PMID
Cmpds
Data
Article Title
Organization
6
Design, synthesis and activity of novel sorafenib analogues bearing chalcone unit.

Jiangxi Science & Technology Normal University
36
A Novel Parkinson's Disease Drug Candidate with Potent Anti-neuroinflammatory Effects through the Src Signaling Pathway.

Peking Union Medical College
5
Synthesis and anticancer activity of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives bearing chromone moiety.

Jiangxi Science & Technology Normal University
34
The discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors.

Merck Research Laboratories
6
Design, synthesis, biological evaluation and docking studies of novel 2-substituted-4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as dual PI3Ka/mTOR inhibitors.

Jiangxi Science & Technology Normal University
5
Synthesis, and docking studies of phenylpyrimidine-carboxamide derivatives bearing 1H-pyrrolo[2,3-b]pyridine moiety as c-Met inhibitors.

Jiangxi Science & Technology Normal University
4
Design, synthesis, and docking studies of afatinib analogs bearing cinnamamide moiety as potent EGFR inhibitors.

Jiangxi Science & Technology Normal University
5
Discovery of novel hybrids of diaryl-1,2,4-triazoles and caffeic acid as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase for cancer therapy.

China Pharmaceutical University
11
Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin.

Merck Research Laboratories
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
2
1-Benzyl-4-phenyl-1H-1,2,3-triazoles improve the transcriptional functions of estrogen-related receptor and promote the browning of white adipose.

Guangzhou Institutes of Biomedicine and Health
27
Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.

Bristol Myers Squibb
8
Design, synthesis and docking studies of novel thienopyrimidine derivatives bearing chromone moiety as mTOR/PI3Ka inhibitors.

Jiangxi Science & Technology Normal University
7
Design, synthesis, anticancer activity and docking studies of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as mTOR inhibitors.

TBA
22
Discovery and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors.

Merck Research Laboratories
30
1-Phenyl-4-benzoyl-1H-1,2,3-triazoles as orally bioavailable transcriptional function suppressors of estrogen-related receptora.

Chinese Academy of Sciences
1
Synthesis, biological evaluation, and molecular modeling of glycyrrhizin derivatives as potent high-mobility group box-1 inhibitors with anti-heart-failure activity in vivo.

Peking Union Medical College
23
Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein.

University of Southern California
27
Discovery of highly potent and selective pan-Aurora kinase inhibitors with enhanced in vivo antitumor therapeutic index.

Ambit Biosciences
13
Substrate-Selective Inhibition of Cyclooxygenase-2: Development and Evaluation of Achiral Profen Probes.

TBA
23
A new class of prolylcarboxypeptidase inhibitors, part 2: the aminocyclopentanes.

Merck Research Laboratories
25
Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine7¿°¿ methionine7¿° mutant.

Chinese Academy of Sciences
37
A new class of prolylcarboxypeptidase inhibitors, part 1: discovery and evaluation.

Merck Research Laboratories
26
Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagement.

Merck Research Laboratories
20
Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors.

Merck
83
Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles.

Amgen
38
Discovery of aminoheterocycles as potent and brain penetrant prolylcarboxypeptidase inhibitors.

Merck Research Laboratories
24
Discovery of benzodihydroisofurans as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase inhibitors.

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

Merck Research Laboratories
46
The discovery of non-benzimidazole and brain-penetrant prolylcarboxypeptidase inhibitors.

Merck Research Laboratories
27
Discovery of N-aryl-2-acylindole human glucagon receptor antagonists.

Merck Research Laboratories
33
Discovery of cyclic guanidines as potent, orally active, human glucagon receptor antagonists.

Merck Research Laboratories
33
Discovery of benzimidazole pyrrolidinyl amides as prolylcarboxypeptidase inhibitors.

Merck Research Laboratories
17
Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.

Amgen
36
Discovery of 3,3-disubstituted piperidine-derived trisubstituted ureas as highly potent soluble epoxide hydrolase inhibitors.

Merck Research Laboratories
46
A strategy of employing aminoheterocycles as amide mimics to identify novel, potent and bioavailable soluble epoxide hydrolase inhibitors.

Merck Research Laboratories
28
Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.

Amgen
27
Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors.

Merck
20
Discovery of spirocyclic secondary amine-derived tertiary ureas as highly potent, selective and bioavailable soluble epoxide hydrolase inhibitors.

Merck Research Laboratories
11
Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold.

