PMID
Cmpds
Data
Article Title
Organization
39
Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy.

Novartis Institutes For Biomedical Research
38
Optimization of spirocyclic proline tryptophan hydroxylase-1 inhibitors.

Karos Pharmaceuticals
4
Rational Design of a Boron-Modified Triphenylethylene (GLL398) as an Oral Selective Estrogen Receptor Downregulator.

Xavier University of Louisiana
11
Design and synthesis of water solubleß-aminosulfone analogues of SCH 900229 as¿-secretase inhibitors.

Merck Research Laboratories
47
Design and Synthesis of 2-Alkylpyrimidine-4,6-diol and 6-Alkylpyridine-2,4-diol as Potent GPR84 Agonists.

East China Normal University
67
Discovery of acyl guanidine tryptophan hydroxylase-1 inhibitors.

Karos Pharmaceuticals
20
Structure-Based Design of an Iminoheterocyclicß-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aß in Nonhuman Primates.

Merck Research Laboratories
15
Approaching the active conformation of 1,3-diaminopyrimidine based covalent inhibitors of Bruton's tyrosine kinase for treatment of Rheumatoid arthritis.

Kbp Biosciences
38
Discovery of spirocyclic proline tryptophan hydroxylase-1 inhibitors.

Karos Pharmaceuticals
19
Identification of orally-bioavailable antagonists of the TRPV4 ion-channel.

Renovis
3
Synthesis and evaluation of benzimidazole carbamates bearing indole moieties for antiproliferative and antitubulin activities.

Shenyang Pharmaceutical University
19
Design, Synthesis, and Pharmacological Evaluation of Fusedß-Homophenylalanine Derivatives as Potent DPP-4 Inhibitors.

Chinese Academy of Sciences
5
Optimization of ADME Properties for Sulfonamides Leading to the Discovery of a T-Type Calcium Channel Blocker, ABT-639.

Abbvie
5
Synthesis and Structure-Activity Relationship Study of 5a-Carbasugar Analogues of SL0101.

Northeastern University
31
2-Aminopyrimidin-4(1H)-one as the novel bioisostere of urea: discovery of novel and potent CXCR2 antagonists.

Glaxosmithkline
31
Discovery of potent iminoheterocycle BACE1 inhibitors.

Merck Research Laboratories
42
Potent and selective inhibitors of human reticulocyte 12/15-lipoxygenase as anti-stroke therapies.

Harvard Medical School
24
Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib.

Chinese Academy of Sciences
38
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.

Intra-Cellular Therapies
1
Biologically active triterpenoid saponins from Acanthopanax senticosus.

Toho University
100
3D-QSAR comparative molecular field analysis on opioid receptor antagonists: pooling data from different studies.

University of Medicine & Dentistry of New Jersey-Robert Wood Johnson Medical School (Umdnj-Rwjms)
1
A perylene derivative regulates HIF-1a and Stat3 signaling pathways.

Baylor College of Medicine
34
Novel complex crystal structure of prolyl hydroxylase domain-containing protein 2 (PHD2): 2,8-Diazaspiro[4.5]decan-1-ones as potent, orally bioavailable PHD2 inhibitors.

Glaxosmithkline
8
Improving the affinity of SL0101 for RSK using structure-based design.

Vanderbilt University
51
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.

Abbott Laboratories
80
Exploration of cathepsin S inhibitors characterized by a triazole P1-P2 amide replacement.

Boehringer Ingelheim Pharmaceuticals
20
Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation.

Merck Research Laboratories
9
Discovery of SCH 900229, a Potent Presenilin 1 Selective ¿-Secretase Inhibitor for the Treatment of Alzheimer's Disease.

TBA
2
Novel enoyl-ACP reductase (FabI) potential inhibitors of Escherichia coli from Chinese medicine monomers.

Huazhong Agricultural University
35
Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor.

Schering-Plough Research Institute
1
Small-molecule synergist of the Wnt/beta-catenin signaling pathway.

The Scripps Research Institute
18
Discovery of novel triazole-based opioid receptor antagonists.

University of Medicine and Dentistry of New Jersey and Umdnj Informatics Institute
21
Fragment-based discovery of indole inhibitors of matrix metalloproteinase-13.

Boehringer Ingelheim Pharmaceuticals
1
Discovery and optimization of pyrazoline compounds as B-Raf inhibitors.

