PMID

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Article Title

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New inhibitors of the thioredoxin-thioredoxin reductase system based on a naphthoquinone spiroketal natural product lead.

University of Pittsburgh

Optimization of pyrazole-containing 1,2,4-triazolo-[3,4-b]thiadiazines, a new class of STAT3 pathway inhibitors.

University of Pittsburgh

Structure-Activity Study of Bioisosteric Trifluoromethyl and Pentafluorosulfanyl Indole Inhibitors of the AAA ATPase p97.

University of Pittsburgh

Design and evaluation of novel glutaminase inhibitors.

University of Pittsburgh

2-Guanidinoquinazolines as new inhibitors of the STAT3 pathway.

University of Pittsburgh

Synthesis and biological evaluation of 3-aminoisoquinolin-1(2H)-one based inhibitors of the dual-specificity phosphatase Cdc25B.

University of Pittsburgh

Ensemble-based virtual screening for cannabinoid-like potentiators of the human glycine receptora1 for the treatment of pain.

University of Pittsburgh

Contributions of academic laboratories to the discovery and development of chemical biology tools.

University of Pittsburgh

Benzimidazole-2-one: a novel anchoring principle for antagonizing p53-Mdm2.

University of Pittsburgh

Trisubstituted Sulfonamides: a New Chemotype for Development of Potent and Selective CB

University of Pittsburgh

Novel triaryl sulfonamide derivatives as selective cannabinoid receptor 2 inverse agonists and osteoclast inhibitors: discovery, optimization, and biological evaluation.

University of Pittsburgh

Lead discovery, chemistry optimization, and biological evaluation studies of novel biamide derivatives as CB2 receptor inverse agonists and osteoclast inhibitors.

University of Pittsburgh

Synthesis and Structure-Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D.

University of Pittsburgh

Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.

University of Pittsburgh

Synthesis and biological evaluation of purealin and analogues as cytoplasmic dynein heavy chain inhibitors.

University of Pittsburgh

Design and synthesis of non-peptide Ras CAAX mimetics as potent farnesyltransferase inhibitors.

University of Pittsburgh

Zebrafish chemical screening reveals an inhibitor of Dusp6 that expands cardiac cell lineages.

University of Pittsburgh

Biphenyl C-cyclopropylalkylamides: New scaffolds for targeting estrogen receptor beta.

University of Pittsburgh

Isosteric exchange of the acylsulfonamide moiety in Abbott's Bcl-XL protein interaction antagonist.

University of Pittsburgh

Small Molecule Inhibitors of Protein Kinase D: Early Development, Current Approaches, and Future Directions.

University of Pittsburgh

Synthesis of Veliparib Prodrugs and Determination of Drug-Release-Dependent PARP-1 Inhibition.

University of Pittsburgh

Structure-activity relationships of [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]- 3'-spiro-5' '-(4' '-amino-1' ',2' '-oxathiole-2' ',2' '-dioxide)thymine derivatives as inhibitors of HIV-1 reverse transcriptase dimerization.

University of Pittsburgh

Synthesis and evaluation of bifunctional PTP4A3 phosphatase inhibitors activating the ER stress pathway.

University of Pittsburgh

Synthesis and evaluation of 11C-labeled 6-substituted 2-arylbenzothiazoles as amyloid imaging agents.

University of Pittsburgh

Allosteric Indole Amide Inhibitors of p97: Identification of a Novel Probe of the Ubiquitin Pathway.

University of Pittsburgh

Synthesis and biological evaluation of structurally highly modified analogues of the antimitotic natural product curacin A.

University of Pittsburgh

Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatase Cdc25.

University of Pittsburgh

Sulfonylated aminothiazoles as new small molecule inhibitors of protein phosphatases.

University of Pittsburgh

Tapping the therapeutic potential of protein tyrosine phosphatase 4A with small molecule inhibitors.

University of Pittsburgh

Synthesis and Optimization of K

University of Pittsburgh

Small Molecule Antagonists of the Nuclear Androgen Receptor for the Treatment of Castration-Resistant Prostate Cancer.

University of Pittsburgh

Allosteric Modulation of Phosphatase Activity May Redefine Therapeutic Value.

University of Pittsburgh

GAC inhibitors with a 4-hydroxypiperidine spacer: Requirements for potency.

University of Pittsburgh

Structural Basis of TLR2/TLR1 Activation by the Synthetic Agonist Diprovocim.

University of Pittsburgh

Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox2) inhibitors.

University of Pittsburgh

Discovery of novel Myc-Max heterodimer disruptors with a three-dimensional pharmacophore model.

University of Pittsburgh

Covalent Modifiers: A Chemical Perspective on the Reactivity ofα,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions.