Amgen
17
3-amino-7-phthalazinylbenzoisoxazoles as a novel class of potent, selective, and orally available inhibitors of p38alpha mitogen-activated protein kinase.

Amgen
2
Bioactive compounds from Peperomia pellucida.

Chinese Academy of Sciences
40
Design, synthesis and biological evaluation of novel 1H-indole-3-carbonitrile derivatives as potent TRK Inhibitors.

Shenyang Pharmaceutical University
2
Discovery of a first-in-class PROTAC degrader of histone lysine demethylase KDM4.

Shanghai Institute of Materia Medica
22
Discovery of β-amino acid substituted naphthalene sulfonamide derivatives as potent Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2 (Keap1-Nrf2) protein-protein interaction inhibitors for ulcerative colitis management.

China Pharmaceutical University
2
Opto-Epigenetic Regulation of Histone Arginine Asymmetric Dimethylation via Type I Protein Arginine Methyltransferase Inhibition.

The University of Hong Kong
24
Design, Synthesis, and biological evaluation of 7H-Pyrrolo[2,3-d]pyrimidines as potent HPK1 kinase inhibitors.

University of Chinese Academy of Sciences
2
Discovery of Selenium-Containing Derivatives as Potent and Orally Bioavailable GLP-1R Agonists.

China Pharmaceutical University
22
Targeting QPCTL: An Emerging Therapeutic Opportunity.

Tongji University Cancer Center
3
Discovery of an Efficacious RET PROTAC Degrader with Enhanced Antiproliferative Activity against Resistant Cancer Cells Harboring RET Solvent-Front Mutations.

Nanjing University of Chinese Medicine
24
A Collection of Novel Antitumor Agents That Regulate Lipid Metabolism in the Tumor Microenvironment.

Shenyang Pharmaceutical University
49
Discovery of Novel 4,5,6,7-Tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one Derivatives as Orally Efficacious ATX Allosteric Inhibitors for the Treatment of Pulmonary Fibrosis.

Shenyang Pharmaceutical University
6
"Pseudosubstrate Envelope"/Free Energy Perturbation-Guided Design and Mechanistic Investigations of Benzothiazole HIV Capsid Modulators with High Ligand Efficiency.

Shandong University
12
Advances in SHP2 tunnel allosteric inhibitors and bifunctional molecules.

China Pharmaceutical University
19
Prioritization of Eleven-Nineteen-Leukemia Inhibitors as Orally Available Drug Candidates for Acute Myeloid Leukemia.

Texas A&M University
43
Discovery and Synthesis of Heterobifunctional Degraders of Rearranged during Transfection (RET) Kinase.

Bristol Myers Squibb
3
Synthesis and bioevaluation of novel stilbene-based derivatives as tubulin/HDAC dual-target inhibitors with potent antitumor activities in vitro and in vivo.

China Pharmaceutical University
2
Design, synthesis and biological evaluation of 4-(4-aminophenoxy)picolinamide derivatives as potential antitumor agents.

The First Affiliated Hospital of Wenzhou Medical University
2
Discovery of novel 2-substituted 2, 3-dihydroquinazolin-4(1H)-one derivatives as tubulin polymerization inhibitors for anticancer therapy: The in vitro and in vivo biological evaluation.

Renmin Hospital of Wuhan University
1
Discovery of MT-1207: A Novel, Potent Multitarget Inhibitor as a Promising Clinical Candidate for the Treatment of Hypertension.

China Pharmaceutical University
73
Discovery of Orally Active Phenylquinoline-Based Soluble Epoxide Hydrolase Inhibitors with Anti-Inflammatory and Analgesic Activity.

Beijing Institute of Technology
35
Discovery of Novel 2-Aminopyridine-Based and 2-Aminopyrimidine-Based Derivatives as Potent CDK/HDAC Dual Inhibitors for the Treatment of Refractory Solid Tumors and Hematological Malignancies.

University of Chinese Academy of Sciences
4
Discovery of a Potent Dual Son of Sevenless 1 (SOS1) and Epidermal Growth Factor Receptor (EGFR) Inhibitor for the Treatment of Prostate Cancer.

China Pharmaceutical University
10
Discovery of First-in-Class PROTAC Degraders of SARS-CoV-2 Main Protease.

Texas A&M University
50
Design, synthesis, and biological evaluation of 4-(2-fluorophenoxy)-7-methoxyquinazoline derivatives as dual EGFR/c-Met inhibitors for the treatment of NSCLC.

