Target Validation Information
TTD ID	T99816
Target Name	Gastrin-releasing peptide receptor (GRPR)
Type of Target	Clinical trial
Drug Potency against Target	(CH3)CCO-His-Trp-Ala-Val-Gly-His-Leu-Met-NH2	Drug Info	IC50 = 4.1 nM	[4]
	(D)Phe-Gln-Trp-Ala-Val-Gly-His-Leu-Leu-NH2	Drug Info	Ki = 6.3 nM	[1]
	Ac-His-Trp-Ala-Val-Ala-His-Leu-Met-NH2	Drug Info	IC50 = 180 nM	[4]
	Ac-His-Trp-Ala-Val-D-Ala-His-Leu-Met-NH2	Drug Info	IC50 = 3.2 nM	[4]
	Ac-His-Trp-Ala-Val-Gly-His-Leu-Met-NH2	Drug Info	IC50 = 1.8 nM	[4]
	JMV 1535	Drug Info	Ki = 1 nM	[1]
	JMV 1693	Drug Info	Ki = 53 nM	[1]
	JMV 1719	Drug Info	Ki = 11 nM	[1]
	JMV 1799	Drug Info	Ki = 1.2 nM	[1]
	JMV 1801	Drug Info	Ki = 2 nM	[1]
	JMV 1802	Drug Info	Ki = 0.8 nM	[1]
	JMV 1803	Drug Info	Ki = 2 nM	[1]
	JMV 1813	Drug Info	Ki = 2 nM	[1]
	[(N4-Bzdig)0,Nle14]BB(7-14)	Drug Info	IC50 = 0.6 nM	[2]
	[N40,Pro1,Tyr4,Nle 14]BB	Drug Info	IC50 = 0.15 nM	[2]
	[Tyr4]Bombesin	Drug Info	IC50 = 0.85 nM	[2]
Action against Disease Model	RC-3095	Drug Info	RC-3095 at 1 nM concentration effectively inhibited the bombesin-stimulated growth of CFPAC-1 cells in cultures. In the presence of 1 microM RC-3095 in the culture medi uM, the bombesin-induced growth of CFPAC-1 cells was totally suppressed.	[3]
References
REF 1	Synthesis and biological evaluation of bombesin constrained analogues. J Med Chem. 2000 Jun 15;43(12):2356-61.
REF 2	Potent bombesin-like peptides for GRP-receptor targeting of tumors with 99mTc: a preclinical study. J Med Chem. 2005 Jan 13;48(1):100-10.
REF 3	Lipid modification of GRN163, an N3'-->P5' thio-phosphoramidate oligonucleotide, enhances the potency of telomerase inhibition. Oncogene. 2005 Aug 4;24(33):5262-8.
REF 4	Gastrin releasing peptide antagonists with improved potency and stability. J Med Chem. 1991 Jul;34(7):2102-7.

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