PMID
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Article Title
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43
Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors.

National Institute On Drug Abuse
38
Discovery and structure activity relationship study of novel indazole amide inhibitors for extracellular signal-regulated kinase1/2 (ERK1/2).

Green Valley Research Institute
21
Novel leucine ureido derivatives as aminopeptidase N inhibitors. Design, synthesis and activity evaluation.

Fudan University
15
Discovery of EBI-907: A highly potent and orally active B-Raf(V600E) inhibitor for the treatment of melanoma and associated cancers.

Shanghai Hengrui Pharmaceutical
29
Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.

Genentech
41
Design, Synthesis, and Structure-Activity Relationships of Pyridine-Based Rho Kinase (ROCK) Inhibitors.

Vertex Pharmaceuticals
7
Chiral Resolution and Serendipitous Fluorination Reaction for the Selective Dopamine D3 Receptor Antagonist BAK2-66.

National Institute On Drug Abuse-Intramural Research Program
13
Design, synthesis and biological evaluation of novel tripeptidyl epoxyketone derivatives constructed fromß-amino acid as proteasome inhibitors.

Zhejiang University
15
Novelß-dicarbonyl derivatives as inhibitors of aminopeptidase N (APN).

Shandong University
22
Novel leucine ureido derivatives as inhibitors of aminopeptidase N (APN).

Shandong University
32
Development of Synthetic Aminopeptidase N/CD13 Inhibitors to Overcome Cancer Metastasis and Angiogenesis.

TBA
13
Molecular determinants of selectivity and efficacy at the dopamine D3 receptor.

National Institute On Drug Abuse-Intramural Research Program
32
Discovery of oxazole-based PDE4 inhibitors with picomolar potency.

Merck Research Laboratories
23
Structure-Activity Relationships at the Monoamine Transporters for a Novel Series of Modafinil (2-[(diphenylmethyl)sulfinyl]acetamide) Analogues.

National Institute On Drug Abuse-Intramural Research Program
20
Dual DAT/sigma1 receptor ligands based on 3-(4-(3-(bis(4-fluorophenyl)amino)propyl)piperazin-1-yl)-1-phenylpropan-1-ol.

National Institute On Drug Abuse-Intramural Research Program
2
Metabolism and pharmacokinetics of a novel Src kinase inhibitor TG100435 ([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine) and its active N-oxide metabolite TG100855 ([7-(2,6-dichloro-phenyl)-5-methylbenzo[1,2,4]triazin-3-yl]-{4-[2-(1-oxy-pyrr

Targegen
9
Development of prodrug 4-chloro-3-(5-methyl-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}-1,2,4-benzotriazin-7-yl)phenyl benzoate (TG100801): a topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degeneration.

Targegen
52
Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays.

Targegen
18
Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation.

National Institute On Drug Abuse-Intramural Research Program
24
Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents.

Nida-Irp
8
[3-cis-3,5-Dimethyl-(1-piperazinyl)alkyl]-bis-(4'-fluorophenyl)amine analogues as novel probes for the dopamine transporter.

National Institute On Drug Abuse-Intramural Research Program
25
3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists.

Merck Research Laboratories
11
Design and synthesis of substituted N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides as positive allosteric modulators of the metabotropic glutamate receptor subtype 5.

National Institute On Drug Abuse-Intramural Research Program
49
Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.

Vertex Pharmaceuticals
40
Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists.

National Institute On Drug Abuse-Intramural Research Program
31
Modifications to 1-(4-(2-Bis(4-fluorophenyl)methyl)sulfinyl)alkyl Alicyclic Amines That Improve Metabolic Stability and Retain an Atypical DAT Inhibitor Profile.

National Institute on Drug Abuse - Intramural Research Program
26
The design and preliminary structure-activity relationship studies of benzotriazines as potent inhibitors of Abl and Abl-T315I enzymes.

Targegen
5
Discovery of LC-MI-3: A Potent and Orally Bioavailable Degrader of Interleukin-1 Receptor-Associated Kinase 4 for the Treatment of Inflammatory Diseases.

Hangzhou Medical College
23
Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.

National Institute On Drug Abuse-Intramural Research Program
36
Design, synthesis and evaluation of antitumor activity of selective PRMT6 inhibitors.

