Therapeutic Targets Database
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TTD Target ID: TTDR01217

Target Information
NameBeta platelet-derived growth factor receptor    
Type of targetResearch target    
SynonymsBeta-PDGFR    
CD140b antigen    
PDGF-R-beta    
Platelet-derived growth factor receptor beta    
DiseaseChronic myeloproliferative diseases
[ICD9: 205.1, 238.4, 289.89, 289.9   ICD10: D47.1]
[1]
Ewing's sarcoma
[ICD9: 170   ICD10: C41]
[2]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.112
PathwayCalcium signaling pathway
Colorectal cancer
Cytokine-cytokine receptor interaction
Focal adhesion
Gap junction
Glioma
MAPK signaling pathway
Melanoma
Pathways in cancer
Prostate cancer
Regulation of actin cytoskeleton
UniProt IDP09619
PDB Structure1GQ5; 1H9O; 1LWP; 2L6W; 3MJG.    
FunctionReceptor that binds specifically to pdgfb and has a tyrosine-protein kinase activity. Phosphorylates tyr residues at the c-terminus of ptpn11 creating a binding site for the sh2 domain of grb2.    
SequenceMRLPGAMPALALKGELLLLSLLLLLEPQISQGLVVTPPGPELVLNVSSTFVLTCSGSAPV VWERMSQEPPQEMAKAQDGTFSSVLTLTNLTGLDTGEYFCTHNDSRGLETDERKRLYIFV PDPTVGFLPNDAEELFIFLTEITEITIPCRVTDPQLVVTLHEKKGDVALPVPYDHQRGFS GIFEDRSYICKTTIGDREVDSDAYYVYRLQVSSINVSVNAVQTVVRQGENITLMCIVIGN EVVNFEWTYPRKESGRLVEPVTDFLLDMPYHIRSILHIPSAELEDSGTYTCNVTESVNDH QDEKAINITVVESGYVRLLGEVGTLQFAELHRSRTLQVVFEAYPPPTVLWFKDNRTLGDS SAGEIALSTRNVSETRYVSELTLVRVKVAEAGHYTMRAFHEDAEVQLSFQLQINVPVRVL ELSESHPDSGEQTVRCRGRGMPQPNIIWSACRDLKRCPRELPPTLLGNSSEEESQLETNV TYWEEEQEFEVVSTLRLQHVDRPLSVRCTLRNAVGQDTQEVIVVPHSLPFKVVVISAILA LVVLTIISLIILIMLWQKKPRYEIRWKVIESVSSDGHEYIYVDPMQLPYDSTWELPRDQL VLGRTLGSGAFGQVVEATAHGLSHSQATMKVAVKMLKSTARSSEKQALMSELKIMSHLGP HLNVVNLLGACTKGGPIYIITEYCRYGDLVDYLHRNKHTFLQHHSDKRRPPSAELYSNAL PVGLPLPSHVSLTGESDGGYMDMSKDESVDYVPMLDMKGDVKYADIESSNYMAPYDNYVP SAPERTCRATLINESPVLSYMDLVGFSYQVANGMEFLASKNCVHRDLAARNVLICEGKLV KICDFGLARDIMRDSNYISKGSTFLPLKWMAPESIFNSLYTTLSDVWSFGILLWEIFTLG GTPYPELPMNEQFYNAIKRGYRMAQPAHASDEIYEIMQKCWEEKFEIRPPFSQLVLLLER LLGEGYKKKYQQVDEEFLRSDHPAILRSQARLPGFHGLRSPLDTSSVLYTAVQPNEGDND YIIPLPDPKPEVADEGPLEGSPSLASSTLNEVNTSSTISCDSPLEPQDEPEPEPQLELQV EPEPELEQLPDSGCPAPRAEAEDSFL
Target ValidationClick to Find Target Validation Information.    
