Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants

Journal of Medicinal Chemistry

Volumn 57, Issue 19, 2014, Pages 7900-7915

  Mohedas, Agustin H ^a   Wang, You ^b   Sanvitale, Caroline E ^c   Canning, Peter ^c   Choi, Sungwoon ^b   Xing, Xuechao ^b   Bullock, Alex N ^c   Cuny, Gregory D ^b,d   Yu, Paul B ^b  

^a MASSACHUSETTS INSTITUTE OF TECHNOLOGY   (United States)

^b BRIGHAM AND WOMEN S HOSPITAL   (United States)

^c UNIVERSITY OF OXFORD   (United Kingdom)

^d UNIVERSITY OF HOUSTON   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 [4 [5 (3,4,5 TRIMETHOXYPHENYL)PYRIDIN 3 YL]PHENYL] PIPERAZINE; 1 [4 [6 CHLORO 5 (3,4,5 TRIMETHOXYPHENYL)PYRIDIN 3 YL]PHENYL] PIPERAZINE; 1 [4 [6 METHOXY 5 (3,4,5 TRIMETHOXYPHENYL)PYRIDIN 3 YL]PHENYL] PIPERAZINE; 2 AMINO 5 ARYL 3 (3,4,5 TRIMETHOXYPHENYL)PYRIDINE; 2 AMINO 5 BROMO 3 (3,4,5 TRIMETHOXYPHENYL)PYRIDINE; 2 AMINOPYRIDINE DERIVATIVE; 3 (2,3-DIHYDROBENZO[B]DIOXIN 6 YL) 5 [4 (PIPERAZIN 1 YL)PHENYL]PYRIDINE 2 AMINE; 3 (3 ISOPROPOXYPHENYL) 5 [4 (PIPERAZIN 1 YL)PHENYL]PYRIDIN 2 AMINE; 3 (3 METHOXY 4 METHYLPHENYL)-5 [4 (PIPERAZIN 1 YL)PHENYL]PYRIDIN 2 AMINE; 3 (3 METHOXYPHENYL) 5 [4 (PIPERAZIN 1 YL)PHENYL]PYRIDIN 2 AMINE; 3 (3,4 DIMETHOXYPHENYL) 5 [4 (PIPERAZIN 1 YL)PHENYL]PYRIDIN 2 AMINE; 3 (4 CHLORO 3 METHOXYPHENYL) 5 [4 (PIPERAZIN 1 YL)PHENYL]PYRIDIN 2 AMINE; 3 (4 METHOXYPHENYL) 5 [4 (PIPERAZIN 1 YL)PHENYL]PYRIDIN 2 AMINE; 3 ARYL 5 (PIPERAZINYLPHENYL)PYRIDINE; 3 ARYL 5 [(N BOC) PIPERAZINYLPHENYL]PYRIDINE; 4 [6 AMINO 5 (3,4,5 TRIMETHOXYPHENYL)PYRIDIN 3 YL] 2 METHOXYPHENOL; 4 [6 MINO 5 (3,4,5 TRIMETHOXYPHENYL)PYRIDIN 3 YL]PHENOL; 5 [3 (PIPERAZIN 1 YL)PHENYL] 3 (3,4,5 TRIMETHOXYPHENYL)PYRIDIN 2 AMINE; 5 [3 (PIPERAZIN 1 YL)PHENYL] 3 (QUINOLIN 4 YL)PYRIDIN 2 AMINE; 5 [4 (PIPERAZIN 1 YL)PHENYL] 3 (3,4,5 TRIMETHOXYPHENYL)PYRIDIN 2 AMINE; 5 [4 (PIPERAZIN 1 YL)PHENYL] 3 (QUINOLIN 4 YL)PYRIDIN 2 AMINE; 5 [4 (PIPERAZIN 1 YL)PHENYL] 3 (QUINOLIN 5 YL)PYRIDIN 2 AMINE; 6 [4 (1 PIPERAZINYL)PHENYL] 3 (4 QUINOLINYL)PYRAZOLO[1,5 A]PYRIMIDINE; N METHYL 5 [4 (PIPERAZIN 1 YL)PHENYL] 3 (3,4,5 TRIMETHOXYPHENYL)PYRIDIN 2 AMINE; N,N DIMETHYL 5 [4 (PIPERAZIN 1 YL)PHENYL] 3 (3,4,5 TRIMETHOXYPHENYL)PYRIDIN 2 AMINE; PIPERAZINE DERIVATIVE; PROTEIN SERINE THREONINE KINASE INHIBITOR; TRANSFORMING GROWTH FACTOR BETA RECEPTOR 1; UNCLASSIFIED DRUG; UNINDEXED DRUG; 3-(6-AMINO-5-(3,4,5-TRIMETHOXYPHENYL)PYRIDIN-3-YL)PHENOL; ACTIVIN RECEPTOR 1; ACVR1 PROTEIN, HUMAN; AMINOPYRIDINE DERIVATIVE; PHENOL DERIVATIVE; PROTEIN KINASE INHIBITOR;

ARTICLE; CELL VIABILITY; COLUMN CHROMATOGRAPHY; CONFORMATIONAL TRANSITION; CONTROLLED STUDY; DRUG BINDING; DRUG DETERMINATION; DRUG EFFICACY; DRUG MECHANISM; DRUG SYNTHESIS; GENE MUTATION; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN CELL; HYDROGEN BOND; OSSIFYING MYOSITIS; PROTEIN EXPRESSION; PROTON NUCLEAR MAGNETIC RESONANCE; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY; ANTAGONISTS AND INHIBITORS; GENETICS; METABOLISM; MUTATION; MYOSITIS OSSIFICANS; SYNTHESIS;

ACTIVIN RECEPTORS, TYPE I; AMINOPYRIDINES; HUMANS; MUTATION; MYOSITIS OSSIFICANS; PHENOLS; PROTEIN KINASE INHIBITORS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84907939471     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm501177w     Document Type: Article

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