168 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sun Yat-Sen University
Effects of 6-paradol, an unsaturated ketone from gingers, on cytochrome P450-mediated drug metabolism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Hanyang University
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![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Suven Life Sciences
Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
East China University of Science and Technology
BMS-933043, a Selectivea7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb
Identification and optimization of a novel series of indoleamine 2,3-dioxygenase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Research and Development
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb
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![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Research and Development
Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-¿ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Infinity Pharmaceuticals
Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARa Selective Agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb
2-(3-Methoxyphenyl)quinazoline Derivatives: A New Class of Direct Constitutive Androstane Receptor (CAR) Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Palacky University In Olomouc
Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Research and Development
Identification and biological activity of 6-alkyl-substituted 3-methyl-pyridine-2-carbonyl amino dimethyl-benzoic acid EP4 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eli Lilly
Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Research and Development
Discovery of Vibegron: A Potent and Selectiveß3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Research Laboratories
Discovery of potent aryl-substituted 3-[(3-methylpyridine-2-carbonyl) amino]-2,4-dimethyl-benzoic acid EP4 antagonists with improved pharmacokinetic profile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eli Lilly
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Research and Development
Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Northshore University Healthsystem
Dimeric Macrocyclic Antagonists of Inhibitor of Apoptosis Proteins for the Treatment of Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Research
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
Discovery and characterization of a potent and selective EP4 receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eli Lilly
Characterization of the in vitro and in vivo metabolism and disposition and cytochrome P450 inhibition/induction profile of saxagliptin in human.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Research
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Mechanism-based inactivation of cytochrome P450 2B6 by methadone through destruction of prosthetic heme.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Michigan
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Washington
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Translational Research Institute
The design and synthesis of novel SGLT2 inhibitors: C-glycosides with benzyltriazolopyridinone and phenylhydantoin as the aglycone moieties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amri
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Synthesis and in vitro and in vivo pharmacological evaluation of new 4-aminoquinoline-based compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Cape Town
Design of substituted imidazolidinylpiperidinylbenzoic acids as chemokine receptor 5 antagonists: potent inhibitors of R5 HIV-1 replication.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sanofi
Tetrazole-based deoxyamodiaquines: synthesis, ADME/PK profiling and pharmacological evaluation as potential antimalarial agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Cape Town
Synthesis and biological evaluation of aminobenzimidazole derivatives with a phenylcyclohexyl acetic acid group as anti-obesity and anti-diabetic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Korea Research Institute of Chemical Technology
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sanofi Us
Pyranoflavones: a group of small-molecule probes for exploring the active site cavities of cytochrome P450 enzymes 1A1, 1A2, and 1B1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Xavier University of Louisiana
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
F. Hoffmann-La Roche
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
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).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Esteve
Optimization of hydroxybenzothiazoles as novel potent and selective inhibitors of 17ß-HSD1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Saarland University
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Research Laboratories
Discovery of a Novel Series of CRTH2 (DP2) Receptor Antagonists Devoid of Carboxylic Acids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
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![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Saarland University
5-substituted, 6-substituted, and unsubstituted 3-heteroaromatic pyridine analogues of nicotine as selective inhibitors of cytochrome P-450 2A6.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Human Biomolecular Research Institute
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Takeda Pharmaceutical
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Saarland University
New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17ß-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Saarland University
In vitro and in vivo studies to characterize the clearance mechanism and potential cytochrome P450 interactions of anidulafungin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Comprehensive in vitro analysis of voriconazole inhibition of eight cytochrome P450 (CYP) enzymes: major effect on CYPs 2B6, 2C9, 2C19, and 3A.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Indiana University
5-(pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as MCH-1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amri
Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amri
Rapid clinical induction of hepatic cytochrome P4502B6 activity by ritonavir.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Washington University
PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth Research
Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Saarland University
Novel aldosterone synthase inhibitors with extended carbocyclic skeleton by a combined ligand-based and structure-based drug design approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Saarland University
