Target Validation Information
TTD ID	T53389
Target Name	TGF-beta receptor type I (TGFBR1)
Type of Target	Clinical trial
Drug Potency against Target	2-phenyl-N-(pyridin-4-yl)quinazolin-4-amine	Drug Info	IC50 = 2465 nM	[4]
	4-Pyridin-2-yl-5-quinolin-2-yl-thiazol-2-ylamine	Drug Info	IC50 = 3540 nM	[1]
	4-Pyridin-2-yl-5-quinolin-4-yl-thiazol-2-ylamine	Drug Info	IC50 = 420 nM	[1]
	4-Pyridin-3-yl-5-quinolin-4-yl-thiazol-2-ylamine	Drug Info	IC50 = 3980 nM	[1]
	5''-Quinolin-4-yl-[2,4'']bithiazolyl-2''-ylamine	Drug Info	IC50 = 6580 nM	[1]
	GW-788388	Drug Info	IC50 = 18 nM	[3]
	HTS-466284	Drug Info	IC50 = 59 nM	[2]
	IN-1130	Drug Info	IC50 = 36 nM	[6]
	SB-431542	Drug Info	IC50 = 250 nM	[5]
References
REF 1	Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors. J Med Chem. 2004 Aug 26;47(18):4494-506.
REF 2	Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity vers... J Med Chem. 2006 Mar 23;49(6):2138-42.
REF 3	Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orall... J Med Chem. 2006 Apr 6;49(7):2210-21.
REF 4	Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2277-81.
REF 5	Pyrazolone based TGFbetaR1 kinase inhibitors. Bioorg Med Chem Lett. 2010 Jan 1;20(1):326-9.
REF 6	Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kina... Bioorg Med Chem. 2010 Jun 15;18(12):4459-67.

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