PMID
Cmpds
Data
Article Title
Organization
70
Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HT

Bristol Myers Squibb
1
Discovery and Pre-Clinical Characterization of Third-Generation 4-H Heteroaryldihydropyrimidine (HAP) Analogues as Hepatitis B Virus (HBV) Capsid Inhibitors.

Roche Innovation Center Shanghai
15
GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved

Genentech
46
Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design.

Pharmaron-Beijing
22
Synthesis and biological evaluation of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors.

Xi'An Jiaotong University
22
Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton's tyrosine kinase (BTK) inhibitors.

China Pharmaceutical University
21
Studies examining the relationship between the chemical structure of protoxin II and its activity on voltage gated sodium channels.

Purdue Pharma
36
Discovery of 5-chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one (BMS-903452), an antidiabetic clinical candidate targeting GPR119.

Departments of Discovery Chemistry, Metabolic Diseases, Lead Evaluation, Computer-Assisted Drug Design, Discovery Toxicology, Exploratory Clinical and Translational Research, and Pharmaceutical Candi
26
Reductions in log P improved protein binding and clearance predictions enabling the prospective design of cannabinoid receptor (CB1) antagonists with desired pharmacokinetic properties.

Bristol Myers Squibb
23
Synthesis and SAR of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones as 5-HT2C receptor agonists.

Bristol Myers Squibb
24
3-Thiomorpholin-8-oxo-8H-acenaphtho [1,2-b] pyrrole-9-carbonitrile (S1) derivatives as pan-Bcl-2-inhibitors of Bcl-2, Bcl-xL and Mcl-1.

Dalian University of Technology
25
Pentacyclic triterpenes. Part 3: Synthesis and biological evaluation of oleanolic acid derivatives as novel inhibitors of glycogen phosphorylase.

China Pharmaceutical University
3
Pentacyclic triterpenes. Part 1: the first examples of naturally occurring pentacyclic triterpenes as a new class of inhibitors of glycogen phosphorylases.

China Pharmaceutical University
10
Probing the difference between BH3 groove of Mcl-1 and Bcl-2 protein: Implications for dual inhibitors design.

Dalian University of Technology
15
3-Thiomorpholin-8-oxo-8H-acenaphtho[1,2-b]pyrrole-9-carbonitrile (S1) based molecules as potent, dual inhibitors of B-cell lymphoma 2 (Bcl-2) and myeloid cell leukemia sequence 1 (Mcl-1): structure-based design and structure-activity relationship studies.

Dalian University of Technology
15
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents.

Bristol Myers Squibb
16
Rational design and synthesis of highly potent anti-acetylcholinesterase activity huperzine A derivatives.

The Chinese Academy of Sciences
10
Carboxyl-promoted enhancement of selectivity for the β
3 adrenergic receptor. Negative charge of the sulfonic acid BMS-187413 introduces-β
3 binding selectivity

TBA
17
Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2.

Bristol Myers Squibb
3
Discovery and Characterization of RP03707: A Highly Potent and Selective KRASG12D PROTAC.

Risen (Shanghai) Pharma Tech Co., Ltd.
20
Discovery of Potent PDEδ/NAMPT Dual Inhibitors: Preclinical Evaluation in KRAS Mutant Pancreatic Cancer Cells.

Shanghai University
1
Design, synthesis and biological evaluation of N-salicyloyl tryptamine derivatives as multifunctional neuroprotectants for the treatment of ischemic stroke.

University of South China
15
Discovery of potent HIV-1 NNRTIs by CuAAC click-chemistry-based miniaturized synthesis, rapid screening and structure optimization.

Shandong University
7
Design, synthesis and antibacterial activity evaluation of ebselen derivatives in NDM-1 producing bacteria.

Ocean University of China
108
pH regulators and their inhibitors in tumor microenvironment.

University of South China
6
Synthesis and structure-activity optimization of 7-azaindoles containing aza-β-amino acids targeting the influenza PB2 subunit.

Zhejiang University
7
Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid.

TBA
42
Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations.

Bristol Myers Squibb
11
Exploration and Biological Evaluation of 1,3-Diamino-7

Chinese Academy of Medical Sciences&Peking Union Medical College
47
Discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol- 6(2H)-one, a selective, orally active agonist of the 5-HT(2C) receptor.

Pharmaceutical Research Institute
3
Recent progress toward developing axial chirality bioactive compounds.

Shandong University
12
Discovery of conformationally constrained c-Abl inhibitors with potential neuroprotective effects against Parkinson's disease.

Southern Medical University
19
Selective degradation of cellular BRD3 and BRD4-L promoted by PROTAC molecules in six cancer cell lines.

Shanghai Institute of Materia Medica
11
Discovery of Linvencorvir (RG7907), a Hepatitis B Virus Core Protein Allosteric Modulator, for the Treatment of Chronic HBV Infection.

China Innovation Center of Roche
12
Therapeutic potential of targeting SHP2 in human developmental disorders and cancers.

Zhejiang University
54
Discovery of Ethyl Ketone-Based Highly Selective HDACs 1, 2, 3 Inhibitors for HIV Latency Reactivation with Minimum Cellular Potency Serum Shift and Reduced hERG Activity.

Merck
44
Syntheses, Biological Evaluations, and Mechanistic Studies of Benzo[

China Pharmaceutical University
46
BMS-201620: a selective beta 3 agonist.

