PMID
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Article Title
Organization
10
Discovery and biological evaluation of some (1H-1,2,3-triazol-4-yl)methoxybenzaldehyde derivatives containing an anthraquinone moiety as potent xanthine oxidase inhibitors.

China Medical University
1
Discovery of highly selective CRAF inhibitors, 3-carboxamido-2H-indazole-6-arylamide: In silico FBLD design, synthesis and evaluation.

Hanyang University
6
6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Regioisomers as Targeted Antifolates for Folate Receptora and the Proton-Coupled Folate Transporter in Human Tumors.

Duquesne University
4
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.

Hanyang University
14
Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition.

Novartis Institutes For Biomedical Research
11
Potent and selective double-headed thiophene-2-carboximidamide inhibitors of neuronal nitric oxide synthase for the treatment of melanoma.

Northwestern University
14
Discovery of tryptanthrin derivatives as potent inhibitors of indoleamine 2,3-dioxygenase with therapeutic activity in Lewis lung cancer (LLC) tumor-bearing mice.

Fudan University
19
Synthesis and biological evaluation of substituted benzoxazoles as inhibitors of mPGES-1: use of a conformation-based hypothesis to facilitate compound design.

Pfizer
9
Design and synthesis of novel 2-methyl-4,5-substitutedbenzo[f]-3,3a,4,5-tetrahydro-pyrazolo[1,5-d][1,4]oxazepin-8(7H)-one derivatives as telomerase inhibitors.

Guizhou University
1
Total synthesis of grassystatin A, a probe for cathepsin E function.

Fudan University
69
Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.

Pfizer
24
TIE-2/VEGF-R2 SAR and in vitro activity of C3-acyl dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole analogs.

Cephalon
15
Structure-activity relationship and enzyme kinetic studies on 4-aryl-1H-1,2,3-triazoles as indoleamine 2,3-dioxygenase (IDO) inhibitors.

Fudan University
16
Quinoline-4-methyl esters as human nonpancreatic secretory phospholipase A2 inhibitors.

Peking University
27
Discovery of dual target inhibitors against cyclooxygenases and leukotriene A4 hydrolyase.

Peking University
5
Synthesis and biological evaluation of novel 5-benzylidenethiazolidine-2,4-dione derivatives for the treatment of inflammatory diseases.

Sichuan University
4
Synthesis and biological evaluation of oleanolic acid derivatives as inhibitors of protein tyrosine phosphatase 1B.

Xihua University
34
Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase.

Pfizer
24
Azole-based inhibitors of AKT/PKB for the treatment of cancer.

Amgen
1
Chemical Constituents of the Roots of Euphorbia micractina.

Peking Union Medical College
30
Discovery of 4-((quinolin-8-ylthio)methyl)benzamide derivatives as a new class of SARS-CoV-2 nsp13 inhibitors.

Sichuan University
51
Discovery of Novel Aromatic Urea-Imidazole Salt Derivatives for Cancer Therapy via Targeting ERK1/2.

Henan Normal University
10
Design, Synthesis, and Unprecedented Interactions of Covalent Dipeptide-Based Inhibitors of SARS-CoV-2 Main Protease and Its Variants Displaying Potent Antiviral Activity.

Eberhard Karls University Tubingen
4
Design and Synthesis of c-Met and HDAC Dual Inhibitors for the Treatment of Breast Cancer.

Tsinghua University
40
Discovery of Novel Spirocyclic MAT2A Inhibitors Demonstrating High In Vivo Efficacy in MTAP-Null Xenograft Models.

Shanghai Haiyan Pharmaceutical Technology 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
2
Discovery of Selenium-Containing Derivatives as Potent and Orally Bioavailable GLP-1R Agonists.

China Pharmaceutical University
26
Discovery and structure-activity relationship study of nicotinamide derivatives as DNA demethylase ALKBH2 inhibitors.

Sichuan University
16
Discovery of Highly Selective Inhibitors of Microtubule-Associated Serine/Threonine Kinase-like (MASTL).

Pfizer
25
Development of a Fluorescence Probe for High-Throughput Screening of Allosteric Inhibitors Targeting TRAP1.

Ewha Womans University
26
Design and synthesis of dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole oximes as potent dual inhibitors of TIE-2 and VEGF-R2 receptor tyrosine kinases.

Cephalon
45
Discovery and structure-activity relationship studies of novel α-ketoamide derivatives targeting the SARS-CoV-2 main protease.

Sichuan University
8
Novel EGFR inhibitors against resistant L858R/T790M/C797S mutant for intervention of non-small cell lung cancer.

Nankai University
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
13
Discovery and preclinical evaluations of TQB3616, a novel CDK4-biased inhibitor.

