Target Validation Information
TTD ID T53524
Target Name Platelet-derived growth factor receptor alpha (PDGFRA)
Type of Target
Successful
Drug Potency against Target TAK-593 Drug Info IC50 = 4.3~13 nM
(1H-indol-2-yl)(5-methoxy-1H-indol-2-yl)methanone Drug Info IC50 = 300 nM [7]
(1H-indol-2-yl)(5-phenoxy-1H-indol-2-yl)methanone Drug Info IC50 = 10000 nM [7]
(1H-indol-2-yl)(6-methoxy-1H-indol-2-yl)methanone Drug Info IC50 = 300 nM [7]
(5-fluoro-1H-indol-2-yl)-(1H-indol-2-yl)methanone Drug Info IC50 = 760 nM [7]
(5-hydroxy-1H-indol-2-yl)(1H-indol-2-yl)methanone Drug Info IC50 = 200 nM [7]
1-Phenyl-1H-benzoimidazol-5-ol Drug Info IC50 = 130 nM [10]
1-Phenyl-1H-benzoimidazole Drug Info IC50 = 2300 nM [10]
3-((E)-Styryl)-quinoline Drug Info IC50 = 200 nM [8]
3-(1H-Indol-3-yl)-6,7-dimethoxy-quinoline Drug Info IC50 = 600 nM [8]
3-(1H-Indol-3-yl)-quinoline Drug Info IC50 = 8000 nM [8]
3-(2-Cyclohexyl-ethyl)-6,7-dimethoxy-quinoline Drug Info IC50 = 500 nM [8]
3-(3,4-Dichloro-phenyl)-6,7-dimethoxy-quinoline Drug Info IC50 = 7000 nM [8]
3-(3,4-Difluoro-phenyl)-6,7-dimethoxy-quinoline Drug Info IC50 = 200 nM [8]
3-(3,4-Dimethoxy-phenyl)-6,7-dimethoxy-quinoline Drug Info IC50 = 10000 nM [8]
3-(3-Fluoro-phenyl)-6,7-dimethoxy-quinoline Drug Info IC50 = 25 nM [8]
3-(4-Fluoro-phenyl)-6,7-dimethoxy-quinoline Drug Info IC50 = 60 nM [8]
3-Benzyloxy-6,7-dimethoxy-quinoline Drug Info IC50 = 70 nM [8]
3-Cyclohexylethynyl-6,7-dimethoxy-quinoline Drug Info IC50 = 1000 nM [8]
3-Cyclopent-1-enyl-6,7-dimethoxy-quinoline Drug Info IC50 = 40 nM [8]
3-Cyclopentyl-6,7-dimethoxy-quinoline Drug Info IC50 = 500 nM [8]
3-Pyridin-3-yl-quinoline-6,7-diol Drug Info IC50 = 10000 nM [8]
3-Pyridin-4-yl-quinolin-7-ol Drug Info IC50 = 9200 nM [9]
3-Pyridin-4-yl-quinoline Drug Info IC50 = 1500 nM [9]
3-Pyridin-4-yl-quinoline-5,7-diol Drug Info IC50 = 1300 nM [9]
3-Thiophen-3-yl-quinoline Drug Info IC50 = 250 nM [8]
4-(3,4-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline Drug Info IC50 = 70 nM
4-(5-Methoxy-benzoimidazol-1-yl)-phenylamine Drug Info IC50 = 1360 nM [1]
4-(6,7-Dimethoxy-quinolin-3-yl)-benzoic acid Drug Info IC50 = 5000 nM [8]
4-(6,7-Dimethoxy-quinolin-3-yl)-phenol Drug Info IC50 = 30 nM [8]
4-Benzoimidazol-1-yl-phenylamine Drug Info IC50 = 2000 nM [10]
5,11-Dimethyl-6H-pyrido[4,3-b]carbazol-9-ol Drug Info IC50 = 600 nM [4]
5,6,7-Trimethoxy-3-pyridin-4-yl-quinoline Drug Info IC50 = 400 nM [9]
5,7-Dimethoxy-3-pyridin-4-yl-quinoline Drug Info Ki = 14 nM [9]
5,7-Dimethoxy-3-thiophen-3-yl-quinoline Drug Info IC50 = 30 nM [8]
5,7-Dimethyl-3-thiophen-3-yl-quinoline Drug Info IC50 = 5 nM [8]
5-(6,7-Dimethoxy-quinolin-3-yl)-1H-pyridin-2-one Drug Info IC50 = 30 nM [8]
5-Fluoro-3-thiophen-3-yl-quinoline Drug Info IC50 = 20 nM [8]
5-Methoxy-1-phenyl-1H-benzoimidazole Drug Info IC50 = 1900 nM [10]
6,7-Dichloro-3-thiophen-3-yl-quinoline Drug Info IC50 = 2000 nM [8]
6,7-Difluoro-3-thiophen-3-yl-quinoline Drug Info IC50 = 4000 nM [8]
6,7-Dimethoxy-3-((E)-styryl)-quinoline Drug Info IC50 = 5 nM [8]
6,7-Dimethoxy-3-(2-methoxy-phenyl)-quinoline Drug Info IC50 = 2000 nM [8]
6,7-Dimethoxy-3-(3-methoxy-phenyl)-quinoline Drug Info IC50 = 2000 nM [8]
6,7-Dimethoxy-3-(4-methoxy-phenyl)-quinoline Drug Info IC50 = 15 nM [8]
6,7-Dimethoxy-3-(4-nitro-phenyl)-quinoline Drug Info IC50 = 150 nM [8]
6,7-Dimethoxy-3-p-tolyl-quinoline Drug Info IC50 = 2000 nM [8]