Bristol Myers Squibb
18
Discovery of BMS-986318, a Potent Nonbile Acid FXR Agonist for the Treatment of Nonalcoholic Steatohepatitis.

Bristol Myers Squibb
25
Discovery of macrocyclic HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.

Merck
30
BMS-196085: a potent and selective full agonist of the human beta(3) adrenergic receptor.

Bristol Myers Squibb
24
Development of a selective HDAC inhibitor aimed at reactivating the HIV latent reservoir.

Merck
19
Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance.

Merck
36
Discovery of ethyl ketone-based HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.

Merck
3
Chemoreactive-Inspired Discovery of Influenza A Virus Dual Inhibitor to Block Hemagglutinin-Mediated Adsorption and Membrane Fusion.

Ocean University of China
1
Design and Synthesis of Orally Bioavailable 4-Methyl Heteroaryldihydropyrimidine Based Hepatitis B Virus (HBV) Capsid Inhibitors.

Roche Innovation Center Shanghai
19
Highly Potent and Selective Plasmin Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold Attenuate Fibrinolysis in Plasma.

The University of Queensland
36
Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.

Shandong University
34
Implementation of the CYP Index for the Design of Selective Tryptophan-2,3-dioxygenase Inhibitors.

Genentech
19
Overview of Recent Strategic Advances in Medicinal Chemistry.

Shandong University
4
Identification of highly potent and selective Cdc25 protein phosphatases inhibitors from miniaturization click-chemistry-based combinatorial libraries.

Shandong University
40
Synthesis and SAR of potent and selective tetrahydropyrazinoisoquinolinone 5-HT(2C) receptor agonists.

Bristol Myers Squibb
4
Discovery of phenylalanine derivatives as potent HIV-1 capsid inhibitors from click chemistry-based compound library.

Shandong University
24
Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.

Shandong University
24
Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site.

Shandong University
23
Scaffold-Hopping Approach To Discover Potent, Selective, and Efficacious Inhibitors of NF-κB Inducing Kinase.

Genentech
30
Aminoisoxazoles as Potent Inhibitors of Tryptophan 2,3-Dioxygenase 2 (TDO2).

Genentech
4
Discovery of Thiophene[3,2-

Shandong University
10
Design, synthesis and biological evaluation of novel 4-phenoxyquinoline derivatives containing 3-oxo-3,4-dihydroquinoxaline moiety as c-Met kinase inhibitors.

Shenyang Pharmaceutical University
2
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.

Shandong University
21
Discovery of a Potent (4 R,5 S)-4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug Guided by Molecular Modeling.

Pharmaron-Beijing
5
Discovery of Potent Small-Molecule Inhibitors of Ubiquitin-Conjugating Enzyme UbcH5c fromα-Santonin Derivatives.

Second Military Medical University
48
4-[[(7-aminopyrazolo[1,5-a]pyrimidin-5-yl)amino methyl]piperidin-3-ol compounds and their therapeutic use

Carrick Therapeutics
42
QUINOLINE COMPOUND AND USE THEREOF

Shanghai Pharmaceuticals Holding Co.
8
Deuterated protease inhibitors

Kansas State University Research Foundation
146
ISOXAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERED RELATED THERETO

Arena Pharmaceuticals
14
TREATMENT OF MYELOPROLIFERATIVE DISEASES AND DISORDERS WITH INHIBITORS OF BET FAMILY BDII BROMODOMAIN

Poseidon Innovation 1
29
COMPOUND USED AS KINASE INHIBITOR AND USE THEREOF

Tyk Medicines
93
SARS-CoV-2 inhibitors for treating coronavirus infections

Insilico Medicine IP
26
Combination therapy for treatment of hematological diseases

Incyte
10
Substituted pyridines as inhibitors of histone deacetylase

Alkermes
15
Selective NR2B antagonists

Bristol Myers Squibb
13
Bipyrazole derivatives as JAK inhibitors

Incyte
123
Autotaxin inhibitors

Cancer Research Technology
10
[5,6]—fused bicyclic antidiabetic compounds

Merck Sharp & Dohme
247
Pyrrolone or pyrrolidinone melanin concentrating hormone receptor-1 antagonists

Bristol Myers Squibb
73
Imidazopyridazine JAK3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases

Bristol Myers Squibb
19
Selective histone deactylase 6 inhibitors

H. Lee Moffitt Cancer Center and Research Institute
52
Aniline derivatives, their preparation and their therapeutic application

Fovea Pharmaceuticals
11
Compositions, synthesis, and methods of using phenylcycloalkylmethylamine derivatives

Reviva Pharmaceuticals
137
Selective NR2B antagonists

Bristol Myers Squibb
22
Coumarin-thiazole and -oxadiazole derivatives: Synthesis, bioactivity and docking studies for aldose/aldehyde reductase inhibitors.

Comsats Institute of Information Technology
64
Sulfamide sodium channel inhibitors

Amgen
6
DiPOA ([8-(3,3-diphenyl-propyl)-4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]dec-3-yl]-acetic acid), a novel, systemically available, and peripherally restricted mu opioid agonist with antihyperalgesic activity: I. In vitro pharmacological characterization and pharmacokinetic properties.

Purdue Pharma Discovery Research
29
Pharmacology and functions of metabotropic glutamate receptors.

Emory University
6
Splicing factor SF3b as a target of the antitumor natural product pladienolide.

Eisai