PMID
Cmpds
Data
Article Title
Organization
18
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.

East China University of Science and Technology
36
Discovery of MK-1832, a Kv1.5 inhibitor with improved selectivity and pharmacokinetics.

Merck Research Laboratories
16
Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.

Vitae Pharmaceuticals
13
Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) Agonist.

Vitae Pharmaceuticals
4
Identification and in Vivo Evaluation of Liver X Receptor -Selective Agonists for the Potential Treatment of Alzheimer's Disease.

Wuxi Apptec
14
Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors.

China Pharmaceutical University
34
Discovery of substituted (4-phenyl-1H-imidazol-2-yl)methanamine as potent somatostatin receptor 3 agonists.

Merck Research Laboratories
6
Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety.

Merck Research Laboratories
44
Diamine Derivatives as Novel Small-Molecule, Potent, and Subtype-Selective Somatostatin SST3 Receptor Agonists.

Merck Research Laboratories
22
Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series.

Merck Research Laboratories
77
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.

Merck Research Laboratories
21
Potent DGAT1 Inhibitors in the Benzimidazole Class with a Pyridyl-oxy-cyclohexanecarboxylic Acid Moiety.

Merck Research Laboratories
30
Novel soluble myeloid cell leukemia sequence 1 (Mcl-1) inhibitor (E,E)-2-(benzylaminocarbonyl)-3-styrylacrylonitrile (4g) developed using a fragment-based approach.

Dalian University of Technology
20
Fragment-based design, synthesis, and biological evaluation of N-substituted-5-(4-isopropylthiophenol)-2-hydroxynicotinamide derivatives as novel Mcl-1 inhibitors.

Dalian University of Technology
24
3-Thiomorpholin-8-oxo-8H-acenaphtho [1,2-b] pyrrole-9-carbonitrile (S1) derivatives as pan-Bcl-2-inhibitors of Bcl-2, Bcl-xL and Mcl-1.

Dalian University of Technology
69
2' biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR.

Glaxosmithkline
53
2' biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling.

Glaxosmithkline
35
N-alkyl-5H-pyrido[4,3-b]indol-1-amines and derivatives as novel urotensin-II receptor antagonists.

Glaxosmithkline
17
New quinoline NK3 receptor antagonists with CNS activity.

Neuroscience Cedd Glaxosmithkline Research & Development
5
Novel N-Substituted Benzimidazolones as Potent, Selective, CNS-Penetrant, and Orally Active M1 mAChR Agonists.

TBA
9
Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility.

TBA
10
Bisubstrate Inhibitors of the MYST HATs Esa1 and Tip60.

Georgia State University
3
2-Aminomethyl piperidines as novel urotensin-II receptor antagonists.

Glaxosmithkline
3
Synthesis of a potent and selective (18)F-labeled delta-opioid receptor antagonist derived from the Dmt-Tic pharmacophore for positron emission tomography imaging.

Stanford University School of Medicine
19
Rapid assembly of diverse and potent allosteric Akt inhibitors.

Merck Research Laboratories
38
Discovery of aminoheterocycles as potent and brain penetrant prolylcarboxypeptidase inhibitors.

Merck Research Laboratories
26
Discovery of a new class of potent prolylcarboxypeptidase inhibitors derived from alanine.

Merck Research Laboratories
56
Discovery of dehydro-oxopiperazine acetamides as novel bradykinin B1 receptor antagonists with enhanced in vitro potency.

Amgen
35
Biphenyl/diphenyl ether renin inhibitors: filling the S1 pocket of renin via the S3 pocket.

Vitae Pharmaceuticals
15
Imidazopyridine CB2 agonists: optimization of CB2/CB1 selectivity and implications for in vivo analgesic efficacy.

Merck Research Laboratories
30
Optimization of orally bioavailable alkyl amine renin inhibitors.

Vitae Pharmaceuticals
56
Camphor sulfonamide derivatives as novel, potent and selective CXCR3 antagonists.

