Target Validation Information
TTD ID	T86428
Target Name	CAAX farnesyltransferase beta (FNTB)
Type of Target	Literature-reported
Drug Potency against Target		Drug Info	IC50 = 50 nM
	(Z)-2-Methyl-3-tetradecyl-but-2-enedioic acid	Drug Info	IC50 = 60 nM	[10]
	A-313326	Drug Info	IC50 = 0.2 nM	[5]
	ABT-839	Drug Info	IC50 = 1.1 nM	[5]
	ACTINOPLANIC ACID A	Drug Info	IC50 = 230 nM	[10]
	Arteminolide	Drug Info	IC50 = 360 nM	[2]
	BMS-316810	Drug Info	IC50 = 13 nM	[6]
	BMS-404683	Drug Info	IC50 = 1.8 nM	[7]
	CLAVARINONE	Drug Info	IC50 = 8000 nM	[11]
	CYLINDROL A	Drug Info	IC50 = 2200 nM	[10]
	FUSIDIENOL	Drug Info	IC50 = 300 nM	[2]
	H-SMGLPCVVM-OH	Drug Info	IC50 = 1600 nM	[4]
	L-731735	Drug Info	IC50 = 18 nM	[10]
	L-739749	Drug Info	IC50 = 240 nM	[10]
	L-739750	Drug Info	IC50 = 240 nM	[10]
	L-745631	Drug Info	IC50 = 500 nM	[10]
	L-778123	Drug Info	IC50 = 2000 nM	[1]
	MANUMYCIN A	Drug Info	IC50 = 11900 nM	[3]
	PB-27	Drug Info	IC50 = 3.8 nM	[7]
	PB-80	Drug Info	IC50 = 6 nM	[7]
	PB-81	Drug Info	IC50 = 160 nM	[7]
	PD-83176	Drug Info	IC50 = 1600 nM	[8]
	Prenyl pyrophosphate analogue	Drug Info	Ki = 380 nM
	PREUSSOMERIN	Drug Info	IC50 = 1200 nM	[10]
	RPR-113829	Drug Info	IC50 = 17.5 nM	[9]
	RPR-114334	Drug Info	IC50 = 500 nM	[9]
	SCH-44342	Drug Info	IC50 = 250 nM	[10]
References
REF 1	Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase. Bioorg Med Chem Lett. 2001 Feb 26;11(4):537-40.
REF 2	Modeling of binding modes and inhibition mechanism of some natural ligands of farnesyl transferase using molecular docking. J Med Chem. 2002 Mar 28;45(7):1460-5.
REF 3	A novel metal-chelating inhibitor of protein farnesyltransferase. Bioorg Med Chem Lett. 2003 May 5;13(9):1523-6.
REF 4	Improvement of biological activity and proteolytic stability of peptides by coupling with a cyclic peptide. Bioorg Med Chem Lett. 2003 Aug 4;13(15):2583-6.
REF 5	Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase. Bioorg Med Chem Lett. 2005 Jan 3;15(1):153-8.
REF 6	Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors. Bioorg Med Chem Lett. 2005 Apr 1;15(7):1895-9.
REF 7	Protein farnesyltransferase inhibitors exhibit potent antimalarial activity. J Med Chem. 2005 Jun 2;48(11):3704-13.
REF 8	Structure-activity relationships of cysteine-lacking pentapeptide derivatives that inhibit ras farnesyltransferase. J Med Chem. 1997 Jan 17;40(2):192-200.
REF 9	Novel conformationally extended naphthalene-based inhibitors of farnesyltransferase. J Med Chem. 1997 Jun 6;40(12):1763-7.
REF 10	Ras farnesyltransferase: a new therapeutic target. J Med Chem. 1997 Sep 12;40(19):2971-90.
REF 11	Clavaric acid and steroidal analogues as Ras- and FPP-directed inhibitors of human farnesyl-protein transferase. J Med Chem. 1998 Nov 5;41(23):4492-501.

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