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Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 22, 2012, Pages 6974-6979

Discovery and characterization of AZD9272 and AZD6538 - Two novel mGluR5 negative allosteric modulators selected for clinical development

(18) Raboisson, Patrick a Breitholtz Emanuelsson, Anna a Dahllöf, Henrik a Edwards, Louise b Heaton, William L c Isaac, Methvin b Jarvie, Keith b Kers, Annika a Minidis, Alexander B E a Nordmark, Anna a Sheehan, Susan M c Slassi, Abdelmalik b Ström, Peter a Terelius, Ylva a Wensbo, David a Wilson, Julie M b Xin, Tao b McLeod, Donald A c

a ASTRAZENECA R AND D (Sweden)

b NPS Pharmaceuticals (Canada)

c NPS Pharmaceutical Inc (United States)

Author keywords

Clinical candidate; GPCR; In vitro pharmacology; mGluR5; Negative allosteric modulator; Pain

Indexed keywords

AZD 6538; AZD 9272; IONOTROPIC RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BINDING SITE; DRUG BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; HIGH THROUGHPUT SCREENING; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; RAT;

ALLOSTERIC REGULATION; ANIMALS; BINDING SITES; CENTRAL NERVOUS SYSTEM; DRUG EVALUATION, PRECLINICAL; HALF-LIFE; HEK293 CELLS; HUMANS; ISOTOPE LABELING; MALE; MICROSOMES; OXADIAZOLES; PYRIDINES; RATS; RECEPTOR, METABOTROPIC GLUTAMATE 5; RECEPTORS, METABOTROPIC GLUTAMATE; STRUCTURE-ACTIVITY RELATIONSHIP;

RATTUS;

EID: 84867865129 PISSN: 0960894X EISSN: 14643405 Source Type: Journal
DOI: 10.1016/j.bmcl.2012.08.100 Document Type: Article

Times cited : (31)

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