PMID
Data
Article Title
Organization
Novel quinazoline-quinoline alkaloids with cytotoxic and DNA topoisomerase II inhibitory activities.

Toho University
Astemizole Derivatives as Fluorescent Probes for hERG Potassium Channel Imaging.

Shandong University
Discovery of the imidazole-derived GPR40 agonist AM-3189.

Amgen
Synthesis and biological evaluation of 2-alkyl-2-methoxymethyl-salvinorin ethers as selective¿-opioid receptor agonists.

Harvard Medical School
Discovery of Quinazoline-Based Fluorescent Probes toa1-Adrenergic Receptors.

Shandong University
Toward fluorescent probes for G-protein-coupled receptors (GPCRs).

Shandong University
Optimization of GPR40 Agonists for Type 2 Diabetes.

Amgen
Synthesis and biological evaluation of the pirfenidone derivatives as antifibrotic agents.

Zhejiang Academy of Medical Sciences
The development of highly potent inhibitors for porcupine.

The University of Texas Southwestern Medical Center
Eleven amino acid glucagon-like peptide-1 receptor agonists with antidiabetic activity.

Bristol-Myers Squibb
Synthesis and biological evaluation of C-12 triazole and oxadiazole analogs of salvinorin A.

Harvard Medical School
Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors.

Harvard Medical School
Triketoacid inhibitors of HIV-integrase: a new chemotype useful for probing the integrase pharmacophore.

Bristol-Myers Squibb
Synthesis and in vitro pharmacological studies of new C(2) modified salvinorin A analogues.

Harvard Medical School
Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2).

Mclean Hospital
Discovery of a potent and novel motilin agonist.

Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and structure-activity relationship of 3-arylbenzoxazines as selective estrogen receptor beta agonists.

Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824).

University of Auckland
Identification of potent, noncovalent fatty acid amide hydrolase (FAAH) inhibitors.

Amgen
Potent biphenyl- and 3-phenyl pyridine-based inhibitors of acetyl-CoA carboxylase.

Bristol-Myers Squibb Research and Development
Structure-activity relationship studies of small-molecule inhibitors of Wnt response.

The University of Texas Southwestern Medical Center At Dallas
Discovery of Potent, Specific, and Orally Available NLRP3 Inflammasome Inhibitors Based on Pyridazine Scaffolds for the Treatment of Septic Shock and Peritonitis.

Sichuan University
Design, Synthesis, and Biological Evaluation of 5-Amino-4-fluoro-1H-benzo[d]imidazole-6-carboxamide Derivatives as Novel and Potential MEK/RAF Complex Inhibitors Based on the "Clamp" Strategy.

Sichuan University
Identification of benzothiazoles as novel PCSK9 inhibitors.

Hebei Normal University
Natural Derivatives of Selective HDAC8 Inhibitors with Potent in Vivo Antitumor Efficacy against Breast Cancer.

Zhejiang University
Fragment growth-based discovery of novel TNIK inhibitors for the treatment of colorectal cancer.

Sichuan University
Discovery of Novel Potent and Fast BTK PROTACs for the Treatment of Osteoclasts-Related Inflammatory Diseases.

The People's Hospital of Guangxi Zhuang Autonomous Region & Guangxi Academy of Medical Sciences
Bipyridine Derivatives as NOP2/Sun RNA Methyltransferase 3 Inhibitors for the Treatment of Colorectal Cancer.

Zhejiang University
Discovery of 4-amino-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazin-7-one derivatives as potential receptor-interacting serine/threonine-protein kinase 1 (RIPK1) inhibitors.

West China Hospital of Sichuan University
Design, Synthesis, and Biological Evaluation of an Orally Bioavailable, Potent, and Selective ROCK2 Inhibitor for Psoriasis Treatment.

Zhejiang University
Discovery of novel SOS1 inhibitors using machine learning.

University of Nottingham Ningbo China
Discovery of unglycosylated indolocarbazoles as ROCK2 isoform-selective inhibitors for the treatment of breast cancer metastasis.

Zhejiang University
Discovery of

TBA
Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2).

University of Texas Medical Branch (UTMB)
Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I.

Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of novel pyridinones as MGAT2 inhibitors for the treatment of metabolic disorders.

Bristol Myers Squibb
Targeted Protein Degradation Induced by HEMTACs Based on HSP90.

Shandong University
Novel strategies targeting bromodomain-containing protein 4 (BRD4) for cancer drug discovery.

