Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist.
Bioorg Med Chem Lett
; 21(1): 137-40, 2011 Jan 01.
Article
em En
| MEDLINE
| ID: mdl-21129964
ABSTRACT
High-throughput screening of 3.87 million compounds delivered a novel series of non-steroidal GR antagonists. Subsequent rounds of optimisation allowed progression from a non-selective ligand with a poor ADMET profile to an orally bioavailable, selective, stable, glucocorticoid receptor antagonist.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Receptores de Glucocorticoides
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2011
Tipo de documento:
Article
País de afiliação:
Reino Unido