Millennium Pharmaceuticals
19
Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.

Millennium Pharmaceuticals
28
Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.

Abbott Laboratories
1
Effects of 7-O substitutions on estrogenic and anti-estrogenic activities of daidzein analogues in MCF-7 breast cancer cells.

Xavier University of Louisiana
3
Discovery of novel alpha7 nicotinic receptor antagonists.

Intra-Cellular Therapies
42
Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization.

Merck Research Laboratories
24
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.

Abbott Laboratories
13
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.

University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School and The Informatics Institute of Umdnj
32
Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors.

Schering-Plough Research Institute
1
Schiff base transition metal complexes as novel inhibitors of xanthine oxidase.

Nanjing University
1
Reversine increases the plasticity of lineage-committed mammalian cells.

The Scripps Research Institute
3
Design, synthesis and biological evaluation of 3-amino-6-(2-hydroxyphenyl)pyridazin-4-aryl derivatives as SMARCA2/4 degraders.

Sichuan University
25
Discovery and Optimization of Potent PROTAC Degraders of Phosphoinositide 3-Kinase with Significant in Vivo Anticancer Efficacy.

Chinese Academy of Medical Sciences and Peking Union Medical College
3
Discovery and Characterization of RP03707: A Highly Potent and Selective KRASG12D PROTAC.

Risen (Shanghai) Pharma Tech Co., Ltd.
1
PCSK9 Targeted Autophagosome-Tethering Compounds: Design, Synthesis, and Antiatherosclerosis Evaluation.

Fudan University
5
Discovery of Oral Degraders of the ROS1 Fusion Protein with Potent Activity against Secondary Resistance Mutations.

Xavier University of Louisiana
24
Progress in the study of anti-Alzheimer's disease activity of pyrimidine-containing bioactive molecules.

Zhengzhou University
2
Cernuosides A and B, two sucrase inhibitors from Pulsatilla cernua.

China Pharmaceutical University
11
Fatty acid conjugated BimBH3 analogues with d‑amino acid substitution as PTPN1 inhibitors with enhanced activity, biostability and orally available potency for the treatment of diabetes.

Qingdao University of Science and Technology
1
AI-Driven Discovery of Highly Specific and Efficacious hCES2A Inhibitors for Ameliorating Irinotecan-Triggered Gut Toxicity.

Hainan University
21
Discovery of Novel Pyrrolo[2,3-b]pyridine-Based CSF-1R Inhibitors with Demonstrated Efficacy against Patient-Derived Colorectal Cancer Organoids.

Nanjing University of Chinese Medicine
35
Design, Synthesis, and Biological Evaluation of Novel Fms-Like Tyrosine Kinase 3/VEGFR2/Histone Deacetylase Inhibitors for the Treatment of Acute Myeloid Leukemia.

Chinese Academy of Medical Sciences and Peking Union Medical College
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
The Discovery and Preclinical Profile of ALG-000184, a Prodrug of the Potent Hepatitis B Virus Capsid Assembly Modulator ALG-001075.

Aligos Belgium BV
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
17
Discovery of peptidomimetic spiropyrrolidine derivatives as novel 3CLpro inhibitors against SARS-CoV -2.

Shanghai Institute of Materia Medica
37
Integrating amino acids into Bcr-Abl inhibitors: design, synthesis, biological evaluation, and in silico studies.

Xi'an Jiaotong University
3
Discovery of 1,2,4-Triazole-3-thione Derivatives as Potent and Selective DCN1 Inhibitors for Pathological Cardiac Fibrosis and Remodeling.

Henan University of Chinese Medicine
10
Recent contributions of pyridazine as a privileged scaffold of anticancer agents in medicinal chemistry: An updated review.

Zhengzhou University
10
F-CPI: A Multimodal Deep Learning Approach for Predicting Compound Bioactivity Changes Induced by Fluorine Substitution.

East China Normal University
4
Modulating Phosphorylation by Proximity-Inducing Modalities for Cancer Therapy.

China Pharmaceutical University
2
Covalent inhibitors meet epigenetics: New opportunities.

Chengdu Normal University
8
Discovery of potent LRRK2 inhibitors by ensemble virtual screening strategy and bioactivity evaluation.

Macao Polytechnic University
1
Discovery of novel G9a/GLP covalent inhibitors for the treatment of triple-negative breast cancer.

