PMID
Cmpds
Data
Article Title
Organization
26
Development of 2, 4-diaminoquinazoline derivatives as potent PAK4 inhibitors by the core refinement strategy.

Shenyang Pharmaceutical University
2
Turning a Substrate Peptide into a Potent Inhibitor for the Histone Methyltransferase SETD8.

Abbvie
17
Design, synthesis and in vitro evaluation of amidoximes as histone deacetylase inhibitors for cancer therapy.

Qilu Normal University
43
Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6.

Icahn School Of Medicine At Mount Sinai
23
Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin.

China Pharmaceutical University
51
Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.

Ariad Pharmaceuticals
31
Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2.

Bayer Pharma
16
Exploiting the co-reliance of tumours upon transport of amino acids and lactate: Gln and Tyr conjugates of MCT1 inhibitors.

The Scripps Research Institute
19
Discovery of a Potent Class I Protein Arginine Methyltransferase Fragment Inhibitor.

University of Toronto
18
Design, synthesis and biological evaluation of novel donepezil-coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease.

China Pharmaceutical University
21
Novel Small Molecule Inhibitors of Choline Kinase Identified by Fragment-Based Drug Discovery.

Ariad Pharmaceuticals
26
Discovery of the imidazole-derived GPR40 agonist AM-3189.

Amgen
33
Discovery of Potent and Selective Inhibitors for ADAMTS-4 through DNA-Encoded Library Technology (ELT).

Glaxosmithkline
11
Discovery of A-893, A New Cell-Active Benzoxazinone Inhibitor of Lysine Methyltransferase SMYD2.

Abbvie
3
Discovery of a Dual PRMT5-PRMT7 Inhibitor.

University of Toronto
22
Synthesis and biological evaluation of 3-phenyl-3-aryl carboxamido propanoic acid derivatives as small molecule inhibitors of retinoic acid 4-hydroxylase (CYP26A1).

Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)
25
Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8.

University of North Carolina at Chapel Hill
22
Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists.

Amgen
12
Synthesis and evaluation of several oleanolic acid glycoconjugates as protein tyrosine phosphatase 1B inhibitors.

North-West University
16
Discovery and development of potent and selective inhibitors of histone methyltransferase g9a.

Abbvie
12
Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.

University of North Carolina at Chapel Hill
23
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.

Amgen
1
Design, synthesis and antithrombotic evaluation of novel dabigatran prodrugs containing methyl ferulate.

China Pharmaceutical University
5
Bromo-deaza-SAH: a potent and selective DOT1L inhibitor.

Entremed
47
Exploiting an allosteric binding site of PRMT3 yields potent and selective inhibitors.

University of North Carolina at Chapel Hill
6
Synthesis and biological evaluation of 1-(6-methylpyridin-2-yl)-5-(quinoxalin-6-yl)-1,2,3-triazoles as transforming growth factor-ß type 1 receptor kinase inhibitors.

Ewha Womans University
14
Fragment growing and linking lead to novel nanomolar lactate dehydrogenase inhibitors.

Ariad Pharmaceuticals
8
Synthesis and evaluation of bivalent, peptidomimetic antagonists of theavß3 integrins.

The Methodist Hospital Research Institute
22
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.

TBA
37
Discovery of SCH 900271, a Potent Nicotinic Acid Receptor Agonist for the Treatment of Dyslipidemia.

TBA
9
Cytochrome P450 3A4 inhibitory constituents of the wood of Taxus yunnanensis.

University of Toyama
10
Synthesis and opioid receptor activity of indolopropellanes.

Chinese Academy of Sciences
33
Design, synthesis, and biological evaluation of novel constrained meta-substituted phenyl propanoic acids as peroxisome proliferator-activated receptor alpha and gamma dual agonists.

Seoul National University
2
Engineering of a VPAC2 receptor peptide agonist to impart dipeptidyl peptidase IV stability and enhance in vivo glucose disposal.

Bayer Pharmaceuticals
6
The design, synthesis and in vitro immunosuppressive evaluation of novel isobenzofuran derivatives.

Shenyang Pharmaceutical University
9
Probes for narcotic receptor mediated phenomena. 43. Synthesis of the ortho-a and para-a, and improved synthesis and optical resolution of the ortho-b and para-b oxide-bridged phenylmorphans: compounds with moderate to low opioid-receptor affinity.

National Institute On Drug Abuse and The National Institute On Alcohol Abuse and Alcoholism
19
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.