Glaxosmithkline
35
Aminomethylpiperazines as selective urotensin antagonists.

Glaxosmithkline
15
Synthesis and biological evaluation of novel 4-Arylaminoquinolines derivatives as EGFR/HDAC inhibitors.

Beijing University of Technology
37
Discovery of Potent and Balanced Dual RIPK2 and 3 Inhibitors as a New Strategy for the Treatment of Inflammatory Bowel Diseases.

Anhui Medical University
1
Synthesis and evolution of 16-membered macrolide carrimycin derivatives as a novel class of anti-HCoV-OC43 agents targeting viral FSE RNA.

Peking Union Medical College and Chinese Academy of Medical Sciences
3
A Prostate-Specific Membrane Antigen-Targeting Small Molecule-Drug Conjugate Strategy to Overcome the Hematological Toxicity of Olaparib.

Zhejiang University
55
Design, Synthesis, and Antitumor Activity Evaluation of 2-Phenylthiazole-5-Carboxylic Acid Derivatives Targeting Transactivation Response RNA-Binding Protein 2.

Chengdu Institute of Biology
67
Design, synthesis, and evaluation of 4-(4-methyl-4H-1,2,4-triazol-3-yl)piperidine derivatives as potential glutaminyl cyclase isoenzyme inhibitors for the treatment of cancer.

Shenzhen University Medical School
1
Discovery of a potent and selective TRPC3 antagonist with neuroprotective effects.

University of Tennessee Health Science Center
31
Inhibitors targeting the PWWP domain-containing proteins.

Central China Normal University
33
Discovery of Sovleplenib, a Selective Inhibitor of Syk in Clinical Development for Autoimmune Diseases and Cancers.

Hutchmed
6
The synthesis of 1,2,3-triazoles as binders of D-dopachrome tautomerase (D-DT) for the development of dual-targeting inhibitors.

University of Groningen
6
Design, synthesis and biological evaluation of biaryl amide derivatives against SARS-CoV-2 with dual-target mechanism.

Chinese Academy of Medical Sciences and Peking Union Medical College
57
Targeting autophagy drug discovery: Targets, indications and development trends.

China Jiliang University
1
Synthesis and Bioevaluation of 3-(Arylmethylene)indole Derivatives: Discovery of a Novel ALK Modulator with Antiglioblastoma Activities.

Nanjing Medical University
4
Design, Synthesis, and Biological Evaluation of Novel Thioureidobenzamide (TBA) Derivatives as HBV Capsid Assembly Modulators.

Weifang Medical University
44
Discovery of orally active 1,4,5,6,8-pentaazaacenaphthylens as novel, selective, and potent covalent BTK inhibitors for the treatment of rheumatoid arthritis.

China Pharmaceutical University
30
Design, synthesis and biological evaluation of novel coumarin derivatives as multifunctional ligands for the treatment of Alzheimer's disease.

Shenyang Pharmaceutical University
4
Discovery of 5-(Pyrimidin-2-ylamino)-1

Xiamen University
41
Design and discovery of new selective and potent VEGF receptor 2 tyrosine kinase inhibitors.

Nankai University
1
Discovery of bipyridine amide derivatives targeting pRXRα-PLK1 interaction for anticancer therapy.

Xiamen University
3
Discovery of 5-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)-1H-indole-2-carboxamide derivatives as novel anti-cancer agents targeting Nur77.

Xiamen University
12
Single and dual target inhibitors based on Bcl-2: Promising anti-tumor agents for cancer therapy.

Shandong First Medical University & Shandong Academy of Medical Sciences
13
Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors.

Sun Yat-Sen University Cancer Center
35
Fragment-Guided Discovery of Pyrazole Carboxylic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2 Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction.

Astex Pharmaceuticals
9
Synthesis and structure-activity relationships of novel dipeptides and reduced dipeptides as ligands for melanocortin subtype-4 receptor.