Sichuan University
7
Synthesis and mechanism of action of new purine derivatives against triple negative breast cancer.

Tianjin University of Science and Technology
32
Design, synthesis and biological evaluation of indazole derivatives as selective covalent inhibitors of FGFR4 in wild-type and gatekeeper mutants.

Sichuan University
9
Perspectives and new aspects of histone deacetylase inhibitors in the therapy of CNS diseases.

Shanghai Institute of Pharmaceutical Industry Co., Ltd.
11
Design, synthesis and biological evaluation of peptidomimetic benzothiazolyl ketones as 3CLpro inhibitors against SARS-CoV-2.

Zhengzhou University
7
Design, synthesis, and biological evaluation of novel 1-amido-2-one-4-thio-deoxypyranose as potential antitumor agents for multiple myeloma.

Chinese Academy of Sciences
14
Advances in dual-targeting inhibitors of HDAC6 for cancer treatment.

Guizhou Medical University
5
Targeting kelch-like (KLHL) proteins: achievements, challenges and perspectives.

China Pharmaceutical University
27
Amide bioisosteric replacement in the design and synthesis of quorum sensing modulators.

Hubei University of Education
12
Design, synthesis, and biological evaluation of aralkyl piperazine and piperidine derivatives targeting SSRI/5-HT1A/5-HT7.

Shanghai Institute of Pharmaceutical Industry Co., Ltd.
3
Allosteric Activation of Protein Phosphatase 5 with Small Molecules.

China Pharmaceutical University
7
Design, synthesis and antitumor activity of a novel FGFR2-selective degrader to overcome resistance of the FGFR2V564F gatekeeper mutation based on a pan-FGFR inhibitor.

Sichuan University
10
Identification of 3-(9H-carbazol-9-yl)-2-(1,3-dioxoisoindolin-2-yl)propanoic acids as promising DNMT1 inhibitors.

Fudan University
41
Discovery of Novel 5,6-Dihydro-4H-pyrido[2,3,4-de]quinazoline Irreversible Inhibitors Targeting Both Wild-Type and A775_G776insYVMA Mutated HER2 Kinases.

Beijing University of Technology
19
Discovery of ITI-333, a Novel Orally Bioavailable Molecule Targeting Multiple Receptors for the Treatment of Pain and Other Disorders.

Intra-Cellular Therapies, Inc.
35
Small conformationally restricted piperidine N-arylsulfonamides as orally active gamma-secretase inhibitors.

Schering-Plough Research Institute
3
Discovery of GPR84 Fluorogenic Probes Based on a Novel Antagonist for GPR84 Bioimaging.

Chinese Academy of Sciences
31
Pyrazolo[3,4-d]pyrimidines as potent inhibitors of the insulin-like growth factor receptor (IGF-IR).

Abbott Laboratories
4
Discovery of a Hidden Pocket beneath the NES Groove by Novel Noncovalent CRM1 Inhibitors.

Sichuan University
3
Design, synthesis and biological evaluation of nitric oxide-releasing 5-cyano-6-phenyl-2, 4-disubstituted pyrimidine derivatives.

Zhengzhou University
27
Identification and Optimization of Small Molecule Pyrazolopyrimidine TLR7 Agonists for Applications in Immuno-oncology.

Bristol Myers Squibb
33
Discovery of Novel TLR7 Agonists as Systemic Agent for Combination With aPD1 for Use in Immuno-oncology.

Bristol Myers Squibb
18
Design, synthesis, and biological evaluation of novel 8-substituted quercetin derivatives targeting the β‑catenin/B-cell lymphoma 9 interaction.

Tongji University
23
Discovery of novel benzbromarone analogs with improved pharmacokinetics and benign toxicity profiles as antihyperuricemic agents.

Southern Medical University
70
Development of Biaryl-Containing Aldo-Keto Reductase 1C3 (AKR1C3) Inhibitors for Reversing AKR1C3-Mediated Drug Resistance in Cancer Treatment.

China Pharmaceutical University
2
Annual review of KRAS inhibitors in 2022.

Zhengzhou University
19
Design, synthesis and biological evaluation of quercetin derivatives as novel β-catenin/B-cell lymphoma 9 protein-protein interaction inhibitors.

