PMID

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Article Title

Organization

High-Potency Phenylquinoxalinone Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Activators.

University of California

Nanomolar-Potency Aminophenyl-1,3,5-triazine Activators of the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Chloride Channel for Prosecretory Therapy of Dry Eye Diseases.

University of California

Synthesis and structure-activity relationship of aminoarylthiazole derivatives as correctors of the chloride transport defect in cystic fibrosis.

Istituto Giannina Gaslini

Flavones: an important scaffold for medicinal chemistry.

Punjabi University

¿F508-CFTR correctors: synthesis and evaluation of thiazole-tethered imidazolones, oxazoles, oxadiazoles, and thiadiazoles.

Wuhan University of Science and Technology

Discovery of N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide (VX-770, ivacaftor), a potent and orally bioavailable CFTR potentiator.

Vertex Pharmaceuticals

Discovery heralds new approach to the treatment of cystic fibrosis.

Jl3Pharma

A new 9-alkyladenine-cyclic methylglyoxal diadduct activates wt- and F508del-cystic fibrosis transmembrane conductance regulator (CFTR) in vitro and in vivo.

Universit£

ABSOLUTE CONFIGURATION AND BIOLOGICAL PROPERTIES OF ENANTIOMERS OF CFTR INHIBITOR BPO-27.

University of California

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

University of Oxford

Potent, metabolically stable benzopyrimido-pyrrolo-oxazine-dione (BPO) CFTR inhibitors for polycystic kidney disease.

University of California

An expeditious access to 5-pyrimidinol derivatives from cyclic methylglyoxal diadducts, formation of argpyrimidines under physiological conditions and discovery of new CFTR inhibitors.

University Joseph Fourier-Grenoble 1/Cnrs

Nanomolar potency pyrimido-pyrrolo-quinoxalinedione CFTR inhibitor reduces cyst size in a polycystic kidney disease model.

University of California

Thiazolidinone CFTR inhibitors with improved water solubility identified by structure-activity analysis.

University of California

Rational design of the first small-molecule antagonists of NHERF1/EBP50 PDZ domains.

St. Jude Children'S Research Hospital

Novel CFTR Modulators for Treating Cystic Fibrosis.

Smith, Gambrell & Russell

Novel Substituted Cyclopropyl Compounds as CFTR Modulators for Treating Cystic Fibrosis.

Smith, Gambrell & Russell

Discovery and SAR of 4-aminopyrrolidine-2-carboxylic acid correctors of CFTR for the treatment of cystic fibrosis.

Abbvie

Discovery of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid diamides that increase CFTR mediated chloride transport.

Genzyme

Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.

Central South University

Discovery of Icenticaftor (QBW251), a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease.

Novartis Institutes For Biomedical Research

Synthesis, SAR, crystal structure, and biological evaluation of benzoquinoliziniums as activators of wild-type and mutant cystic fibrosis transmembrane conductance regulator channels.

Université

In silico drug repositioning on F508del-CFTR: A proof-of-concept study on the AIFA library.

National Research Council (Itb-Cnr)

Novel CFTR Modulators for Treating Cystic Fibrosis.

Smith, Gambrell & Russell

Discovery of GLPG2451, a Novel Once Daily Potentiator for the Treatment of Cystic Fibrosis.

Galapagos

Targeting different binding sites in the CFTR structures allows to synergistically potentiate channel activity.

Universit£

Identification, Structure-Activity Relationship, and Biological Characterization of 2,3,4,5-Tetrahydro-1

D3-Pharmachemistry

Discovery of novel VX-809 hybrid derivatives as F508del-CFTR correctors by molecular modeling, chemical synthesis and biological assays.

University of Genoa

Synthesis and biological evaluation of thiazole derivatives on basic defects underlying cystic fibrosis.

Rccs Istituto Giannina Gaslini

Targeting the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Protein for the Treatment of Cystic Fibrosis.

Therachem Research Medilab (India)

An overview on chemical structures as ?F508-CFTR correctors.

University of Palermo

Synthesis and biological activity of structurally diverse phthalazine derivatives: A systematic review.

Y. B. Chavan College of Pharmacy

Discovery of ABBV/GLPG-3221, a Potent Corrector of CFTR for the Treatment of Cystic Fibrosis.

Abbvie

Novel Hits in the Correction of ?F508-Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Protein: Synthesis, Pharmacological, and ADME Evaluation of Tetrahydropyrido[4,3-d]pyrimidines for the Potential Treatment of Cystic Fibrosis.

Siena Biotech

Constrained bithiazoles: small molecule correctors of defective ?F508-CFTR protein trafficking.

University of California

Click-based synthesis of triazolobithiazole ?F508-CFTR correctors for cystic fibrosis.

University of California Davis

Structure-activity relationships of cyanoquinolines with corrector-potentiator activity in ?F508 cystic fibrosis transmembrane conductance regulator protein.

University of California Davis

Fluorinated ?F508-CFTR correctors and potentiators for PET imaging.

University of California Davis

Pyrazolylthiazole as DeltaF508-cystic fibrosis transmembrane conductance regulator correctors with improved hydrophilicity compared to bithiazoles.

University of California Davis

4'-Methyl-4,5'-bithiazole-based correctors of defective delta F508-CFTR cellular processing.

University of California

Asperidines A-C, pyrrolidine and piperidine derivatives from the soil-derived fungus Aspergillus sclerotiorum PSU-RSPG178.

Prince of Songkla University

Modulators of the Cystic Fibrosis Transmembrane Conductance Regulator Protein.

Usona Institute

Synthesis and biological evaluation of novel thiazole- VX-809 hybrid derivatives as F508del correctors by QSAR-based filtering tools.

University of Genoa

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

University of California

Acyclic, orally bioavailable ketone-based cathepsin K inhibitors.

Gsk

Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity.

Methylgene

Design and Synthesis of Classical and Nonclassical 6-Arylthio-2,4-diamino-5-ethylpyrrolo[2,3-d]pyrimidines as Antifolates.

Duquesne University

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

Bristol-Myers Squibb Pharmaceutical Research Institute

L-687,908, a potent hydroxyethylene-containing HIV protease inhibitor.

Merck Research Laboratories