Target Validation Information
Target ID T53389
Target Name TGF-beta receptor type I
Target Type
Clinical Trial
Drug Potency against Target 4-Pyridin-3-yl-5-quinolin-4-yl-thiazol-2-ylamine Drug Info IC50 = 3980 nM [527174]
4-Pyridin-2-yl-5-quinolin-2-yl-thiazol-2-ylamine Drug Info IC50 = 3540 nM [527174]
SB-431542 Drug Info IC50 = 250 nM [530518]
4-Pyridin-2-yl-5-quinolin-4-yl-thiazol-2-ylamine Drug Info IC50 = 420 nM [527174]
HTS-466284 Drug Info IC50 = 59 nM [528084]
IN-1130 Drug Info IC50 = 36 nM [530924]
2-phenyl-N-(pyridin-4-yl)quinazolin-4-amine Drug Info IC50 = 2465 nM [530015]
5''-Quinolin-4-yl-[2,4'']bithiazolyl-2''-ylamine Drug Info IC50 = 6580 nM [527174]
GW-788388 Drug Info IC50 = 18 nM [528108]
References
Ref 527174J Med Chem. 2004 Aug 26;47(18):4494-506.Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.
Ref 527174J Med Chem. 2004 Aug 26;47(18):4494-506.Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.
Ref 530518Bioorg Med Chem Lett. 2010 Jan 1;20(1):326-9. Epub 2009 Oct 29.Pyrazolone based TGFbetaR1 kinase inhibitors.
Ref 527174J Med Chem. 2004 Aug 26;47(18):4494-506.Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.
Ref 528084J Med Chem. 2006 Mar 23;49(6):2138-42.Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7.
Ref 530924Bioorg Med Chem. 2010 Jun 15;18(12):4459-67. Epub 2010 Apr 28.Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.
Ref 530015Bioorg Med Chem Lett. 2009 Apr 15;19(8):2277-81. Epub 2009 Feb 26.Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors.
Ref 527174J Med Chem. 2004 Aug 26;47(18):4494-506.Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.
Ref 528108J Med Chem. 2006 Apr 6;49(7):2210-21.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 orally active transforming growth factor-beta type I receptor inhibitor.

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