Sichuan University
11
Screening and optimization of phage display cyclic peptides against the WDR5 WBM site.

University of Chinese Academy of Sciences
9
Discovery of a Novel Covalent EZH2 Inhibitor Based on Tazemetostat Scaffold for the Treatment of Ovarian Cancer.

Sichuan University
6
Design, synthesis and biological evaluation of covalent peptidomimetic 3CL protease inhibitors containing nitrile moiety.

An Hui University of Traditional Chinese Medicine
5
Design and synthesis of a novel photoaffinity ligand for the dopamine and serotonin transporters based on 2beta-carbomethoxy-3beta-biphenyltropane.

National Institute On Drug Abuse-Intramural Research Program
45
Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.

Targegen
23
The synthesis of substituted bipiperidine amide compounds as CCR3 ligands: antagonists versus agonists.

Schering-Plough Research Institute
46
The synthesis of substituted bipiperidine amide compounds as CCR3 antagonists.

Schering-Plough Research Institute
39
Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor.

National Institute On Drug Abuse-Intramural Research Program
12
Novel azido and isothiocyanato analogues of [3-(4-phenylalkylpiperazin-1-yl)propyl]bis(4-fluorophenyl)amines as potential irreversible ligands for the dopamine transporter.

National Institute On Drug Abuse
51
Novel Dual-Target μ-Opioid Receptor and Dopamine D

National Institute On Drug Abuse-Intramural Research Program
7
Noncovalent CDK12/13 dual inhibitors-based PROTACs degrade CDK12-Cyclin K complex and induce synthetic lethality with PARP inhibitor.

Zhejiang University
27
Discovery of Novel, Orally Bioavailable Pyrimidine Ether-Based Inhibitors of ELOVL1.

Vertex Pharmaceuticals
25
Structure Activity Relationships for a Series of Eticlopride-Based Dopamine D

National Institute On Drug Abuse - Intramural Research Program
26
N-(4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl, butenyl and butynyl)arylcarboxamides as novel dopamine D(3) receptor antagonists.

National Institute On Drug Abuse-Intramural Research Program
5
Structure-based optimization identified novel furyl-containing 2,4-diarylaminopyrimidine analogues as ALK/ROS1 dual inhibitors with anti-mutation effects.

Shenyang Pharmaceutical University
3
Simultaneous Inhibition of SIRT2 Deacetylase and Defatty-Acylase Activities via a PROTAC Strategy.

Cornell University
43
Structure-activity relationships for a series of (Bis(4-fluorophenyl)methyl)sulfinylethyl-aminopiperidines and -piperidine amines at the dopamine transporter: Bioisosteric replacement of the piperazine improves metabolic stability.

National Institute On Drug Abuse - Intramural Research Program
29
Discovery of (

Hefei Institutes of Physical Science
30
Discovery of a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3Kγ Inhibitors.

Vertex Pharmaceuticals
12
Specific and dual antagonists of alpha(4)beta(1) and alpha(4)beta(7) integrins.

Merck Research Laboratories
31
Structure-Activity Relationships for a Series of (Bis(4-fluorophenyl)methyl)sulfinyl Alkyl Alicyclic Amines at the Dopamine Transporter: Functionalizing the Terminal Nitrogen Affects Affinity, Selectivity, and Metabolic Stability.

National Institute On Drug Abuse-Intramural Research Program
14
Novel Lysine-Based Thioureas as Mechanism-Based Inhibitors of Sirtuin 2 (SIRT2) with Anticancer Activity in a Colorectal Cancer Murine Model.

TBA
40
Leucine ureido derivatives as aminopeptidase N inhibitors using click chemistry. Part II.

Shandong University
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
44
Elucidation of structural elements for selectivity across monoamine transporters: novel 2-[(diphenylmethyl)sulfinyl]acetamide (modafinil) analogues.

National Institute On Drug Abuse-Intramural Research Program
41
The optimization of pyridazinone series of glucan synthase inhibitors.

Merck Research Laboratories
20
SAR studies of pyridazinone derivatives as novel glucan synthase inhibitors.

Merck Research Laboratories
35
The synthesis and structure-activity relationship of pyridazinones as glucan synthase inhibitors.

Merck Research Laboratories
24
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.

Vertex Pharmaceuticals
15
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.

