Discovery of AMG 853, a CRTH2 and DP dual antagonist

ACS Medicinal Chemistry Letters

Volumn 2, Issue 5, 2011, Pages 326-330

  Liu, Jiwen ^a   Li, An Rong ^a   Wang, Yingcai ^a   Johnson, Mike G ^a   Su, Yongli ^a   Shen, Wang ^a   Wang, Xuemei ^a   Lively, Sarah ^a   Brown, Matthew ^a   Lai, Sujen ^a   Gonzalez Lopez De Turiso, Felix ^a   Xu, Qingge ^a   Van Lengerich, Bettina ^a   Schmitt, Mike ^a   Fu, Zice ^a   Sun, Ying ^a   Lawlis, Shanna ^a   Seitz, Lisa ^a   Danao, Jay ^a   Wait, Jill ^a   Ye, Qiuping ^a   Tang, Hua Lucy ^a   Grillo, Mark ^a   Collins, Tassie L ^a   Sullivan, Timothy J ^a   Medina, Julio C ^a   more..

^a AMGEN INC   (United States)

Author keywords

AMG 853; antagonist; asthma; CRTH2 receptor; DP receptor; prostaglandin D2

Indexed keywords

4 HYDROXYPHENYLACETIC ACID; [2 [4 [4 (TERT BUTYLCARBAMOYL) 2 (2 CHLORO 4 CYCLOPROPYLPHENYL SULFONAMIDO)PHENOXY] 5 CHLORO 2 FLUOROPHENYL]ACETIC ACID]; AMG 009; AMIDE; ANILINE; ANTIASTHMATIC AGENT; CHEMOATTRACTANT RECEPTOR HOMOLOGOUS MOLECULE EXPRESSED ON TH2 CELL; G PROTEIN COUPLED RECEPTOR; PHENYLACETIC ACID DERIVATIVE; PROSTAGLANDIN D2; PROSTANOID D RECEPTOR; UNCLASSIFIED DRUG; VIDUPIPRANT;

ARTICLE; ASTHMA; DRUG ABSORPTION; DRUG ANTAGONISM; DRUG BIOAVAILABILITY; DRUG HYDROLYSIS; DRUG POTENCY; DRUG SYNTHESIS; HUMAN; IC 50; IN VIVO STUDY; NONHUMAN; PLASMA; PLASMA CLEARANCE; PRIORITY JOURNAL; RECEPTOR AFFINITY;

EID: 79956066242     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml1002234     Document Type: Article

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24. 50) was determined. The binding buffer contains either 0.5% BSA (buffer binding) or 50% human plasma (plasma binding).
25. b was determined using the Schild equation.
26. b using the Schild equation.
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