PMID
Data
Article Title
Organization
Pterin-sulfa conjugates as dihydropteroate synthase inhibitors and antibacterial agents.

St. Jude Children'S Research Hospital
Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.

Ariad Pharmaceuticals
Novel Small Molecule Inhibitors of Choline Kinase Identified by Fragment-Based Drug Discovery.

Ariad Pharmaceuticals
Biased multicomponent reactions to develop novel bromodomain inhibitors.

Dana-Farber Institute
Design and synthesis of phenylisoxazole derivatives as novel human acrosin inhibitors.

Second Military Medical University
Synthesis and acrosin inhibitory activities of 5-phenyl-1H-pyrazole-3-carboxylic acid amide derivatives.

Second Military Medical University
Fragment growing and linking lead to novel nanomolar lactate dehydrogenase inhibitors.

Ariad Pharmaceuticals
Design and synthesis of novel benzoheterocyclic derivatives as human acrosin inhibitors by scaffold hopping.

Second Military Medical University
Discovery of small molecule inhibitors of integrin alphavbeta3 through structure-based virtual screening.

Peking Union Medical College
Synthesis and acrosin inhibitory activity of methyl 5-substituted-1H-benzo[d]imidazol-2-yl carbamate derivatives.

Second Military Medical University
Structural studies of pterin-based inhibitors of dihydropteroate synthase.

University of Tennessee Health Science Center
Synthesis and acrosin inhibitory activity of substituted 4-amino-N-(diaminomethylene) benzenesulfonamide derivatives.

Second Military Medical University
Synthesis and acrosin inhibitory activities of substituted ethyl 5-(4-aminophenyl)-1H-pyrazole-3-carboxylate derivatives.

Second Military Medical University
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.

Ariad Pharmaceuticals
Design, synthesis and biological activity of pyrazolo[1,5-a]pyrimidin-7(4H)-ones as novel Kv7/KCNQ potassium channel activators.

Hebei Medical University
Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant.

Ariad Pharmaceuticals
Nonpeptide urotensin-II receptor antagonists: a new ligand class based on piperazino-phthalimide and piperazino-isoindolinone subunits.

Johnson & Johnson Pharmaceutical Research & Development
Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.

University of Toronto
Phenylpiperidine-benzoxazinones as urotensin-II receptor antagonists: synthesis, SAR, and in vivo assessment.

Johnson & Johnson Pharmaceutical Research & Development
Resveratrol-derived inhibitors of the E3 ubiquitin ligase PELI1 inhibit the metastasis of triple-negative breast cancer.

Shandong University
Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan.

Wyeth Research
Transformation of a Dopamine D

Shanghaitech University
PKM2/PDK1 dual-targeted shikonin derivatives restore the sensitivity of EGFR-mutated NSCLC cells to gefitinib by remodeling glucose metabolism.

Nanjing University
Oxetane Promise Delivered: Discovery of Long-Acting IDO1 Inhibitors Suitable for Q3W Oral or Parenteral Dosing.

Pharmaron Beijing
Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma.

Zhejiang University
Triazine-Based Covalent DNA-Encoded Libraries for Discovery of Covalent Inhibitors of Target Proteins.

Chinese Academy of Sciences
Bivalent BET Bromodomain Inhibitors Confer Increased Potency and Selectivity for BRDT via Protein Conformational Plasticity.

University of Minnesota
Development of Dimethylisoxazole-Attached Imidazo[1,2-

University of Massachusetts Boston
Design, synthesis and biological evaluation of 4-aryl-5-aminoalkyl-thiazole-2-amines derivatives as ROCK II inhibitors.

Yantai University
Hit-to-lead optimization and discovery of a potent, and orally bioavailable G protein coupled receptor kinase 2 (GRK2) inhibitor.

Janssen Research & Development
Selective inhibition of BET bromodomains.

University of Oxford
Design, synthesis and biological evaluation of AZD9291 derivatives as selective and potent EGFR

Jiangxi Science & Technology Normal University
Development of Small-Molecules Targeting Receptor Activator of Nuclear Factor-κB Ligand (RANKL)-Receptor Activator of Nuclear Factor-κB (RANK) Protein-Protein Interaction by Structure-Based Virtual Screening and Hit Optimization.

Shanghai Jiaotong University School of Medicine
Discovery of a GPR40 Superagonist: The Impact of Aryl Propionic Acid α-Fluorination.

Janssen Research & Development
6-Benzhydryl-4-amino-quinolin-2-ones as Potent Cannabinoid Type 1 (CB

Janssen Research & Development
Synthesis and biological evaluation of benzocyclobutane-C-glycosides as potent and orally active SGLT1/SGLT2 dual inhibitors.

Janssen Research and Development
Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors.

University of Massachusetts-Boston
BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen.

University of Minnesota
PHOSPHONATES AS INHIBITORS OF ENPP1 AND CDNP

Stingray Therapeutics
AAK1 INHIBITOR AND USE THEREOF

Xizang Haisco Pharmaceutical
HETEROAROMATIC COMPOUNDS

Astrazeneca
Metabolites of [3-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4 yl}-phenoxy)-propyl]-diethyl-amine

Vtv Therapeutics
TYK2 inhibitors and uses thereof

Nimbus Lakshmi
Chemical compounds

Glaxosmithkline Intellectual Property (No. 2)
Triazolopyridines

Hoffmann-La Roche
Catecholamine prodrugs for use in the treatment of Parkinson's disease

H. Lundbeck
Composition for suppressing neuraminidase activity comprising geranylated flavonoid derived from Paulownia tomentosa as active ingredient

Industry-Academic Cooperation Foundation Gyeongsang National University
Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors

Incyte
Heterocyclic compound

Takeda Pharmaceutical
Chemical compounds

Boehringer Ingelheim International
Protease inhibitors. Part 8: synthesis of potent Clostridium histolyticum collagenase inhibitors incorporating sulfonylated L-alanine hydroxamate moieties.

Universita Degli Studi Di Firenze