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 |
| 28274629 |
76 |
Effects of 6-paradol, an unsaturated ketone from gingers, on cytochrome P450-mediated drug metabolism. |
Hanyang University |
| 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 |
| 28337332 |
41 |
BMS-933043, a Selectivea7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia. |
Bristol-Myers Squibb |
| 28003141 |
65 |
Identification and optimization of a novel series of indoleamine 2,3-dioxygenase inhibitors. |
Bristol-Myers Squibb Research and Development |
| 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 |
| 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 |
| 27145071 |
37 |
2-(3-Methoxyphenyl)quinazoline Derivatives: A New Class of Direct Constitutive Androstane Receptor (CAR) Agonists. |
Palacky University In Olomouc |
| 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 |
| 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 |
| 26344593 |
5 |
Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation. |
Northshore University Healthsystem |
| 26191364 |
10 |
Dimeric Macrocyclic Antagonists of Inhibitor of Apoptosis Proteins for the Treatment of Cancer. |
Bristol-Myers Squibb Research |
| 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 |
| 26091726 |
41 |
Discovery and characterization of a potent and selective EP4 receptor antagonist. |
Eli Lilly |
| 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 |
| 22685215 |
1 |
Mechanism-based inactivation of cytochrome P450 2B6 by methadone through destruction of prosthetic heme. |
University of Michigan |
| 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 |
| 22679214 |
13 |
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes. |
University of Washington |
| 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 |
| 25415535 |
118 |
Inhibitors of c-Jun N-terminal kinases: an update. |
Eberhard Karls Universit£T T£Bingen |
| 25330343 |
49 |
Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro. |
Translational Research Institute |
| 24842618 |
56 |
The design and synthesis of novel SGLT2 inhibitors: C-glycosides with benzyltriazolopyridinone and phenylhydantoin as the aglycone moieties. |
Amri |
| 24755431 |
59 |
The discovery of diazepinone-based 5-HT3 receptor partial agonists. |
Amri |
| 24512187 |
69 |
Discovery of isoquinolinone indole acetic acids as antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases. |
Pfizer |
| 24900630 |
16 |
Synthesis and in vitro and in vivo pharmacological evaluation of new 4-aminoquinoline-based compounds. |
University of Cape Town |
| 24090135 |
201 |
Design of substituted imidazolidinylpiperidinylbenzoic acids as chemokine receptor 5 antagonists: potent inhibitors of R5 HIV-1 replication. |
Sanofi |
| 23896611 |
16 |
Tetrazole-based deoxyamodiaquines: synthesis, ADME/PK profiling and pharmacological evaluation as potential antimalarial agents. |
University of Cape Town |
| 23810496 |
31 |
Synthesis and biological evaluation of aminobenzimidazole derivatives with a phenylcyclohexyl acetic acid group as anti-obesity and anti-diabetic agents. |
Korea Research Institute of Chemical Technology |
| 23769643 |
28 |
Synthesis, characterization, and biological assessment of the four stereoisomers of the H(3) receptor antagonist 5-fluoro-2-methyl-N-[2-methyl-4-(2-methyl[1,3']bipyrrolidinyl-1'-yl)phenyl]benzamide. |
Sanofi Us |
| 23600958 |
57 |
Pyranoflavones: a group of small-molecule probes for exploring the active site cavities of cytochrome P450 enzymes 1A1, 1A2, and 1B1. |
Xavier University of Louisiana |
| 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 |
| 22409598 |
28 |
Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks. |
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 |
| 22277094 |
59 |
Optimization of hydroxybenzothiazoles as novel potent and selective inhibitors of 17ß-HSD1. |
Saarland University |
| 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 |
| 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 |
| 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 |
| 18324762 |
20 |
Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseases. |
Saarland University |
| 15634016 |
232 |
5-substituted, 6-substituted, and unsubstituted 3-heteroaromatic pyridine analogues of nicotine as selective inhibitors of cytochrome P-450 2A6. |
Human Biomolecular Research Institute |
| 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 |
| 21384875 |
67 |
Fine-tuning the selectivity of aldosterone synthase inhibitors: structure-activity and structure-selectivity insights from studies of heteroaryl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-one derivatives. |
Saarland University |
| 21189020 |
54 |
New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17ß-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases. |
Saarland University |
| 19029327 |
7 |
In vitro and in vivo studies to characterize the clearance mechanism and potential cytochrome P450 interactions of anidulafungin. |
Pfizer |
| 19029318 |
15 |
Comprehensive in vitro analysis of voriconazole inhibition of eight cytochrome P450 (CYP) enzymes: major effect on CYPs 2B6, 2C9, 2C19, and 3A. |
Indiana University |
| 20961756 |
61 |
5-(pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as MCH-1 antagonists. |
Amri |
| 20952195 |
62 |
Tetrahydrocarboline analogs as MCH-1 antagonists. |
Amri |
| 20951036 |
47 |
Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity. |
Amri |
| 18285471 |
1 |
Rapid clinical induction of hepatic cytochrome P4502B6 activity by ritonavir. |
Washington University |
| 20797855 |
63 |
PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor. |
Pfizer |
| 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 |
| 19541481 |
57 |
Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors. |
Bristol-Myers Squibb |
| 19049427 |
98 |
In vivo active aldosterone synthase inhibitors with improved selectivity: lead optimization providing a series of pyridine substituted 3,4-dihydro-1H-quinolin-2-one derivatives. |
Saarland University |
| 18763754 |
57 |
Novel aldosterone synthase inhibitors with extended carbocyclic skeleton by a combined ligand-based and structure-based drug design approach. |
Saarland University |
| 18672861 |
91 |
Overcoming undesirable CYP1A2 inhibition of pyridylnaphthalene-type aldosterone synthase inhibitors: influence of heteroaryl derivatization on potency and selectivity. |
Saarland University |
| 18249473 |
97 |
Structure-activity relationships for the inhibition of recombinant human cytochromes P450 by curcumin analogues. |
Vrije Universiteit |
| 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 |
| 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 |
| 32551019 |
31 |
Discovery of CPI-1612: A Potent, Selective, and Orally Bioavailable EP300/CBP Histone Acetyltransferase Inhibitor. |
Constellation 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 |
| 31898999 |
42 |
Design, synthesis and identification of novel, orally bioavailable non-covalent Nrf2 activators. |
Biogen |
| 31862412 |
60 |
Scaffold-hopping identifies furano[2,3-d]pyrimidine amides as potent Notum inhibitors. |
University College London |
| 32390424 |
9 |
Discovery of the First Vitamin K Analogue as a Potential Treatment of Pharmacoresistant Seizures. |
Ocean University of China |
| 30996792 |
20 |
Discovery of Stereospecific PARP-1 Inhibitor Isoindolinone NMS-P515. |
Nerviano Medical Sciences |
| 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 |
| 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 |
| 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 |
| 30576901 |
24 |
Synthesis and anti-tumor activity of imidazopyrazines as TAK1 inhibitors. |
Chung-Ang University |
| 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 |
| 32115956 |
46 |
Discovery and Optimization of ?-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia. |
Guangzhou University of Chinese Medicine |
| 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 |
| 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 |
| 31023512 |
76 |
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors. |
Sabila Biosciences |
| 30916555 |
43 |
Discovery of Potent, Selective, and Orally Bioavailable Inhibitors against Phosphodiesterase-9, a Novel Target for the Treatment of Vascular Dementia. |
Sun Yat-Sen University |
| 32208614 |
7 |
CN128: A New Orally Active Hydroxypyridinone Iron Chelator. |
Zhejiang University |
| 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 |
| 26608552 |
46 |
Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists. |
Eli Lilly |
| 22815312 |
3 |
Quantitative prediction of CYP2B6 induction by estradiol during pregnancy: potential explanation for increased methadone clearance during pregnancy. |
Amgen |
| 31026162 |
25 |
Modification and Biological Evaluation of a Series of 1,5-Diaryl-1,2,4-triazole Compounds as Novel Agents against Pancreatic Cancer Metastasis through Targeting Myoferlin. |
East China Normal University |
| 30172617 |
28 |
Discovery of benzothiazole amides as potent antimycobacterial agents. |
Crestone |
| 30392954 |
57 |
Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles. |
Chinese Academy of Sciences |
| 30122225 |
25 |
Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit. |
Emd Serono Research & Development Institute |
| 30148362 |
36 |
Optimization of Chromeno[2,3- c]pyrrol-9(2 H)-ones as Highly Potent, Selective, and Orally Bioavailable PDE5 Inhibitors: Structure-Activity Relationship, X-ray Crystal Structure, and Pharmacodynamic Effect on Pulmonary Arterial Hypertension. |
Sun Yat-Sen University |
| 30034607 |
60 |
Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines. |
Shanghai Haiyan Pharmaceutical Technology |
| 29459274 |
69 |
Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
Shanghai Haihe Pharmaceutical |
| 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 |
| 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 |
| 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 |
| 29259755 |
55 |
Discovery of JTZ-951: A HIF Prolyl Hydroxylase Inhibitor for the Treatment of Renal Anemia. |
Japan Tobacco |
| 28772235 |
39 |
Discovery of methylsulfonyl indazoles as potent and orally active respiratory syncytial Virus(RSV) fusion inhibitors. |
Roche Innovation Center Shanghai |
| 29724589 |
40 |
Discovery of evocalcet, a next-generation calcium-sensing receptor agonist for the treatment of hyperparathyroidism. |
Mitsubishi Tanabe Pharma |
| 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 |
| 28753313 |
45 |
Neuroactive Steroids. 2. 3?-Hydroxy-3?-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5?-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (?-Aminobutyric Acid) |
Sage Therapeutics |
| 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 |
| 28968083 |
4 |
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity. |
S£O Paulo State University (Unesp) |
| 28442253 |
68 |
Optimization of M |
Vanderbilt University Medical Center |
| 29381358 |
65 |
3-((R)-4-(((R)-6-(2-Bromo-4-fluorophenyl)-5-(ethoxycarbonyl)-2-(thiazol-2-yl)-3,6-dihydropyrimidin-4-yl)methyl)morpholin-2-yl)propanoic Acid (HEC72702), a Novel Hepatitis B Virus Capsid Inhibitor Based on Clinical Candidate GLS4. |
Hec Pharma Group |
| 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 |
| 28209465 |
124 |
Identification of highly potent and selective PI3K? inhibitors. |
Bristol-Myers Squibb |
| 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 |
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