Target Validation Information
Target ID T86428
Target Name Protein farnesyltransferase beta subunit
Target Type
Discontinued
Drug Potency against Target Prenyl pyrophosphate analogue Drug Info Ki = 380 nM
PB-27 Drug Info IC50 = 3.8 nM [527568]
MANUMYCIN A Drug Info IC50 = 11900 nM [526603]
PD-83176 Drug Info IC50 = 1600 nM [534307]
ARTEMINOLIDE Drug Info IC50 = 360 nM [526296]
PREUSSOMERIN Drug Info IC50 = 1200 nM [534466]
L-739749 Drug Info IC50 = 240 nM [534466]
PB-80 Drug Info IC50 = 6 nM [527568]
BMS-404683 Drug Info IC50 = 1.8 nM [527568]
L-731735 Drug Info IC50 = 18 nM [534466]
CYLINDROL A Drug Info IC50 = 2200 nM [534466]
SCH-44342 Drug Info IC50 = 250 nM [534466]
RPR-113829 Drug Info IC50 = 17.5 nM [534405]
RPR-114334 Drug Info IC50 = 500 nM [534405]
Pseudopeptide derivative Drug Info IC50 = 50 nM
CLAVARINONE Drug Info IC50 = 8000 nM [534739]
ACTINOPLANIC ACID A Drug Info IC50 = 230 nM [534466]
BMS-316810 Drug Info IC50 = 13 nM [527491]
L-778123 Drug Info IC50 = 2000 nM [525992]
H-SMGLPCVVM-OH Drug Info IC50 = 1600 nM [526670]
ABT-839 Drug Info IC50 = 1.1 nM [527321]
A-313326 Drug Info IC50 = 0.2 nM [527321]
FUSIDIENOL Drug Info IC50 = 300 nM [526296]
L-745631 Drug Info IC50 = 500 nM [534466]
PB-81 Drug Info IC50 = 160 nM [527568]
(Z)-2-Methyl-3-tetradecyl-but-2-enedioic acid Drug Info IC50 = 60 nM [534466]
L-739750 Drug Info IC50 = 240 nM [534466]
References
Ref 527568J Med Chem. 2005 Jun 2;48(11):3704-13.Protein farnesyltransferase inhibitors exhibit potent antimalarial activity.
Ref 526603Bioorg Med Chem Lett. 2003 May 5;13(9):1523-6.A novel metal-chelating inhibitor of protein farnesyltransferase.
Ref 534307J Med Chem. 1997 Jan 17;40(2):192-200.Structure-activity relationships of cysteine-lacking pentapeptide derivatives that inhibit ras farnesyltransferase.
Ref 526296J Med Chem. 2002 Mar 28;45(7):1460-5.Modeling of binding modes and inhibition mechanism of some natural ligands of farnesyl transferase using molecular docking.
Ref 534466J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target.
Ref 534466J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target.
Ref 527568J Med Chem. 2005 Jun 2;48(11):3704-13.Protein farnesyltransferase inhibitors exhibit potent antimalarial activity.
Ref 527568J Med Chem. 2005 Jun 2;48(11):3704-13.Protein farnesyltransferase inhibitors exhibit potent antimalarial activity.
Ref 534466J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target.
Ref 534466J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target.
Ref 534466J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target.
Ref 534405J Med Chem. 1997 Jun 6;40(12):1763-7.Novel conformationally extended naphthalene-based inhibitors of farnesyltransferase.
Ref 534405J Med Chem. 1997 Jun 6;40(12):1763-7.Novel conformationally extended naphthalene-based inhibitors of farnesyltransferase.
Ref 534739J Med Chem. 1998 Nov 5;41(23):4492-501.Clavaric acid and steroidal analogues as Ras- and FPP-directed inhibitors of human farnesyl-protein transferase.
Ref 534466J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target.
Ref 527491Bioorg Med Chem Lett. 2005 Apr 1;15(7):1895-9.Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors.
Ref 525992Bioorg Med Chem Lett. 2001 Feb 26;11(4):537-40.Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase.
Ref 526670Bioorg Med Chem Lett. 2003 Aug 4;13(15):2583-6.Improvement of biological activity and proteolytic stability of peptides by coupling with a cyclic peptide.
Ref 527321Bioorg Med Chem Lett. 2005 Jan 3;15(1):153-8.Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase.
Ref 527321Bioorg Med Chem Lett. 2005 Jan 3;15(1):153-8.Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase.
Ref 526296J Med Chem. 2002 Mar 28;45(7):1460-5.Modeling of binding modes and inhibition mechanism of some natural ligands of farnesyl transferase using molecular docking.
Ref 534466J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target.
Ref 527568J Med Chem. 2005 Jun 2;48(11):3704-13.Protein farnesyltransferase inhibitors exhibit potent antimalarial activity.
Ref 534466J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target.
Ref 534466J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target.

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