Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR00998

Target Information
NameTGF-beta receptor type I    
Type of targetClinical trial target    
SynonymsALK-5    
Activin receptor-like kinase 5    
SKR4    
Serine/threonine-protein kinase receptor R4    
TGF-beta type I receptor    
TGFR-1    
TbetaRI    
Type I TGFbeta receptor kinase    
DiseaseCancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[1]
Fibrosis
[ICD9: 709.2   ICD10: L90.5]
[1]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.37
UniProt IDP36897
PDB Structure1B6C; 1IAS; 1PY5; 1RW8; 1TBI; 1VJY; 2L5S; 2PJY; 2WOT; 2WOU; 2X7O; 3FAA; 3GXL; 3HMM; 3KCF; 3KFD; 3TZM.    
FunctionType i/type ii tgf-beta receptors form an heteromeric complex after binding tgf-beta at the cell surface and act as signal transducers.    
SequenceMEAAVAAPRPRLLLLVLAAAAAAAAALLPGATALQCFCHLCTKDNFTCVTDGLCFVSVTE TTDKVIHNSMCIAEIDLIPRDRPFVCAPSSKTGSVTTTYCCNQDHCNKIELPTTVKSSPG LGPVELAAVIAGPVCFVCISLMLMVYICHNRTVIHHRVPNEEDPSLDRPFISEGTTLKDL IYDMTTSGSGSGLPLLVQRTIARTIVLQESIGKGRFGEVWRGKWRGEEVAVKIFSSREER SWFREAEIYQTVMLRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVE GMIKLALSTASGLAHLHMEIVGTQGKPAIAHRDLKSKNILVKKNGTCCIADLGLAVRHDS ATDTIDIAPNHRVGTKRYMAPEVLDDSINMKHFESFKRADIYAMGLVFWEIARRCSIGGI HEDYQLPYYDLVPSDPSVEEMRKVVCEQKLRPNIPNRWQSCEALRVMAKIMRECWYANGA ARLTALRIKKTLSQLSQQEGIKM
Target ValidationClick to Find Target Validation Information.    
Inhibitor2-phenyl-N- (pyridin-4-yl)quinazolin-4-amine[2]
4- (3-Pyridin-2-Yl-1h-Pyrazol-4-Yl)Quinoline[3]
4-Pyridin-2-yl-5-quinolin-2-yl-thiazol-2-ylamine[4]
4-Pyridin-2-yl-5-quinolin-4-yl-thiazol-2-ylamine[4]
4-Pyridin-3-yl-5-quinolin-4-yl-thiazol-2-ylamine[4]
5''-Quinolin-4-yl-[2,4'']bithiazolyl-2''-ylamine[4]
GW-788388[5]
HTS-466284,   LY-364947[6]
IN-1130[7]
IN-1166[8]
Naphthyridine Inhibitor[3]
SB-431542[9]
SB-505124[10]
SB-525334[10]
TGF-beta receptor kinase inhibitor[11]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Successful shape-based virtual screening: the discovery of a potent inhibitor of the type I TGFbeta receptor kinase (TbetaRI). Bioorg Med Chem Lett. 2003 Dec 15;13(24):4355-9. To Reference
Ref 2Bioorg Med Chem Lett. 2009 Apr 15;19(8):2277-81. Epub 2009 Feb 26.Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors. To Reference
Ref 3Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 4J Med Chem. 2004 Aug 26;47(18):4494-506.Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors. To Reference
Ref 5J Med Chem. 2006 Apr 6;49(7):2210-21.Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor. To Reference
Ref 6J Med Chem. 2006 Mar 23;49(6):2138-42.Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7. To Reference
Ref 7Bioorg Med Chem. 2010 Jun 15;18(12):4459-67. Epub 2010 Apr 28.Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors. To Reference
Ref 8J Med Chem. 2007 Jun 28;50(13):3143-7. Epub 2007 Jun 7.Synthesis and biological evaluation of 4(5)-(6-alkylpyridin-2-yl)imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors. To Reference
Ref 9Bioorg Med Chem Lett. 2010 Jan 1;20(1):326-9. Epub 2009 Oct 29.Pyrazolone based TGFbetaR1 kinase inhibitors. To Reference
Ref 10Bioorg. Med. Chem. Lett. 20(14):4228-4232 (2010) To Reference
Ref 11Current and emerging drugs for idiopathic pulmonary fibrosis. Expert Opin Emerg Drugs. 2007 Nov;12(4):627-46. To Reference



 

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