PMID

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Article Title

Organization

Synthetic derivatives of aromatic abietane diterpenoids and their biological activities.

Universidad De Valencia

Discovery of biarylaminoquinazolines as novel tubulin polymerization inhibitors.

Universit£

Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.

Nerviano Medical Sciences

Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents.

Qilu Pharmaceutical

Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors.

Chinese Academy Of Sciences

Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: optimization of in vitro potencies and pharmacokinetic properties.

Development Center For Biotechnology

Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors.

Chinese Academy Of Sciences

Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors.

Astrazeneca

Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.

Takeda Pharmaceutical

Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis.

East China University Of Science And Technology

Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).

Exelixis

Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.

Hoffmann-La Roche

Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.

Pfizer

Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.

Pfizer

The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.

Exelixis

Protein-ligand crystal structures can guide the design of selective inhibitors of the FGFR tyrosine kinase.

Astrazeneca

Irreversible protein kinase inhibitors: balancing the benefits and risks.

Covalution Pharma

Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors.

Takeda Pharmaceutical

Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.

Cellzome

Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.

University Of Genoa

Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.

Exelixis

Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.

TBA

Design and synthesis of pyrrolo[3,2-d]pyrimidine HER2/EGFR dual inhibitors: improvement of the physicochemical and pharmacokinetic profiles for potent in vivo anti-tumor efficacy.

Takeda Pharmaceutical

Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors.

Chinese Academy Of Sciences

Design and synthesis of pyrrolo[3,2-d]pyrimidine human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors: exploration of novel back-pocket binders.

Takeda Pharmaceutical

Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.

Hanmi Research Center

Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.

Amgen

Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.

Abbott Laboratories

Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c

Cephalon

Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.

Merck Research Laboratories

A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.

Nerviano Medical Sciences Oncology

Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase.

Chinese Academy Of Sciences

Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.

Glaxosmithkline

Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.

Nerviano Medical Sciences

A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences

Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.

National Cancer Institute-Bethesda

Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120).

Boehringer Ingelheim Pharma

Discovery and development of aurora kinase inhibitors as anticancer agents.

Vertex Pharmaceuticals

Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.

Harvard Medical School

Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.

Bristol-Myers Squibb

Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.

Bristol-Myers Squibb Research And Development

A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.

University Of Oxford

Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.

Abbott Laboratories

Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.

Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories

Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.

Hoffmann-La Roche

Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.

Astrazeneca

Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.

Novartis Pharma

7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.

Ludwig-Maximilians University Of Munich

Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905).

Millennium Pharmaceuticals

Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase.

Shenyang Pharmaceutical University

5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors.

Nerviano Medical Sciences

Novel and selective spiroindoline-based inhibitors of Sky kinase.

Pfizer

Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).

Ansaris

Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.

Takeda Pharmaceutical

1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.

RhôNe-Poulenc Rorer

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.

Novartis Institute For Biomedical Research

Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d]pyrimidine or furo[2,3-d]pyrimidine scaffold.

Chinese Academy Of Sciences

Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.

Bristol-Myers Squibb

Discovery and optimization of N-acyl and N-aroylpyrazolines as B-Raf kinase inhibitors.

Millennium Pharmaceuticals

Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.

Ariad Pharmaceuticals

Acenaphtho[1,2-b]pyrrole-based selective fibroblast growth factor receptors 1 (FGFR1) inhibitors: design, synthesis, and biological activity.

East China University Of Science And Technology

NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.

Nerviano Medical Sciences

Synthesis and c-Met kinase inhibition of 3,5-disubstituted and 3,5,7-trisubstituted quinolines: identification of 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7- (trifluoromethyl)quinoline as a novel anticancer agent.

Chinese Academy Of Sciences

Inhibitors of the tyrosine kinase EphB4. Part 4: Discovery and optimization of a benzylic alcohol series.

Astrazeneca

Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.

TBA

5-amino-pyrazoles as potent and selective p38a inhibitors.

Bristol-Myers Squibb Research And Development

Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.

Nerviano Medical Sciences

Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.

Nerviano Medical Sciences Oncology

N-phenyl-N'-[4-(5H-pyrrolo[3,2-d]pyrimidin-4-yloxy)phenyl]ureas as novel inhibitors of VEGFR and FGFR kinases.

Takeda Pharmaceutical

Design, synthesis, and evaluation of 5-methyl-4-phenoxy-5H-pyrrolo[3,2-d]pyrimidine derivatives: novel VEGFR2 kinase inhibitors binding to inactive kinase conformation.

Takeda Pharmaceutical

AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).

Ambit Biosciences

BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.

Boehringer Ingelheim Austria

Rational design of inhibitors that bind to inactive kinase conformations.

Novartis Research Foundation

Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.

Nerviano Medical Sciences

Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).

