title: Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy.
abstract: Adenosine monophosphate-activated protein kinase (AMPK) is a protein kinase involved in maintaining energy homeostasis within cells. On the basis of human genetic association data, AMPK activators were pursued for the treatment of diabetic nephropathy. Identification of an indazole amide high throughput screening (HTS) hit followed by truncation to its minimal pharmacophore provided an indazole acid lead compound. Optimization of the core and aryl appendage improved oral absorption and culminated in the identification of indole acid, PF-06409577 (7). Compound 7 was advanced to first-in-human trials for the treatment of diabetic nephropathy.
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Kimberly O
authors.initials: KO
authors.lastname: Cameron
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Daniel W
authors.initials: DW
authors.lastname: Kung
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Amit S
authors.initials: AS
authors.lastname: Kalgutkar
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Ravi G
authors.initials: RG
authors.lastname: Kurumbail
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Russell
authors.initials: R
authors.lastname: Miller
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Christopher T
authors.initials: CT
authors.lastname: Salatto
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Jessica
authors.initials: J
authors.lastname: Ward
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Jane M
authors.initials: JM
authors.lastname: Withka
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Samit K
authors.initials: SK
authors.lastname: Bhattacharya
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Markus
authors.initials: M
authors.lastname: Boehm
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Kris A
authors.initials: KA
authors.lastname: Borzilleri
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Janice A
authors.initials: JA
authors.lastname: Brown
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Matthew
authors.initials: M
authors.lastname: Calabrese
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Nicole L
authors.initials: NL
authors.lastname: Caspers
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Emily
authors.initials: E
authors.lastname: Cokorinos
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Edward L
authors.initials: EL
authors.lastname: Conn
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Matthew S
authors.initials: MS
authors.lastname: Dowling
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: David J
authors.initials: DJ
authors.lastname: Edmonds
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Heather
authors.initials: H
authors.lastname: Eng
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Dilinie P
authors.initials: DP
authors.lastname: Fernando
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Richard
authors.initials: R
authors.lastname: Frisbie
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: David
authors.initials: D
authors.lastname: Hepworth
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: James
authors.initials: J
authors.lastname: Landro
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Yuxia
authors.initials: Y
authors.lastname: Mao
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Francis
authors.initials: F
authors.lastname: Rajamohan
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Allan R
authors.initials: AR
authors.lastname: Reyes
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Colin R
authors.initials: CR
authors.lastname: Rose
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Tim
authors.initials: T
authors.lastname: Ryder
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Andre
authors.initials: A
authors.lastname: Shavnya
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Aaron C
authors.initials: AC
authors.lastname: Smith
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Meihua
authors.initials: M
authors.lastname: Tu
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Angela C
authors.initials: AC
authors.lastname: Wolford
authors.affiliation: Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ‡Cardiovascular, Metabolic and Endocrine Diseases Research Unit, and §Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.|Cardiovascular, Metabolic and Endocrine Diseases Medicinal Chemistry, ⊥Cardiovascular, Metabolic and Endocrine Diseases Research Unit, #Worldwide Medicinal Chemistry, ∇Pharmacokinetics, Dynamics and Metabolism, ○Pharmaceutical Sciences, Pfizer Worldwide Research & Development , Groton, Connecticut 06340, United States.
authors.forename: Jun
authors.initials: J
authors.lastname: Xiao
mesh_terms: D055372:AMP-Activated Protein Kinases / Q000378:metabolism*; D000284:Administration, Oral; D000327:Adsorption; D000818:Animals; D018360:Crystallography, X-Ray; D003928:Diabetic Nephropathies / Q000188:drug therapy*; D004285:Dogs; D020536:Enzyme Activators / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D057166:High-Throughput Screening Assays; D006801:Humans; D007191:Indazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D007275:Injections, Intravenous; D008252:Macaca fascicularis; D008297:Male; D008958:Models, Molecular; D011487:Protein Conformation; D051381:Rats
chemical_list: D020536:Enzyme Activators; D007191:Indazoles; D007211:Indoles; C000617640:PF-6409577; D055372:AMP-Activated Protein Kinases