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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