University of Pittsburgh

Ketone inhibitors of lysine gingipain

Cortexyme

Organosilicon carriers for use in treating infections and/or diseases caused by SARS viruses

Individual

Pyrazolo[3,4-b]pyridine compounds as inhibitors of TAM and MET kinases

Array Biopharma

CGRP receptor antagonists

Heptares Therapeutics

Compounds for cancer chemotherapeutic sensitization

Regents of The University of Minnesota

Imidazopyrazines and pyrazolopyrimidines and their use as AMPA receptor modulators

Janssen Pharmaceutica

Substituted prolines/piperidines as orexin receptor antagonists

Eolas Therapeutics

COMPOUNDS USEFUL AS T CELL ACTIVATORS

Gossamer Bio Services

Hydroxmethyl piperidine orexin receptor antagonists

Merck Sharp & Dohme

Pyrazolo pyrimidine derivatives and their use as MALT1 inhibitors

Novartis

Chemically modified quinoline and quinolone derivatives useful as CB-1 inverse agonists

Janssen Pharmaceutica

2-aryl selenazole compound and pharmaceutical composition thereof

Jiangsu Atom Bioscience and Pharmaceutical

Bicyclic heterocycles as FGFR4 inhibitors

Incyte

Pyrimidine compounds as mTOR and PI3K inhibitors

Development Center For Biotechnology

Quinoline derivatives as PDE10A enzyme inhibitors

H. Lundbeck

Pyridinyl and fused pyridinyl triazolone derivatives

Takeda Pharmaceutical

Compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders

Galapagos

Kinase inhibitors

Respivert

Aryl, heteroaryl, and heterocyclic compounds for treatment of complement mediated disorders

Achillion Pharmaceuticals

Pyridopyrimidine or pyrimidopyrimidine compound, prepration method, pharmaceutical composition, and use thereof

Shandong Luoxin Pharmaceutical Group Stock

Method of treatment using substituted imidazo[1,2b]pyridazine compounds

Array Biopharma

Imidazole-derived modulators of the glucocorticoid receptor

Bristol-Myers Squibb

Selective inhibitors of Tec and Src protein kinase families

Pharmascience

Pyrrolo [2,3-B] pyridine CDK9 kinase inhibitors

Abbvie

2-aminopyridine-based selective neuronal nitric oxide synthase inhibitors

Northwestern University

Substituted 4,5,6,7-tetrahydropyrazolo[4,3-c]pyridines as factor XIa inhibitors

Bristol-Myers Squibb

Heterocyclic amide derivatives as P2X7 receptor antagonists

Actelion Pharmaceuticals

Heterocyclic oxime compounds

Novartis

Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor.

Wyeth Research

Development of GlcNAc-inspired iminocyclitiols as potent and selective N-acetyl-beta-hexosaminidase inhibitors.

Academia Sinica

Optimization of 2,3,5-trisubstituted pyridine derivatives as potent allosteric Akt1 and Akt2 inhibitors.

Merck Research Laboratories

Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.

Novartis Pharmaceuticals

Synthesis of beta-ketophosphonate analogs of glutamyl and glutaminyl adenylate, and selective inhibition of the corresponding bacterial aminoacyl-tRNA synthetases.

Crefsip

Binding thermodynamics of substituted diaminopyrimidine renin inhibitors.

Pfizer

Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors.

Pfizer

Crystal structures of prostaglandin D(2) 11-ketoreductase (AKR1C3) in complex with the nonsteroidal anti-inflammatory drugs flufenamic acid and indomethacin.

The University of Birmingham

Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids.

Abbott Laboratories

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

Abbott Laboratories

Structure-activity based study of the Smac-binding pocket within the BIR3 domain of XIAP.

Princeton University

Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives.

Abbott Laboratories

Pyridone derivatives as potent, orally bioavailable VLA-4 integrin antagonists.

Glaxosmithkline

Carbonic anhydrase inhibitors. Inhibition of mitochondrial isozyme V with aromatic and heterocyclic sulfonamides.

Universita Degli Studi Di Firenze

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 alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV.

Takeda Pharmaceutical

Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 (beta-secretase).

University of Illinois At Chicago

Design, synthesis, and X-ray structure of potent memapsin 2 (beta-secretase) inhibitors with isophthalamide derivatives as the P2-P3-ligands.

Purdue University

2-(S)-phenethylaminothiazolones as potent, orally efficacious inhibitors of 11beta-hydroxysteriod dehydrogenase type 1.

Amgen

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

Factorizing selectivity determinants of inhibitor binding toward aldose and aldehyde reductases: structural and thermodynamic properties of the aldose reductase mutant Leu300Pro-fidarestat complex.

Institute of Genetics and Molecular and Cellular Biology (Igbmc)