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240 articles for Y Hu


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
Discovery and Pre-Clinical Characterization of Third-Generation 4-H Heteroaryldihydropyrimidine (HAP) Analogues as Hepatitis B Virus (HBV) Capsid Inhibitors.EBI
Roche Innovation Center Shanghai
Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors.EBI
Chinese Academy of Sciences
Discovery of novel substituted octahydropyrrolo[3,4-c]pyrroles as dual orexin receptor antagonists for insomnia treatment.EBI
Wuxi Apptec (Shanghai)
Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors.EBI
Hangzhou Xixi Hospital
Recent Advances in Scaffold Hopping.EBI
Rheinische Friedrich-Wilhelms-Universit£T
Structure-Guided Design of Novel, Potent, and Selective Macrocyclic Plasma Kallikrein Inhibitors.EBI
Global Blood Therapeutics
Discovery of 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl)benzamides as novel RET kinase inhibitors.EBI
Ocean University of China
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.EBI
Zhejiang University
Design and synthesis of novel benzo[d]oxazol-2(3H)-one derivatives bearing 7-substituted-4-enthoxyquinoline moieties as c-Met kinase inhibitors.EBI
Shanghai Institute of Materia Medica
Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.EBI
Chinese Academy of Sciences
Discovery of novel nonpeptide allosteric inhibitors interrupting the interaction of CDK2/cyclin A3 by virtual screening and bioassays.EBI
Dalian Medical University
Design, synthesis and evaluation of rivastigmine and curcumin hybrids as site-activated multitarget-directed ligands for Alzheimer's disease therapy.EBI
Zhejiang University
Synthesis and Biological Evaluation of Novel Olean-28,13ß-lactams as Potential Antiprostate Cancer Agents.EBI
China Pharmaceutical University
Species-dependent uptake of glycylsarcosine but not oseltamivir in Pichia pastoris expressing the rat, mouse, and human intestinal peptide transporter PEPT1.EBI
University of Michigan
Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis.EBI
Chinese Academy of Sciences
Identification of novel inhibitors of Aurora A with a 3-(pyrrolopyridin-2-yl)indazole scaffold.EBI
Zhejiang University
Design, synthesis, and biological evaluation of novel 2-methylpiperazine derivatives as potent CCR5 antagonists.EBI
Zhejiang University
Design, synthesis and biological evaluation of thienopyridinones as Chk1 inhibitors.EBI
Zhejiang University
Identification of novel 4-anilinoquinazoline derivatives as potent EGFR inhibitors both under normoxia and hypoxia.EBI
TBA
Design, synthesis and biological evaluation of 6-(nitroimidazole-1H-alkyloxyl)-4-anilinoquinazolines as efficient EGFR inhibitors exerting cytotoxic effects both under normoxia and hypoxia.EBI
Zhejiang University
Design, synthesis and biological evaluation of novel tripeptidyl epoxyketone derivatives constructed fromß-amino acid as proteasome inhibitors.EBI
Zhejiang University
Integrating docking scores, interaction profiles and molecular descriptors to improve the accuracy of molecular docking: toward the discovery of novel Akt1 inhibitors.EBI
Zhejiang University
Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors.EBI
Zhejiang University
Design, synthesis, and biological evaluation of novel piperidine-4-carboxamide derivatives as potent CCR5 inhibitors.EBI
Zhejiang University
Characterization of a novela-conotoxin TxID from Conus textile that potently blocks rata3ß4 nicotinic acetylcholine receptors.EBI
Hainan University
Design, synthesis and evaluation of 7-azaindazolyl-indolyl-maleimides as glycogen synthase kinase-3ß (GSK-3ß) inhibitors.EBI
Zhejiang University
Synthesis and biological evaluation of novel benzyl-substituted (S)-phenylalanine derivatives as potent dipeptidyl peptidase 4 inhibitors.EBI
Zhejiang University
Hit-to-lead optimization and kinase selectivity of imidazo[1,2-a]quinoxalin-4-amine derived JNK1 inhibitors.EBI
Activx Biosciences
Amides of 4-hydroxy-8-methanesulfonylamino-quinoline-2-carboxylic acid as zinc-dependent inhibitors of Lp-PLA2.EBI
Activx Biosciences