Vertex Pharmaceuticals
15
Discovery of EBI-1051: A novel and orally efficacious MEK inhibitor with benzofuran scaffold.

Shanghai Hengrui Pharmaceutical
19
Design, Synthesis, and Biological Evaluation of the First c-Met/HDAC Inhibitors Based on Pyridazinone Derivatives.

Chinese Academy of Sciences
20
Discovery of a class of diheteroaromatic amines as orally bioavailable CDK1/4/6 inhibitors.

Shanghai Haihe Pharmaceutial
14
Design, synthesis and pharmacological evaluation of ALK and Hsp90 dual inhibitors bearing resorcinol and 2,4-diaminopyrimidine motifs.

Chinese Academy of Sciences
25
Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin's Lymphoma.

Shanghai Hengrui Pharmaceutical
42
Novel leucine ureido derivatives as aminopeptidase N inhibitors using click chemistry.

Shandong University
16
Design and Synthesis of a Novel Series of Orally Bioavailable, CNS-Penetrant, Isoform Selective Phosphoinositide 3-Kinaseγ (PI3Kγ) Inhibitors with Potential for the Treatment of Multiple Sclerosis (MS).

Vertex Pharmaceuticals
22
Structure-Activity Relationship Studies on a Series of 3α-[Bis(4-fluorophenyl)methoxy]tropanes and 3α-[Bis(4-fluorophenyl)methylamino]tropanes As Novel Atypical Dopamine Transporter (DAT) Inhibitors for the Treatment of Cocaine Use Disorders.

National Institute On Drug Abuse-Intramural Research Program
136
TRICYCLIC TRIAZOLO COMPOUNDS AS DGK INHIBITORS

Incyte
26
PTGR2 INHIBITORS AND THEIR USE

National Health Research Institutes
364
Bicyclic-fused heteroaryl or aryl compounds

Pfizer
7
Antibody-drug conjugates comprising a cyclic dinucleotide

Takeda Pharmaceutical
22
MAP4K1 INHIBITORS

Blueprint Medicines
51
Substituted Imidazo[1,2-a]-pyridines as IRAK 1/4 and FLT3 inhibitors

Children'S Hospital Medical Center
34
Compounds and their use for reducing uric acid levels

Acquist
145
Inhibiting agents for Bruton's tyrosine kinase

Biogen Ma
7
Treatment of conditions associated with hyperinsulinaemia

Tensha Therapeutics
32
Benzothiazole compounds and uses thereof

Incyte
33
Apoptosis signal-regulating kinase inhibitors

Gilead Sciences
841
Pyridyl substituted indole compounds

Bristol Myers Squibb
158
Imidazopyridines and imidazopyrazines as LSD1 inhibitors

Incyte
33
Dopamine D3 receptor antagonists having a morpholine moiety

Indivior
34
Acetyl-CoA carboxylase modulators

Monsanto Technology
214
Compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders

Galapagos
1
Discovery of a Novel Inhibitor of Coronavirus 3CL Protease as a Clinical Candidate for the Potential Treatment of COVID-19.

Pfizer
11
TRPA1 antagonists

Abbvie
29
Fluoroalkyl and fluorocycloalkyl 1,4-benzodiazepinone compounds

Bristol Myers Squibb
48
Pyridine derivatives

Hoffmann-La Roche
71
Substituted 4-aminocyclohexane derivatives

Gruenenthal
134
Triazolo compounds as PDE10 inhibitors

Hoffmann-La Roche
4
Compound for increasing kinase active and application thereof

Fujian Haixi Pharmaceuticals
2
Oxazetidine derivatives, process for preparing them and use in human medicine and in cosmetics

Galderma Research & Development
16
Novel N-hydroxybenzamides incorporating 2-oxoindoline with unexpected potent histone deacetylase inhibitory effects and antitumor cytotoxicity.

Hanoi University of Pharmacy
33
Substituted pyrazolo[3,4-d]pyrimidines as kinase inhibitors

Principia Biopharma
394
Amidopyrazole inhibitors of interleukin receptor-associated kinases

Merck Sharp & Dohme
16
Synthesis and anti-acetylcholinesterase activity of scopoletin derivatives.

Chulabhorn Research Institute
13
Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles.

Wyeth Research
55
Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.

Bristol Myers Squibb