Overcoming undesirable CYP1A2 inhibition of pyridylnaphthalene-type aldosterone synthase inhibitors: influence of heteroaryl derivatization on potency and selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Saarland University
Structure-activity relationships for the inhibition of recombinant human cytochromes P450 by curcumin analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vrije Universiteit
In vitro activity of novel dual action MDR anthranilamide modulators with inhibitory activity on CYP-450 (Part 2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Université
Design and synthesis of selective, high-affinity inhibitors of human cytochrome P450 2J2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Universite Paris 5 René
Discovery of Vixotrigine: A Novel Use-Dependent Sodium Channel Blocker for the Treatment of Trigeminal Neuralgia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Convergence Pharmaceuticals
Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ontario Institute For Cancer Research
Discovery of CPI-1612: A Potent, Selective, and Orally Bioavailable EP300/CBP Histone Acetyltransferase Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Constellation Pharmaceuticals
Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Haisco Pharmaceutical Group
Design, synthesis and identification of novel, orally bioavailable non-covalent Nrf2 activators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Biogen
Scaffold-hopping identifies furano[2,3-d]pyrimidine amides as potent Notum inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University College London
Discovery of the First Vitamin K Analogue as a Potential Treatment of Pharmacoresistant Seizures.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ocean University of China
Discovery of Stereospecific PARP-1 Inhibitor Isoindolinone NMS-P515.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
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).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Research and Development
Discovery and Structure-Activity Relationship (SAR) of a Series of Ethanolamine-Based Direct-Acting Agonists of Sphingosine-1-phosphate (S1P1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb
Design and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
The Scripps Research Institute
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Recordati
Synthesis and anti-tumor activity of imidazopyrazines as TAK1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chung-Ang University
Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Toronto
Design and Characterization of the First Selective and Potent Mechanism-Based Inhibitor of Cytochrome P450 4Z1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Washington
Discovery and Optimization of ?-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Guangzhou University of Chinese Medicine
Preclinical Optimization of gp120 Entry Antagonists as anti-HIV-1 Agents with Improved Cytotoxicity and ADME Properties through Rational Design, Synthesis, and Antiviral Evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Lindsley F. Kimball Research Institute
Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as ROR?t inverse agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sabila Biosciences
Discovery of Potent, Selective, and Orally Bioavailable Inhibitors against Phosphodiesterase-9, a Novel Target for the Treatment of Vascular Dementia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sun Yat-Sen University
Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective Na![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Research and Development
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![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Suven Life Sciences
Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Japanese Foundation For Cancer Research
Discovery of new indole-based acylsulfonamide Na![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Research and Development
Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eli Lilly
Quantitative prediction of CYP2B6 induction by estradiol during pregnancy: potential explanation for increased methadone clearance during pregnancy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
East China Normal University
Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chinese Academy of Sciences
Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Emd Serono Research & Development Institute
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sun Yat-Sen University
Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Shanghai Haiyan Pharmaceutical Technology
Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Shanghai Haihe Pharmaceutical
(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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
De Montfort University
Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Idorsia Pharmaceuticals
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).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Peloton Therapeutics
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Washington State University
BMS-986163, a Negative Allosteric Modulator of GluN2B with Potential Utility in Major Depressive Disorder.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Research and Development
Discovery of JTZ-951: A HIF Prolyl Hydroxylase Inhibitor for the Treatment of Renal Anemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Japan Tobacco
Discovery of methylsulfonyl indazoles as potent and orally active respiratory syncytial Virus(RSV) fusion inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Roche Innovation Center Shanghai
Discovery of evocalcet, a next-generation calcium-sensing receptor agonist for the treatment of hyperparathyroidism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Mitsubishi Tanabe Pharma
Inhibitors of 15-Prostaglandin Dehydrogenase To Potentiate Tissue Repair.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ut Southwestern Medical Center
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Corcept Therapeutics
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)![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sage Therapeutics
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vanderbilt University Institute of Imaging Science
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
S£O Paulo State University (Unesp)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Hec Pharma Group
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
East China University of Science and Technology
Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bayer
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase? (PI3K?) Inhibitor for the Treatment of Immunological Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb