Therapeutic Targets Database
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Target Validation Information
TTD IDTTDR01217
Target NameBeta platelet-derived growth factor receptor    
Type of TargetResearch target    
Drug Potency against TargetSU-11652IC50 < 70 nM[1]
di(1H-indol-2-yl)methanoneIC50 = 1000 nM[2]
3-Cyclohexylethynyl-6,7-dimethoxy-quinolineIC50 = 1000 nM[3]
bis(5-methoxybenzo[b]furan-2-yl)methanoneIC50 = 1000 nM[4]
(1H-indol-2-yl)(5-phenoxy-1H-indol-2-yl)methanoneIC50 = 10000 nM[2]
3-(3,4-Dimethoxy-phenyl)-6,7-dimethoxy-quinolineIC50 = 10000 nM[3]
3-Pyridin-3-yl-quinoline-6,7-diolIC50 = 10000 nM[3]
(benzo[b]furan-2-yl)-(1H-indol-2-yl)methanoneIC50 = 1070 nM[4]
bis(5-aminobenzo[b]furan-2-yl)methanoneIC50 = 1200 nM[4]
bis(benzo[b]furan-2-yl)methanoneIC50 = 1200 nM[4]
PD-0173956IC50 = 1250 nM[5]
4-(3-Ethoxy-phenoxy)-6,7-dimethoxy-quinolineIC50 = 12900 nM[6]
1-Phenyl-1H-benzoimidazol-5-olIC50 = 130 nM[7]
3-Pyridin-4-yl-quinoline-5,7-diolIC50 = 1300 nM[8]
4-(5-Methoxy-benzoimidazol-1-yl)-phenylamineIC50 = 1360 nM[9]
PD-0166326;PD-166326IC50 = 139 nM[5]
PD-0180970IC50 = 1430 nM[5]
4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinazolineIC50 = 14800 nM[6]
6,7-Dimethoxy-3-(4-methoxy-phenyl)-quinolineIC50 = 15 nM[3]
6,7-Dimethoxy-3-(4-nitro-phenyl)-quinolineIC50 = 150 nM[3]
6,7-Dimethoxy-3-phenyl-quinolineIC50 = 150 nM[3]
3-Pyridin-4-yl-quinolineIC50 = 1500 nM[8]
4-(3-Fluoro-phenoxy)-6,7-dimethoxy-quinolineIC50 = 1500 nM[6]
RPR-108514AIC50 = 15000 nM[10]
PD-0173955;PD-17395IC50 = 1660 nM[5]
3-(6,7-Dimethoxy-quinolin-4-yloxy)-phenylamineIC50 = 1700 nM[6]
PD-173074IC50 = 17000 nM[11]
5-Methoxy-1-phenyl-1H-benzoimidazoleIC50 = 1900 nM[7]
6,7-Dimethoxy-4-(4-methoxy-phenoxy)-quinolineIC50 = 1900 nM[6]
RPR-101511IC50 = 20 nM[3]
3-(3,4-Difluoro-phenyl)-6,7-dimethoxy-quinolineIC50 = 200 nM[3]
3-((E)-Styryl)-quinolineIC50 = 200 nM[3]
(5-hydroxy-1H-indol-2-yl)(1H-indol-2-yl)methanoneIC50 = 200 nM[2]
4-Benzoimidazol-1-yl-phenylamineIC50 = 2000 nM[7]
6,7-Dichloro-3-thiophen-3-yl-quinolineIC50 = 2000 nM[3]
6,7-Dimethoxy-3-(3-methoxy-phenyl)-quinolineIC50 = 2000 nM[3]
6,7-Dimethoxy-3-p-tolyl-quinolineIC50 = 2000 nM[3]
1-Phenyl-1H-benzoimidazoleIC50 = 2300 nM[7]
PD-0173958IC50 = 2340 nM[5]
3-(3-Fluoro-phenyl)-6,7-dimethoxy-quinolineIC50 = 25 nM[3]
7-Fluoro-3-thiophen-3-yl-quinolineIC50 = 25 nM[3]
3-Thiophen-3-yl-quinolineIC50 = 250 nM[3]
4-(6,7-Dimethoxy-quinolin-3-yl)-phenolIC50 = 30 nM[3]
5,7-Dimethoxy-3-thiophen-3-yl-quinolineIC50 = 30 nM[3]
5-(6,7-Dimethoxy-quinolin-3-yl)-1H-pyridin-2-oneIC50 = 30 nM[3]
(1H-indol-2-yl)(5-methoxy-1H-indol-2-yl)methanoneIC50 = 300 nM[2]
6,7-Dimethoxy-3-pyridin-4-yl-quinolineIC50 = 300 nM[8]
7-Chloro-3-pyridin-4-yl-quinolineIC50 = 300 nM[8]
Bis-(5-hydroxy-1H-indol-2-yl)-methanoneIC50 = 300 nM[2]
(1H-indol-2-yl)(6-methoxy-1H-indol-2-yl)methanoneIC50 = 300 nM[2]
RG-13022IC50 = 3000 nM[3]
(2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamineIC50 = 317 nM[12]
2-(1H-indazol-3-yl)-1H-benzo[d]imidazoleIC50 = 3400 nM[13]
3-(4-dimethylamino-benzylidenyl)-2-indolinoneIC50 = 3700 nM[14]
JNJ-10198409IC50 = 4.2 nM[12]
3-Cyclopent-1-enyl-6,7-dimethoxy-quinolineIC50 = 40 nM[3]
5,6,7-Trimethoxy-3-pyridin-4-yl-quinolineIC50 = 400 nM[8]
6-Methoxy-3-pyridin-4-yl-quinolineIC50 = 400 nM[8]
6,7-Difluoro-3-thiophen-3-yl-quinolineIC50 = 4000 nM[3]