Eli Lilly
7
Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain.

Eli Lilly
6
Insights into the modular design of kinase inhibitors and application to Abl and Axl.

University of Michigan
25
Diminishing GSH-Adduct Formation of Tricyclic Diazepine-based Mutant IDH1 Inhibitors.

Merck
15
Lead Optimization to Advance Protease-Activated Receptor-1 Antagonists in Early Discovery.

TBA
2
Design, synthesis, and structure-activity relationships of haloenol lactones: site-directed and isozyme-selective glutathione S-transferase inhibitors.

Chinese Academy of Sciences
66
Discovery and Development of a Potent, Selective, and Orally Bioavailable CHK1 Inhibitor Candidate: 5-((4-((3-Amino-3-methylbutyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)picolinonitrile.

Zhejiang University
1
Synthesis and biological evaluation of selective survivin inhibitors derived from the MX-106 hydroxyquinoline scaffold.

University of Tennessee Health Science Center
3
Using porphyrins as albumin-binding molecules to enhance antitumor efficacies and reduce systemic toxicities of antimicrobial peptides.

Fuzhou University
18
Discovery of novel and potent PARP/PI3K dual inhibitors for the treatment of cancer.

China Pharmaceutical University
1
Design, synthesis, and biological evaluation of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as novel Nur77 modulators.

Xiamen University
2
Discovery of a Highly Selective and Potent TRPC3 Inhibitor with High Metabolic Stability and Low Toxicity.

The University of Tennessee Health Science Center
20
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide.

China Pharmaceutical University
27
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.

Merck And
8
Design and synthesis of novel dual-cyclic RGD peptides for α

Nanchang University
12
Protein Tyrosine Phosphatase 1B Inhibitory Iridoids from

University of Illinois At Chicago
8
A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARalpha agonist with potent lipid-lowering activity.

Glaxo Wellcome Research & Development
53
Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC).

Merck
13
Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships.

Schering-Plough Research Institute
20
Structure-Activity and Structure-Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein-Protein Interaction.

Astex Pharmaceuticals
5
Novel Cell-Penetrating Peptide Conjugated Proteasome Inhibitors: Anticancer and Antifungal Investigations.

University of Auckland
10
Flavipesines A and B and Asperchalasines E-H: Cytochalasans and Merocytochalasans from

Huazhong University of Science and Technology
2
Development of Novel

East China University of Science and Technology
6
Benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moiety.

Merck
22
Discovery of novel triazolobenzazepinones as γ-secretase modulators with central Aβ42 lowering in rodents and rhesus monkeys.

Merck Research Laboratories Boston
31
GluK1 antagonists from 6-(tetrazolyl)phenyl decahydroisoquinoline derivatives: in vitro profile and in vivo analgesic efficacy.

Centro De Investigaci�N Lilly
26
GluK1 antagonists from 6-(carboxy)phenyl decahydroisoquinoline derivatives. SAR and evaluation of a prodrug strategy for oral efficacy in pain models.

Centro De Investigaci�N Lilly
25
A novel necroptosis inhibitor-necrostatin-21 and its SAR study.

Chinese Academy of Sciences
3
Natural Product Micheliolide (MCL) Irreversibly Activates Pyruvate Kinase M2 and Suppresses Leukemia.

Nankai University
50
Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl-1H-benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors.

Merck
47
Improvement of hERG-ROMK index of spirocyclic ROMK inhibitors through scaffold optimization and incorporation of novel pharmacophores.

