Fragment based lead discovery of small molecule inhibitors for the EPHA4 receptor tyrosine kinase

European Journal of Medicinal Chemistry

Volumn 47, Issue 1, 2012, Pages 493-500

  Van Linden, Oscar P J ^a   Farenc, Carine ^b   Zoutman, Willem H ^c   Hameetman, Liesbeth ^c   Wijtmans, Maikel ^a   Leurs, Rob ^a   Tensen, Cornelis P ^c   Siegal, Gregg ^b   De Esch, Iwan J P ^a  

^a VU UNIVERSITY AMSTERDAM   (Netherlands)

^b LEIDEN UNIVERSITY   (Netherlands)

^c LEIDEN UNIVERSITY MEDICAL CENTER   (Netherlands)

Author keywords

Cancer; Crystallization; Docking; EPH receptor; EPHA4; Ephrin; Fragment; In silico; Inhibition; Kinase; Pharmacophore; Screening

Indexed keywords

6,7,8,9 TETRAHYDRO 3H PYRAZOLO(3,4 C)ISOQUINOLIN 1 AMINE; DASATINIB; EPHRIN RECEPTOR A3; EPHRIN RECEPTOR A4; PROTEIN TYROSINE KINASE INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; COMPUTER MODEL; CONTROLLED STUDY; DRUG DETERMINATION; DRUG PROTEIN BINDING; DRUG SCREENING; DRUG SELECTIVITY; ENZYME ACTIVITY; IC 50; INHIBITION KINETICS; MOLECULAR DOCKING; PHARMACOPHORE; PROTEIN PHOSPHORYLATION; REACTOR OPTIMIZATION;

ADENOSINE TRIPHOSPHATE; BINDING SITES; COMPUTATIONAL BIOLOGY; DRUG DISCOVERY; MODELS, MOLECULAR; PROTEIN CONFORMATION; PROTEIN KINASE INHIBITORS; RECEPTOR, EPHA4; SMALL MOLECULE LIBRARIES;

EID: 84855809166     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2011.11.020     Document Type: Article

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