Design, modification and 3D QSAR studies of novel naphthalin-containing pyrazoline derivatives with/without thiourea skeleton as anticancer agents.EBI
Nanjing University
Design, synthesis and evaluation of novel heterodimers of donepezil and huperzine fragments as acetylcholinesterase inhibitors.EBI
The Hong Kong University of Science and Technology
Development of substituted N-[3-(3-methoxylphenyl)propyl] amides as MT(2)-selective melatonin agonists: improving metabolic stability.EBI
Hong Kong University of Science and Technology
Synthesis and biological evaluation of crown ether fused quinazoline analogues as potent EGFR inhibitors.EBI
Zhejiang Betapharma
Potent and orally efficacious benzothiazole amides as TRPV1 antagonists.EBI
Astrazeneca
Synthesis and structure-activity relationship of (1-halo-2-naphthyl) carbamate-based inhibitors of KIAA1363 (NCEH1/AADACL1).EBI
Activx Biosciences
5-Cyano-6-oxo-1,6-dihydro-pyrimidines as potent antagonists targeting exchange proteins directly activated by cAMP.EBI
University of Texas Medical Branch
Discovery of novel 2-piperidinol-3-(arylsulfonyl)quinoxalines as phosphoinositide 3-kinasea (PI3Ka) inhibitors.EBI
Zhejiang University
Structure-activity relationship of a new series of reversible dual monoacylglycerol lipase/fatty acid amide hydrolase inhibitors.EBI
Universidad Complutense De Madrid
Pharmacophore identification, synthesis, and biological evaluation of carboxylated chalcone derivatives as CysLT1 antagonists.EBI
Zhejiang University
Dual-target-directed 1,3-diphenylurea derivatives: BACE 1 inhibitor and metal chelator against Alzheimer's disease.EBI
Zhejiang University
Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors.EBI
Wyeth Research
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1' substrate binding pocket.EBI
Wyeth Research
Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors.EBI
Zhejiang University
Synthesis, molecular docking and biological evaluation of 1,3,4-oxadiazole derivatives as potential immunosuppressive agents.EBI
Nanjing University
Amides of xanthurenic acid as zinc-dependent inhibitors of Lp-PLA(2).EBI
Activx Biosciences
Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H3R and BACE 1 inhibitory activities.EBI
Zhejiang University
Structure-based design of isoindoline-1,3-diones and 2,3-dihydrophthalazine-1,4-diones as novel B-Raf inhibitors.EBI
Pfizer
Pharmacophore identification, virtual screening and biological evaluation of prenylated flavonoids derivatives as PKB/Akt1 inhibitors.EBI
Zhejiang University
Continued exploration of biphenylsulfonamide scaffold as a platform for aggrecanase-1 inhibition.EBI
Pfizer
Synthesis and biological evaluation of novel 2-arylamino-3-(arylsulfonyl)quinoxalines as PI3Ka inhibitors.EBI
Zhejiang University
Identification and SAR of a new series of thieno[3,2-d]pyrimidines as Tpl2 kinase inhibitors.EBI
Pfizer
Discovery of indazoles as inhibitors of Tpl2 kinase.EBI
Pfizer
Macrocyclic lactams as potent Hsp90 inhibitors with excellent tumor exposure and extended biomarker activity.EBI
Pfizer
Design and SAR of macrocyclic Hsp90 inhibitors with increased metabolic stability and potent cell-proliferation activity.EBI
Pfizer
Compounds structurally related to ellagic acid show improved antiplasmodial activity.EBI
Justus-Liebig-University
Aminopyridinecarboxamide-based inhaled IKK-2 inhibitors for asthma and COPD: Structure-activity relationship.EBI
Pfizer
Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.EBI
Pfizer
The identification of 8,9-dimethoxy-5-(2-aminoalkoxy-pyridin-3-yl)-benzo[c][2,7]naphthyridin-4-ylamines as potent inhibitors of 3-phosphoinositide-dependent kinase-1 (PDK-1).EBI
Wyeth Research
B-Raf kinase inhibitors: hit enrichment through scaffold hopping.EBI
Wyeth Research
Synthesis of substituted N-[3-(3-methoxyphenyl)propyl] amides as highly potent MT(2)-selective melatonin ligands.EBI
Hong Kong University of Science and Technology
Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors.EBI
Wyeth
Pyridinyl aminohydantoins as small molecule BACE1 inhibitors.EBI
Wyeth Research
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.EBI
