Discovery and optimization of CRTH2 and DP dual antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 22, 2009, Pages 6419-6423

  Liu, Jiwen ^a   Fu, Zice ^a   Wang, Yingcai ^a   Schmitt, Mike ^a   Huang, Alan ^a   Marshall, Derek ^a   Tonn, George ^a   Seitz, Lisa ^a   Sullivan, Tim ^a   Lucy Tang, H ^a   Collins, Tassie ^a   Medina, Julio ^a  

^a AMGEN INC   (United States)

Author keywords

Antagonists; Asthma; CRTH2; DP; GPCR; PGD2

Indexed keywords

AMG 009; PHENYLACETIC ACID DERIVATIVE; PROSTAGLANDIN INHIBITOR; UNCLASSIFIED DRUG;

AIRWAY OBSTRUCTION; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; ASTHMA; CONTROLLED STUDY; DOSE RESPONSE; DRUG EFFICACY; DRUG STRUCTURE; DRUG SYNTHESIS; HYDROGEN BOND; IC 50; IMMUNOPATHOLOGY; IN VIVO STUDY; NONHUMAN;

ANIMALS; ASTHMA; DRUG DESIGN; HUMANS; RECEPTORS, PROSTAGLANDIN; STRUCTURE-ACTIVITY RELATIONSHIP; TH2 CELLS;

EID: 71049187691     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.09.052     Document Type: Article

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35. 50) was determined. The binding buffer contains either 0.5% BSA (buffer binding) or 50% human plasma (plasma binding).
36. 50 of the compounds determined. The migration buffer contains 0.5% BSA.
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38. i using Schild equation.
39. i was 44 μM.
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42. 2.
43. 2 displacement assay was done in the same way as in Ref. 35 using 293 cells stably expressing guinea pig CRTH2.
44. i using Schild equation.