Target Validation Information
TTD ID	T92144
Target Name	Angiopoietin 1 receptor (TEK)
Type of Target	Clinical trial
Drug Potency against Target	CEP-11981	Drug Info	EC50 = 10.9 nM	[4]
	(4-Phenoxy-phenyl)-quinazolin-4-yl-amine	Drug Info	IC50 = 17870 nM	[1]
	A-420983	Drug Info	IC50 = 1484 nM	[2]
Action against Disease Model	CEP-11981	Drug Info	CEP-7055, a fully synthetic, orally active N,N-dimethylglycine ester of CEP-5214, a C3-(isopropylmethoxy)-fused pyrrolocarbazole with potent pan-vascular endothelial growth factor receptor (VEGFR) kinase inhibitory activity. Reductions in neurologic dysfunction, brain edema, hemorrhage, and intrat uMoral microvessel density (CD34 staining) were observed in glioma-bearing mice receiving CEP-7055 alone, temozolomide alone, and the combination of CEP-7055 and temozolomide relative to vehicle and to temozolomide monotherapy. The administration of CEP-7055 in combination withirinotecan (20 mg/kg/dose i.p. ???5 days), and to a lesser degree with oxaliplatin (10 mg/kg/dose i.v.), showed reductions on primary colon carcinoma and hepatic metastatic burden in the CT-26 t uMormodel relative to that achieved by irinotecan and oxaliplatin monotherapy.	[3]
References
REF 1	Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I. Bioorg Med Chem Lett. 2000 Oct 2;10(19):2167-70.
REF 2	A-420983: a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection. Bioorg Med Chem Lett. 2004 May 17;14(10):2613-6.
REF 3	The effects of the oral, pan-VEGF-R kinase inhibitor CEP-7055 and chemotherapy in orthotopic models of glioblastoma and colon carcinoma in mice. Mol Cancer Ther. 2006 Jul;5(7):1744-53.
REF 4	Therapeutic potential of monoamine transporter substrates. Curr Top Med Chem. 2006;6(17):1845-59.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.