Wyeth Research
Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.EBI
Wyeth Research
Discovery of highly potent and selective type I B-Raf kinase inhibitors.EBI
Wyeth Research
Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors.EBI
Zhejiang University
Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors.EBI
Wyeth Research
Novel pyrazolopyrimidines as highly potent B-Raf inhibitors.EBI
Wyeth Research
Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors.EBI
Wyeth Research
QSAR study of Akt/protein kinase B (PKB) inhibitors using support vector machine.EBI
Zhejiang University
Synthesis and biological evaluation of 1,2,4-trisubstituted imidazoles and 1,3,5-trisubstituted pyrazoles as inhibitors of transforming growth factor beta type 1 receptor (ALK5).EBI
Institute of Pharmacology and Toxicology
3,4-Disubstituted benzofuran P1' MMP-13 inhibitors: optimization of selectivity and reduction of protein binding.EBI
Wyeth Research
Synthesis and optimization of 2-pyridin-3-yl-benzo[d][1,3]oxazin-4-one based inhibitors of human neutrophil elastase.EBI
Activx Biosciences
Synthesis and biological evaluation of novel 4-azaindolyl-indolyl-maleimides as glycogen synthase kinase-3beta (GSK-3beta) inhibitors.EBI
Zhejiang University
Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.EBI
Wyeth Research
 
Synthesis and biological activity of 2-desamino and 4-deoxy analogs of 5,10-dideazatetrahydrofolic acid (DDATHF)EBI
TBA
Synthesis and biological evaluation of ((4-keto)-phenoxy)methyl biphenyl-4-sulfonamides: a class of potent aggrecanase-1 inhibitors.EBI
Wyeth Research
Identification of pharmacophore model, synthesis and biological evaluation of N-phenyl-1-arylamide and N-phenylbenzenesulfonamide derivatives as BACE 1 inhibitors.EBI
Zhejiang University
Discovery of the catechol structural moiety as a Stat3 SH2 domain inhibitor by virtual screening.EBI
Wyeth Pharmaceuticals
2-Phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors: a study on the importance of modifications at the side chain on the activity.EBI
Zhejiang University
Design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors.EBI
Zhejiang University
Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives.EBI
Zhejiang University
Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood.EBI
Wyeth Research
Recent advances in small molecule and peptide inhibitors of glucose-regulated protein 78 for cancer therapy.EBI
The First Affiliated Hospital of Henan University
Research progress of VEGFR small molecule inhibitors in ocular neovascular diseases.EBI
Southwest Jiaotong University
Discovery of new tetrahydroisoquinolines as potent and selective LSD1 inhibitors for the treatment of MLL-rearranged leukemia.EBI
Zhejiang Ocean University
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets.EBI
Wyeth Research
Cellular, Structural Basis, and Recent Progress for Targeting Murine Double Minute X (MDMX) in Tumors.EBI
Yantai University
Discovery and Optimization of Hsp110 and sGC Dual-Target Regulators for the Treatment of Pulmonary Arterial Hypertension.EBI
Central South University
Total synthesis/semi-synthesis of natural isopentenyl flavonoids with inhibitory activity on NLRP3 inflammasome.EBI
East China University of Science and Technology
Benzodioxane Carboxamide Derivatives As Novel Monoamine Oxidase B Inhibitors with Antineuroinflammatory Activity.EBI
Zunyi Medical University
Design, synthesis and evaluation of novel UDCA-aminopyrimidine hybrids as ATX inhibitors for the treatment of hepatic and pulmonary fibrosis.EBI
Chinese Academy of Medical Sciences and Peking Union Medical College
Coumarin-furo[2,3-d]pyrimidone hybrid molecules targeting human liver cancer cells: synthesis, anticancer effect, EGFR inhibition and molecular docking studies.EBI
Hubei University
Discovery of N-alkyl-N-benzyl thiazoles as novel TRPC antagonists for the treatment of glioblastoma multiforme.EBI
Yantai University
Discovery and Optimization of Tetrahydroisoquinoline Derivatives To Enhance Lysosome Biogenesis as Preclinical Candidates for the Treatment of Alzheimer's Disease.EBI
