Successful shape-Based virtual screening: The discovery of a potent inhibitor of the type I TGFβ receptor kinase (TβRI)

Bioorganic and Medicinal Chemistry Letters

Volumn 13, Issue 24, 2003, Pages 4355-4359

  Singh, Juswinder ^a   Chuaqui, Claudio E ^a   Boriack Sjodin, P Ann ^a   Lee, Wen Cherng ^a   Pontz, Timothy ^a   Corbley, Michael J ^a   Cheung, H Kam ^a   Arduini, Robert M ^a   Mead, Jonathan N ^a   Newman, Miki N ^a   Papadatos, James L ^a   Bowes, Scott ^a   Josiah, Serene ^a   Ling, Leona E ^a  

^a BIOGEN   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 (4 FLUOROPHENYL) 2 (4 METHYLSULFINYLPHENYL) 5 (4 PYRIDYL)IMIDAZOLE; FKBP 12; HTS 466284; NPC 30345; PHOSPHOTRANSFERASE INHIBITOR; RECEPTOR BLOCKING AGENT; TRANSFORMING GROWTH FACTOR BETA RECEPTOR KINASE INHIBITOR; TRANSFORMING GROWTH FACTOR BETA1; UNCLASSIFIED DRUG;

ARTICLE; CANCER; CONTROLLED STUDY; DRUG BINDING; DRUG POTENCY; DRUG SCREENING; DRUG TARGETING; ENZYME ACTIVITY; FIBROSIS; HUMAN; HUMAN CELL; PROTEIN CONFORMATION; VALIDATION PROCESS;

EID: 0344496021     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2003.09.028     Document Type: Article

References (15)

1. Massague J. Annu. Rev. Biochem. 67:1998;753.
2. Massague J.B., Blain S.W., Lo R.S. Cell. 103:2000;295.
3. Franklin T.J. Int. J. Biochem. Cell Biol. 29:1997;78.
4. Border W.A., Roslahti E. J. Clin. Invest. 90:1992;1.
5. Laping N.J. IDRUGS. 2:1999;907.
6. Heldin C.H., Miyazono K., ten Dijke P. Nature. 390:1997;465.
7. Huse M., Chen Y.G., Massague J., Kuriyan J. Cell. 96:1999;425.
8. Bajorath J. Nature Rev. Drug Discov. 1:2002;882.
9. Joseph-McCarthy D. Pharmacol. Therap. 84:1999;179.
10. Mason J.S., Good A.C., Martin E.J. Curr. Pharm. Des. 7:2001;567.
11. Hahn M.J. Chem. Inf. Comput. Sci. 37:1997;80.
12. Putta S., Lemmen C., Beroza P., Greene J. J. Chem. Inf. Comput. Sci. 42:2002;1230.
13. Eyers P.A., Craxton M., Morrice N., Cohen P., Goedert M. Chem. Biol. 5:1998;321.
14. Catalyst; Accelrys Inc., San Diego, CA.
15. Carson M. Methods Enzymol. 277:1997;493.