RESUMO
Following the identification of a potent IRAK inhibitor through routine project cross screening, a novel class of IRAK-4 inhibitor was established. The SAR of imidazo[1,2-a]pyridino-pyridines and benzimidazolo-pyridines was explored.
Assuntos
Quinases Associadas a Receptores de Interleucina-1/antagonistas & inibidores , Inibidores de Proteínas Quinases/farmacologia , Piridinas/farmacologia , Avaliação Pré-Clínica de Medicamentos , Estrutura Molecular , Inibidores de Proteínas Quinases/síntese química , Inibidores de Proteínas Quinases/química , Piridinas/síntese química , Piridinas/química , Estereoisomerismo , Relação Estrutura-AtividadeRESUMO
Over the past few years, high content screening has firmly established itself as a high-throughput technology for the analysis of microscopy-based cellular assays. In particular, it has opened new areas of cell biology for the large-scale analysis of cellular phenotypes and has enabled the application of increasingly sophisticated assays for large-scale genetic and compound screening, benefiting both the academic and pharmaceutical research environment.
Assuntos
Bioensaio , Desenho de Fármacos , Avaliação Pré-Clínica de Medicamentos/métodos , Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos , Interferência de RNA , Receptores Acoplados a Proteínas G/efeitos dos fármacosRESUMO
High-content analysis (HCA) has rapidly established itself as a core technology in drug discovery for secondary cell-based screening. When combined with our knowledge of genetics, HCA can provide a powerful tool for target validation, but excitingly, HCA may also enable the increased use of cellular assays in high-throughput screening for novel drug leads.