Inhibitor (1H-indol-2-yl)[3]
(1H-indol-2-yl)[3]
(1H-indol-2-yl)[3]
(2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamine[4]
(5-fluoro-1H-indol-2-yl)-[3]
(5-hydroxy-1H-indol-2-yl)[3]
(benzo[b]furan-2-yl)-[5]
1-Phenyl-1H-benzoimidazol-5-ol[6]
1-Phenyl-1H-benzoimidazole[6]
2- (1H-indazol-3-yl)-1H-benzo[d]imidazole[7]
3- ([8]
3- (1H-Indol-3-yl)-6,7-dimethoxy-quinoline[8]
3- (1H-Indol-3-yl)-quinoline[8]
3- (2-Cyclohexyl-ethyl)-6,7-dimethoxy-quinoline[8]
3- (3,4-Dichloro-phenyl)-6,7-dimethoxy-quinoline[8]
3- (3,4-Difluoro-phenyl)-6,7-dimethoxy-quinoline[8]
3- (3,4-Dimethoxy-phenyl)-6,7-dimethoxy-quinoline[8]
3- (3-Fluoro-phenyl)-6,7-dimethoxy-quinoline[8]
3- (4-Fluoro-phenyl)-6,7-dimethoxy-quinoline[8]
3- (4-dimethylamino-benzylidenyl)-2-indolinone[9]
3- (6,7-Dimethoxy-quinolin-4-yloxy)-phenol[10]
3- (6,7-Dimethoxy-quinolin-4-yloxy)-phenylamine[10]
3-Benzimidazol-2-ylhydroquinolin-2-one[11]
3-Benzyloxy-6,7-dimethoxy-quinoline[8]
3-Cyclohexylethynyl-6,7-dimethoxy-quinoline[8]
3-Cyclopent-1-enyl-6,7-dimethoxy-quinoline[8]
3-Cyclopentyl-6,7-dimethoxy-quinoline[8]
3-Pyridin-3-yl-quinoline-6,7-diol[8]
3-Pyridin-4-yl-quinolin-7-ol[12]
3-Pyridin-4-yl-quinoline[12]
3-Pyridin-4-yl-quinoline-5,7-diol[12]
3-Thiophen-3-yl-quinoline[8]
4- (2,3-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline[10]
4- (3,4-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline[10]
4- (3,5-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline[10]
4- (3-Bromo-phenoxy)-6,7-dimethoxy-quinazoline[10]
4- (3-Bromo-phenoxy)-6,7-dimethoxy-quinoline[10]
4- (3-Ethoxy-phenoxy)-6,7-dimethoxy-quinoline[10]
4- (3-Ethyl-phenoxy)-6,7-dimethoxy-quinoline[10]
4- (3-Fluoro-phenoxy)-6,7-dimethoxy-quinoline[10]
4- (5-Methoxy-benzoimidazol-1-yl)-phenylamine[13]
4- (6,7-Dimethoxy-quinolin-3-yl)-benzoic acid[8]
4- (6,7-Dimethoxy-quinolin-3-yl)-phenol[8]
4-Benzoimidazol-1-yl-phenylamine[6]
5,6,7-Trimethoxy-3-pyridin-4-yl-quinoline[12]
5,7-Dimethoxy-3-pyridin-4-yl-quinoline[12]
5,7-Dimethoxy-3-thiophen-3-yl-quinoline[8]
5,7-Dimethyl-3-thiophen-3-yl-quinoline[8]
5- (6,7-Dimethoxy-quinolin-3-yl)-1H-pyridin-2-one[8]
5-Methoxy-1-phenyl-1H-benzoimidazole[6]
6,7-Dichloro-3-thiophen-3-yl-quinoline[8]
6,7-Difluoro-3-thiophen-3-yl-quinoline[8]
6,7-Dimethoxy-3- ([8]
6,7-Dimethoxy-3- (3-methoxy-phenyl)-quinoline[8]
6,7-Dimethoxy-3- (4-methoxy-phenyl)-quinoline[8]
6,7-Dimethoxy-3- (4-nitro-phenyl)-quinoline[8]
6,7-Dimethoxy-3-p-tolyl-quinoline[8]
6,7-Dimethoxy-3-phenyl-quinoline[8]
6,7-Dimethoxy-3-phenylethynyl-quinoline[8]
6,7-Dimethoxy-3-pyridin-3-yl-quinoline[8]
6,7-Dimethoxy-3-pyridin-4-yl-quinoline[12]
6,7-Dimethoxy-3-thiophen-2-yl-quinoline[8]
6,7-Dimethoxy-4- (2-methoxy-phenoxy)-quinoline[10]
6,7-Dimethoxy-4- (3-methoxy-phenoxy)-quinoline[10]
6,7-Dimethoxy-4- (3-nitro-phenoxy)-quinoline[10]
6,7-Dimethoxy-4- (4-methoxy-phenoxy)-quinoline[10]
6,7-Dimethoxy-4-m-tolyloxy-quinoline[10]
6,7-Dimethoxy-4-phenoxy-quinoline[10]
6-Methoxy-3-pyridin-4-yl-quinoline[12]
6-Methoxy-3-thiophen-3-yl-quinoline[8]
7-Chloro-3-pyridin-4-yl-quinoline[12]
7-Fluoro-3-thiophen-3-yl-quinoline[8]
7-Methoxy-3-pyridin-4-yl-quinoline[12]
7-Methoxy-3-thiophen-3-yl-quinoline[8]
7-Thiophen-3-yl-[1,3]dioxolo[4,5-g]quinoline[8]
AG1295[5]
BMS-536924[14]
Benzyl- (6,7-dimethoxy-quinolin-3-yl)-amine[8]
Bis- (5-hydroxy-1H-indol-2-yl)-methanone[3]
JNJ-10198409[4]
PD-0166326,   PD-166326[15]
PD-0173952[15]
PD-0173955,   PD-17395[15]
PD-0173956[15]
PD-0173958[15]
PD-0179483[15]
PD-0180970[15]
PD-173074[16]
