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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