Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action

Olivier René, Benjamin P. Fauber, Gladys de Leon Boenig, +13

ACS Medicinal Chemistry Letters

Rorc AgonistsMinor Structural ChangePharmacotherapyChemistryChemical Biology +17

The discovery of RPR 200765A, a p38 MAP kinase inhibitor displaying a good oral anti-arthritic efficacy

Iain M. McLay, Frank Halley, John E. Souness, +23

Bioorganic & Medicinal Chemistry

Rheumatoid DisorderRheumatologyAnti-inflammatoryMedicineOsteoarthritis +6

Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc

Benjamin P. Fauber, Gladys de Leon Boenig, Brenda Burton, +11

Bioorganic & Medicinal Chemistry Letters

Fluorous SynthesisStructure-based DesignMolecule-based MaterialChemistry

Reduction in lipophilicity improved the solubility, plasma–protein binding, and permeability of tertiary sulfonamide RORc inverse agonists

Benjamin P. Fauber, Olivier René, Gladys de Leon Boenig, +14

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyPharmaceutical ScienceProteinlipid InteractionBiochemistryMedicine +9

Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479

Kirk Robarge, Wendy Lee, Charles Eigenbrot, +14

Bioorganic & Medicinal Chemistry Letters

Combinatorial ChemistryMedicinal ChemistryBiochemistryNatural SciencesMedicine +7

Discovery of Novel Allosteric Mitogen-Activated Protein Kinase Kinase (MEK) 1,2 Inhibitors Possessing Bidentate Ser212 Interactions

Robert A. Heald, Philip S. Jackson, Pascal Savy, +15

Journal of Medicinal Chemistry

Drug TargetEngineeringBidentate Ser212 InteractionsMedicinal ChemistrySignaling Pathway +14

Identification of tertiary sulfonamides as RORc inverse agonists

Benjamin P. Fauber, Olivier René, Brenda Burton, +8

Bioorganic & Medicinal Chemistry Letters

Tertiary SulfonamidesMedicinal ChemistryBiochemistryNatural SciencesMedicine +6

Mitigation of Acetylcholine Esterase Activity in the 1,7-Diazacarbazole Series of Inhibitors of Checkpoint Kinase 1

Lewis Gazzard, Karen Williams, Huifen Chen, +29

Journal of Medicinal Chemistry

Ache ActivityDrug TargetPharmacotherapyChemical BiologyPharmaceutical Chemistry +14

Discovery of LRRK2 inhibitors by using an ensemble of virtual screening methods

Emanuela Gancia, Marcel de Groot, Brenda Burton, +1

Bioorganic & Medicinal Chemistry Letters

5-Aminopyrimidin-2-ylnitriles as Cathepsin K inhibitors

Andrew Morley, Peter W. Kenny, Brenda Burton, +9

Bioorganic & Medicinal Chemistry Letters

Cathepsin K InhibitorsMedicinal ChemistryBiochemistryMedicineNatural Sciences +7