RG-13022[8]
RPR-101511[8]
RPR-108514A[17]
Ro-4396686[18]
SEMAXINIB[19]
SU-11652[19]
TG-100435[20]
bis (5-acetoxybenzo[b]furan-2-yl)methanone[5]
bis (5-aminobenzo[b]furan-2-yl)methanone[5]
bis (5-hydroxybenzo[b]furan-2-yl)methanone[5]
bis (5-methoxybenzo[b]furan-2-yl)methanone[5]
bis (6-hydroxybenzo[b]furan-2-yl)methanone[5]
bis (benzo[b]furan-2-yl)methanone[5]
di (1H-indol-2-yl)methanone[3]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Response to imatinib mesylate in patients with chronic myeloproliferative diseases with rearrangements of the platelet-derived growth factor receptor beta. N Engl J Med. 2002 Aug 15;347(7):481-7. To Reference
Ref 2Beta-platelet-derived growth factor receptor mediates motility and growth of Ewing's sarcoma cells. Oncogene. 2003 Apr 17;22(15):2334-42. To Reference
Ref 3J Med Chem. 2006 Jun 1;49(11):3101-15.Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase. To Reference
Ref 4J Med Chem. 2005 Dec 29;48(26):8163-73.(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells. To Reference
Ref 5Bioorg Med Chem. 2007 Mar 1;15(5):2187-97. Epub 2006 Dec 12.Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones. To Reference
Ref 6J Med Chem. 1998 Dec 31;41(27):5457-65.Structure-activity relationships for 1-phenylbenzimidazoles as selective ATP site inhibitors of the platelet-derived growth factor receptor. To Reference
Ref 7Bioorg Med Chem Lett. 2006 Jul 1;16(13):3595-9. Epub 2006 Apr 5.Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases. To Reference
Ref 8J Med Chem. 1994 Jul 8;37(14):2129-37.A new series of PDGF receptor tyrosine kinase inhibitors: 3-substituted quinoline derivatives. To Reference
Ref 9Bioorg Med Chem. 2010 May 15;18(10):3575-87. Epub 2010 Mar 27.Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents. To Reference
Ref 10Bioorg. Med. Chem. Lett. 7(23):2935-2940 (1997) To Reference
Ref 11J Med Chem. 2009 Jan 22;52(2):278-92.Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors. To Reference
Ref 12J Med Chem. 1994 Aug 19;37(17):2627-9.5,7-Dimethoxy-3-(4-pyridinyl)quinoline is a potent and selective inhibitor of human vascular beta-type platelet-derived growth factor receptor tyrosine kinase. To Reference
Ref 13J Med Chem. 1999 Jul 1;42(13):2373-82.Structure-activity relationships for 5-substituted 1-phenylbenzimidazoles as selective inhibitors of the platelet-derived growth factor receptor. To Reference
Ref 14J Med Chem. 2005 Sep 8;48(18):5639-43.Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. To Reference
Ref 15Biochem Pharmacol. 2000 Oct 1;60(7):885-98.Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors. To Reference
Ref 16J Med Chem. 2005 Jul 14;48(14):4628-53.Synthesis and structure-activity relationships of soluble 7-substituted 3-(3,5-dimethoxyphenyl)-1,6-naphthyridin-2-amines and related ureas as dual inhibitors of the fibroblast growth factor receptor-1 and vascular endothelial growth factor receptor-2 tyrosine kinases. To Reference
Ref 17Bioorg. Med. Chem. Lett. 7(4):421-424 (1997) To Reference
Ref 18Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3. Epub 2006 Feb 3.Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. To Reference
Ref 19J Med Chem. 2003 Mar 27;46(7):1116-9.Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase. To Reference
Ref 20Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8. Epub 2006 Nov 7.Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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