Wyeth Research

BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.

The Institute Of Cancer Research

Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.

Nerviano Medical Sciences

Discovery of novel fibroblast growth factor receptor 1 kinase inhibitors by structure-based virtual screening.

Yale University

2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.

Abbott Laboratories

Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.

Hanmi Research Center

Identification of death-associated protein kinases inhibitors using structure-based virtual screening.

Pharmadesign

 

A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation

TBA

Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors.

Novartis Institutes For Biomedical Research

5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases.

Mahidol University

Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity.

Astrazeneca R&D Boston

Beyond the MEK-pocket: can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK?

Pfizer

Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors.

Astrazeneca Pharmaceuticals

Naturally occurring homoisoflavonoids function as potent protein tyrosine kinase inhibitors by c-Src-based high-throughput screening.

Institute Of Materia Medica

Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.

Genomics Institute Of The Novartis Research Foundation

Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors.

New York University Medical Center

Entry into a new class of protein kinase inhibitors by pseudo ring design.

Novartis Institutes For Biomedical Research

Optimization of triarylimidazoles for Tie2: influence of conformation on potency.

Glaxosmithkline

Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.

Abbott Laboratories

Novel inhibitor for fibroblast growth factor receptor tyrosine kinase.

Mahidol University

Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.

Abbott Laboratories

Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.

Targegen

Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.

Bristol-Myers Squibb Pharmaceutical Research Institute

Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors.

Abbott Laboratories

Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases.

Chiron

Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.

Pharmaceutical Research Institute

Design and structure-activity relationship of heterocyclic analogs of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones as inhibitors of receptor tyrosine kinases.

Chiron

(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.

Johnson & Johnson Pharmaceutical Research And Development

Naphthofuroquinone derivatives: inhibition of receptor tyrosine kinases.

Korea Research Institute Of Chemical Technology

Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

A small molecule-kinase interaction map for clinical kinase inhibitors.

Ambit Biosciences

Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.

Bristol-Myers Squibb Pharmaceutical Research Institute

Design and synthesis of aminopropyl tetrahydroindole-based indolin-2-ones as selective and potent inhibitors of Src and Yes tyrosine kinase.

Sugen

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

Plant-derived flavones as inhibitors of aurora B kinase and their quantitative structure-activity relationships.

Konkuk University

Evidence for the preferential involvement of 5-HT2A serotonin receptors in stress- and drug-induced dopamine release in the rat medial prefrontal cortex.

Case Western Reserve University

N-[3H]methylscopolamine labeling of non-M1, non-M2 muscarinic receptor binding sites in rat brain.

University Of California

Structural requirements for the occupancy of pituitary adenylate-cyclase-activating-peptide (PACAP) receptors and adenylate cyclase activation in human neuroblastoma NB-OK-1 cell membranes. Discovery of PACAP(6-38) as a potent antagonist.

UniversitÉ

Human liver glycogen phosphorylase inhibitors bind at a new allosteric site.

Pfizer

Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.

Abbott Laboratories

Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs.

Genentech

Beta-secretase (BACE-1) inhibitors: accounting for 10s loop flexibility using rigid active sites.

Merck Research Laboratories

A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.

Pfizer

Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase b/akt inhibitors with reduced hypotension.

Abbott Laboratories

p38 MAP kinase inhibitors. Part 6: 2-arylpyridazin-3-ones as templates for inhibitor design.

Merck Research Laboratories

Quantitative evaluation of each catalytic subsite of cathepsin B for inhibitory activity based on inhibitory activity-binding mode relationship of epoxysuccinyl inhibitors by X-ray crystal structure analyses of complexes.

Osaka University Of Pharmaceutical Sciences

Discovery of 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications.

The Institute For Diabetes Discovery

A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one.

Pfizer

Structural and thermodynamic studies of simple aldose reductase-inhibitor complexes.

Medical College Of Wiscosin

Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1).

Merck Research Laboratories

Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: identification of candidates for clinical development.

Pfizer

The structure of dimeric ROCK I reveals the mechanism for ligand selectivity.

Vertex Pharmaceuticals

Discovery and structure-activity relationship of oxalylarylaminobenzoic acids as inhibitors of protein tyrosine phosphatase 1B.

Abbott Laboratories

Discovery of a potent, selective protein tyrosine phosphatase 1B inhibitor using a linked-fragment strategy.

Abbott Laboratories

Design and quantitative structure-activity relationship of 3-amidinobenzyl-1H-indole-2-carboxamides as potent, nonchiral, and selective inhibitors of blood coagulation factor Xa.

Aventis Pharma Deutschland

Conformation-assisted inhibition of protein-tyrosine phosphatase-1B elicits inhibitor selectivity over T-cell protein-tyrosine phosphatase.