Fudan University
5
Discovery of Dual Lysine Methyltransferase G9a and EZH2 Inhibitors with In Vivo Efficacy against Malignant Rhabdoid Tumor.

Shenyang Pharmaceutical University
36
Design, synthesis and evaluation of antitumor activity of selective PRMT6 inhibitors.

Sichuan University
34
A decade of approved first-in-class small molecule orphan drugs: Achievements, challenges and perspectives.

China Pharmaceutical University
28
Discovery of a novel GPR35 agonist with high and equipotent species potency for oral treatment of IBD.

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

Nankai University
11
Dual function of protein phosphatase 5 (PPP5C): An emerging therapeutic target for drug discovery.

China Pharmaceutical University
4
DNA-Encoded Macrocyclic Peptide Libraries Enable the Discovery of a Neutral MDM2-p53 Inhibitor.

Unnatural Products
9
Discovery of a Novel Covalent EZH2 Inhibitor Based on Tazemetostat Scaffold for the Treatment of Ovarian Cancer.

Sichuan University
46
Discovery of Novel 3-Phenylpiperidine Derivatives Targeting the β-Catenin/B-Cell Lymphoma 9 Interaction as a Single Agent and in Combination with the Anti-PD-1 Antibody for the Treatment of Colorectal Cancer.

Fudan University
6
Design, synthesis and biological evaluation of covalent peptidomimetic 3CL protease inhibitors containing nitrile moiety.

An Hui University of Traditional Chinese Medicine
2
Salutaxel, a Conjugate of Docetaxel and a Muramyl Dipeptide (MDP) Analogue, Acts as Multifunctional Prodrug That Inhibits Tumor Growth and Metastasis.

Shenzhen Salubris Pharmaceuticals Co.
22
Discovery of PF-06873600, a CDK2/4/6 Inhibitor for the Treatment of Cancer.

Pfizer
11
Strategies for Targeting Serine/Threonine Protein Phosphatases with Small Molecules in Cancer.

China Pharmaceutical University
43
Scaffold Hopping Strategy to Identify Prostanoid EP4 Receptor Antagonists for Cancer Immunotherapy.

East China Normal University
11
Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies.

Novartis Institutes For Biomedical Research
14
Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma.

Wenzhou Medical University
46
Phosphodiesters as GPR84 Antagonists for the Treatment of Ulcerative Colitis.

Shanghai Institute of Materia Medica
37
Discovery of novel verinurad analogs as dual inhibitors of URAT1 and GLUT9 with improved Druggability for the treatment of hyperuricemia.

Southern Medical University
27
Design and Synthesis of Fibroblast Growth Factor Receptor (FGFR) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Cancer.

Sichuan University
28
Discovery of Novel Benzo[4,5]imidazo[1,2-

Sun Yat-Sen University
9
In silico, synthesis and anticancer evaluation of benzamide tryptamine derivatives as novel eEF2K inhibitors.

Ningbo University
7
Synthesis and biological evaluation of new series of quinazoline derivatives as EGFR/HER2 dual-target inhibitors.

Jiangnan University
9
Histone deacetylase 6 inhibitors with blood-brain barrier penetration as a potential strategy for CNS-Disorders therapy.

Shanghai Institute of Pharmaceutical Industry
9
Discovery of honokiol thioethers containing 1,3,4-oxadiazole moieties as potential α-glucosidase and SARS-CoV-2 entry inhibitors.

Zhengzhou University
1
General Pharmacological Activation Mechanism of K

East China Normal University
41
Design, synthesis, and biological evaluation of trizole-based heteroaromatic derivatives as Bcr-Abl kinase inhibitors.

Xi'An Jiaotong University
2
The overview of Mitogen-activated extracellular signal-regulated kinase (MEK)-based dual inhibitor in the treatment of cancers.

Zhengzhou University
29
Design, synthesis, and biological evaluation of novel Bcr-Abl

Xi'An Jiaotong University
7
Identification of novel influenza polymerase PB2 inhibitors using virtual screening approach and molecular dynamics simulation analysis of active compounds.

Beijing Institute of Pharmacology & Toxicology
4
Rational Design and Synthesis of Novel Dual PROTACs for Simultaneous Degradation of EGFR and PARP.

Huazhong University of Science and Technology
22
Design and Synthesis of EZH2-Based PROTACs to Degrade the PRC2 Complex for Targeting the Noncatalytic Activity of EZH2.

