tipifarnib [Ligand Id: 8025] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL289228 (R-115777, R-11577, Tipifarnib, R115777)
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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]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]
ChEMBL Inhibition of Geranylgeranylprotein transferase-I -catalyzed incorporation of [3H]GGPP into biotin YRASNRSCAIL substrate B 5 pIC50 10000 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1543-1547 [PMID:12699751]
ChEMBL Inhibition of Geranylgeranylprotein transferase-I catalyzed incorporation of [3H]GGPP into biotinYRASNRSCAIL peptide B 5 pIC50 10000 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 4365-4369 [PMID:14643327]
ChEMBL Inhibition of GGTase1 isolated from Kirsten virus-transformed human osteosarcoma cells using biotin-YRASNRSCAIL peptide as substrate after 120 mins in presence of [ 1-[ 3 H](n)]geranylgeranylpyrophosphate by scintillation proximity assay B 6 pIC50 >1000 nM IC50 J Med Chem (2018) 61: 3239-3252 [PMID:28505447]
Geranylgeranyl transferase type I in Bovine (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096987] [UniProtKB: P29702Q5EAD5]
ChEMBL Inhibition of bovine geranylgeranyl transferase type I in presence of Lonafarnib B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2918-2922 [PMID:15911281]
ChEMBL Inhibition of Bovine geranylgeranyltransferase (GGT) B 5.96 pIC50 1100 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 5367-5370 [PMID:15454228]
ChEMBL Inhibition of bovine Geranylgeranyltransferase B 5.96 pIC50 1100 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 5371-5376 [PMID:15454229]
ChEMBL Inhibition of bovine geranylgeranyl transferase B 5.96 pIC50 1100 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2033-2039 [PMID:15808463]
ChEMBL Inhibition of bovine geranylgeranyl transferase type I in presence of Tipifarnib B 5.96 pIC50 1100 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2918-2922 [PMID:15911281]
farnesyltransferase, CAAX box, alpha/farnesyltransferase, CAAX box, beta/Protein farnesyltransferase in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094108] [GtoPdb: 28252826] [UniProtKB: P49354P49356]
ChEMBL Inhibition of FTase isolated from Kirsten virus-transformed human osteosarcoma cells using K-rasB peptide as substrate in presence of [3H]farnesyl PPi by scintillation proximity assay B 8.1 pIC50 7.9 nM IC50 J Med Chem (2018) 61: 3239-3252 [PMID:28505447]
ChEMBL Inhibition of human FTase using farnesyl pyrophosphate as substrate by fluorescent assay B 8.52 pIC50 3 nM IC50 MedChemComm (2013) 4: 962-971
ChEMBL Inhibition of Farnesyltransferase B 9.05 pIC50 0.9 nM IC50 J. Med. Chem. (2004) 47: 612-626 [PMID:14736242]
ChEMBL Inhibition of [3H]FPP incorporation into biotinylated laminB peptide by farnesyl transferase B 9.05 pIC50 0.9 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 4365-4369 [PMID:14643327]
ChEMBL Inhibition of [3H]FPP incorporation into biotinylated lamin B peptide by farnesyl transferase B 9.05 pIC50 0.9 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 4361-4364 [PMID:14643326]
ChEMBL Inhibition of human recombinant FTase using [3H]farnesyldiphosphate B 9.05 pIC50 0.9 nM IC50 MedChemComm (2013) 4: 476-492 [PMID:25530833]
ChEMBL Inhibitory concentration against farnesyltransferase was determined B 9.07 pIC50 0.86 nM IC50 J. Med. Chem. (2004) 47: 1869-1878 [PMID:15055985]
GtoPdb Inhibition of [3H]FPP incorporation into biotinylated laminB peptide by farnesyltransferase protein complex - 9.07 pIC50 0.86 nM IC50 Bioorg Med Chem Lett (2003) 13: 1543-7 [PMID:12699751];
Cancer Res (2001) 61: 131-7 [PMID:11196150]
ChEMBL Inhibition of [3H]FPP incorporation into biotinylated laminB peptide by farnesyl transferase B 9.1 pIC50 0.8 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1543-1547 [PMID:12699751]
Protein farnesyltransferase in Bovine (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095178] [UniProtKB: P29702P49355]
ChEMBL Inhibition of Bovine farnesyltransferase (FTase) B 9.19 pIC50 0.65 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 5367-5370 [PMID:15454228]
ChEMBL Inhibition of bovine farnesyltransferase B 9.19 pIC50 0.65 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 5371-5376 [PMID:15454229]
ChEMBL Inhibition of bovine farnesyltransferase B 9.19 pIC50 0.65 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2033-2039 [PMID:15808463]
ChEMBL In vitro inhibitory activity against farnesyltransferase (FTase) B 9.24 pIC50 0.57 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 processing in H-ras transformed NIH3T3 cells in presence of Lonafarnib F 7 pEC50 100 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 2918-2922 [PMID:15911281]
ChEMBL Inhibition of Ras farnesylation in H-Ras transformed NIH3T3 cells F 8.8 pEC50 1.6 nM EC50 Bioorg. Med. Chem. Lett. (2004) 14: 5367-5370 [PMID:15454228]
ChEMBL Inhibition of H-Ras transformed NIH-3T3-cell proliferation F 8.8 pEC50 1.6 nM EC50 Bioorg. Med. Chem. Lett. (2004) 14: 5371-5376 [PMID:15454229]
ChEMBL Inhibition of Ras processing in H-ras transformed NIH3T3 cells in presence of Tipifarnib F 8.8 pEC50 1.6 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 2918-2922 [PMID:15911281]
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 7.77 pIC50 17 nM IC50 J. Med. Chem. (2005) 48: 3704-3713 [PMID:15916422]

ChEMBL data shown on this page come from version 28:

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]