tipifarnib [Ligand Id: 8025] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL289228 (NSC-702818, R-11577, R-115777, R115777, Tipifarnib, Zarnestra) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
