Dataset Information

Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia.

ABSTRACT: Herein, we report the structure-activity relationship of a novel series of (2(phenoxymethyl)-6,7-dihydrooxazolo[5,4-c]pyridine-5(4H)-yl(aryl)methanones as potent, selective, and orally bioavailable metabotropic glutamate receptor subtype 5 (mGlu5) positive allosteric modulators (PAMs). On the basis of its robust in vitro potency and in vivo efficacy in multiple preclinical models of multiple domains of schizophrenia, coupled with a good DMPK profile and an acceptable therapeutic window, 17a (VU0409551/JNJ-46778212) was selected as a candidate for further development.

SUBMITTER: Conde-Ceide S

PROVIDER: S-EPMC4492464 | biostudies-literature | 2015 Jun

REPOSITORIES: biostudies-literature

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Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia.

Conde-Ceide Susana S Martínez-Viturro Carlos M CM Alcázar Jesús J Garcia-Barrantes Pedro M PM Lavreysen Hilde H Mackie Claire C Vinson Paige N PN Rook Jerri M JM Bridges Thomas M TM Daniels J Scott JS Megens Anton A Langlois Xavier X Drinkenburg Wilhelmus H WH Ahnaou Abdellah A Niswender Colleen M CM Jones Carrie K CK Macdonald Gregor J GJ Steckler Thomas T Conn P Jeffrey PJ Stauffer Shaun R SR Bartolomé-Nebreda José Manuel JM Lindsley Craig W CW

ACS medicinal chemistry letters 20150520 6

Herein, we report the structure-activity relationship of a novel series of (2(phenoxymethyl)-6,7-dihydrooxazolo[5,4-c]pyridine-5(4H)-yl(aryl)methanones as potent, selective, and orally bioavailable metabotropic glutamate receptor subtype 5 (mGlu5) positive allosteric modulators (PAMs). On the basis of its robust in vitro potency and in vivo efficacy in multiple preclinical models of multiple domains of schizophrenia, coupled with a good DMPK profile and an acceptable therapeutic window, 17a (VU0 ...[more]

PMID: 26157544

Dataset Information

Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia.

Publications

Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia.

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