Nanjing University of Chinese Medicine
Thiophene substituted acylguanidines as BACE1 inhibitors.EBI
Wyeth Research
New Strategies for Responding to SARS-CoV-2: The Present and Future of Dual-Target Drugs.EBI
China Pharmaceutical University
Identification of a novel class of selective Tpl2 kinase inhibitors: 4-Alkylamino-[1,7]naphthyridine-3-carbonitriles.EBI
Wyeth Research
Design, Synthesis, and Antitumor Efficacy of Substituted 2-Amino[1,2,4]triazolopyrimidines and Related Heterocycles as Dual Inhibitors for Microtubule Polymerization and Janus Kinase 2.EBI
Wuyi University
A novel BODIPY-based theranostic agent for EBI
Shanghai Institute of Materia Medica
Discovery of marine phidianidine-based Nrf2 activators and their potential against oxLDL- and HG-induced injury in HUVECs.EBI
University of Jinan
Degradation of Cyclin-Dependent Kinase 9/Cyclin T1 by Optimized Microtubule-Associated Protein 1 Light Chain 3 Beta-Recruiting Coumarin Analogs.EBI
Shanghai Institute of Materia Medica
Machine learning- and structure-based discovery of a novel chemotype as FXR agonists for potential treatment of nonalcoholic fatty liver disease.EBI
Chinese Academy of Medical Sciences&Peking Union Medical College
Discovery of (EBI
Shanghai Institute of Materia Medica
Discovery of Novel Sesquiterpene Lactone Derivatives as Potent PKM2 Activators for the Treatment of Ulcerative Colitis.EBI
Nanjing University of Chinese Medicine
Discovery of selective NaEBI
Shanghai Institute of Materia Medica
Affinity of Rimantadine Enantiomers against Influenza A/M2 Protein Revisited.EBI
National and Kapodistrian University of Athens
Recent advances of dual FGFR inhibitors as a novel therapy for cancer.EBI
Southwest Jiaotong University
Discovery of mobocertinib, a potent, oral inhibitor of EGFR exon 20 insertion mutations in non-small cell lung cancer.EBI
Ariad Pharmaceuticals
Inhibition of Tpl2 kinase and TNFalpha production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis.EBI
Wyeth Research
Discovery and preclinical evaluations of GST-HG131, a novel HBV antigen inhibitor for the treatment of chronic hepatitis B infection.EBI
Wuxi Apptec
Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors.EBI
Sun Yat-Sen University Cancer Center
Adjusted degradation of BRD4 S and BRD4 L based on fine structural modifications of the pyrrolopyridone scaffold.EBI
University of Chinese Academy of Sciences
Long Residence Time at the Vasopressin VEBI
Xuzhou Medical University
Discovery of BP3 as an efficacious proteolysis targeting chimera (PROTAC) degrader of HSP90 for treating breast cancer.EBI
Fujian Medical University (Fmu)
Expedited Approach toward the Rational Design of Noncovalent SARS-CoV-2 Main Protease Inhibitors.EBI
The University of Arizona
Discovery of 2,4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety as novel ALK inhibitors.EBI
Shenyang Pharmaceutical University
Discovery of highly potent SARS-CoV-2 MEBI
Nanjing University of Chinese Medicine
Progress and Challenges in Targeting the SARS-CoV-2 Papain-like Protease.EBI
The State University of New Jersey
Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships.EBI
Wyeth Research
Synthesis and SAR of highly selective MMP-13 inhibitors.EBI
Wyeth Research
Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7.EBI
Activx Biosciences
Boro-norleucine as a P1 residue for the design of selective and potent DPP7 inhibitors.EBI
Activx Biosciences
NAE modulators: A potential therapy for gastric carcinoma.EBI
Southwest Jiaotong University
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.EBI
Schering-Plough Research Institute
Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent.EBI
Wuxi Apptec
Synthesis and application of phosphorylated saccharides in researching carbohydrate-based drugs.EBI
Henan University of Chinese Medicine
Identification of the Benzoimidazole Compound as a Selective FLT3 Inhibitor by Cell-Based High-Throughput Screening of a Diversity Library.EBI
Sun Yat-Sen University Cancer Center
Identification of Novel Carbocyclic Pyrimidine Cyclic Dinucleotide STING Agonists for Antitumor Immunotherapy Using Systemic Intravenous Route.EBI
