Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.

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Thompson CF, Quraishi N, Ali A, Tata JR, Hammond ML, Balkovec JM, Einstein M, Ge L, Harris G, Kelly TM, Mazur P, Pandit S, Santoro J, Sitlani A, Wang C, Williamson J, Miller DK, Yamin TT, Thompson CM, O'Neill EA, Zaller D, Forrest MJ, Carballo-Jane E, Luell S

Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.

Bioorg Med Chem Lett. 2005 Apr 15;15(8):2163-7.

PubMed ID

15808489 [ View in PubMed

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Abstract

A series of novel ligands for the glucocorticoid receptor containing two heterocycles were synthesized. These compounds were investigated for a dissociative profile using transrepression and transactivation assays. Several compounds were tested in vivo and showed the ability to reduce inflammation in a mouse.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Prednisolone	Glucocorticoid receptor	IC 50 (nM)	13.8	N/A	N/A	Details
Prednisolone	Glucocorticoid receptor	EC 50 (nM)	4.5	N/A	N/A	Details
Prednisolone	Glucocorticoid receptor	EC 50 (nM)	24	N/A	N/A	Details