Ariad Pharmaceuticals
17
3-Amino-pyrazolo[3,4-d]pyrimidines as p38a kinase inhibitors: design and development to a highly selective lead.

Roche Palo Alto
37
Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors

Roche Palo Alto
48
Discovery of a Potent Nicotinic Acid Receptor Agonist for the Treatment of Dyslipidemia

TBA
21
Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators.

Chinese Academy of Sciences
56
Discovery of CHD1 Antagonists for PTEN-Deficient Prostate Cancer.

University of North Carolina at Chapel Hill
24
Design, Structure Optimization, and Preclinical Characterization of JAB-21822, a Covalent Inhibitor of KRASG12C.

Jacobio Pharmaceuticals Group Co., Ltd.
3
Design, Synthesis, and Biological Evaluation of 1,3,4-Thiadiazole Derivatives as Novel Potent Peptide Deformylase Inhibitors for Combating Drug-Resistant Gram-Positive and -Negative Bacteria.

Henan Normal University
56
Synthesis and evaluation of novel ebselen derivatives as urease inhibitors for combating Helicobacter pylori infections.

Shandong Second Medical University
26
Discovery and structure-activity relationship study of nicotinamide derivatives as DNA demethylase ALKBH2 inhibitors.

Sichuan University
28
A Target Class Ligandability Evaluation of WD40 Repeat-Containing Proteins.

University of Toronto
31
Design, synthesis and biological evaluation of novel benzimidazole-derived p21-activited kinase 4 (PAK4) inhibitors bearing a 4-(4-methylpiperazin-1-yl)phenyl scaffold as potential antitumor agents.

China Medical University
1
211At radiolabeled APBA-FAPI for enhanced targeted-alpha therapy of glioma.

Sichuan University
1
Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia.

CeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences
3
(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.

University of Toronto
11
An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1.

UNC Eshelman School of Pharmacy
1
The MLL1 trimeric catalytic complex is a dynamic conformational ensemble stabilized by multiple weak interactions.

University of Toronto
1
LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2.

Eli Lilly
28
Discovery of the SMYD3 Inhibitor BAY-6035 Using Thermal Shift Assay (TSA)-Based High-Throughput Screening.

Bayer AG
3
A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3).

Icahn School Of Medicine At Mount Sinai
5
Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.

University of Toronto
1
Discovery of a chemical probe for PRDM9.

University of Toronto
26
Development of selective class I protein arginine methyltransferase inhibitors through fragment-based drug design approach.

CSIR-Indian Institute of Chemical Biology (IICB)
1
Discovery of highly potent and selective VEGFR2 kinase inhibitors for the treatment of rheumatoid arthritis.

Anhui Medical University
1
Design, synthesis and biological evaluation of indazole derivatives as VEGFR-2 kinase inhibitors with anti-angiogenic properties.

Anhui Medical University
15
Synthesis and Optimization of Small Molecule Inhibitors of Prostate Specific Antigen.

University of Missouri - Columbia
53
Structural Optimization and Structure-Activity Relationship of 1H-Pyrazole-4-carboxylic Acid Derivatives as DNA 6mA Demethylase ALKBH1 Inhibitors and Their Antigastric Cancer Activity.

Sichuan University
1
Distinct Amino Acid-Based PROTACs Target Oncogenic Kinases for Degradation in Non-Small Cell Lung Cancer (NSCLC).

Southern University of Science and Technology
18
Discovery of a Potent, Selective, and Cell-Active SPIN1 Inhibitor.

Icahn School Of Medicine At Mount Sinai
19
Exploiting the Carboxylate-Binding Pocket of β-Lactamase Enzymes Using a Focused DNA-Encoded Chemical Library.

Baylor College of Medicine
42
Discovery of matrix metalloproteinase inhibitors as anti-skin photoaging agents.

Hangzhou Normal University
6
Plant-derived strategies to fight against severe acute respiratory syndrome coronavirus 2.

Zhengzhou University
9
Design, synthesis and biological evaluation of matrine contains benzimidazole derivatives as dual TOPOI and PARP inhibitors for cancer therapy.

Guangxi University
2
The activity and mechanism of vidofludimus as a potent enzyme inhibitor against NDM-1-positive E. coli.

Northeast Agricultural University
17
Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARalpha/gamma dual agonists.

Seoul National University
9
Synthesis and pharmacological evaluation of 6,7-indolo/thiazolo-morphinans--further SAR of levorphanol.

Chinese Academy of Sciences
38
Discovery of benzodiazepine derivatives as a new class of covalent inhibitors of SARS-CoV-2 main protease.