Takeda Pharmaceuticals International
A tacrine-tetrahydroquinoline heterodimer potently inhibits acetylcholinesterase activity and enhances neurotransmission in mice.EBI
The Hong Kong University of Science and Technology
Discovery of Potent Antiallergic Agents Based on an EBI
Chinese Academy of Sciences
Discovery of hydrazide-containing oseltamivir analogues as potent inhibitors of influenza A neuraminidase.EBI
Shenyang Pharmaceutical University
Discovery of TAK-981, a First-in-Class Inhibitor of SUMO-Activating Enzyme for the Treatment of Cancer.EBI
Millennium Pharmaceuticals, A Wholly Owned Subsidiary of Takeda Pharmaceuticals
SAR development of polycyclic guanine derivatives targeted to the discovery of a selective PDE5 inhibitor for treatment of erectile dysfunction.EBI
Schering-Plough Research Institute
Discovery of EBI
Zhejiang University
Synthesis, biological evaluation and molecular modeling of benzofuran piperidine derivatives as Aβ antiaggregant.EBI
Shanghai Jiao Tong University (Sjtu)
A theranostic probe of indoleamine 2,3-dioxygenase 1 (IDO1) for small molecule cancer immunotherapy.EBI
Second Military Medical University
Identification of N-phenyl-3-methoxy-4-pyridinones as orally bioavailable HEBI
Zhejiang University
Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.EBI
Shanghai Institute of Materia Medica
Discovery of 1,5-Dihydro-4EBI
Zhejiang University
GPR52 Antagonist Reduces Huntingtin Levels and Ameliorates Huntington's Disease-Related Phenotypes.EBI
Fudan University
Structure-based design, synthesis and bioactivity evaluation of macrocyclic inhibitors of mutant isocitrate dehydrogenase 2 (IDH2) displaying activity in acute myeloid leukemia cells.EBI
Hangzhou Institute of Innovative Medicine
Structurally novel PI3Kδ/γ dual inhibitors characterized by a seven-membered spirocyclic spacer: The SARs investigation and PK evaluation.EBI
Anhui University of Chinese Medicine
Discovery of a Bioactive Inhibitor with a New Scaffold for Cystathionine γ-Lyase.EBI
Shanghai Jiao Tong University
Synthesis and Anti-HCV Activity of Sugar-Modified Guanosine Analogues: Discovery of EBI
Janssen Biopharma
3-Deoxy-3-substituted-D-myo-inositol imidazolyl ether lipid phosphates and carbonate as inhibitors of the phosphatidylinositol 3-kinase pathway and cancer cell growth.EBI
Georgetown University Medical Center
Synthesis and aromatase inhibitory evaluation of 4-N-nitrophenyl substituted amino-4H-1,2,4-triazole derivatives.EBI
Key Laboratory of Industrial Fermentation Microbiology (Tianjin University of Science & Technology)
Novel tricyclic poly (ADP-ribose) polymerase-1/2 inhibitors with potent anticancer chemopotentiating activity: Design, synthesis and biological evaluation.EBI
China Pharmaceutical University
Effective Virtual Screening Strategy toward heme-containing proteins: Identification of novel IDO1 inhibitors.EBI
China Pharmaceutical University
Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design.EBI
Chinese Academy of Sciences
Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies.EBI
Zhejiang University
Synthesis and Anti-HCV Activities of 4'-Fluoro-2'-Substituted Uridine Triphosphates and Nucleotide Prodrugs: Discovery of 4'-Fluoro-2'- C-methyluridine 5'-Phosphoramidate Prodrug (AL-335) for the Treatment of Hepatitis C Infection.EBI
Janssen Biopharma
Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies.EBI
Zhejiang University
Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression.EBI
TBA
Development of Macrocyclic Peptides Containing Epoxyketone with Oral Availability as Proteasome Inhibitors.EBI
Zhejiang University
Synthesis and biological evaluation of 3-aryl-4-indolyl-maleimides as potent mutant isocitrate dehydrogenase-1 inhibitors.EBI
Zhejiang University
Discovery of NEBI
Zhuhai Campus of Zunyi Medical University
Novel Class of Colony-Stimulating Factor 1 Receptor Kinase Inhibitors Based on an EBI
Chinese Academy of Sciences
Discovery of pyrazole-thiophene derivatives as highly Potent, orally active Akt inhibitors.EBI
Hangzhou Institute of Innovative Medicine
Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation.EBI
Zhejiang University
Design and synthesis of novel 3-substituted-indole derivatives as selective H3 receptor antagonists and potent free radical scavengers.EBI
Zhejiang University
Structure-based drug design using GPCR homology modeling: toward the discovery of novel selective CysLT2 antagonists.EBI
Zhejiang University
Discovery of novel 2,6-disubstituted pyridazinone derivatives as acetylcholinesterase inhibitors.EBI
Chinese Academy of Sciences
Identification and synthesis of substituted pyrrolo[2,3-d]pyrimidines as novel firefly luciferase inhibitors.EBI
Chinese Academy of Sciences
Synthesis and biological evaluation of novel amprenavir-based P1-substituted bi-aryl derivatives as ultra-potent HIV-1 protease inhibitors.EBI
Chinese Academy of Sciences
Synthesis and biological evaluation of 2,4,5-substituted pyrimidines as a new class of tubulin polymerization inhibitors.EBI
Chinese Academy of Sciences
Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide gamma-secretase inhibitors.EBI
Wyeth Research
3-(Hydroxymethyl)-bearing phosphatidylinositol ether lipid analogues and carbonate surrogates block PI3-K, Akt, and cancer cell growth.EBI
Georgetown University Medical Center
Design, synthesis, and evaluation of carboxyl-modified oseltamivir derivatives with improved lipophilicity as neuraminidase inhibitors.EBI
Shenyang Pharmaceutical University
Synthesis and biological evaluation of coumarin derivatives containing imidazole skeleton as potential antibacterial agents.EBI
Northwest A&F University
Synthesis and biological evaluation of NHEBI
Shenyang Pharmaceutical University
Design, synthesis and structure-activity relationship study of novel naphthoindolizine and indolizinoquinoline-5,12-dione derivatives as IDO1 inhibitors.EBI
Peking University
Discovery of N-aryl-N'-pyrimidin-4-yl ureas as irreversible L858R/T790M mutant selective epidermal growth factor receptor inhibitors.EBI
Shanghai Haiyan Pharmaceutical Technology Co. Itd.
Discovery of imidazoleisoindole derivatives as potent IDO1 inhibitors: Design, synthesis, biological evaluation and computational studies.EBI
China Pharmaceutical University
Design, Synthesis, and Biological Evaluation of the First c-Met/HDAC Inhibitors Based on Pyridazinone Derivatives.EBI
Chinese Academy of Sciences
Surrogating and redirection of pyrazolo[1,5-a]pyrimidin-7(4H)-one core, a novel class of potent and selective DPP-4 inhibitors.EBI
Shanghai Jiao Tong University
Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor.EBI
University of Michigan
Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor.EBI
TBA
Discovery of Highly Potent Pinanamine-Based Inhibitors against Amantadine- and Oseltamivir-Resistant Influenza A Viruses.EBI
School of Pharmaceutical Sciences & The Fifth Affiliated Hospital
Slow but Steady Wins the Race: Dissimilarities among New Dual Inhibitors of the Wild-Type and the V27A Mutant M2 Channels of Influenza A Virus.EBI
Universitat De Barcelona
Discovery of a low-systemic-exposure DGAT-1 inhibitor with a picolinoylpyrrolidine-2-carboxylic acid moiety.EBI
Xinxiang Medical University
In Vitro Pharmacokinetic Optimizations of AM2-S31N Channel Blockers Led to the Discovery of Slow-Binding Inhibitors with Potent Antiviral Activity against Drug-Resistant Influenza A Viruses.EBI
The University of Arizona
BICYCLIC CX3CR1 RECEPTOR AGONISTSBDB
University of Texas System
SUBSTITUTED 6,7-DIHYDRO-5H-BENZO[7]ANNULENE DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THERAPEUTIC USES THEREOFBDB
Sanofi
Compounds and uses thereofBDB
Foghorn Therapeutics
InhibitorsBDB
Vivoryon Therapeutics
3-BETA-HSD1 INHIBITORS AND COMPOSITIONS AND USES THEREOFBDB
The Cleveland Clinic Foundation
3-[(1H-PYRAZOL-4-YL)OXY]PYRAZIN-2-AMINE COMPOUNDS AS HPK1 INHIBITOR AND USE THEREOFBDB
BeiGene
METHODS FOR INHIBITING PARASITIC GLUCOKINASE AND/OR HEXOKINASEBDB
University of South Carolina
TYK2 INHIBITORSBDB
Biogen Ma
Substituted benzodiazoles and use thereof in therapyBDB
Thomas Helledays Stiftelse FÖR Medicinsk Forskning
Methods of inhibiting cyclooxygenaseBDB
