lonafarnib [Ligand Id: 8024] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL298734 (Lonafarnib, Sarasar, SCH66336, SCH 66336, SCH-66336, Zokinvy)
  • farnesyltransferase, CAAX box, alpha/geranylgeranyltransferase type-I in Rat [ChEMBL: CHEMBL2111479] [GtoPdb: 2825] [UniProtKB: P53610Q04631]
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  • farnesyltransferase, CAAX box, alpha/farnesyltransferase, CAAX box, beta/Protein farnesyltransferase in Human [ChEMBL: CHEMBL2094108] [GtoPdb: 28252826] [UniProtKB: P49354P49356]
  • Protein farnesyltransferase in Bovine [ChEMBL: CHEMBL2095178] [UniProtKB: P29702P49355]
  • farnesyltransferase, CAAX box, alpha/farnesyltransferase, CAAX box, beta/Protein farnesyltransferase in Mouse [ChEMBL: CHEMBL2096912] [GtoPdb: 28252826] [UniProtKB: Q61239Q8K2I1]
  • farnesyltransferase, CAAX box, beta/farnesyltransferase, CAAX box, alpha/Protein farnesyltransferase in Rat [ChEMBL: CHEMBL2095197] [GtoPdb: 28262825] [UniProtKB: Q02293Q04631]
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  • HRAS/Transforming protein p21/H-Ras-1 in Human [ChEMBL: CHEMBL2167] [GtoPdb: 2822] [UniProtKB: P01112]
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  • NRAS in Human [GtoPdb: 2823] [UniProtKB: P01111]
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  • KRAS in Human [GtoPdb: 2824] [UniProtKB: P01116]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
farnesyltransferase, CAAX box, alpha/geranylgeranyltransferase type-I in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111479] [GtoPdb: 2825] [UniProtKB: P53610Q04631]
ChEMBL Inhibition of rat brain GGTase1 assessed as decrease in transfer of [3H]H]geranylgeranyl from [3H]geranylgeranyl PPi to H-Ras-CVLL after 30 mins by liquid scintillation counting method B 6 pIC50 >1000 nM IC50 J Med Chem (2018) 61: 3239-3252 [PMID:28505447]
farnesyltransferase, CAAX box, alpha/Geranylgeranyl transferase type I in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095164] [GtoPdb: 2825] [UniProtKB: P49354P53609]
ChEMBL Inhibition of human GGTase1 in human Burkitt lymphoma (Daudi) cell supernatant using [3H]geranylgeranyl B 4.3 pIC50 >50000 nM IC50 MedChemComm (2013) 4: 476-492 [PMID:25530833]
Geranylgeranyl transferase type I in Bovine (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096987] [UniProtKB: P29702Q5EAD5]
ChEMBL Inhibition of Bovine geranylgeranyltransferase (GGT) B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 5367-5370 [PMID:15454228]
ChEMBL Inhibition of bovine geranylgeranyl transferase B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2033-2039 [PMID:15808463]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: inhibition of DNR efflux (DNR: ? uM) in MDR1-expressing NIH3T3 cells F 5.57 pIC50 2700 nM IC50 Cancer Res. (2001) 61: 7525-7529 [PMID:11606389]
farnesyltransferase, CAAX box, alpha/farnesyltransferase, CAAX box, beta/Protein farnesyltransferase in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094108] [GtoPdb: 28252826] [UniProtKB: P49354P49356]
ChEMBL In vitro inhibition of human Farnesyltransferase B 5.72 pIC50 1900 nM IC50 Bioorg. Med. Chem. Lett. (1999) 9: 1875-1880 [PMID:10406658]
ChEMBL Inhibiting the farnesylation of H-ras proteins in COS-7 monkey cells transiently expressing H-ras[Val12]-CVLS in the whole cell assay. F 8 pIC50 10 nM IC50 J. Med. Chem. (1998) 41: 4890-4902 [PMID:9822558]
ChEMBL Inhibition of FTase in human COS7 cells B 8 pIC50 10 nM IC50 J. Med. Chem. (2010) 53: 6779-6810 [PMID:20925433]
ChEMBL Effect on Ras processing in Cos-1 monkey kidney cells expressing either H-Ras-Val 12-CVLS or H-Ras-Val12. F 8 pIC50 10 nM IC50 J. Med. Chem. (1999) 42: 2651-2661 [PMID:10411485]
ChEMBL Inhibition of Farnesyltransferase B 8.7 pIC50 2 nM IC50 J. Med. Chem. (2004) 47: 612-626 [PMID:14736242]
ChEMBL Inhibition of [3H]FPP incorporation into H-ras CVLS by Farnesyltransferase B 8.7 pIC50 2 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 5899-5902 [PMID:15501065]
ChEMBL Inhibition of human recombinant FTase using [3H]farnesyldiphosphate B 8.72 pIC50 1.9 nM IC50 MedChemComm (2013) 4: 476-492 [PMID:25530833]
ChEMBL Inhibition of Protein farnesyltransferase in Cos-1 monkey kidney cells expressing H-Ras-val B 8.72 pIC50 1.9 nM IC50 J. Med. Chem. (2002) 45: 3854-3864 [PMID:12190309]
ChEMBL Inhibitory activity against Hras Farnesyltransferase (FPT). B 8.72 pIC50 1.9 nM IC50 J. Med. Chem. (1999) 42: 2651-2661 [PMID:10411485]
ChEMBL Compound ability to inhibit the transfer of [3H]- farnesyl from Farnesyltransferase to H-Ras-CVLS, a process that is mediated by FPT B 8.72 pIC50 1.9 nM IC50 J. Med. Chem. (1998) 41: 4890-4902 [PMID:9822558]
ChEMBL Inhibition of Farnesyl protein transferase B 8.72 pIC50 1.9 nM IC50 J. Med. Chem. (1999) 42: 2125-2135 [PMID:10377218]
ChEMBL Inhibitory concentration against farnesyltransferase was determined B 8.72 pIC50 1.9 nM IC50 J. Med. Chem. (2004) 47: 1869-1878 [PMID:15055985]
Protein farnesyltransferase in Bovine (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095178] [UniProtKB: P29702P49355]
ChEMBL Inhibition of Bovine farnesyltransferase (FTase) B 8.08 pIC50 8.3 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 5367-5370 [PMID:15454228]
ChEMBL Inhibition of bovine farnesyltransferase B 8.08 pIC50 8.3 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2033-2039 [PMID:15808463]
ChEMBL In vitro inhibitory activity against farnesyltransferase (FTase) B 8.11 pIC50 7.8 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1367-1371 [PMID:12657284]
farnesyltransferase, CAAX box, alpha/farnesyltransferase, CAAX box, beta/Protein farnesyltransferase in Mouse (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096912] [GtoPdb: 28252826] [UniProtKB: Q61239Q8K2I1]
ChEMBL Inhibition of Ras farnesylation in H-Ras transformed NIH3T3 cells F 7 pEC50 100 nM EC50 Bioorg. Med. Chem. Lett. (2004) 14: 5367-5370 [PMID:15454228]
farnesyltransferase, CAAX box, beta/farnesyltransferase, CAAX box, alpha/Protein farnesyltransferase in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095197] [GtoPdb: 28262825] [UniProtKB: Q02293Q04631]
ChEMBL Inhibition of rat brain FTase assessed as decrease in transfer of [3H]farnesyl from [3H]farnesyl PPi to H-Ras-CVLS after 30 mins by liquid scintillation counting method B 8.72 pIC50 1.9 nM IC50 J Med Chem (2018) 61: 3239-3252 [PMID:28505447]
Protein farnesyltransferase (PFT) in Plasmodium falciparum (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111381] [UniProtKB: Q5EI73Q5EI74]
ChEMBL Inhibition of biotinylated lamin B peptide farnesylation by Plasmodium falciparum farnesyltransferase B 6.6 pIC50 >250 nM IC50 J. Med. Chem. (2005) 48: 3704-3713 [PMID:15916422]
HRAS/Transforming protein p21/H-Ras-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2167] [GtoPdb: 2822] [UniProtKB: P01112]
ChEMBL Compound was measured for inhibition of H-ras NIH tumor cell line under soft agar assay. F 7.15 pIC50 70 nM IC50 J. Med. Chem. (1998) 41: 4890-4902 [PMID:9822558]
GtoPdb Measuring inhibition of farnesylation of HRAS by human farnesyltransferase - 8.72 pIC50 1.9 nM IC50 Cancer Res (1998) 58: 4947-56 [PMID:9810004]
NRAS in Human [GtoPdb: 2823] [UniProtKB: P01111]
GtoPdb Measuring inhibition of farnesylation of NRAS by human farnesyltransferase - 8.55 pIC50 2.8 nM IC50 Cancer Res (1998) 58: 4947-56 [PMID:9810004]
KRAS in Human [GtoPdb: 2824] [UniProtKB: P01116]
GtoPdb Measuring inhibition of farnesylation of KRAS4B by human farnesyltransferase - 8.28 pIC50 5.2 nM IC50 Cancer Res (1998) 58: 4947-56 [PMID:9810004]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]