Sichuan University
3
Chemical Catalysis Guides Structural Identification for the Major

Baylor College of Medicine
26
Structure-Based Discovery of Inhibitors of the SARS-CoV-2 Nsp14 N7-Methyltransferase.

University of California San Francisco
16
Discovery of cysteine-targeting covalent histone methyltransferase inhibitors.

Nanjing Medical University
25
Discovery of Highly Potent and BMPR2-Selective Kinase Inhibitors Using DNA-Encoded Chemical Library Screening.

Baylor College of Medicine
1
Discovery of N-(4-(6-Acetamidopyrimidin-4-yloxy)phenyl)-2-(2-(trifluoromethyl)phenyl)acetamide (CHMFL-FLT3-335) as a Potent FMS-like Tyrosine Kinase 3 Internal Tandem Duplication (FLT3-ITD) Mutant Selective Inhibitor for Acute Myeloid Leukemia.

Hefei Institutes of Physical Science
12
A novel long-acting oxyntomodulin analogue eliminates diabetes and obesity in mice.

Beijing University of Chinese Medicine
15
Discovery of aromatic 2-(3-(methylcarbamoyl) guanidino)-N-aylacetamides as highly potent chitinase inhibitors.

China Agricultural University
33
Discovery of mobocertinib, a potent, oral inhibitor of EGFR exon 20 insertion mutations in non-small cell lung cancer.

Ariad Pharmaceuticals
22
Structure-activity relationships of Wee1 inhibitors: A review.

Sichuan University
30
Potent Uncompetitive Inhibitors of Nicotinamide

Harvard University
23
Discovery of 1-(Hetero)aryl-β-carboline Derivatives as IDO1/TDO Dual Inhibitors with Antidepressant Activity.

Nanjing Medical University
9
Discovery of a Novel Small-Molecule Inhibitor Disrupting TRBP-Dicer Interaction against Hepatocellular Carcinoma via the Modulation of microRNA Biogenesis.

Chinese Academy of Sciences
2
Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.

University of Science and Technology of China
29
Carbon-silicon switch led to the discovery of novel synthetic cannabinoids with therapeutic effects in a mouse model of multiple sclerosis.

Shanghaitech University
23
Rational Remodeling of Atypical Scaffolds for the Design of Photoswitchable Cannabinoid Receptor Tools.

Shanghaitech University
5
Identification of a Novel TAR RNA-Binding Protein 2 Modulator with Potential Therapeutic Activity against Hepatocellular Carcinoma.

Chinese Academy of Sciences
10
Discovery of Pyrazolo[3,4-

Bytedance Ai Lab
4
Structure-Based Design of a Selective Class I Histone Deacetylase (HDAC) Near-Infrared (NIR) Probe for Epigenetic Regulation Detection in Triple-Negative Breast Cancer (TNBC).

China Pharmaceutical University
8
A First-in-Class, Highly Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 6.

Icahn School Of Medicine At Mount Sinai
26
Lactams as EP4 prostanoid receptor subtype selective agonists. Part 1: 2-Pyrrolidinones-stereochemical and lower side-chain optimization.

Roche Palo Alto
14
Discovery of Small-Molecule Antagonists of the PWWP Domain of NSD2.

University of Toronto
29
Discovery of (

Hefei Institutes of Physical Science
2
Discovery of 6'-chloro-N-methyl-5'-(phenylsulfonamido)-[3,3'-bipyridine]-5-carboxamide (CHMFL-PI4K-127) as a novel Plasmodium falciparum PI(4)K inhibitor with potent antimalarial activity against both blood and liver stages of Plasmodium.

Chinese Academy of Sciences
17
G-Protein biased opioid agonists: 3-hydroxy-

National Institute On Drug Abuse
3
Structure-Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase.

Icahn School Of Medicine At Mount Sinai
25
Multi-step parallel synthesis enabled optimization of benzofuran derivatives as pan-genotypic non-nucleoside inhibitors of HCV NS5B.

Merck
7
Synthesis, biological evaluation and SAR studies of ursolic acid 3β-ester derivatives as novel CETP inhibitors.

Nanjing Medical University
15
New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms.

University College London
54
Structure-Activity Relationship Studies for Enhancer of Zeste Homologue 2 (EZH2) and Enhancer of Zeste Homologue 1 (EZH1) Inhibitors.

Icahn School Of Medicine At Mount Sinai
18
Design, synthesis and biological evaluation of novel desloratadine derivatives with anti-inflammatory and H

China Pharmaceutical University
7
Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1).

Icahn School Of Medicine At Mount Sinai
7
Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3-9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase.

Pfizer
3
Discovery of Inhibitors of Aurora/PLK Targets as Anticancer Agents.

Chengdu University
3
Discovery of a First-in-Class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor.

Icahn School Of Medicine At Mount Sinai
19
A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function.

University of Oxford
14
Discovery and Development of a Series of Pyrazolo[3,4-

Shanghai University
9
Design and evaluation of novel tetracyclic benzofurans as palm site allosteric inhibitors of HCV NS5B polymerase.

Merck
27
Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase.

Icahn School Of Medicine At Mount Sinai
3
Discovery of Highly Potent Inhibitors Targeting the Predominant Drug-Resistant S31N Mutant of the Influenza A Virus M2 Proton Channel.

The University of Arizona
27
Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.

China Pharmaceutical University
7
Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitors†Electronic supplementary information (ESI) available. See DOI: 10.1039/c4md00274a.

Imperial College London
12
Peptidomimetics of Arg-Phe-NH2 as small molecule agonists of Mas-related gene C (MrgC) receptors.

Johns Hopkins University
25
Determination of stereoselective interaction between enantiomers of chiral gamma-aryl-1H-1,2,4-triazole derivatives and Penicillium digitatum.

Central China Normal University
39
Rational Design, Synthesis, and Pharmacological Characterization of Novel Ghrelin Receptor Inverse Agonists as Potential Treatment against Obesity-Related Metabolic Diseases.

Sib Swiss Institute of Bioinformatics
1
In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent.

Ocean University of China
22
Novel cinnamamide-dibenzylamine hybrids: Potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease.

China Pharmaceutical University
25
Design, synthesis and evaluation of coumarin-pargyline hybrids as novel dual inhibitors of monoamine oxidases and amyloid-β aggregation for the treatment of Alzheimer's disease.

Shenyang Pharmaceutical University
4
Optimization of novel monobactams with activity against carbapenem-resistant Enterobacteriaceae - Identification of LYS228.

Novartis Institutes For Biomedical Research
33
Andrographolide derivative as STAT3 inhibitor that protects acute liver damage in mice.

University of Macau
39
Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor.

Chinese Academy of Sciences
2
LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity.

Lilly Research Laboratories
29
Structure-activity relationship studies of G9a-like protein (GLP) inhibitors.

Icahn School Of Medicine At Mount Sinai
25
Synthesis and pharmacological evaluation of novel chromone derivatives as balanced multifunctional agents against Alzheimer's disease.

China Pharmaceutical University
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
2
Discovery of Bisubstrate Inhibitors of Nicotinamide N-Methyltransferase (NNMT).

Icahn School Of Medicine At Mount Sinai
39
Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3).

Icahn School Of Medicine At Mount Sinai
769
Heteroaromatic amide derivative and medicament containing the same

Kaken Pharmaceutical Co.
17
Substituted pyrimidines as IRE1 kinase inhibitors

University Of California
24
INDOLINE DERIVATIVES AS DDR1 AND DDR2 INHIBITORS

Chiesi Farmaceutici
22
S-CONFIGURATION-CONTAINING AMINO BENZAMIDE PYRIDAZINONE COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF

Shanghai Institute of Materia Medica
83
Compound exhibiting enteropeptidase inhibitory activity

LG Chem
19
Inhibitors of histone deacetylase

The Broad Institute
5
Imidazo[1,2-B][1,2,4]triazines as c-Met inhibitors

Incyte Holdings
8
Pteridines as FGFR inhibitors

Astex Therapeutics
76
Heteroaromatic compounds and their use as dopamine D1 ligands

Pfizer
29
5-HT3 receptor antagonists

Takeda Pharmaceutical
5
Tryptophan-Rich Sensory Protein/Translocator Protein (TSPO) from Cyanobacterium Fremyella diplosiphon Binds a Broad Range of Functionally Relevant Tetrapyrroles.

Michigan State University
5
Imidazo[1,2-a]pyridines and imidazo[1,2-b]pyridazines as mark inhibitors

Merck Sharp & Dohme
61
Compounds and compositions as protein kinase inhibitors

TBA
80
Heterocyclic hydrazone compounds

Novartis
2
Cloning, expression, and pharmacological characterization of a novel human histamine receptor.

Smithkline Beecham Pharmaceuticals
11
Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors.

F. Hoffmann-La Roche