PMID
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Article Title
Organization
14
Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines.

Dalian Medical University
8
Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines.

Dalian Medical University
15
Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a

Dalian Medical University
1
Discovery of 8-Membered Ring Sulfonamides as Inhibitors of Oncogenic Mutant Isocitrate Dehydrogenase 1.

Harvard University
11
Synthesis and biological evaluation of azole-diphenylpyrimidine derivatives (AzDPPYs) as potent T790M mutant form of epidermal growth factor receptor inhibitors.

Dalian Medical University
13
Novel 4-anilinoquinazoline derivatives featuring an 1-adamantyl moiety as potent EGFR inhibitors with enhanced activity against NSCLC cell lines.

Dalian Medical University
1
Highly Efficient Synthesis of 1,3-Dihydroxy-2-carboxycarbazole and Its Neuroprotective Effects.

Virginia Commonwealth University
20
Design, synthesis, and biological evaluation of amide imidazole derivatives as novel metabolic enzyme CYP26A1 inhibitors.

Shenyang Pharmaceutical University
37
Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.

Merck Research Laboratories
1
Involvement of organic anion-transporting polypeptides in the hepatic uptake of dioscin in rats and humans.

Dalian Medical University
22
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics.

Beijing Institute of Pharmacology & Toxicology
29
Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide s receptor.

National Institutes of Health
14
Discovery of a novel noniminosugar acida glucosidase chaperone series.

National Center For Advancing Translational Sciences
21
N-4-t-Butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the A-region.

Seoul National University
32
Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor¿ (PPAR¿) modulators.

Merck Research Laboratories
45
2-(4-Methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the B and C-regions.

Shenyang Pharmaceutical University
11
Synthesis, molecular modeling and biological evaluation of 2-(benzylthio)-5-aryloxadiazole derivatives as anti-tumor agents.

Nanjing University
18
The combination of 4-anilinoquinazoline and cinnamic acid: a novel mode of binding to the epidermal growth factor receptor tyrosine kinase.

Nanjing University
18
SHAFTS: a hybrid approach for 3D molecular similarity calculation. 2. Prospective case study in the discovery of diverse p90 ribosomal S6 protein kinase 2 inhibitors to suppress cell migration.

East China University of Science and Technology
18
Selective Kv1.5 blockers: development of (R)-1-(methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a potential treatment for atrial arrhythmia.

Wyeth Research
7
Expedient solid-phase synthesis of both symmetric and asymmetric diol libraries targeting aspartic proteases.

National University of Singapore
14
Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.

Merck Research Laboratories
7
Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus with a reduced potential to increase plasma a

Merck Research Laboratories
8
Nocathiacin analogs: Synthesis and antibacterial activity of novel water-soluble amides.

Merck Research Laboratories
27
Discovery of Isobenzofuran-1(3H)-one Derivatives as Selective TREK-1 Inhibitors with In Vitro and In Vivo Neuroprotective Effects.

Chinese Academy of Medical Sciences and Peking Union Medical College
71
Design, Synthesis, and Biological Evaluation of Chiral-Proline Derivatives as Novel HSP90 Inhibitors.

Dezhou University
3
PaAP-Activatable NIR Probe for Diagnosing, Imaging, and Discovering Small-Molecule Therapeutics against Implant-Associated Biofilm Infections.

Chinese Academy of Medical Sciences & Peking Union Medical College
48
Discovery of a Novel 1,4-Benzodiazepine Derivative as a Highly Selective ANXA3 Degrader for the Treatment of Triple-Negative Breast Cancer.

Fudan University
4
Hit to lead optimization of the 4-trifluoromethylquinoline derivatives as novel SGK1 inhibitors with potent anti-prostate cancer activity.

Guizhou Medical University
31
Inhibitors targeting the PWWP domain-containing proteins.

Central China Normal University
39
Discovery, Optimization, and Evaluation of Potent and Selective DNA-PK Inhibitors in Combination with Chemotherapy or Radiotherapy for the Treatment of Malignancies.

West China Hospital
29
The discovery of potent USP2/USP8 dual-target inhibitors for the treatment of breast cancer via structure guided optimization of ML364.

China Pharmaceutical University
17
Design and Optimization of Novel Competitive, Non-peptidic, SARS-CoV-2 M

Emory University
36
Discovery and Evaluation of 3-Quinoxalin Urea Derivatives as Potent, Selective, and Orally Available ATM Inhibitors Combined with Chemotherapy for the Treatment of Cancer via Goal-Oriented Molecule Generation and Virtual Screening.

Sichuan University
1
Target discovery of bioactive natural products with native-compound-coupled CNBr-activated Sepharose 4B beads (NCCB): Applications, mechanisms and outlooks.

Zhengzhou University
32
Potent and Selective Biaryl Amide Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1).

Incyte Research Institute
18
Discovery of Pyrazolopyridine Derivatives as HPK1 Inhibitors.

Incyte Research Institute
14
Discovery of pyrimidine-bridged CA-4 CBSIs for the treatment of cervical cancer in combination with cisplatin with significantly reduced nephrotoxicity.

Fudan University
16
Oxetane Promise Delivered: Discovery of Long-Acting IDO1 Inhibitors Suitable for Q3W Oral or Parenteral Dosing.

Pharmaron Beijing
19
Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases.

National Clinical Research Center For Geriatrics
34
Discovery of 3, 6-disubstituted isobenzofuran-1(3H)-ones as novel inhibitors of monoamine oxidases.

Peking Union Medical College
1
Discovery and preclinical profile of LX-039, a novel indole-based oral selective estrogen receptor degrader (SERD).

Wuxi Apptec
22
Discovery of Potent Small-Molecule USP8 Inhibitors for the Treatment of Breast Cancer through Regulating ERα Expression.

China Pharmaceutical University
24
Discovery of Potent and Selective Receptor-Interacting Serine/Threonine Protein Kinase 2 (RIPK2) Inhibitors for the Treatment of Inflammatory Bowel Diseases (IBDs).

West China Hospital
16
Discovery of Novel Pyrazolopyrimidines as Potent, Selective, and Orally Bioavailable Inhibitors of ALK2.

Incyte
8
Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies.

West China Hospital
39
Structure-Based Discovery of a Series of NSD2-PWWP1 Inhibitors.

Chinese Academy of Sciences
17
Selective PPARgamma modulators with improved pharmacological profiles.

Merck Research Laboratories
9
Discovery of a novel series of peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes and dyslipidemia.

Merck Research Laboratories
27
Exploring Marine-Derived Ascochlorins as Novel Human Dihydroorotate Dehydrogenase Inhibitors for Treatment of Triple-Negative Breast Cancer.

Guangxi University of Chinese Medicine
39
Discovery of 3-(4-(2-((1

West China Hospital of Sichuan University
29
SAR towards indoline and 3-azaindoline classes of IDO1 inhibitors.

Merck
20
Design, synthesis, and biological evaluation of a novel dual peroxisome proliferator-activated receptor alpha/delta agonist for the treatment of diabetic kidney disease through anti-inflammatory mechanisms.

China Pharmaceutical University
13
Discovery of IDO1 inhibitors containing a decahydroquinoline, decahydro-1,6-naphthyridine, or octahydro-1H-pyrrolo[3,2-c]pyridine scaffold.

Merck
40
-(Pyrimidin-2-yl)-1,2,3,4-tetrahydroisoquinolin-6-amine Derivatives as Selective Janus Kinase 2 Inhibitors for the Treatment of Myeloproliferative Neoplasms.

West China Hospital of Sichuan University
30
Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists.

Merck And
29
Carbamate and

Merck
13
Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidines as atypical protein kinase C inhibitors to control retinal vascular permeability and cytokine-induced edema.

University of Michigan
10
Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis.

Dalian Medical University
8
Discovery of a potent, highly selective, and orally efficacious small-molecule activator of the insulin receptor.

Merck Research Laboratories
8
Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer.

Dalian Medical University
2
Ac

Nankai University
19
Discovery of Amino-cyclobutarene-derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors for Cancer Immunotherapy.

Merck
17
The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC.

Shenyang Pharmaceutical University
3
Bioactivatable Pseudotripeptidization of Cyclic Dipeptides To Increase the Affinity toward Oligopeptide Transporter 1 for Enhanced Oral Absorption: An Application to Cyclo(l-Hyp-l-Ser) (JBP485).

Dalian Medical University
49
Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies.

Merck
7
Structure-based modification of carbonyl-diphenylpyrimidines (Car-DPPYs) as a novel focal adhesion kinase (FAK) inhibitor against various stubborn cancer cells.

The First Affiliated Hospital of Dalian Medical University
11
Development of indazole mineralocorticoid receptor antagonists and investigation into their selective late-stage functionalization.

Merck
14
Design and Biological Evaluation of

Shenyang Pharmaceutical University
5
Discovery of Potent and Orally Effective Dual Janus Kinase 2/FLT3 Inhibitors for the Treatment of Acute Myelogenous Leukemia and Myeloproliferative Neoplasms.

West China Hospital of Sichuan University
3
Design, synthesis and biological evaluation of oseltamivir derivatives containing pyridyl group as potent inhibitors of neuraminidase for influenza A.

Wuyi University
9
Covalent binding design strategy: A prospective method for discovery of potent targeted anticancer agents.

Dalian Medical University
14
Synthesis and biological evaluation of morpholine-substituted diphenylpyrimidine derivatives (Mor-DPPYs) as potent EGFR T790M inhibitors with improved activity toward the gefitinib-resistant non-small cell lung cancers (NSCLC).

Dalian Medical University
8
Design, synthesis, and evaluation of carboxyl-modified oseltamivir derivatives with improved lipophilicity as neuraminidase inhibitors.

Shenyang Pharmaceutical University
16
Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.

The First Affiliated Hospital of Dalian Medical University
8
Synthesis and biological evaluation of NH

Shenyang Pharmaceutical University
10
Design, synthesis, and activity evaluation of novel erythropoietin mimetic peptides.

Beijing Institute of Pharmacology & Toxicology
5
Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines.

Dalian Medical University
1
De Novo Design of α-Helical Lipopeptides Targeting Viral Fusion Proteins: A Promising Strategy for Relatively Broad-Spectrum Antiviral Drug Discovery.

Beijing Institute of Pharmacology & Toxicology
7
Phosphamide-containing diphenylpyrimidine analogues (PA-DPPYs) as potent focal adhesion kinase (FAK) inhibitors with enhanced activity against pancreatic cancer cell lines.

Dalian Medical University
10
Design, synthesis and biological evaluation of sulfonamide-substituted diphenylpyrimidine derivatives (Sul-DPPYs) as potent focal adhesion kinase (FAK) inhibitors with antitumor activity.

Dalian Medical University
13
Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia.

Dalian Medical University
10
C-2 (E)-4-(Styryl)aniline substituted diphenylpyrimidine derivatives (Sty-DPPYs) as specific kinase inhibitors targeting clinical resistance related EGFR

Dalian Medical University
42
Compound modulators of sting

Ctxt
22
NOVEL MODULATORS OF THE 5-HYDROXYTRYPTAMINE RECEPTOR 7 AND THEIR METHOD OF USE

Temple University
894
KHK inhibitors

Gilead Sciences
17
Substituted pyrimidines as IRE1 kinase inhibitors

University Of California
157
HDAC INHIBITORS AND THERAPEUTIC USE THEREOF

Tango Therapeutics
45
Class of DNA gyrase and/or topoisomerase IV inhibitors with activity against gram-positive and gram-negative bacteria

Univerza V Ljubljani
29
3-amino-4H-benzo[e][1,2,4]thiadiazine 1,1-dioxide derivatives as inhibitors of MRGX2

Solent Therapeutics
369
BIFUNCTIONAL SULPHONAMIDE COMPOUNDS

Anaxis Pharma
19
Heterocyclic kinase inhibitors and uses thereof

iOMx Therapeutics
302
SMALL MOLECULAR INHIBITORS OF NF-kB INDUCING KINASE

Janssen Pharmaceutica
400
6-azaindole compounds

Bristol Myers Squibb
58
Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor.

Ontario Institute for Cancer Research
44
Carboxylic acid, acyl sulfonamide and acyl sulfamide-derivatized bicyclic aza-heteroaromatics as selective Mcl-1 inhibitors and as dual Mcl-1/Bcl-2 inhibitors

University of Maryland, Baltimore
111
Substituted 4-phenylpiperidines, their preparation and use

Columbia University
155
Dihydropyrrolopyridine inhibitors of ROR-gamma

Vitae Pharmaceuticals
1
Biochemical binding of RET9 and VEGFR2 inhibitors

Kala Pharmaceuticals
23
1,4-substituted isoquinoline inhibitors of KEAP1/NRF2 protein-protein interaction

University of Illinois
19
Inhibitors of histone deacetylase

The Broad Institute
85
3-(5-amino-pyrazin-2-yl)-benzenesulfonamide derivatives and related compounds as PI3K-gamma kinase inhibitors