Sichuan University
12
Development of Multifunctional and Orally Active Cyclic Peptide Agonists of Opioid/Neuropeptide FF Receptors that Produce Potent, Long-Lasting, and Peripherally Restricted Antinociception with Diminished Side Effects.

Lanzhou University
27
Structure-guided design and development of novel N-phenylpyrimidin-2-amine derivatives as potential c-Met inhibitors.

Hebei University of Science and Technology
25
Synthesis and evaluation of FAK inhibitors with a 5-fluoro-7H-pyrrolo[2,3-d]pyrimidine scaffold as anti-hepatocellular carcinoma agents.

Fudan University
8
Design, synthesis, docking, molecular dynamics and bioevaluation studies on novel N-methylpicolinamide and thienopyrimidine derivatives with inhibiting NF-κB and TAK1 activities: Cheminformatics tools RDKit applied in drug design.

China Pharmaceutical University
16
An affinity prediction approach for the ligand of E3 ligase Cbl-b and an insight into substrate binding pattern.

China Pharmaceutical University
28
Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction.

Shanghai Institute of Pharmaceutical Industry
53
From a Designer Drug to the Discovery of Selective Cannabinoid Type 2 Receptor Agonists with Favorable Pharmacokinetic Profiles for the Treatment of Systemic Sclerosis.

East China Normal University
35
Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management.

The State University of New Jersey
8
Discovery of novel anti-angiogenesis agents. Part 11: Development of PROTACs based on active molecules with potency of promoting vascular normalization.

The First Affiliated Hospital of Xi'An Jiaotong University
9
Design, synthesis and bioevaluation of inhibitors targeting HSP90-CDC37 protein-protein interaction based on a hydrophobic core.

China Pharmaceutical University
7
Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors.

Jiangxi Science & Technology Normal University
13
Design, synthesis, and biological activity of 4-(imidazo[1,2-b]pyridazin-3-yl)-1H-pyrazol-1-yl-phenylbenzamide derivatives as BCR-ABL kinase inhibitors.

Beijing University of Technology
6
Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR

Sun Yat-Sen University
2
The discovery of novel small molecule allosteric activators of aldehyde dehydrogenase 2.

Second Military Medical University
20
Modulation of the G-Protein-Coupled Receptor 84 (GPR84) by Agonists and Antagonists.

Chinese Academy of Sciences
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
49
Novel Tetrahydropyrido[4,3-d]pyrimidines as Potent Inhibitors of Chaperone Heat Shock Protein 90.

China Pharmaceutical University
10
Synthesis and Biological Characterization of Cyclic Disulfide-Containing Peptide Analogs of the Multifunctional Opioid/Neuropeptide FF Receptor Agonists That Produce Long-Lasting and Nontolerant Antinociception.

Lanzhou University
7
Synthesis and biological evaluation of all possible inosine-mixed cyclic dinucleotides that activate different hSTING variants.

Nankai University
21
Pyrazolo[1,5-a]pyrimidine based Trk inhibitors: Design, synthesis, biological activity evaluation.

Jiangnan University
8
Synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors.

Jiangnan University
1
Discovery of an Inhibitor for the TREK-1 Channel Targeting an Intermediate Transition State of Channel Gating.

Shanghai Institute of Materia Medica
5
Design, synthesis and biological evaluation of 4-(pyridin-4-yloxy)benzamide derivatives bearing a 5-methylpyridazin-3(2H)-one fragment.

Jiangxi Science & Technology Normal University
28
Design and synthesis of (E)-1,2-diphenylethene-based EZH2 inhibitors.

Sichuan University and Collaborative Innovation Center
19
Discovery of 5-(pyridin-3-yl)-1H-indole-4,7-diones as indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors.

Fudan University
26
Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors.

Shandong University
24
Design, synthesis, and biological characterization of novel PEG-linked dimeric modulators for CXCR4.

Upstate Medical University
2
Fulvestrant-3 Boronic Acid (ZB716): An Orally Bioavailable Selective Estrogen Receptor Downregulator (SERD).

Xavier University of Louisiana
2
Structure-Based Discovery of a Subtype-Selective Inhibitor Targeting a Transient Receptor Potential Vanilloid Channel.

Chinese Academy of Sciences
21
Discovery of novel anti-angiogenesis agents. Part 9: Multiplex inhibitors suppressing compensatory activations of RTKs.

