |
Suven Life Sciences |
| 31264862 |
231 |
Discovery of Clinical Candidate (1 |
Newlink Genetics |
| 30964988 |
26 |
Design and Identification of a Novel, Functionally Subtype Selective GABA |
Pfizer |
| 32202790 |
160 |
Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer. |
Japanese Foundation For Cancer Research |
| 30891142 |
121 |
Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active ROR?t Inverse Agonists. |
Bristol-Myers Squibb |
| 30891124 |
36 |
Discovery of Imidazo[1,2- |
Sanford Burnham Prebys Medical Discovery Institute |
| 30891123 |
204 |
1 |
Janssen Research & Development |
| 32071685 |
40 |
Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGF?R1 Inhibitor as an Immuno-oncology Agent. |
Bristol-Myers Squibb Research & Development |
| 31638797 |
193 |
Rationally Designed, Conformationally Constrained Inverse Agonists of ROR?t-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy. |
Bristol-Myers Squibb |
| 30655946 |
27 |
Maximizing ER-? Degradation Maximizes Activity in a Tamoxifen-Resistant Breast Cancer Model: Identification of GDC-0927. |
Seragon Pharmaceuticals |
| 30638874 |
64 |
Discovery of new indole-based acylsulfonamide Na |
Bristol-Myers Squibb Research and Development |
| 30587450 |
22 |
Lead generation and optimization of novel GPR119 agonists with a spirocyclic cyclohexane structure. |
Japan Tobacco |
| 30563338 |
66 |
Discovery and Characterization of the Potent and Highly Selective (Piperidin-4-yl)pyrido[3,2- d]pyrimidine Based in Vitro Probe BAY-885 for the Kinase ERK5. |
Bayer |
| 31746599 |
78 |
Discovery and Characterization of the Potent and Selective P2X4 Inhibitor |
Bayer |
| 31670515 |
79 |
Discovery of BAY-298 and BAY-899: Tetrahydro-1,6-naphthyridine-Based, Potent, and Selective Antagonists of the Luteinizing Hormone Receptor Which Reduce Sex Hormone Levels in Vivo. |
Bayer |
| 26608552 |
46 |
Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists. |
Eli Lilly |
| 26565745 |
165 |
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
Janssen Pharmaceutica |
| 30429955 |
44 |
Discovery of 4-Azaindole Inhibitors of TGF?RI as Immuno-oncology Agents. |
Bristol-Myers Squibb Research and Development |
| 30172617 |
28 |
Discovery of benzothiazole amides as potent antimycobacterial agents. |
Crestone |
| 30143425 |
12 |
Design and synthesis of tetrahydropyridopyrimidine based Toll-Like Receptor (TLR) 7/8 dual agonists. |
Janssen Infectious Diseases |
| 30429097 |
29 |
PPAR?-sparing thiazolidinediones as insulin sensitizers. Design, synthesis and selection of compounds for clinical development. |
Sptanis Pharmachem Consulting |
| 30122225 |
25 |
Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
Emd Serono Research & Development Institute |
| 30034615 |
46 |
MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology. |
Merck |
| 30034607 |
60 |
Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines. |
Shanghai Haiyan Pharmaceutical Technology |
| 30034586 |
90 |
Design of Selective sPLA |
Astrazeneca |
| 29459274 |
69 |
Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
Shanghai Haihe Pharmaceutical |
| 29519733 |
26 |
Design and synthesis of novel and potent GPR119 agonists with a spirocyclic structure. |
Japan Tobacco |
| 29366653 |
71 |
Discovery of selective 2,4-diaminoquinazoline toll-like receptor 7 (TLR 7) agonists. |
Janssen Infectious Diseases Diagnostics |
| 29138024 |
213 |
(E)-3-(3,4,5-Trimethoxyphenyl)-1-(pyridin-4-yl)prop-2-en-1-one, a heterocyclic chalcone is a potent and selective CYP1A1 inhibitor and cancer chemopreventive agent. |
De Montfort University |
| 29116786 |
265 |
Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies. |
Idorsia Pharmaceuticals |
| 29029933 |
45 |
Highly potent and selective Na |
Pfizer |
| 30289716 |
109 |
Design and Activity of Specific Hypoxia-Inducible Factor-2? (HIF-2?) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate ( S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385). |
Peloton Therapeutics |
| 30091920 |
113 |
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101). |
Oric Pharmaceuticals |
| 29995408 |
293 |
Identification of the 4-Position of 3-Alkynyl and 3-Heteroaromatic Substituted Pyridine Methanamines as a Key Modification Site Eliciting Increased Potency and Enhanced Selectivity for Cytochrome P-450 2A6 Inhibition. |
Washington State University |
| 29795762 |
25 |
BMS-986163, a Negative Allosteric Modulator of GluN2B with Potential Utility in Major Depressive Disorder. |
Bristol-Myers Squibb Research and Development |
| 29906396 |
10 |
Synthesis and Evaluation of N-Phenyl-3-sulfamoyl-benzamide Derivatives as Capsid Assembly Modulators Inhibiting Hepatitis B Virus (HBV). |
Janssen Pharmaceutical Companies of Johnson & Johnson |
