Target Validation Information
Target ID T47101
Target Name Basic fibroblast growth factor receptor 1
Target Type
Successful
Drug Potency against Target PD-0173958 Drug Info IC50 = 451 nM [525862]
SU-6668 Drug Info Ki = 1200 nM [552226]
PD-0183812 Drug Info IC50 = 8620 nM [525924]
NP-506 Drug Info IC50 = 100 nM [529888]
BMS-695735 Drug Info IC50 < 5000 nM [529668]
3-Benzimidazol-2-ylhydroquinolin-2-one Drug Info IC50 = 390 nM [529891]
PD-0179483 Drug Info IC50 = 244 nM [525862]
Brivanib Drug Info IC50 = 148 nM [528103]
Ro-4396686 Drug Info IC50 = 92 nM [528018]
PD-0166326 Drug Info IC50 = 61.5 nM [525862]
PD-0180970 Drug Info IC50 = 934 nM [525862]
2-(1H-indazol-3-yl)-1H-benzo[d]imidazole Drug Info IC50 = 1400 nM [528122]
PD-0173955 Drug Info IC50 = 1250 nM [525862]
PD-0173952 Drug Info IC50 = 98.8 nM [525862]
PD-0173956 Drug Info IC50 = 933 nM [525862]
Action against Disease Model SU-6668 To determine whether inhibition of purified receptors translated into a biological effect in cells, the ability of SU6668 to modulate VEGF- and acidic FGF-induced mitogenesis ofendothelial cells was examined. SU6668 inhibited VEGF-driven mitogenesis of HUVECs in a dose-dependent manner with a mean IC50 of 0.34 ???0.05 uM.In comparison, FGF-driven mitogenesis of HUVECs was inhibited with a mean IC50 of 9.6 ???0.4 uM. [552226] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations Impaired neurogenesis, memory and Long term potentiation in brain Fgfr1 -/- [525862]
References
Ref 525862Biochem Pharmacol. 2000 Oct 1;60(7):885-98.Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors.
Ref 552226SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Res. 2000 Aug 1;60(15):4152-60.
Ref 552226SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Res. 2000 Aug 1;60(15):4152-60.
Ref 525924J Med Chem. 2000 Nov 30;43(24):4606-16.Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases.
Ref 529888Bioorg Med Chem Lett. 2009 Feb 1;19(3):745-50. Epub 2008 Dec 10.5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases.
Ref 529668J Med Chem. 2008 Oct 9;51(19):5897-900. Epub 2008 Sep 3.Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor activity.
Ref 529891J Med Chem. 2009 Jan 22;52(2):278-92.Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors.
Ref 525862Biochem Pharmacol. 2000 Oct 1;60(7):885-98.Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors.
Ref 528103J Med Chem. 2006 Apr 6;49(7):2143-6.Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.
Ref 528018Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3. Epub 2006 Feb 3.Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.
Ref 525862Biochem Pharmacol. 2000 Oct 1;60(7):885-98.Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors.
Ref 525862Biochem Pharmacol. 2000 Oct 1;60(7):885-98.Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors.
Ref 528122Bioorg Med Chem Lett. 2006 Jul 1;16(13):3595-9. Epub 2006 Apr 5.Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases.
Ref 525862Biochem Pharmacol. 2000 Oct 1;60(7):885-98.Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors.
Ref 525862Biochem Pharmacol. 2000 Oct 1;60(7):885-98.Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors.
Ref 525862Biochem Pharmacol. 2000 Oct 1;60(7):885-98.Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors.

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