WuXi AppTec
29
Discovery of a New Anti-Inflammatory Agent from Anemoside B4 Derivatives and Its Therapeutic Effect on Colitis by Targeting Pyruvate Carboxylase.

Soochow University
2
Design, Synthesis, and Activity Evaluation of Fluorine-Containing Scopolamine Analogues as Potential Antidepressants.

Henan Normal University
51
From Hit to Lead: Structure-Based Optimization of Novel Selective Inhibitors of Receptor-Interacting Protein Kinase 1 (RIPK1) for the Treatment of Inflammatory Diseases.

Sichuan University
2
Discovery of a Potent Nicotinamide Phosphoribosyltransferase Activator for Improving Aging-associated Dysfunctions.

Second Military Medical University (Naval Medical University)
19
Therapeutic potential of targeting polo-like kinase 4.

Sichuan University
86
Discovery of the Clinical Candidate Sonrotoclax (BGB-11417), a Highly Potent and Selective Inhibitor for Both WT and G101V Mutant Bcl-2.

BeiGene(Beiing) Co., Ltd.
42
Discovery of novel imidazole chemotypes as isoform-selective JNK3 inhibitors for the treatment of Alzheimer's disease.

Hanyang University
48
Novel tetrahydro-beta-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).

Pfizer
4
Discovery of a Hidden Pocket beneath the NES Groove by Novel Noncovalent CRM1 Inhibitors.

Sichuan University
38
Discovery of benzodiazepine derivatives as a new class of covalent inhibitors of SARS-CoV-2 main protease.

Sichuan University
35
Discovery of 5-((1H-indazol-3-yl) methylene)-2-thioxoimidazolidin-4-one derivatives as a new class of AHR agonists with anti-psoriasis activity in a mouse model.

Sichuan University
1
Discovery of 4-(1,2,4-Oxadiazol-5-yl)azepan-2-one Derivatives as a New Class of Cannabinoid Type 2 Receptor Agonists for the Treatment of Inflammatory Pain.

Sichuan University
5
Carbamate JNK3 Inhibitors Show Promise as Effective Treatments for Alzheimer's Disease: In Vivo Studies on Mouse Models.

Hanyang University
33
Discovery of 2-Amino-7-sulfonyl-7

China Pharmaceutical University
32
Novel C-3 N-urea, amide, and carbamate dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole analogs as potent TIE-2 and VEGF-R2 dual inhibitors.

Cephalon
44
Discovery of a potent and highly selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase: Structural activity relationship and antitumor activity both in vitro and in vivo.

Sichuan University
39
Identification of triazolopyridine derivatives as a new class of AhR agonists and evaluation of anti-psoriasis effect in a mouse model.

Sichuan University
59
Discovery of 3,4-Dihydrobenzo[

Sichuan University
40
Discovery of Orally Bioavailable

China Pharmaceutical University
39
Discovery of benzo[d]oxazol-2(3H)-one derivatives as a new class of TNIK inhibitors for the treatment of colorectal cancer.

Sichuan University
67
Discovery of a novel and potent inhibitor with differential species-specific effects against NLRP3 and AIM2 inflammasome-dependent pyroptosis.

Sichuan University
5
Discovery and structural optimization of potent epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M/C797S resistance mutation for lung cancer treatment.

Nankai University
52
Discovery of a potent, selective and cell active inhibitor of m

Nankai University
5
Discovery of 2-vinyl-10H-phenothiazine derivatives as a class of ferroptosis inhibitors with minimal human Ether-a-go-go related gene (hERG) activity for the treatment of DOX-induced cardiomyopathy.

Sichuan University
2
Covalent sortase A inhibitor ML346 prevents

Shanghai Institute of Materia Medica
1
In vitro and in vivo neuroprotective effect of novel mPGES-1 inhibitor in animal model of Parkinson's disease.

Kyung Hee University
42
Structural Optimization and Structure-Activity Relationship Studies of 6,6-Dimethyl-4-(phenylamino)-6

Sichuan University
49
Design, Synthesis, and Biological Evaluation of Triazolone Derivatives as Potent PPARα/δ Dual Agonists for the Treatment of Nonalcoholic Steatohepatitis.

China Pharmaceutical University
21
Design, synthesis and biological evaluation of sphingosine-1-phosphate receptor 2 antagonists as potent 5-FU-resistance reversal agents for the treatment of colorectal cancer.

Laboratory For Marine Drugs and Bioproducts of Qingdao National Laboratory For Marine Science and Technology
69
Structure-activity relationship investigation for imidazopyrazole-3-carboxamide derivatives as novel selective inhibitors of Bruton's tyrosine kinase.

