tipifarnib [Ligand Id: 8025] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL289228 (NSC-702818, R-11577, R-115777, R115777, Tipifarnib, Zarnestra) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| farnesyltransferase, CAAX box, subunit alpha/Geranylgeranyl transferase type I in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095164] [GtoPdb: 2825] [UniProtKB: P49354, P53609] | ||||||||
| 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: P29702, Q5EAD5] | ||||||||
| 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, subunit alpha/farnesyltransferase, CAAX box, subunit beta/Protein farnesyltransferase in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094108] [GtoPdb: 2825, 2826] [UniProtKB: P49354, P49356] | ||||||||
| 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: P29702, P49355] | ||||||||
| 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, subunit alpha/farnesyltransferase, CAAX box, subunit beta/Protein farnesyltransferase in Mouse (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096912] [GtoPdb: 2825, 2826] [UniProtKB: Q61239, Q8K2I1] | ||||||||
| 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: Q5EI73, Q5EI74] | ||||||||
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