The First Affiliated Hospital of Xi'An Jiaotong University
25
Recent advances in the development of cyclin-dependent kinase 7 inhibitors.

Tianjin University of Science and Technology
7
Design, synthesis and activity of novel 2,6-disubstituted purine derivatives, potential small molecule inhibitors of signal transducer and activator of transcription 3.

Wenzhou Medical University
12
1-Phenyl-dihydrobenzoindazoles as novel colchicine site inhibitors: Structural basis and antitumor efficacy.

Second Military Medical University
13
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.

Janssen Biopharma
9
Discovery and Optimization of Small Molecules Targeting the Protein-Protein Interaction of Heat Shock Protein 90 (Hsp90) and Cell Division Cycle 37 as Orally Active Inhibitors for the Treatment of Colorectal Cancer.

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
52
Discovery and Characterization of 1

East China Normal University
21
Discovery of novel Bcr-Abl

Xi'An Jiaotong University
1
TREK Channel Family Activator with a Well-Defined Structure-Activation Relationship for Pain and Neurogenic Inflammation.

East China Normal University
7
Synthesis and biological evaluation of 7-methoxy-1-(3,4,5-trimethoxyphenyl)-4,5-dihydro-2H-benzo[e]indazoles as new colchicine site inhibitors.

Second Military Medical University
1
Glucoconjugated Monoterpene Indole Alkaloids from

Peking University Health Science Center
3
Monosaccharide Analogues of Anticancer Peptide R-Lycosin-I: Role of Monosaccharide Conjugation in Complexation and the Potential of Lung Cancer Targeting and Therapy.

TBA
5
Discovery of two novel branched peptidomimetics containing endomorphin-2 and RF9 pharmacophores: Synthesis and neuropharmacological evaluation.

Lanzhou University
23
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.

University of South China
50
Identification of novel azaindazole CCR1 antagonist clinical candidates.

Boehringer Ingelheim Pharmaceuticals
10
Design, synthesis, and bioactivity evaluation of novel Bcl-2/HDAC dual-target inhibitors for the treatment of multiple myeloma.

Wuhan Polytechnic University
19
Discovery of potent Pan-Raf inhibitors with increased solubility to overcome drug resistance.

China Pharmaceutical University
17
Discovery of novel anti-angiogenesis agents. Part 10: Multi-target inhibitors of VEGFR-2, Tie-2 and EphB4 incorporated with 1,2,3-triazol.

Xi'An Jiaotong University
18
Development of small molecule inhibitors targeting NLRP3 inflammasome pathway for inflammatory diseases.

Shandong University
24
Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease.

Chinese Academy of Sciences
2
Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.

Northwest University
21
Structure activity relationship studies of tricyclic bispyran sulfone γ-secretase inhibitors.

Merck Research Laboratories
33
Discovery of gamma-secretase inhibitors efficacious in a transgenic animal model of Alzheimer's disease.

Schering-Plough Research Institute
31
2,6-Disubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors.

Schering-Plough Research Institute
21
Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR.

East China Normal University
3
Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors.

Xavier University of Louisiana
16
A series of camptothecin prodrugs exhibit HDAC inhibition activity.

East China Normal University
22
Structure optimization and preliminary bioactivity evaluation of N-hydroxybenzamide-based HDAC inhibitors with Y-shaped cap.

Shandong University
17
BACE1 Inhibitory Meroterpenoids from Aspergillus terreus.

Huazhong University of Science and Technology
23
Synthesis and biological evaluation of novel 6,11-dihydro-5H-benzo[e]pyrimido- [5,4-b][1,4]diazepine derivatives as potential c-Met inhibitors.

Shanghai Institute of Pharmaceutical Industry
3
Natural Product Micheliolide (MCL) Irreversibly Activates Pyruvate Kinase M2 and Suppresses Leukemia.

Nankai University
1
Design and synthesis of novel dasatinib derivatives as inhibitors of leukemia stem cells.

Tianjin International Joint Academy of Biomedicine
8
Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.

Novartis Institutes For Biomedical Research
43
Rational Design and Structure Validation of a Novel Peptide Inhibitor of the Adenomatous-Polyposis-Coli (APC)-Rho-Guanine-Nucleotide-Exchange-Factor-4 (Asef) Interaction.

Jinan University
18
Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis.

