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 527568 | J Med Chem. 2005 Jun 2;48(11):3704-13.Protein farnesyltransferase inhibitors exhibit potent antimalarial activity. | ||||
Ref 526603 | Bioorg Med Chem Lett. 2003 May 5;13(9):1523-6.A novel metal-chelating inhibitor of protein farnesyltransferase. | ||||
Ref 534307 | J Med Chem. 1997 Jan 17;40(2):192-200.Structure-activity relationships of cysteine-lacking pentapeptide derivatives that inhibit ras farnesyltransferase. | ||||
Ref 526296 | J 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 534466 | J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target. | ||||
Ref 534466 | J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target. | ||||
Ref 527568 | J Med Chem. 2005 Jun 2;48(11):3704-13.Protein farnesyltransferase inhibitors exhibit potent antimalarial activity. | ||||
Ref 527568 | J Med Chem. 2005 Jun 2;48(11):3704-13.Protein farnesyltransferase inhibitors exhibit potent antimalarial activity. | ||||
Ref 534466 | J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target. | ||||
Ref 534466 | J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target. | ||||
Ref 534466 | J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target. | ||||
Ref 534405 | J Med Chem. 1997 Jun 6;40(12):1763-7.Novel conformationally extended naphthalene-based inhibitors of farnesyltransferase. | ||||
Ref 534405 | J Med Chem. 1997 Jun 6;40(12):1763-7.Novel conformationally extended naphthalene-based inhibitors of farnesyltransferase. | ||||
Ref 534739 | J 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 534466 | J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target. | ||||
Ref 527491 | Bioorg Med Chem Lett. 2005 Apr 1;15(7):1895-9.Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors. | ||||
Ref 525992 | Bioorg Med Chem Lett. 2001 Feb 26;11(4):537-40.Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase. | ||||
Ref 526670 | Bioorg 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 527321 | Bioorg 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 527321 | Bioorg 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 526296 | J 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 534466 | J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target. | ||||
Ref 527568 | J Med Chem. 2005 Jun 2;48(11):3704-13.Protein farnesyltransferase inhibitors exhibit potent antimalarial activity. | ||||
Ref 534466 | J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target. | ||||
Ref 534466 | J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target. |
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