Merck
19
Discovery of N-(6-Fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-[(3R)-3-hydroxypyrrolidin-1-yl]thiophene-2-sulfonamide (LSN 3213128), a Potent and Selective Nonclassical Antifolate Aminoimidazole-4-carboxamide Ribonucleotide Formyltransferase (AICARFT) Inhibitor Effective at Tumor Suppression in a Can

Eli Lilly
8
New potent and selectiveαvβ

Jiangnan University
160
INDAZOLES AS HEMATOPOIETIC PROGENITOR KINASE 1 (HPK1) INHIBITORS AND METHODS FOR USING SAME

1ST Biotherapeutics
27
Indane derivatives as hypoxia inducible factor-2(α) inhibitors

Nikang Therapeutics
122
Pyrrolotriazinones and imidazotriazinones as ubiquitin-specific protease 7 inhibitors

Valo Health
9
BENZYLAMINE OR BENZYL ALCOHOL DERIVATIVE AND USES THEREOF

Chengdu Hyperway Pharmaceuticals
29
TRIAZINE COMPOUND AND COMPOSITION AND USE THEREOF

Beijing Findcure Biosciences
32
3-arylindazoles as selective MEK4 inhibitors

Northwestern University
86
(4-hydroxypyrrolidin-2-yl)-heterocyclic compounds and methods of use thereof

Genentech
6
Inhibiting the transient receptor potential al ion channel

Eli Lilly
13
Pyrimidine compounds and pyrimido indole compounds and methods of use

Duquesne University of The Holy Spirit
57
Heteroaromatic compounds as Vanin inhibitors

Boehringer Ingelheim International
13
Beta-lactamase inhibitors, formulations, and uses thereof

University of South Florida
32
Six-membered ring benzo derivatives as DPP-4 inhibitor and use thereof

East China University of Science and Technology
815
Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors

Array Biopharma
59
Permeable glycosidase inhibitors and uses thereof

Alectos Therapeutics
116
P2X7 modulators

Janssen Pharmaceutica
390
Therapeutically active compounds and their methods of use

Agios Pharmaceuticals
114
Heterocyclic derivates

Kalvista Pharmaceuticals
46
8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and thier use as pharmaceutical compositions

Boehringer Ingelheim International
58
Pyrrolidino heterocycles

Hoffmann-La Roche
247
Pyrrolone or pyrrolidinone melanin concentrating hormone receptor-1 antagonists

Bristol Myers Squibb
1
Structural basis for the recognition of mycolic acid precursors by KasA, a condensing enzyme and drug target from Mycobacterium tuberculosis.

University of Wuerzburg
9
Discovery of novel purine-based heterocyclic P2X7 receptor antagonists.

Gwangju Institute of Science and Technology
12
Spirocyclic morphinans and their use

Purdue Pharma
10
Benzodioxole or benzodioxepine heterocyclic compounds as phosphodiesterase inhibitors

Leo Pharma
27
Soft protease inhibitors and pro-soft forms thereof

Tufts College
37
Pyrazolo pyrimidine derivatives

Novartis
95
Small molecule inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase

Genzyme
5
Piperidinyl derivative as a modulator of chemokine receptor activity

Bristol Myers Squibb
3
Fused pyrrolidino-cyclopropane derivatives as selective 11-beta-hydroxysteroid dehydrogenase type 1 inhibitors

Merck Patent
1
Affinity and selectivity of PD156707, a novel nonpeptide endothelin antagonist, for human ET(A) and ET(B) receptors.

University of Cambridge
3
Conformation-assisted inhibition of protein-tyrosine phosphatase-1B elicits inhibitor selectivity over T-cell protein-tyrosine phosphatase.

Merck Frosst Center For Therapeutic Research
34
Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents.

Hoffmann-La Roche
30
Structure-activity relationships of a new family of steroidal aromatase inhibitors. 1. Synthesis and evaluation of a series of analogs related to 19-[(methylthio)methyl]androstenedione (RU54115).

Centre De Recherche De Roussel Uclaf
2
Development of a technique to determine bicyclomycin-rho binding and stoichiometry by isothermal titration calorimetry and mass spectrometry.

University of North Carolina
1
Recognition of a cognate RNA aptamer by neomycin B: quantitative evaluation of hydrogen bonding and electrostatic interactions.

The Ohio State University