SEMAXINIBIC50 = 4050 nM[1]
6,7-Dimethoxy-4-(3-methoxy-phenoxy)-quinolineIC50 = 440 nM[6]
4-(2,3-Dimethoxy-phenoxy)-6,7-dimethoxy-quinolineIC50 = 4400 nM[6]
PD-0179483IC50 = 463 nM[5]
5,7-Dimethyl-3-thiophen-3-yl-quinolineIC50 = 5 nM[3]
6,7-Dimethoxy-3-((E)-styryl)-quinolineIC50 = 5 nM[3]
6,7-Dimethoxy-3-phenylethynyl-quinolineIC50 = 50 nM[3]
3-(2-Cyclohexyl-ethyl)-6,7-dimethoxy-quinolineIC50 = 500 nM[3]
3-Cyclopentyl-6,7-dimethoxy-quinolineIC50 = 500 nM[3]
4-(6,7-Dimethoxy-quinolin-3-yl)-benzoic acidIC50 = 5000 nM[3]
AG1295IC50 = 5400 nM[4]
4-(3,5-Dimethoxy-phenoxy)-6,7-dimethoxy-quinolineIC50 = 5500 nM[6]
3-(6,7-Dimethoxy-quinolin-4-yloxy)-phenolIC50 = 560 nM[6]
3-(4-Fluoro-phenyl)-6,7-dimethoxy-quinolineIC50 = 60 nM[3]
7-Methoxy-3-thiophen-3-yl-quinolineIC50 = 60 nM[3]
3-(1H-Indol-3-yl)-6,7-dimethoxy-quinolineIC50 = 600 nM[3]
7-Thiophen-3-yl-[1,3]dioxolo[4,5-g]quinolineIC50 = 600 nM[3]
bis(5-hydroxybenzo[b]furan-2-yl)methanoneIC50 = 600 nM[4]
7-Methoxy-3-pyridin-4-yl-quinolineIC50 = 600 nM[8]
6,7-Dimethoxy-4-(2-methoxy-phenoxy)-quinolineIC50 = 600 nM[6]
PD-0173952IC50 = 636 nM[5]
6,7-Dimethoxy-4-m-tolyloxy-quinolineIC50 = 6900 nM[6]
3-Benzimidazol-2-ylhydroquinolin-2-oneIC50 = 70 nM[15]
4-(3,4-Dimethoxy-phenoxy)-6,7-dimethoxy-quinolineIC50 = 70 nM[6]
6-Methoxy-3-thiophen-3-yl-quinolineIC50 = 70 nM[3]
3-Benzyloxy-6,7-dimethoxy-quinolineIC50 = 70 nM[3]
6,7-Dimethoxy-4-(3-nitro-phenoxy)-quinolineIC50 = 700 nM[6]
bis(5-acetoxybenzo[b]furan-2-yl)methanoneIC50 = 700 nM[4]
3-(3,4-Dichloro-phenyl)-6,7-dimethoxy-quinolineIC50 = 7000 nM[3]
(5-fluoro-1H-indol-2-yl)-(1H-indol-2-yl)methanoneIC50 = 760 nM[2]
6,7-Dimethoxy-4-phenoxy-quinolineIC50 = 760 nM[6]
6,7-Dimethoxy-3-thiophen-2-yl-quinolineIC50 = 80 nM[3]
Benzyl-(6,7-dimethoxy-quinolin-3-yl)-amineIC50 = 80 nM[3]
6,7-Dimethoxy-3-pyridin-3-yl-quinolineIC50 = 800 nM[3]
3-(1H-Indol-3-yl)-quinolineIC50 = 8000 nM[3]
Ro-4396686IC50 = 83 nM[16]
4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinolineIC50 = 8400 nM[6]
4-(3-Ethyl-phenoxy)-6,7-dimethoxy-quinolineIC50 = 8400 nM[6]
3-Pyridin-4-yl-quinolin-7-olIC50 = 9200 nM[8]
bis(6-hydroxybenzo[b]furan-2-yl)methanoneIC50 = 9700 nM[4]
5,7-Dimethoxy-3-pyridin-4-yl-quinolineKi = 14 nM[8]
TG-100435Ki = 2090 nM[17]
Ref 1J 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 2J 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 3J 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 4Bioorg 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 5Biochem 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 6Bioorg. Med. Chem. Lett. 7(23):2935-2940 (1997) To Reference
Ref 7J 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 8J 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 9J 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 10Bioorg. Med. Chem. Lett. 7(4):421-424 (1997) To Reference
Ref 11J 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 12J 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 13Bioorg 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 14Bioorg 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 15J 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 16Bioorg 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 17Bioorg 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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