Merck Frosst Center For Therapeutic Research

Discovery of novel heterocyclic factor VIIa inhibitors.

Celera

Discovery of adamantane ethers as inhibitors of 11beta-HSD-1: Synthesis and biological evaluation.

Abbott Laboratories

Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.

Ambit

Design, synthesis, and biological activity of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as potent and selective farnesyltransferase inhibitors.

Globe Pharmaceutical R And Abbott Laboratories

Synthesis, pharmacological evaluation, and molecular modeling studies of novel peptidic CAAX analogues as farnesyl-protein-transferase inhibitors.

Universita Di Napoli Federico Ii

Design, synthesis, and evaluation of a potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase (Smac) mimetic.

University Of Michigan

SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa.

Bristol-Myers Squibb

Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.

Bristol-Myers Squibb Pharmaceutical Research Institute

Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa.

Bristol-Myers Squibb

1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4-[(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Abbott Laboratories

Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]-4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.

Abbott Laboratories

Structure- and property-based design of factor Xa inhibitors: pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs.

Glaxosmithkline

Novel potent hepatitis C virus NS3 serine protease inhibitors derived from proline-based macrocycles.

Schering-Plough Research Institute

Fluoro-olefins as peptidomimetic inhibitors of dipeptidyl peptidases.

University Of Antwerp

Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.

National Health Research Institutes

Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors.

National Health Research Institutes

Design of Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase with Improved Drug Resistance Properties. 1.

University Of Oxford

Structural Insight into the Stereoselective Inhibition of MMP-8 by Enantiomeric Sulfonamide Phosphonates.

Istituto Di Cristallografia

Structure-based design of caspase-1 inhibitor containing a diphenyl ether sulfonamide.

Pfizer

Structure-based design of nonpeptide inhibitors of interleukin-1beta converting enzyme (ICE, caspase-1).

Pfizer

Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives.

Universidad Central De Venezuela

Inhibitors of the Diadenosine Tetraphosphate Phosphorylase Rv2613c of Mycobacterium tuberculosis.

University Of Konstanz

4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.

Palacky University

Fluoroaromatic-fluoroaromatic interactions between inhibitors bound in the crystal lattice of human carbonic anhydrase II.

University Of Pennsylvania

Selectively guanidinylated derivatives of neamine. Syntheses and inhibition of anthrax lethal factor protease.

Hawaii Biotech

Carbonic anhydrase inhibitors: stacking with Phe131 determines active site binding region of inhibitors as exemplified by the X-ray crystal structure of a membrane-impermeant antitumor sulfonamide complexed with isozyme II.

Istituto Di Biostrutture E Bioimmagini-Cnr

Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives.

University Of Agricultural Sciences And Veterinary Medicine

Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents.

Hoffmann-La Roche

The reversed binding of beta-phenethylamine inhibitors of DPP-IV: X-ray structures and properties of novel fragment and elaborated inhibitors.

Santhera Pharmaceuticals

Sultam hydroxamates as novel matrix metalloproteinase inhibitors.

Bristol-Myers Squibb

Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of potent and selective phenylalanine based dipeptidyl peptidase IV inhibitors.

Merck Research Laboratories

Crystal structure of human cyclin-dependent kinase 2 in complex with the adenine-derived inhibitor H717.

Lawrence Berkeley National Laboratory

Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR.

Vernalis (R&D)

Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2.

Vernalis (R&D)

Discovery of a series of hydroximic acid derivatives as potent histone deacetylase inhibitors.

Qingdao University

Cholinesterase inhibitors: xanthostigmine derivatives blocking the acetylcholinesterase-induced beta-amyloid aggregation.

University Of Bologna

Syntheses and anticholinesterase activities of (3aS)-N1, N8-bisnorphenserine, (3aS)-N1,N8-bisnorphysostigmine, their antipodal isomers, and other potential metabolites of phenserine.

University Of North Carolina At Chapel Hill

Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors.

Merck Frosst Canada

Reducing the peptidyl features of caspase-3 inhibitors: a structural analysis.

Merck Research Laboratories

Suzuki-type Pd(0) coupling reactions in the synthesis of 2-arylpurines as Cdk inhibitors.

Institut Curie

Docking-based development of purine-like inhibitors of cyclin-dependent kinase-2.

Palacky University

X-ray structures of Torpedo californica acetylcholinesterase complexed with (+)-huperzine A and (-)-huperzine B: structural evidence for an active site rearrangement.

Weizmann Institute Of Science

Kinetic and structural studies on the interaction of cholinesterases with the anti-Alzheimer drug rivastigmine.

Weizmann Institute Of Science

Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.

National Institutes Of Health

Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites.

Universita Di Siena