| 29456793 |
72 |
Synthesis of Novel Tetrahydroisoquinoline CXCR4 Antagonists with Rigidified Side-Chains. |
Emory University |
| 29348807 |
32 |
Discovery of Spiro Oxazolidinediones as Selective, Orally Bioavailable Inhibitors of p300/CBP Histone Acetyltransferases. |
Abbvie |
| 29259755 |
55 |
Discovery of JTZ-951: A HIF Prolyl Hydroxylase Inhibitor for the Treatment of Renal Anemia. |
Japan Tobacco |
| 29809004 |
50 |
Optimization of 1,4-Oxazine ?-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate. |
Janssen Pharmaceutica |
| 29779975 |
53 |
Design and synthesis of a series of bioavailable fatty acid synthase (FASN) KR domain inhibitors for cancer therapy. |
Janssen Research and Development |
| 29735425 |
45 |
Discovery of tetrahydroindazoles as a novel class of potent and in vivo efficacious gamma secretase modulators. |
Boehringer Ingelheim Pharma |
| 29724589 |
40 |
Discovery of evocalcet, a next-generation calcium-sensing receptor agonist for the treatment of hyperparathyroidism. |
Mitsubishi Tanabe Pharma |
| 29350534 |
211 |
Discovery of Tetrahydroisoquinoline-Containing CXCR4 Antagonists with Improved in Vitro ADMET Properties. |
Emory University |
| 28493698 |
56 |
4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate. |
Janssen Research and Development |
| 28112924 |
149 |
Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode. |
Bristol-Myers Squibb |
| 28398755 |
79 |
Inhibitors of 15-Prostaglandin Dehydrogenase To Potentiate Tissue Repair. |
Ut Southwestern Medical Center |
| 28368581 |
82 |
Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist. |
Corcept Therapeutics |
| 28838696 |
45 |
Synthesis and optimization of 4,5,6,7-tetrahydrooxazolo[4,5-c]pyridines as potent and orally-active metabotropic glutamate receptor 5 negative allosteric modulators. |
Sumitomo Dainippon Pharma |
| 28530802 |
121 |
Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation. |
Vanderbilt University Institute of Imaging Science |
| 29211470 |
64 |
A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate. |
Janssen Research and Development |
| 29161514 |
7 |
Discovery of an Orally Bioavailable Benzofuran Analogue That Serves as a?-Amyloid Aggregation Inhibitor for the Potential Treatment of Alzheimer's Disease. |
Medifron Dbt |
| 28968083 |
4 |
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity. |
S£O Paulo State University (Unesp) |
| 28671847 |
70 |
Identification and Optimization of Pyrrolo[3,2-d]pyrimidine Toll-like Receptor 7 (TLR7) Selective Agonists for the Treatment of Hepatitis B. |
Janssen Pharmaceutica |
| 28431879 |
123 |
Improvement of hERG-ROMK index of spirocyclic ROMK inhibitors through scaffold optimization and incorporation of novel pharmacophores. |
Merck |
| 29243920 |
134 |
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity. |
East China University of Science and Technology |
| 29211475 |
65 |
Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquin |
Wuxi Apptec |
| 28209465 |
124 |
Identification of highly potent and selective PI3K? inhibitors. |
Bristol-Myers Squibb |
| 28653847 |
9 |
Glucuronides as Potential Anionic Substrates of Human Cytochrome P450 2C8 (CYP2C8). |
Celgene |
| 28557445 |
11 |
Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure. |
Bayer |
| 28541707 |
119 |
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase? (PI3K?) Inhibitor for the Treatment of Immunological Disorders. |
Bristol-Myers Squibb |
| 28537398 |
114 |
Discovery of Clinical Candidate 2-((2S,6S)-2-Phenyl-6-hydroxyadamantan-2-yl)-1-(3'-hydroxyazetidin-1-yl)ethanone [BMS-816336], an Orally Active Novel Selective 11?-Hydroxysteroid Dehydrogenase Type 1 Inhibitor. |
Bristol-Myers Squibb |
| 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 |
| 8522988 |
39 |
Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor. |
University of Washington |
| 19041240 |
41 |
Lead identification to generate 3-cyanoquinoline inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment. |
Wyeth Research |
| 16451071 |
44 |
Dual inhibitors of thymidylate synthase and dihydrofolate reductase as antitumor agents: design, synthesis, and biological evaluation of classical and nonclassical pyrrolo[2,3-d]pyrimidine antifolates(1). |
Duquesne University |
| 16620080 |
15 |
Design, synthesis and X-ray structure of protein-ligand complexes: important insight into selectivity of memapsin 2 (beta-secretase) inhibitors. |
Purdue University |
| 7683725 |
30 |
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase. |
Merck Research Laboratories |
| | 35 |
Cycloalkylpiperazines as HIV-1 Protease Inhibitors: Enhanced Oral Absorption |
Merck Research Laboratories |
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