Jiangxi Science & Technology Normal University
14
SARS-CoV-2 Main Protease Inhibitors That Leverage Unique Interactions with the Solvent Exposed S3 Site of the Enzyme.

Texas A&M University
37
Discovery of 2-Ethoxy-5-isobutyramido-N-1-substituted Benzamide Derivatives as Selective Kv2.1 Inhibitors with In Vivo Neuroprotective Effects.

Chinese Academy of Medical Sciences and Peking Union Medical College
9
Discovery of a Novel Thienopyrimidine Compound as a Urate Transporter 1 and Glucose Transporter 9 Dual Inhibitor with Improved Efficacy and Favorable Druggability.

Shandong University
1
Design, Synthesis, and Biological Evaluation for First GPX4 and CDK Dual Inhibitors.

China Pharmaceutical University
20
Design and synthesis of dual BRD4/Src inhibitors for treatment of triple-negative breast cancer.

Shenzhen University
36
Pyrrole-containing hybrids as potential anticancer agents: An insight into current developments and structure-activity relationships.

Jiangxi Science & Technology Normal University
29
Discovery of Pyrido[2,3-d]pyrimidin-7-one Derivatives as Highly Potent and Efficacious Ectonucleotide Pyrophosphatase/Phosphodiesterase 1 (ENPP1) Inhibitors for Cancer Treatment.

Shanghai Institute of Materia Medica
33
Hit-to-Lead Optimization of the Natural Product Oridonin as Novel NLRP3 Inflammasome Inhibitors with Potent Anti-Inflammation Activity.

China Pharmaceutical University
6
Discovery of a Dual Tubulin and Neuropilin-1 (NRP1) Inhibitor with Potent In Vivo Anti-Tumor Activity via Pharmacophore-based Docking Screening, Structure Optimization, and Biological Evaluation.

China Pharmaceutical University
34
Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors.

Merck Research Laboratories
48
Design and Synthesis of Novel Cereblon Binders for Use in Targeted Protein Degradation.

Bristol Myers Squibb
21
Discovery and Structural Optimization of Covalent ZAP-70 Kinase Inhibitors against Psoriasis.

Shanghai Institute of Materia Medica
33
A Systematic Survey of Reversibly Covalent Dipeptidyl Inhibitors of the SARS-CoV-2 Main Protease.

Texas A&M University
1
Advances of bioorthogonal coupling reactions in drug development.

China Pharmaceutical University
4
Discovery, Crystallographic Studies, and Mechanistic Investigations of Novel Phenylalanine Derivatives Bearing a Quinazolin-4-one Scaffold as Potent HIV Capsid Modulators.

Shandong University
40
Discovery of 2-(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase-3 (GSK-3) Inhibitors.

Biocon-Bristol Myers Squibb Research and Development Center
1
Discovery of a potent and selective proteolysis targeting chimera (PROTAC) degrader of NSD3 histone methyltransferase.

Shanghai Institute of Materia Medica
34
Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists.

Merck Research Laboratories
3
Design, synthesis, and mechanistic study of 2-piperazineone-bearing peptidomimetics as novel HIV capsid modulators.

Shandong University
2
Small-Molecule Hydrophobic Tagging: A Promising Strategy of Druglike Technology for Targeted Protein Degradation.

China Pharmaceutical University
1
Research progress of STAT3-based dual inhibitors for cancer therapy.

Xinxiang University
44
Discovery of 7H-Pyrrolo[2,3-d]pyrimidine Derivatives as potent hematopoietic progenitor kinase 1 (HPK1) inhibitors.

Shanghai Institute of Materia Medica
3
Discovery of Aminoratjadone Derivatives as Potent Noncovalent CRM1 Inhibitors.

Sichuan University
10
Design, synthesis and antitumor activity of novel thiophene- triazine derivatives bearing arylurea unit as potent PI3K/mTOR inhibitorss.

Shenyang Pharmaceutical University
5
Identification of a Novel Potent CYP4Z1 Inhibitor Attenuating the Stemness of Breast Cancer Cells through Lead Optimization.

China Pharmaceutical University
11
Design and synthesis of boron-containing ALK inhibitor with favorable in vivo efficacy.

Nanjing University
54
Discovery of Ethyl Ketone-Based Highly Selective HDACs 1, 2, 3 Inhibitors for HIV Latency Reactivation with Minimum Cellular Potency Serum Shift and Reduced hERG Activity.

