title: Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
abstract: A series of quinazolinone-derived inhibitors of the CXCR3 receptor have been synthesized and their affinity for the receptor evaluated. Compounds were evaluated in a (125)I-IP10 displacement assay and in in vitro cell migration assays to IP10, ITAC, and MIG using human peripheral blood mononuclear cells.
authors: Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
authors: Michael
authors: M
authors: Johnson
authors: An-Rong
authors: AR
authors: Li
authors: Jiwen
authors: J
authors: Liu
authors: Zice
authors: Z
authors: Fu
authors: Liusheng
authors: L
authors: Zhu
authors: Shichang
authors: S
authors: Miao
authors: Xuemei
authors: X
authors: Wang
authors: Qingge
authors: Q
authors: Xu
authors: Alan
authors: A
authors: Huang
authors: Andrew
authors: A
authors: Marcus
authors: Feng
authors: F
authors: Xu
authors: Karen
authors: K
authors: Ebsworth
authors: Emmanuel
authors: E
authors: Sablan
authors: Jay
authors: J
authors: Danao
authors: Jeff
authors: J
authors: Kumer
authors: Dan
authors: D
authors: Dairaghi
authors: Chris
authors: C
authors: Lawrence
authors: Tim
authors: T
authors: Sullivan
authors: George
authors: G
authors: Tonn
authors: Thomas
authors: T
authors: Schall
authors: Tassie
authors: T
authors: Collins
authors: Julio
authors: J
authors: Medina
mesh_terms: D000818:Animals; D018929:Cell Culture Techniques; D002465:Cell Movement / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D036341:Intercellular Signaling Peptides and Proteins / Q000378:metabolism; D007457:Iodine Radioisotopes; D007963:Leukocytes, Mononuclear / Q000166:cytology / Q000378:metabolism; D051379:Mice; D008956:Models, Chemical; D009842:Oligopeptides / Q000378:metabolism; D052999:Quinazolinones / Q000138:chemical synthesis / Q000494:pharmacology*; D011869:Radioligand Assay; D054367:Receptors, CXCR3; D019707:Receptors, Chemokine / Q000037:antagonists & inhibitors*; D018121:Receptors, Cytokine / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: C515187:CXCR3 protein, human; C515188:Cxcr3 protein, mouse; C104577:IP10-Mig receptor; C519300:ITAC peptide; D036341:Intercellular Signaling Peptides and Proteins; D007457:Iodine Radioisotopes; D009842:Oligopeptides; D052999:Quinazolinones; D054367:Receptors, CXCR3; D019707:Receptors, Chemokine; D018121:Receptors, Cytokine