Henan Normal University
59
Discovery of 1-Amino-1

Henan Normal University
34
Discovery of a new class of JMJD6 inhibitors and structure-activity relationship study.

Nankai University
55
Discovery of a potent and selective inhibitor of histone lysine demethylase KDM4D.

Nankai University
31
Design and Synthesis of TRAP1 Selective Inhibitors: H-Bonding with Asn171 Residue in TRAP1 Increases Paralog Selectivity.

Ewha Womans University
30
A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clin

Cephalon
1
Structure-activity relationship studies of phenothiazine derivatives as a new class of ferroptosis inhibitors together with the therapeutic effect in an ischemic stroke model.

Sichuan University
1
SAR study of bisamides as cyclophilin a inhibitors for the development of host-targeting therapy for hepatitis C virus infection.

Chonnam National University
38
Discovery and structure-activity relationship studies of 1-aryl-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione derivatives as potent dual inhibitors of indoleamine 2,3-dioxygenase 1 (IDO1) and trytophan 2,3-dioxygenase (TDO).

Sichuan University
24
Discovery of small molecule FLT3 inhibitors that are able to overcome drug-resistant mutations.

Sichuan University
1
Molecular design, synthesis, and biological evaluation of bisamide derivatives as cyclophilin A inhibitors for HCV treatment.

Chonnam National University
3
Discovery of Potent Small-Molecule SIRT6 Activators: Structure-Activity Relationship and Anti-Pancreatic Ductal Adenocarcinoma Activity.

Sichuan University
13
Discovery of 5-(4-methylpiperazin-1-yl)-2-nitroaniline derivatives as a new class of SIRT6 inhibitors.

Sichuan University
41
Tideglusib and Its Analogues As Inhibitors of

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

Ocean University of China
32
Discovery of 2-((4-resorcinolyl)-5-aryl-1,2,3-triazol-1-yl)acetates as potent Hsp90 inhibitors with selectivity over TRAP1.

Daegu-Gyeongbuk Medical Innovation Foundation (Dgmif)
5
Discovery of Novel Dual Histone Deacetylase and Mammalian Target of Rapamycin Target Inhibitors as a Promising Strategy for Cancer Therapy.

TBA
1
Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis.

Nankai University
24
The chemical biology of apoptosis: Revisited after 17 years.

Tsinghua University
65
Design, Synthesis, and Biological Evaluation of Novel Allosteric Protein Disulfide Isomerase Inhibitors.

University of Michigan
39
Identification of Pyrrolo[2,3- d]pyrimidine-Based Derivatives as Potent and Orally Effective Fms-like Tyrosine Receptor Kinase 3 (FLT3) Inhibitors for Treating Acute Myelogenous Leukemia.

TBA
57
Discovery of 4

TBA
15
Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer.

Nankai University
17
-Benzyl/Aryl Substituted Tryptanthrin as Dual Inhibitors of Indoleamine 2,3-Dioxygenase and Tryptophan 2,3-Dioxygenase.

Fudan University
40
Discovery of Pyrrolo[3,2- d]pyrimidin-4-one Derivatives as a New Class of Potent and Cell-Active Inhibitors of P300/CBP-Associated Factor Bromodomain.

Sichuan University
1
Synthesis and bioevaluation of diarylpyrazoles as antiproliferative agents.

Shenyang Pharmaceutical University
1
Discovery of 1,8-disubstituted-[1,2,3]triazolo[4,5-c]quinoline derivatives as a new class of Hippo signaling pathway inhibitors.

Sichuan University
3
Structure-Based Discovery of Novel Cyclophilin A Inhibitors for the Treatment of Hepatitis C Virus Infections.

Chonnam National University
8
Phenolic 4-hydroxy and 3,5-dihydroxy derivatives of 3-phenoxyquinoxalin-2(1H)-one as potent aldose reductase inhibitors with antioxidant activity.

Beijing Institute of Technology
13
Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer.

Qilu Pharmaceutical
14
Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.

Fudan University
1
Discovery of RG7834: The First-in-Class Selective and Orally Available Small Molecule Hepatitis B Virus Expression Inhibitor with Novel Mechanism of Action.

TBA
34
Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model.

Sichuan University/Collaborative Innovation Center of Biotherapy
1
Design, synthesis, and biological evaluation of polo-like kinase 1/eukaryotic elongation factor 2 kinase (PLK1/EEF2K) dual inhibitors for regulating breast cancer cells apoptosis and autophagy.

Sichuan University
13
Design, synthesis and evaluation of novel N-phenylbutanamide derivatives as KCNQ openers for the treatment of epilepsy.

Nanjing University of Technology
1
High anticancer potency on tumor cells of dehydroabietylamine Schiff-base derivatives and a copper(II) complex.