Merck
24
The new opportunities in medicinal chemistry of fourth-generation EGFR inhibitors to overcome C797S mutation.

Jiangxi Science & Technology Normal University
27
Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease.

China Pharmaceutical University
4
Indolylarylsulfones bearing phenylboronic acid and phenylboronate ester functionalities as potent HIV‑1 non-nucleoside reverse transcriptase inhibitors.

Shandong University
1
Design, synthesis and biological evaluation of nitrofuran-1,3,4-oxadiazole hybrids as new antitubercular agents.

Peking Union Medical College
6
Design, synthesis, and mechanism study of dimerized phenylalanine derivatives as novel HIV-1 capsid inhibitors.

Shandong University
4
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.

China Pharmaceutical University
1
Evolutionary and Structural Insights about Potential SARS-CoV-2 Evasion of Nirmatrelvir.

Texas A&M University
5
Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.

Shandong University
3
Design, synthesis, and mechanistic investigations of phenylalanine derivatives containing a benzothiazole moiety as HIV-1 capsid inhibitors with improved metabolic stability.

Shandong University
32
Design and synthesis of alpha-aryloxyphenylacetic acid derivatives: a novel class of PPARalpha/gamma dual agonists with potent antihyperglycemic and lipid modulating activity.

Merck Research Laboratories
39
Structure-Based Discovery of a Series of NSD2-PWWP1 Inhibitors.

Chinese Academy of Sciences
8
Rational design, synthesis and biological evaluation of dual PARP-1/2 and TNKS1/2 inhibitors for cancer therapy.

Nanjing University
21
A systematic exploration of boceprevir-based main protease inhibitors as SARS-CoV-2 antivirals.

Texas A&M University
22
Design, synthesis, and biological evaluation of novel double-winged galloyl derivatives as HIV-1 RNase H inhibitors.

Shandong University
25
A multi-pronged evaluation of aldehyde-based tripeptidyl main protease inhibitors as SARS-CoV-2 antivirals.

Texas A&M University
15
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides.

Amgen
17
Discovery and Crystallographic Studies of Trisubstituted Piperazine Derivatives as Non-Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity and Low Toxicity.

Shandong University
15
Synthesis and activity evaluation of selenazole-coupled CPI-1 irreversible bifunctional inhibitors for botulinum toxin A light chain.

Guizhou Medical University
5
Development of Alectinib-Based PROTACs as Novel Potent Degraders of Anaplastic Lymphoma Kinase (ALK).

China Pharmaceutical University
4
Recent advances of quinones as a privileged structure in drug discovery.

Jinan Second People'S Hospital
1
An insight on medicinal aspects of novel HIV-1 capsid protein inhibitors.

Shandong University
39
Design and synthesis of Grp94 selective inhibitors based on Phe199 induced fit mechanism and their anti-inflammatory effects.

China Pharmaceutical University
13
Identification of (6S)-cyclopropyl-6,7-dihydropyrazolo[1,5-a]pyrazine-5(4H)-carboxamines as new HBV capsid assembly modulators.

Cams Key Laboratory of Antiviral Drug Research
20
Discovery of M-1121 as an Orally Active Covalent Inhibitor of Menin-MLL Interaction Capable of Achieving Complete and Long-Lasting Tumor Regression.

University of Michigan
52
Discovery of Novel Tacrine-Pyrimidone Hybrids as Potent Dual AChE/GSK-3 Inhibitors for the Treatment of Alzheimer's Disease.

China Pharmaceutical University
17
N-Aryl-gamma-lactams as integrin alphavbeta3 antagonists.

Amgen
3
BMS-813160: A Potent CCR2 and CCR5 Dual Antagonist Selected as a Clinical Candidate.

Bristol Myers Squibb
18
Discovery of novel N-1 substituted pyrazolopyrimidinones as potent, selective PDE2 inhibitors.

Merck
19
Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core.

Amgen
2
Discovery of a potent, selective, and covalent ZAP-70 kinase inhibitor.

University of Chinese Academy of Science
40
Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate.

Chinese Academy of Sciences
28
Discovery of Selective Small-Molecule Inhibitors for the ENL YEATS Domain.

Texas A&M University
6
Harmaline Analogs as Substrate-Selective Cyclooxygenase-2 Inhibitors.

