PMID
Data
Article Title
Organization
Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors.

Astrazeneca
Design, biological evaluation and 3D QSAR studies of novel dioxin-containing triaryl pyrazoline derivatives as potential B-Raf inhibitors.

Nanjing University
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.

Zhejiang University
Discovery of KDM5A inhibitors: Homology modeling, virtual screening and structure-activity relationship analysis.

Sichuan University
Identification and Optimization of Benzimidazole Sulfonamides as Orally Bioavailable Sphingosine 1-Phosphate Receptor 1 Antagonists with in Vivo Activity.

Astrazeneca
Synthesis and biological evaluation of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists.

China Pharmaceutical University
Discovery of potent KIFC1 inhibitors using a method of integrated high-throughput synthesis and screening.

Astrazeneca
Structure-based design and synthesis of tricyclic IAP (Inhibitors of Apoptosis Proteins) inhibitors.

Astrazeneca
Integrating docking scores, interaction profiles and molecular descriptors to improve the accuracy of molecular docking: toward the discovery of novel Akt1 inhibitors.

Zhejiang University
Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors.

Zhejiang University
The discovery and optimization of novel dual inhibitors of topoisomerase II and histone deacetylase.

East China Normal University
A Potent and Orally Efficacious, Hydroxyethylamine-Based Inhibitor of ß-Secretase.

TBA
Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO.

Astrazeneca
Discovery of novel 2-piperidinol-3-(arylsulfonyl)quinoxalines as phosphoinositide 3-kinasea (PI3Ka) inhibitors.

Zhejiang University
Pharmacophore identification, synthesis, and biological evaluation of carboxylated chalcone derivatives as CysLT1 antagonists.

Zhejiang University
(-)-3 beta-Substituted ecgonine methyl esters as inhibitors for cocaine binding and dopamine uptake.

University of Maryland
Pharmacophore identification, virtual screening and biological evaluation of prenylated flavonoids derivatives as PKB/Akt1 inhibitors.

Zhejiang University
Synthesis and biological evaluation of novel 2-arylamino-3-(arylsulfonyl)quinoxalines as PI3Ka inhibitors.

Zhejiang University
Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors.

Zhejiang University
Design, synthesis and biological evaluation of novel compounds with conjugated structure as anti-tumor agents.

China Pharmaceutical University
2-Phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors: a study on the importance of modifications at the side chain on the activity.

Zhejiang University
Design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors.

Zhejiang University
Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives.

Zhejiang University
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
Discovery of LHQ490 as a highly selective fibroblast growth factor receptor 2 (FGFR2) inhibitor.

East China Normal University
Discovery of Novel Oxazepine Derivatives as Akt/ROCK Inhibitors for Growth Arrest and Differentiation Induction in Neuroblastoma Treatment.

Zhejiang University
Discovery of thienopyridines as Src-family selective Lck inhibitors.

Abbott Bioresearch Center
Discovery of Novel

Shenyang Pharmaceutical University
Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma.

Zhejiang University
Design, synthesis, and biological evaluation of novel dual FFA1 and PPARδ agonists possessing phenoxyacetic acid scaffold.

Guangdong Pharmaceutical University
A chemical strategy to promote helical peptide-protein interactions involved in apoptosis.

University of Illinois At Urbana-Champaign
Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448).

The State University of New York
Discovery of a Series of 7-Azaindoles as Potent and Highly Selective CDK9 Inhibitors for Transient Target Engagement.

Astrazeneca
Noncovalent CDK12/13 dual inhibitors-based PROTACs degrade CDK12-Cyclin K complex and induce synthetic lethality with PARP inhibitor.

Zhejiang University
-Terphenyls as Anti-HSV-1/2 Agents from a Deep-Sea-Derived

Chinese Academy of Sciences
Discovery of a Candidate Containing an (

Peking Union Medical College
N-(4-acetamidophenyl)-5-acetylfuran-2-carboxamide as a novel orally available diuretic that targets urea transporters with improved PD and PK properties.

Peking University
Discovery of LYC-55716: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ) Agonist for Use in Treating Cancer.

