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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