Vanderbilt University School of Medicine
7
Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors.

Jiangxi Science & Technology Normal University
11
Discovery of BMS-753426: A Potent Orally Bioavailable Antagonist of CC Chemokine Receptor 2.

Bristol Myers Squibb
20
Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.

Shenyang Pharmaceutical University
6
Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors.

Shenyang Pharmaceutical University
5
Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations.

Jiangxi Science & Technology Normal University
4
Design, synthesis and biological evaluation of new Axl kinase inhibitors containing 1,3,4-oxadiazole acetamide moiety as novel linker.

Shenyang Pharmaceutical University
30
Identification of 5H-chromeno[3,4-c]pyridine and 6H-isochromeno[3,4-c]pyridine derivatives as potent and selective dual ROCK inhibitors.

Bristol Myers Squibb
26
Discovery of a phenylpyrazole amide ROCK inhibitor as a tool molecule for in vivo studies.

Bristol Myers Squibb
18
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(S)-methyl-4-[1(S)-[4-(trifluoromethyl)phenyl]ethyl]-1-piperazinyl]- piperidine N1-oxide (Sch-350634), an orally bioavailable, potent CCR5 antagonist.

Schering-Plough Research Institute
14
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-methyl piperazine as a key pharmacophore element.

Schering-Plough Research Institute
3
Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.

China Pharmaceutical University
31
Design, synthesis and biological evaluation of AZD9291 derivatives as selective and potent EGFR

Jiangxi Science & Technology Normal University
13
Discovery of a Novel cGAMP Competitive Ligand of the Inactive Form of STING.

Merck
8
Small molecules as inhibitors of PCSK9: Current status and future challenges.

China Pharmaceutical University
35
Synthesis and Biological Evaluation of B-Cell Lymphoma 6 Inhibitors of

East China Normal University and Shanghai Fengxian District Central Hospital Joint Center For Translational Medicine
43
Structure-Based Discovery of M-89 as a Highly Potent Inhibitor of the Menin-Mixed Lineage Leukemia (Menin-MLL) Protein-Protein Interaction.

TBA
3
Identification of benzothiazinones containing an oxime functional moiety as new anti-tuberculosis agents.

Peking Union Medical College
14
Multi-target design strategies for the improved treatment of Alzheimer's disease.

China Pharmaceutical University
15
Discovery of M-808 as a Highly Potent, Covalent, Small-Molecule Inhibitor of the Menin-MLL Interaction with Strong

TBA
8
Design, Synthesis, and Mechanism Study of Benzenesulfonamide-Containing Phenylalanine Derivatives as Novel HIV-1 Capsid Inhibitors with Improved Antiviral Activities.

Shandong University
8
Design, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors.

China Pharmaceutical University
7
Use of a Conformational-Switching Mechanism to Modulate Exposed Polarity: Discovery of CCR2 Antagonist BMS-741672.

Bristol Myers Squibb
2
Discovery of Novel Quinoline-Chalcone Derivatives as Potent Antitumor Agents with Microtubule Polymerization Inhibitory Activity.

China Pharmaceutical University
11
Design, synthesis and 3D-QSAR analysis of novel thiopyranopyrimidine derivatives as potential antitumor agents inhibiting A549 and Hela cancer cells.

Jiangxi Science & Technology Normal University
25
Design, synthesis, and docking studies of phenylpicolinamide derivatives bearing 1H-pyrrolo[2,3-b]pyridine moiety as c-Met inhibitors.

Jiangxi Science & Technology Normal University
1
Design, synthesis, and biological evaluation of 1,2,4-triazole bearing 5-substituted biphenyl-2-sulfonamide derivatives as potential antihypertensive candidates.

China Pharmaceutical University
22
Design, synthesis, and biological evaluation of 2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidinyl derivatives as new irreversible epidermal growth factor receptor inhibitors with improved pharmacokinetic properties.

Chinese Academy of Sciences
11
Exploring the molecular determinants of substrate-selective inhibition of cyclooxygenase-2 by lumiracoxib.

Vanderbilt University
20
Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties.

Chinese Academy of Sciences
3
Synthesis and bioevaluation and doking study of 1H-pyrrolo[2,3-b]pyridine derivatives bearing aromatic hydrazone moiety as c-Met inhibitors.

Jiangxi Science & Technology Normal University
17
Optimization of 5-arylidene barbiturates as potent, selective, reversible LSD1 inhibitors for the treatment of acute promyelocytic leukemia.

