lonafarnib [Ligand Id: 8024] 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: CHEMBL298734 (Lonafarnib, Sarasar, SCH 66336, SCH-66336, SCH66336, Zokinvy) |
|---|
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!
|
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!
|
|
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/geranylgeranyltransferase type-I in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111479] [GtoPdb: 2825] [UniProtKB: P53610, Q04631] | ||||||||
| 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, 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] |
| Geranylgeranyl transferase type I in Bovine (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096987] [UniProtKB: P29702, Q5EAD5] | ||||||||
| 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, subunit alpha/farnesyltransferase, CAAX box, subunit beta/Protein farnesyltransferase in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094108] [GtoPdb: 2825, 2826] [UniProtKB: P49354, P49356] | ||||||||
| 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: P29702, P49355] | ||||||||
| 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, 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 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, subunit beta/farnesyltransferase, CAAX box, subunit alpha/Protein farnesyltransferase in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095197] [GtoPdb: 2826, 2825] [UniProtKB: Q02293, Q04631] | ||||||||
| 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: Q5EI73, Q5EI74] | ||||||||
| 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 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]
