lonafarnib [Ligand Id: 8024] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL298734 (Lonafarnib, Sarasar, SCH 66336, SCH-66336, SCH66336, Zokinvy) |
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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/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 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]