Fudan University
34
Conversion of carbazole carboxamide based reversible inhibitors of Bruton's tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series.

Bristol Myers Squibb
20
( R)- N-(1-Methyl-2-hydroxyethyl)-13-( S)-methyl-arachidonamide (AMG315): A Novel Chiral Potent Endocannabinoid Ligand with Stability to Metabolizing Enzymes.

Northeastern University
4
Synthesis and bioevaluation study of novel N-methylpicolinamide and thienopyrimidine derivatives as selectivity c-Met kinase inhibitors.

Jiangxi Science & Technology Normal University
6
Design, synthesis and antitumor activity of Novel Sorafenib derivatives bearing pyrazole scaffold.

Jiangxi Science & Technology Normal University
1
Discovery of MK-8722: A Systemic, Direct Pan-Activator of AMP-Activated Protein Kinase.

Merck Research Laboratories
5
Discovery of novel pyrrolo-pyridine/pyrimidine derivatives bearing pyridazinone moiety as c-Met kinase inhibitors.

Jiangxi Science & Technology Normal University
3
Design, synthesis, and docking studies of quinazoline analogues bearing aryl semicarbazone scaffolds as potent EGFR inhibitors.

Jiangxi Science & Technology Normal University
47
Improvement of hERG-ROMK index of spirocyclic ROMK inhibitors through scaffold optimization and incorporation of novel pharmacophores.

Merck
1
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.

The University of Arizona
21
Hit-to-Lead Optimization and Discovery of 5-((5-([1,1'-Biphenyl]-4-yl)-6-chloro-1H-benzo[d]imidazol-2-yl)oxy)-2-methylbenzoic Acid (MK-3903): A Novel Class of Benzimidazole-Based Activators of AMP-Activated Protein Kinase.

Metabasis Therapeutics
99
Substituted pyrrolidine amides III

GrÜNenthal
28
DITHIENYL DISULFIRAM DERIVATIVES AS SELECTIVE ALDH1A1 INHIBITORS

Batterjee Medical College
40
Aminonorbornane derivative and manufacture method therefor and use thereof

Transthera Sciences (Nanjing)
59
PYRROLIDINE DERIVATIVES AS DDRS INHIBITORS

Chiesi Farmaceutici
72
4H-PYRROLO[3,2-c]PYRIDIN-4-ONE COMPOUNDS

Bayer Aktiengesellschaft
16
Alkynyl (hetero) aromatic ring compounds used for inhibiting protein kinase activity

Shenzhen Targetrx
321
MTA-cooperative PRMT5 inhibitors

Mirati Therapeutics
32
Potent Inhibition of SARS-CoV-2 nsp14

University of Montpellier
18
Compounds, compositions and methods

Denali Therapeutics
11
TYK2 inhibitors, uses, and methods for production thereof

Nimbus Lakshmi
69
PDE9 inhibitor and use thereof

Nanjing Transthera Biosciences
85
Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors

Boehringer Ingelheim International
118
Treatment of relapsed and/or refractory solid tumors and non-hodgkin's lymphomas

Celgene Quanticel Research
341
TGFβ receptor antagonist

Bristol Myers Squibb
4
Purinone derivative

Ono Pharmaceutical
21
Azabenzimidazole derivatives

Boehringer Ingelheim International
15
Hydroxylated aminotriazole derivatives as ALX receptor agonists

Actelion Pharmaceuticals
7
Compositions and methods for treating neoplasia, inflammatory disease and other disorders

Dana-Farber Cancer Institute
99
Compounds and compositions as inhibitors of MEK

Novartis
16
Benzamide derivatives

Dong-A Pharm.
42
Pyrrolo[2,3-D]pyrimidine derivatives

Pfizer
24
Derivatives of [1,3]Oxazin-2-one useful for the treatment of metabolic diseases such as lipid disorders

Vitae Pharmaceuticals
141
Anellated pyridine compounds

Hoffmann-La Roche
8
The Substrate Capture Mechanism of Mycobacterium tuberculosis Anthranilate Phosphoribosyltransferase Provides a Mode for Inhibition.

University of Auckland
16
Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.

The R. W. Johnson Pharmaceutical Research Institute
17
Role of hydrophilic interaction in binding of hydroxylated 3-deoxy C(19) steroids to the active site of aromatase.

Tohoku Pharmaceutical University