Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist

Bioorganic and Medicinal Chemistry Letters

Volumn 27, Issue 5, 2017, Pages 1186-1192

  Okumura, Yoshiyuki ^a   Yamagishi, Tatsuya ^b   Nukui, Seiji ^c   Nakao, Kazunari ^d  

^a AskAt Inc   (Japan)

^b RaQualia Pharma Inc   (Japan)

^c SYNEOS HEALTH   (United States)

^d MOCHIDA PHARMACEUTICAL CO   (Japan)

Author keywords

Autoimmune diseases; Cancer; Clinical candidate; EP4 receptor antagonist; Inflammation; Pain; Prostaglandin E2; Structure activity relationship (SAR)

Indexed keywords

AAT 008; GRAPIPRANT; PROSTAGLANDIN E RECEPTOR 4; PROSTAGLANDIN E RECEPTOR 4 ANTAGONIST; PROSTAGLANDIN RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG; AAT-008; BENZOIC ACID DERIVATIVE; NICOTINAMIDE;

ANALGESIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CHRONIC INFLAMMATORY PAIN; DRUG ANTAGONISM; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DOSE COMPARISON; DRUG PENETRATION; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; ELIMINATION HALF-LIFE; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IC50; IN VITRO STUDY; IN VIVO STUDY; INTRINSIC ACTIVITY; MALE; MECHANICAL HYPERALGESIA; METABOLIC STABILITY; NONHUMAN; PHYSICAL CHEMISTRY; RECEPTOR AFFINITY; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS; TIME TO MAXIMUM PLASMA CONCENTRATION; VOLUME OF DISTRIBUTION; ANALOGS AND DERIVATIVES; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DRUG DEVELOPMENT;

ANIMALS; BENZOATES; DRUG DISCOVERY; HUMANS; NIACINAMIDE; PROSTAGLANDIN ANTAGONISTS; RECEPTORS, PROSTAGLANDIN E, EP4 SUBTYPE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 85011307883     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2017.01.067     Document Type: Article

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