China Pharmaceutical University
Synthesis and in vitro pharmacological studies of new C(4)-modified salvinorin A analogues.

Harvard Medical School
Potent Uncompetitive Inhibitors of Nicotinamide

Harvard University
High-throughput screening for Hsp90 ATPase inhibitors.

The University of Kansas
Design, synthesis, and bioevaluation of imidazo [1,2-a] pyrazine derivatives as tubulin polymerization inhibitors with potent anticancer activities.

Southern Medical University
Discovery and development of selective aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors.

China Pharmaceutical University
Discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines as calcium-sensing receptor antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues.

Harvard Medical School
Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and lipid-lowering activities.

Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery and structure-activity relationships of 2-benzylpyrrolidine-substituted aryloxypropanols as calcium-sensing receptor antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute
Heteroaryl ether analogues of an antileishmanial 7-substituted 2-nitroimidazooxazine lead afford attenuated hERG risk: In vitro and in vivo appraisal.

University of Auckland
Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders.

TBA
Discovery of benzimidazole derivatives as potent and selective aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors with glucose consumption improving activity.

China Pharmaceutical University
Structure-Based Design of Selective LONP1 Inhibitors for Probing

Genomics Institute of The Novartis Research Foundation
Multifunctional agents based on benzoxazolone as promising therapeutic drugs for diabetic nephropathy.

Beijing Institute of Technology
Identification, Structure-Activity Relationships of Marine-Derived Indolocarbazoles, and a Dual PKCθ/δ Inhibitor with Potent Antipancreatic Cancer Efficacy.

Zhejiang University
Novel phenanthridin-6(5H)-one derivatives as potent and selective BET bromodomain inhibitors: Rational design, synthesis and biological evaluation.

Henan University of Traditional Chinese Medicine
Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant.

Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)
7-Substituted 2-Nitro-5,6-dihydroimidazo[2,1-b][1,3]oxazines: Novel Antitubercular Agents Lead to a New Preclinical Candidate for Visceral Leishmaniasis.

University of Auckland
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
PYRAZOLEAMIDE DERIVATIVES

Hoffmann-La Roche
Compounds and compositions for the treatment of parasitic diseases

Novartis
Substituted heteroaryls as inhibitors of the BCL6 BTB domain protein-protein interaction

Ontario Institute For Cancer Research (Oicr)
Azaspirocycles as monoacylglycerol lipase modulators

Janssen Pharmaceutica
Crystalline forms of a phosphoinositide 3-kinase (PI3K) inhibitor

Incyte
Compounds

Mission Therapeutics
3-aryl- heteroaryl substituted 5-trifluoromethyl oxadiazoles as histonedeacetylase 6 (HDAC6) inhibitors

Merck Sharp & Dohme
Pyridazine derivatives as RORc modulators

Genentech
Fused tricyclic ring derivatives as SRC homology-2 phosphatase inhibitors

Nikang Therapeutics
Bicyclic heteroaryl substituted compounds

Bristol-Myers Squibb
Benzothiazol compounds and methods using the same for treating neurodegenerative disorders

1St Biotherapeutics
4-heteroaryl substituted benzoic acid compounds as RORgammaT inhibitors and uses thereof

Merck Sharp & Dohme
2-oxothiazole compounds and method of using same for chronic inflammatory disorders

Avexxin
Structure of REV-ERBß ligand-binding domain bound to a porphyrin antagonist.

The Scripps Research Institute
The Parkinson disease-linked LRRK2 protein mutation I2020T stabilizes an active state conformation leading to increased kinase activity.

Harvard Neurodiscovery Center
New cholinesterase inhibitors for Alzheimer's disease: Structure Activity Studies (SARs) and molecular docking of isoquinolone and azepanone derivatives.

Universidade De Evora
Discovery of a Highly Selective STK16 Kinase Inhibitor.

Chinese Academy of Sciences
Inhibition of small ubiquitin-like modifier enzymes with substituted pyrrolo[2,3-b]quinoxalines

City of Hope
Combination therapy with MDM2 and EFGR inhibitors

TBA
Inhibition of arginine aminopeptidase by bestatin and arphamenine analogues. Evidence for a new mode of binding to aminopeptidases.

University of Wisconsin
Optimization of P1-P3 groups in symmetric and asymmetric HIV-1 protease inhibitors.

Uppsala University
Discovery of potent and selective orally bioavailable beta-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors.

Merck Research Laboratories