King Faisal University
Advantageous benzofuran compositions for mental disorders or enhancementBDB
Tactogen
Substituted pyridopyrimidinonyl compounds useful as T cell activatorsBDB
Bristol-Myers Squibb
ACLY inhibitors and uses thereofBDB
Nimbus Artemis
Compounds that interact with the Ras superfamily for the treatment of cancers, inflammatory diseases, Rasopathies, and fibrotic diseaseBDB
Shy Therapeutics
Heterocyclic compounds for the inhibition of PASKBDB
Bioenergenix
PyridazinesBDB
Boehringer Ingelheim International
Imidazopyrimidine and imidazotriazine derivative, and pharmaceutical composition comprising the sameBDB
Sk Biopharmaceuticals
Inhibitors of lysine specific demethylase-1BDB
Celgene Quanticel Research
Therapeutically active compounds and their methods of useBDB
Agios Pharmaceuticals
Imidazopyrazine compounds, preparation methods and uses thereofBDB
Dongguan Zhenxing-Beite Medicine Technology
KV1.3 inhibitors and their medical applicationBDB
4Sc
4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenaseBDB
Eastern Virginia Medical School
Macrocylic compounds as ROS1 kinase inhibitorsBDB
Array Biopharma
Chemokine CXCR1 and CXCR2 receptor antagonist compounds, and use thereof in the treatment of chemokine-mediated pathologiesBDB
Galderma Research & Development
Inhibitors of RETBDB
Blueprint Medicines
2-azabicyclo[3.1.0]hexan-3-one derivatives and methods of useBDB
Genentech
[4-(1,3,3-trimethyl-2-oxo-3,4-dihydro-1H-quinoxalin-7-yl)phenoxy]ethyloxy compound or salt thereofBDB
Santen Pharmaceutical
Pyridinone and pyrimidinone derivatives as factor XiaBDB
Ono Pharmaceutical
7-azaindole derivativesBDB
Merck Patent
Inhibitors of RETBDB
Blueprint Medicines
Somatostatin receptor subtype 4 (SSTR4) agonistsBDB
Centrexion Therapeutics
Alkylene derivativesBDB
Shionogi
Piperidinone derivatives as MDM2 inhibitors for the treatment of cancerBDB
Amgen
Inhibitors of lysine specific demethylase-1BDB
Celgene Quanticel Research
Synthesis and HIV-1 RT inhibitory action of novel (4/6-substituted benzo[d]thiazol -2-yl)thiazolidin-4-ones. Divergence from the non-competitive inhibition mechanism.BDB
Aristotle University of Thessaloniki
Allosteric inhibitors of the Eya2 phosphatase are selective and inhibit Eya2-mediated cell migration.BDB
University of Colorado School of Medicine
Synthesis and biological evaluation of novel flavanone derivatives as potential antipsychotic agents.BDB
Key Laboratory For Neurodegenerative Diseases of Ministry of Education
Synthesis and in silico studies of novel sulfonamides having oxadiazole ring: As ß-glucuronidase inhibitors.BDB
Universiti Teknologi Mara (Uitm)
Piperidylpyrimidine derivatives as modulators of protein kinase inhibitors and of vascular endothelial growth factor receptor 2BDB
Allergan
Triazolopyridinone PDE10 inhibitorsBDB
Merck Sharp & Dohme
Discovery and Characterization of Allosteric WNK Kinase Inhibitors.BDB
Novartis Institutes For Biomedical Research
Morpholinylbenzotriazines for use in cancer therapyBDB
Merck Patent
Inhibitors of human EZH2, and methods of use thereofBDB
Epizyme
Rosuvastatin and atorvastatin derivativesBDB
Redx Pharma
Design, Synthesis, and Evaluation of Polyamine Deacetylase Inhibitors, and High-Resolution Crystal Structures of Their Complexes with Acetylpolyamine Amidohydrolase.BDB
University of Pennsylvania
Mechanistic studies of inactivation of inducible nitric oxide synthase by amidines.BDB
Northwestern University
Modulators of calcium release-activated calcium channelBDB
Rhizen Pharmaceuticals
Piperazine compound capable of inhibiting prostaglandin D synthaseBDB
Taiho Pharmaceutical
Substituted benzamide analogs as mGluR5 negative allosteric modulators and methods of making and using the sameBDB
Vanderbilt University
Synthesis of casimiroin and optimization of its quinone reductase 2 and aromatase inhibitory activities.BDB
Purdue University
The reversed binding of beta-phenethylamine inhibitors of DPP-IV: X-ray structures and properties of novel fragment and elaborated inhibitors.BDB
Santhera Pharmaceuticals
Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2.BDB
Vernalis (R&D)