Shenyang Pharmaceutical University
12
Design, synthesis and evaluation of derivatives based on pyrimidine scaffold as potent Pan-Raf inhibitors to overcome resistance.

China Pharmaceutical University
1
Fragment-Based Drug Discovery of Inhibitors of Phosphopantetheine Adenylyltransferase from Gram-Negative Bacteria.

Novartis Institutes For Biomedical Research
3
Design, synthesis and biological evaluation of novel histone deacetylase inhibitors incorporating 4-aminoquinazolinyl systems as capping groups.

Shanghai Institute of Pharmaceutical Industry
39
Structure-Based Design of 6-Chloro-4-aminoquinazoline-2-carboxamide Derivatives as Potent and Selective p21-Activated Kinase 4 (PAK4) Inhibitors.

Shenyang Pharmaceutical University
5
Design, synthesis and biological evaluation of 4-piperazinyl-containing Chidamide derivatives as HDACs inhibitors.

Shanghai Institute of Pharmaceutical Industry
238
BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS

Oncopia Therapeutics, Inc. D/B/A/ Sk Life Science Labs
328
Heteroaryl Compounds As HPK1 Inhibitors And Methods Of Using Same

Shenzhen Yuanli Shenwan Innovative Medicine
3
Organic compound

Intra-Cellular Therapies
6
RNA virus inhibitor compounds and uses thereof

University of Alberta
47
Psychedelics and the human receptorome.

University of Oklahoma
14
TREATMENT OF MYELOPROLIFERATIVE DISEASES AND DISORDERS WITH INHIBITORS OF BET FAMILY BDII BROMODOMAIN

Poseidon Innovation 1
48
Cathepsin L inhibitors

Biofront Therapeutics (Beijing) Co.
3
SALT OF DIHYDROPYRIDO[2,3-D]PYRIMIDINONE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF

Nanjing Chia Tai Tianqing Pharmaceutical
295
EIF4E inhibitors and uses thereof

Pic Therapeutics
96
Substituted imidazolidin-2-one derivatives as PRMT5 inhibitors

Aurigene Discovery Technologies
14
Cyclic dinucleotides as sting agonists

Janssen Biotech
20
Annulated glycosidase inhibitors

Asceneuron
62
Macrocyclic indole derivatives

The Broad Institute
33
Inhibitors of lysine gingipain

Cortexyme
14
Personal care compositions comprising fatty acid amide derivatives

Conopco
25
Fused ring derivative used as FGFR4 inhibitor

Jacobio Pharmaceuticals
45
Isoquinoline ether compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction

Vanderbilt University
337
Substituted purine derivative

Sumitomo Dainippon Pharma
296
Cycloalkyl nitrile pyrazolo pyridones as Janus kinase inhibitors

Merck Sharp & Dohme
42
4-ETHYNYLPYRIDINE DERIVATIVES USEFUL AS GCN2 INHIBITORS

IP2IPO Innovations
19
Substituted pyrrolidines as factor XIa inhibitors for the treatment thromboembolic diseases

Ono Pharmaceutical
22
HCV polymerase inhibitors

Medivir
36
Compounds and methods of use

Medivation Technologies
155
Piperazinyl and piperidinyl ureas as modulators of fatty acid amide hydrolase

Janssen Pharmaceutica
4
Saccharide conjugates

Curators of The University of Missouri
37
Indole or indazole derivative or salt thereof

Taiho Pharmaceutical
20
Substituted imidazolones, compositions containing such compounds and methods of use

Merck Sharp & Dohme
8
Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes

Merck Sharpe & Dohme
3
Characterization of the CHK1 allosteric inhibitor binding site.

Pfizer
4
Interactions of (+)- and (-)-8- and 7-hydroxy-2-(di-n-propylamino)tetralin at human (h)D3, hD2 and h serotonin1A receptors and their modulation of the activity of serotoninergic and dopaminergic neurones in rats.

Institut De Recherches Servier
3
A-85380 [3-(2(S)-azetidinylmethoxy) pyridine]: in vitro pharmacological properties of a novel, high affinity alpha 4 beta 2 nicotinic acetylcholine receptor ligand.

Abbott Laboratories
15
A novel approach for the development of selective Cdk4 inhibitors: library design based on locations of Cdk4 specific amino acid residues.

Banyu Tsukuba Research Institute