6,7-Dimethoxy-3-phenyl-quinoline Drug Info IC50 = 150 nM [8]
6,7-Dimethoxy-3-phenylethynyl-quinoline Drug Info IC50 = 50 nM [8]
6,7-Dimethoxy-3-pyridin-3-yl-quinoline Drug Info IC50 = 800 nM [8]
6,7-Dimethoxy-3-pyridin-4-yl-quinoline Drug Info IC50 = 300 nM [9]
6,7-Dimethoxy-3-thiophen-2-yl-quinoline Drug Info IC50 = 80 nM [8]
6-Methoxy-3-pyridin-4-yl-quinoline Drug Info IC50 = 400 nM [9]
6-Methoxy-3-thiophen-3-yl-quinoline Drug Info IC50 = 70 nM [8]
7-Chloro-3-pyridin-4-yl-quinoline Drug Info IC50 = 300 nM [9]
7-Fluoro-3-thiophen-3-yl-quinoline Drug Info IC50 = 25 nM [8]
7-Methoxy-3-pyridin-4-yl-quinoline Drug Info IC50 = 600 nM [9]
7-Methoxy-3-thiophen-3-yl-quinoline Drug Info IC50 = 60 nM [8]
7-Thiophen-3-yl-[1,3]dioxolo[4,5-g]quinoline Drug Info IC50 = 600 nM [8]
AG1295 Drug Info IC50 = 5400 nM [7]
Benzyl-(6,7-dimethoxy-quinolin-3-yl)-amine Drug Info IC50 = 80 nM [8]
Bis-(5-hydroxy-1H-indol-2-yl)-methanone Drug Info IC50 = 300 nM [7]
Di(1H-indol-2-yl)methanone Drug Info IC50 = 1000 nM [7]
HKI-9924129 Drug Info IC50 = 1430 nM [2]
JNJ-10198409 Drug Info IC50 = 45 nM [5]
PD-0166326 Drug Info IC50 = 139 nM [2]
PD-0173952 Drug Info IC50 = 636 nM [2]
PD-0173955 Drug Info IC50 = 1660 nM [2]
PD-0173956 Drug Info IC50 = 1250 nM [2]
PD-0173958 Drug Info IC50 = 2340 nM [2]
PD-0179483 Drug Info IC50 = 463 nM [2]
RG-13022 Drug Info IC50 = 3000 nM [8]
Ro-4396686 Drug Info IC50 = 83 nM [6]
Romiplostim Drug Info IC50 = 4050 nM [3]
RPR-101511 Drug Info IC50 = 20 nM [8]
RPR-108514A Drug Info IC50 = 15000 nM
SU-11652 Drug Info IC50 < 70 nM [3]
Action against Disease Model TAK-593 Drug Info TAK-593 acts on the colorectal cancer cell lines that were analysed revealed varying expression intensities of PDGFRalpha and PDGFRbeta. [11]
References
REF 1 Structure-activity relationships for 5-substituted 1-phenylbenzimidazoles as selective inhibitors of the platelet-derived growth factor receptor. J Med Chem. 1999 Jul 1;42(13):2373-82.
REF 2 Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors. Biochem Pharmacol. 2000 Oct 1;60(7):885-98.
REF 3 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... J Med Chem. 2003 Mar 27;46(7):1116-9.
REF 4 Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases. J Med Chem. 2005 Oct 6;48(20):6194-201.
REF 5 (6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad ant... J Med Chem. 2005 Dec 29;48(26):8163-73.
REF 6 Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3.
REF 7 Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase. J Med Chem. 2006 Jun 1;49(11):3101-15.
REF 8 A new series of PDGF receptor tyrosine kinase inhibitors: 3-substituted quinoline derivatives. J Med Chem. 1994 Jul 8;37(14):2129-37.
REF 9 5,7-Dimethoxy-3-(4-pyridinyl)quinoline is a potent and selective inhibitor of human vascular beta-type platelet-derived growth factor receptor tyro... J Med Chem. 1994 Aug 19;37(17):2627-9.
REF 10 Structure-activity relationships for 1-phenylbenzimidazoles as selective ATP site inhibitors of the platelet-derived growth factor receptor. J Med Chem. 1998 Dec 31;41(27):5457-65.
REF 11 PDGFRalpha/beta expression correlates with the metastatic behavior of human colorectal cancer: a possible rationale for a molecular targeting strategy. Oncol Rep. 2008 Mar;19(3):697-704.

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