Target Validation Information
TTD ID T59102
Target Name Platelet-derived growth factor receptor beta (PDGFRB)
Type of Target
Successful
Drug Potency against Target (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]
(2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamine Drug Info IC50 = 317 nM [4]
(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]
(benzo[b]furan-2-yl)-(1H-indol-2-yl)methanone Drug Info IC50 = 1070 nM [9]
1-Phenyl-1H-benzoimidazol-5-ol Drug Info IC50 = 130 nM [14]
1-Phenyl-1H-benzoimidazole Drug Info IC50 = 2300 nM [14]
2-(1H-indazol-3-yl)-1H-benzo[d]imidazole Drug Info IC50 = 3400 nM [6]
3-((E)-Styryl)-quinoline Drug Info IC50 = 200 nM [12]
3-(1H-Indol-3-yl)-6,7-dimethoxy-quinoline Drug Info IC50 = 600 nM [12]
3-(1H-Indol-3-yl)-quinoline Drug Info IC50 = 8000 nM [12]
3-(2-Cyclohexyl-ethyl)-6,7-dimethoxy-quinoline Drug Info IC50 = 500 nM [12]
3-(3,4-Dichloro-phenyl)-6,7-dimethoxy-quinoline Drug Info IC50 = 7000 nM [12]
3-(3,4-Difluoro-phenyl)-6,7-dimethoxy-quinoline Drug Info IC50 = 200 nM [12]
3-(3,4-Dimethoxy-phenyl)-6,7-dimethoxy-quinoline Drug Info IC50 = 10000 nM [12]
3-(3-Fluoro-phenyl)-6,7-dimethoxy-quinoline Drug Info IC50 = 25 nM [12]
3-(4-dimethylamino-benzylidenyl)-2-indolinone Drug Info IC50 = 3700 nM [11]
3-(4-Fluoro-phenyl)-6,7-dimethoxy-quinoline Drug Info IC50 = 60 nM [12]
3-(6,7-Dimethoxy-quinolin-4-yloxy)-phenol Drug Info IC50 = 560 nM
3-(6,7-Dimethoxy-quinolin-4-yloxy)-phenylamine Drug Info IC50 = 1700 nM
3-Benzimidazol-2-ylhydroquinolin-2-one Drug Info IC50 = 70 nM [10]
3-Benzyloxy-6,7-dimethoxy-quinoline Drug Info IC50 = 70 nM [12]
3-Cyclohexylethynyl-6,7-dimethoxy-quinoline Drug Info IC50 = 1000 nM [12]
3-Cyclopent-1-enyl-6,7-dimethoxy-quinoline Drug Info IC50 = 40 nM [12]
3-Cyclopentyl-6,7-dimethoxy-quinoline Drug Info IC50 = 500 nM [12]
3-Pyridin-3-yl-quinoline-6,7-diol Drug Info IC50 = 10000 nM [12]
3-Pyridin-4-yl-quinolin-7-ol Drug Info IC50 = 9200 nM [13]
3-Pyridin-4-yl-quinoline Drug Info IC50 = 1500 nM [13]
3-Pyridin-4-yl-quinoline-5,7-diol Drug Info IC50 = 1300 nM [13]
3-Thiophen-3-yl-quinoline Drug Info IC50 = 250 nM [12]
4-(2,3-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline Drug Info IC50 = 4400 nM
4-(3,4-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline Drug Info IC50 = 70 nM
4-(3,5-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline Drug Info IC50 = 5500 nM
4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinazoline Drug Info IC50 = 14800 nM
4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinoline Drug Info IC50 = 8400 nM
4-(3-Ethoxy-phenoxy)-6,7-dimethoxy-quinoline Drug Info IC50 = 12900 nM
4-(3-Ethyl-phenoxy)-6,7-dimethoxy-quinoline Drug Info IC50 = 8400 nM
4-(3-Fluoro-phenoxy)-6,7-dimethoxy-quinoline Drug Info IC50 = 1500 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 [12]
4-(6,7-Dimethoxy-quinolin-3-yl)-phenol Drug Info IC50 = 30 nM [12]
4-Benzoimidazol-1-yl-phenylamine Drug Info IC50 = 2000 nM [14]
5,6,7-Trimethoxy-3-pyridin-4-yl-quinoline Drug Info IC50 = 400 nM [13]
5,7-Dimethoxy-3-pyridin-4-yl-quinoline Drug Info Ki = 14 nM [13]
5,7-Dimethoxy-3-thiophen-3-yl-quinoline Drug Info IC50 = 30 nM [12]
5,7-Dimethyl-3-thiophen-3-yl-quinoline Drug Info IC50 = 5 nM [12]
5-(6,7-Dimethoxy-quinolin-3-yl)-1H-pyridin-2-one Drug Info IC50 = 30 nM [12]
5-Methoxy-1-phenyl-1H-benzoimidazole Drug Info IC50 = 1900 nM [14]
6,7-Dichloro-3-thiophen-3-yl-quinoline Drug Info IC50 = 2000 nM [12]
6,7-Difluoro-3-thiophen-3-yl-quinoline Drug Info IC50 = 4000 nM [12]