Nanjing Forestry University
2
Design, synthesis and structure-activity relationship studies of a focused library of pyrimidine moiety with anti-proliferative and anti-metastasis activities in triple negative breast cancer.

Shenyang Pharmaceutical University
5
Design, synthesis and evaluation of substituted piperidine based KCNQ openers as novel antiepileptic agents.

Nanjing University of Technology
3
Discovery of a highly potent, selective and novel CDK9 inhibitor as an anticancer drug candidate.

Nankai University
19
Discovery of potent and selective CDK8 inhibitors through FBDD approach.

Roche Innovation Center Shanghai
19
Design, synthesis and bioactivities of Celecoxib analogues or derivatives.

Chongqing Normal University
44
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer.

Nankai University
21
Highly Selective, Potent, and Oral mTOR Inhibitor for Treatment of Cancer as Autophagy Inducer.

Nankai University
2
TRKA (G667C) AND FLT3 TARGET INHIBITOR AND COMBINATION OF SAME WITH CHIDAMIDE

Shenzhen Chipscreen Biosciences
6
Indoline-1-formamide compound, preparation method therefor, and medical use thereof

Beijing Innocare Pharma Tech
6
ACRYLAMIDE COMPOUNDS

NRG Therapeutics
390
7H-PYRROLO[2,3-D]PYRIMIDINES AND PREPARATION AND USES THEREOF

Biosplice Therapeutics
39
THERAPEUTIC ALKALOID COMPOUNDS

Sensorium Therapeutics
73
RET inhibitors, pharmaceutical compositions and uses thereof

Sunshine Lake Pharma
47
Psychedelics and the human receptorome.

University of Oklahoma
42
SMALL MOLECULE INHIBITORS OF BACTERIAL TOXINS

Artizan Biosciences
11
PYRAZOLE COMPOUND AND PREPARATION METHOD THEREFOR AND USE THEREOF

Sichuan Kelun-Biotech Biopharmaceutical
29
TRIAZINE COMPOUND AND COMPOSITION AND USE THEREOF

Beijing Findcure Biosciences
25
CDK7 SELECTIVE INHIBITORS AS ANTICANCER AGENTS

Jingrui Biopharma
156
2-arylsulfonamido-N-arylacetamide derivatized STAT3 inhibitors

University of Hawaii
124
Benzimidazole compounds and derivatives as EGFR inhibitors

Boehringer Ingelheim International
20
Isoxazolidines as RIPK1 inhibitors and use thereof

Genzyme
38
Disubstituted pyrazole compounds

Eli Lilly
2
Salts of TAM inhibitors

Incyte
13
Macrocylic compounds as ROS1 kinase inhibitors

Array Biopharma
1
Inhibitor of the mutated isocitrate dehydrogenase IDH1 R132H

Bayer
98
N-substituted benzamides and methods of use thereof

Genentech
133
Plasminogen activator inhibitor-1 inhibitors and methods of use thereof

University of Michigan
11
Carbonic anhydrase inhibitors: in vitro inhibition of a isoforms (hCA I, hCA II, bCA III, hCA IV) by flavonoids.

Ondokuz Mayis University
26
Bicyclic heteroaryl cycloalkyldiamine derivatives

Novartis
49
Cyclic amides

Hoffmann-La Roche
41
2-substituted-3-phenylpropionic acid derivatives and their use in the treatment of inflammatory bowel disease

Albireo
2
Pyrrolo[2,3-d]pyrimidine compounds

Zoetis Services
40
Pyridine compounds as sodium channel blockers

Purdue Pharma
6
Alicyclic[c] benzopyrone derivatives and uses thereof

Huazhong University of Science & Technology
25
Discovery and Structure Optimization of a Series of Isatin Derivatives as Mycobacterium tuberculosis Chorismate Mutase Inhibitors.

Birla Institute of Technology
80
Heterocyclic hydrazone compounds

Novartis
5
Probing the peripheral site of human butyrylcholinesterase.

Dalhousie University
13
Thiazololactam compound as ERK inhibitor and use thereof

D3 Bio (Wuxi)
3
Novel structure having antagonist actions at both the glycine site of the N-methyl-D-aspartate receptor and neuronal voltage-sensitive sodium channels: biochemical, electrophysiological, and behavioral characterization.

University of Colorado
16
Somatostatin and its receptor family.

Royal Victoria Hospital
14
Novel selective thiol inhibitors of neutral endopeptidase containing heterocycles at P'2 position.

R & D, Zambon Group
14
Biexponential kinetics of (R)-alpha-[3H]methylhistamine binding to the rat brain H3 histamine receptor.

Schering-Plough Research Institute