title: Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists.
abstract: Starting from a non-steroidal glucocorticoid agonist aryl pyrazole derivative, the NFkappaB agonist activity was optimised in an iterative process from pIC(50) 7.5 (for 7), to pIC(50) 10.1 (for 38E1). An explanation for the SAR observed based is presented along with a proposed docking of 38E1 into the active site of the glucocorticoid receptor.
authors: Medicines Research Centre, Respiratory CEDD, GlaxoSmithKline, Gunnels Wood Road, Stevenage SG1 2NY, United Kingdom.
authors: Keith
authors: K
authors: Biggadike
authors: Matilde
authors: M
authors: Caivano
authors: Margaret
authors: M
authors: Clackers
authors: Diane M
authors: DM
authors: Coe
authors: George W
authors: GW
authors: Hardy
authors: Davina
authors: D
authors: Humphreys
authors: Haydn T
authors: HT
authors: Jones
authors: David
authors: D
authors: House
authors: Annette
authors: A
authors: Miles-Williams
authors: Philip A
authors: PA
authors: Skone
authors: Iain
authors: I
authors: Uings
authors: Vicki
authors: V
authors: Weller
authors: Iain M
authors: IM
authors: McLay
authors: Simon J F
authors: SJ
authors: Macdonald
mesh_terms: D020134:Catalytic Domain; D002460:Cell Line; D003198:Computer Simulation; D006801:Humans; D007191:Indazoles / Q000737:chemistry; D016328:NF-kappa B / Q000378:metabolism; D011720:Pyrazoles / Q000737:chemistry*; D011965:Receptors, Glucocorticoid / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D007191:Indazoles; D016328:NF-kappa B; D011720:Pyrazoles; D011965:Receptors, Glucocorticoid