6,7-Dimethoxy-3-((E)-styryl)-quinoline Drug Info IC50 = 5 nM [12]
6,7-Dimethoxy-3-(3-methoxy-phenyl)-quinoline Drug Info IC50 = 2000 nM [12]
6,7-Dimethoxy-3-(4-methoxy-phenyl)-quinoline Drug Info IC50 = 15 nM [12]
6,7-Dimethoxy-3-(4-nitro-phenyl)-quinoline Drug Info IC50 = 150 nM [12]
6,7-Dimethoxy-3-p-tolyl-quinoline Drug Info IC50 = 2000 nM [12]
6,7-Dimethoxy-3-phenyl-quinoline Drug Info IC50 = 150 nM [12]
6,7-Dimethoxy-3-phenylethynyl-quinoline Drug Info IC50 = 50 nM [12]
6,7-Dimethoxy-3-pyridin-3-yl-quinoline Drug Info IC50 = 800 nM [12]
6,7-Dimethoxy-3-pyridin-4-yl-quinoline Drug Info IC50 = 300 nM [13]
6,7-Dimethoxy-3-thiophen-2-yl-quinoline Drug Info IC50 = 80 nM [12]
6,7-Dimethoxy-4-(2-methoxy-phenoxy)-quinoline Drug Info IC50 = 600 nM
6,7-Dimethoxy-4-(3-methoxy-phenoxy)-quinoline Drug Info IC50 = 440 nM
6,7-Dimethoxy-4-(3-nitro-phenoxy)-quinoline Drug Info IC50 = 700 nM
6,7-Dimethoxy-4-(4-methoxy-phenoxy)-quinoline Drug Info IC50 = 1900 nM
6,7-Dimethoxy-4-m-tolyloxy-quinoline Drug Info IC50 = 6900 nM
6,7-Dimethoxy-4-phenoxy-quinoline Drug Info IC50 = 760 nM
6-Methoxy-3-pyridin-4-yl-quinoline Drug Info IC50 = 400 nM [13]
6-Methoxy-3-thiophen-3-yl-quinoline Drug Info IC50 = 70 nM [12]
7-Chloro-3-pyridin-4-yl-quinoline Drug Info IC50 = 300 nM [13]
7-Fluoro-3-thiophen-3-yl-quinoline Drug Info IC50 = 25 nM [12]
7-Methoxy-3-pyridin-4-yl-quinoline Drug Info IC50 = 600 nM [13]
7-Methoxy-3-thiophen-3-yl-quinoline Drug Info IC50 = 60 nM [12]
7-Thiophen-3-yl-[1,3]dioxolo[4,5-g]quinoline Drug Info IC50 = 600 nM [12]
AG1295 Drug Info IC50 = 5400 nM [9]
Benzyl-(6,7-dimethoxy-quinolin-3-yl)-amine Drug Info IC50 = 80 nM [12]
Bis(5-acetoxybenzo[b]furan-2-yl)methanone Drug Info IC50 = 700 nM [9]
Bis(5-aminobenzo[b]furan-2-yl)methanone Drug Info IC50 = 1200 nM [9]
Bis(5-hydroxybenzo[b]furan-2-yl)methanone Drug Info IC50 = 600 nM [9]
Bis(5-methoxybenzo[b]furan-2-yl)methanone Drug Info IC50 = 1000 nM [9]
Bis(6-hydroxybenzo[b]furan-2-yl)methanone Drug Info IC50 = 9700 nM [9]
Bis(benzo[b]furan-2-yl)methanone Drug Info IC50 = 1200 nM [9]
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 = 4.2 nM [4]
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 [12]
Ro-4396686 Drug Info IC50 = 83 nM [5]
Romiplostim Drug Info IC50 = 4050 nM [3]
RPR-101511 Drug Info IC50 = 20 nM [12]
RPR-108514A Drug Info IC50 = 15000 nM
SU-11652 Drug Info IC50 < 70 nM [3]
TG-100435 Drug Info Ki = 2090 nM [8]
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 (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 5 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 6 Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3595-9.
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 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 kinas... Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8.
REF 9 Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones. Bioorg Med Chem. 2007 Mar 1;15(5):2187-97.
REF 10 Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor... J Med Chem. 2009 Jan 22;52(2):278-92.
REF 11 Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endo... Bioorg Med Chem. 2010 May 15;18(10):3575-87.
REF 12 A new series of PDGF receptor tyrosine kinase inhibitors: 3-substituted quinoline derivatives. J Med Chem. 1994 Jul 8;37(14):2129-37.
REF 13 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 14 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.

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