Incyte
182
Substituted heterocyclic sulfonamide compounds useful as TRPA1 modulators

Genentech
92
N-((het)arylmethyl)-heteroaryl-carboxamides compounds as kallikrein inhibitors

Kalvista Pharmaceuticals
71
5-alkyl pyrrolidine orexin receptor agonists

Merck Sharp & Dohme
30
Substituted purines as TLR7 agonists

Primmune Therapeutics
18
Second generation GRP94-selective inhibitors

University of Kansas
6
Aminopyrimidinecarboxamides as CXCR2 modulators

Syntrix Biosystems
49
Heteroaryl-substituted sulfonamide compounds and their use as therapeutic agents

Xenon Pharmaceuticals
66
Chemical compounds

AstraZeneca
56
Spiro[3H-indole-3,2′-pyrrolidin]-2(1H)-one compounds and derivatives as MDM2-p53 inhibitors

Boehringer Ingelheim International
18
Cyclohexene compounds and use thereof

Guangzhou Henovcom Bioscience
22
Alpha-D-galactoside inhibitors of galectins

Galecto Biotech
260
WDR5-MLL1 inhibitors and modulators

Vanderbilt University
28
Signaling-biased mu opioid receptor agonists

The Scripps Research Institute
115
Cyclopropylamines as LSD1 inhibitors

Incyte
72
Pyridyl benzothiophenes as kinase inhibitors

Allergan
427
Quinazolinones as PARP14 inhibitors

Ribon Therapeutics
117
Purine inhibitors of human phosphatidylinositol 3-kinase delta

Merck Sharp & Dohme
15
Non-aromatic difluoro analogues of resorcylic acid lactones

University of North Carolina At Greensboro
295
COMPOUNDS AS SUMO ACTIVATING ENZYME INHIBITORS

Wigen Biomedicine Technology (Shanghai)
6
Enantiomers of the 1′,6′-isomer of neplanocin A

Auburn University
47
[1,2,4] triazol [4,3-A] pyridine derivative, preparation method therefor or medical application thereof

Jiangsu Hansoh Pharmaceutical
5
Method for inhibiting Trypanosoma cruzi

Howard University
22
Alpha-(3,5-dimethoxybenzylidene)-alpha′-hydrocarbyl methylene cyclic ketone and preparation method thereof

Pharmaxyn Laboratories
3
Inhibitory effects of thioethers on fatty acid synthase and 3T3-L1 cells.

Graduate University of Chinese Academy of Sciences
8
Trimethylation of histone H3 lysine 36 by human methyltransferase PRDM9 protein.

University of Toronto
144
Pyrrolopyrimidine compounds and uses thereof

Hutchison Medipharma
34
Synthesis, crystal structure determination, biological screening and docking studies of N1-substituted derivatives of 2,3-dihydroquinazolin-4(1H)-one as inhibitors of cholinesterases.

University of Sargodha
122
Chemokine receptor modulators

Altiris Therapeutics
11
Beta-amyloid-directed multitarget compounds for the treatment of alzheimer's disease

Universitat De Barcelona
16
2-aminoquinoline-based compounds for potent and selective neuronal nitric oxide synthase inhibition

Northwestern University
6
Selective PI3K delta inhibitors

Rhizen Pharmaceuticals
40
Hydroxymethylaryl-substituted pyrrolotriazines as ALK1 inhibitors

Bayer Intellectual Property
4
Pharmacological properties of (2R)-N-[1-(6-aminopyridin-2-ylmethyl)piperidin-4-yl]-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: a novel mucarinic antagonist with M(2)-sparing antagonistic activity.

Banyu Pharmaceutical
5
Characterization of the binding site for a novel class of noncompetitive alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonists.

Pfizer
22
Comparison of the pharmacological characteristics of [3H]raclopride and [3H]SCH 23390 binding to dopamine receptors in vivo in mouse brain.

Novo Industri
4
8-Cyclopentyl-1,3-dipropylxanthine (DPCPX)--a selective high affinity antagonist radioligand for A1 adenosine receptors.

UniversitÄT Heidelberg
1
Neurochemical profile of eltoprazine.

Duphar
21
Structure-based drug design of pyrrolidine-1, 2-dicarboxamides as a novel series of orally bioavailable factor Xa inhibitors.

Pfizer