Lycera
Identification of Novel Tricyclic Benzo[1,3]oxazinyloxazolidinones as Potent Antibacterial Agents with Excellent Pharmacokinetic Profiles against Drug-Resistant Pathogens.

Peking Union Medical College
Discovery of

Zhejiang University
Optimization of Truncated Glucagon Peptides to Achieve Selective, High Potency, Full Antagonists.

Indiana University
Design, synthesis, biological evaluation and molecular docking study of novel thieno[3,2-d]pyrimidine derivatives as potent FAK inhibitors.

Shenyang Pharmaceutical University
Addition of Fluorine and a Late-Stage Functionalization (LSF) of the Oral SERD AZD9833.

Astrazeneca
Discovery of Proteolysis-Targeting Chimera Molecules that Selectively Degrade the IRAK3 Pseudokinase.

Astrazeneca
Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors.

Shanghai Institute of Materia Medica
Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.

Astrazeneca
Discovery of AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist.

Astrazeneca
Ene-yne Hydroquinones from a Marine-derived Strain of the Fungus

Chinese Academy of Sciences
Heteroarylamide smoothened inhibitors: Discovery of N-[2,4-dimethyl-5-(1-methylimidazol-4-yl)phenyl]-4-(2-pyridylmethoxy)benzamide (AZD8542) and N-[5-(1H-imidazol-2-yl)-2,4-dimethyl-phenyl]-4-(2- pyridylmethoxy)benzamide (AZD7254).

Astrazeneca
Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design.

Chinese Academy of Sciences
Discovery and optimization of thienopyridine derivatives as novel urea transporter inhibitors.

Peking University
Design, synthesis and biological evaluation of novel 7H-pyrrolo[2,3-d]pyrimidine derivatives as potential FAK inhibitors and anticancer agents.

Shenyang Pharmaceutical University
Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry.

Astrazeneca
Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation.

Zhejiang University
Constrained bithiazoles: small molecule correctors of defective ΔF508-CFTR protein trafficking.

University of California
4'-Methyl-4,5'-bithiazole-based correctors of defective delta F508-CFTR cellular processing.

University of California
A novel glucagon-like peptide-1/glucagon receptor dual agonist exhibits weight-lowering and diabetes-protective effects.

China Pharmaceutical University
Adventures in Scaffold Morphing: Discovery of Fused Ring Heterocyclic Checkpoint Kinase 1 (CHK1) Inhibitors.

Astrazeneca
KAT6 Inhibitors

Beigene Switzerland
17-beta-hydroxysteroid dehydrogenase type 13 inhibitors and methods of use thereof

Enanta Pharmaceuticals
Pyrazolo[3,4-d]pyrrolo[1,2-b]pyridazinyl compounds useful as IRAK4 inhibitors

Bristol-Myers Squibb
QUINAZOLINONES, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, AND METHODS OF USING THE SAME

Repare Therapeutics
Cot modulators and methods of use thereof

Gilead Sciences
Pyrazole derivatives as MALT1 inhibitors

Janssen Pharmaceutica
Imidazooxazole derivative having antitumor effect, and pharmaceutical composition including same

Korea Institute of Science and Technology
Substituted pyrrolopyrimidine CDK inhibitor, pharmaceutical composition containing same and use thereof

Chia Tai Tianqing Pharmaceutical Group
Tetrahydroisoquinoline derivatives, pharmaceutical compositions and uses thereof

Boehringer Ingelheim International
Non-steroidal Anti-inflammatory Drugs Are Caspase Inhibitors.

University of Colorado
Substituted N-phenethyltriazoloneacetamides and use thereof

Bayer Intellectual Property
Reactivators of organophosphorous inhibited acetylcholinesterase

Southwest Research Institute
Heterocyclic compounds containing an indole core

Boehringer Ingelheim International
3-substituted-2-(arlyalkyl)-1-azabicycloalkanes and methods of use thereof

Targacept
Interactive binding between the substrate and allosteric sites of carbamoyl-phosphate synthetase.

Pennsylvania State University
DL-threo-beta-benzyloxyaspartate, a potent blocker of excitatory amino acid transporters.

Suntory Institute For Bioorganic Research
(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]-pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Merck Research Laboratories
Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.

Johnson & Johnson Pharmaceutical