An EC 2.5.1.* (non-methyl-alkyl or aryl transferase) inhibitor that interferes with the action of protein farnesyltransferase (EC 2.5.1.58), one of the three enzymes in the prenyltransferase group.
ChEBI ID: 64133
| Member | Definition | Class |
|---|---|---|
| b 581 | A dipeptide obtained from the tetrapeptide Cys-Val-Phe-Met by reduction of the amide carbonyl groups of the Cys and Val residues. | B 581 |
| bms 214662 | A member of the class of benzodiazepines that is 2,3,4,5-tetrahydro-1H-1,4-benzodiazepine substituted by (1H-imidazol-5-yl)methyl, benzyl, (thiophen-2-yl)sulfonyl, and cyano groups at positions 1, 3R, 4 and 7, respectively. It is a potent inhibitor of farnesyltransferase (IC50 = 1.35nM) which was under clinical development for the treatment of solid tumors. | BMS-214662 |
| gliotoxin | A pyrazinoindole with a disulfide bridge spanning a dioxo-substituted pyrazine ring; mycotoxin produced by several species of fungi. | gliotoxin |
| l 744832 | A secondary carboxamide resulting from the formal condensation of the carboxy group of 2-{[(2S,3S)-2-{[(2R)-2-amino-3-sulfanylpropyl]amino}-3-methylpentyl]oxy}-3-phenylpropanoic acid with the amino group of propan-2-yl (2S)-2-amino-4-(methylsulfonyl)butanoate. It is a farnesyltransferase inhibitor that exhibits anticancer properties. | L-744,832 |
| l 778,123 | The hydrochloride salt of L-778,123. It is a dual inhibitor of FPTase and GGPTase-I (IC50 of 2nM and 98nm, respectively) and exhibits anti-cancer properties. | L-778,123 hydrochloride |
| l 778,123 | A member of the class of imidazoles that is 1H-imidazole substituted by (4-cyanophenyl)methyl and [4-(3-chlorophenyl)-3-oxopiperazin-1-yl]methyl groups at positions 1 and 5, respectively. It is a dual inhibitor of FPTase and GGPTase-I. | L-778,123 (free base) |
| lonafarnib | A 4-{2-[4-(3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl]-2-oxoethyl}piperidine-1-carboxamide that has R configuration. It is used as oral farnesyltransferase inhibitor. | lonafarnib |
| manumycin | A polyketide with formula C31H38N2O7 initially isolated from Streptomyces parvulus as a result of a random screening program for farnesyl transferase (FTase) inhibitors. It is a natural product that exhibits anticancer and antibiotic properties. | manumycin A |
| tipifarnib | A quinolone that is 1-methylquinolin-2-one which carries a 3-chlorophenyl and an amino(4-chlorophenyl)(1-methyl-imidazol-5-yl)methyl groups at the 4 and 6 positions, respectively (the R-isomer). | tipifarnib |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 70 (5.91) | 18.7374 |
| 1990's | 110 (9.28) | 18.2507 |
| 2000's | 576 (48.61) | 29.6817 |
| 2010's | 333 (28.10) | 24.3611 |
| 2020's | 96 (8.10) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 138 (10.55%) | 5.53% |
| Reviews | 183 (13.99%) | 6.00% |
| Case Studies | 13 (0.99%) | 4.05% |
| Observational | 1 (0.08%) | 0.25% |
| Other | 973 (74.39%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 25.1189 | 1 | 1 |
| Chain A, ATP-DEPENDENT DNA HELICASE Q1 | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 31.6228 | 1 | 1 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 22.3872 | 1 | 1 |
| Chain A, Putative fructose-1,6-bisphosphate aldolase | Giardia intestinalis | Potency | 22.3342 | 1 | 1 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 4.7957 | 1 | 2 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 0.1693 | 1 | 1 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 16.9330 | 1 | 1 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 0.5355 | 1 | 1 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 26.6795 | 1 | 1 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 19.9526 | 1 | 1 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 9.7281 | 4 | 8 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 37.2212 | 1 | 2 |
| G | Vesicular stomatitis virus | Potency | 0.1693 | 1 | 1 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 0.1693 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 0.1693 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 15.9975 | 2 | 13 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 21.4509 | 2 | 2 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 0.5834 | 2 | 3 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 5.7122 | 1 | 2 |
| polyprotein | Zika virus | Potency | 37.2212 | 1 | 2 |
| PPM1D protein | Homo sapiens (human) | Potency | 17.3165 | 1 | 8 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 0.1192 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 24.8115 | 1 | 1 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 12.6534 | 1 | 4 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Acetolactate synthase catalytic subunit, mitochondrial | Saccharomyces cerevisiae S288C | IC50 | 0.2000 | 1 | 1 |
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | IC50 | 2.7000 | 1 | 1 |
| CAAX farnesyltransferase subunit beta | Plasmodium falciparum (malaria parasite P. falciparum) | IC50 | 0.1335 | 1 | 2 |
| Chain A, Protein farnesyltransferase alpha subunit | Rattus norvegicus (Norway rat) | IC50 | 0.0019 | 1 | 1 |
| Chain A, Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Homo sapiens (human) | Ki | 0.0024 | 1 | 2 |
| Chain A, Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Rattus norvegicus (Norway rat) | Ki | 0.0024 | 1 | 2 |
| Chain B, Geranylgeranyl transferase type I beta subunit | Rattus norvegicus (Norway rat) | Ki | 0.0024 | 1 | 2 |
| Chain B, Protein farnesyltransferase beta subunit | Rattus norvegicus (Norway rat) | IC50 | 0.0013 | 1 | 2 |
| Chain B, Protein farnesyltransferase beta subunit | Homo sapiens (human) | Ki | 0.0024 | 1 | 2 |
| Cysteine protease | Trypanosoma brucei rhodesiense | IC50 | 50.0000 | 1 | 1 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 2.8800 | 2 | 2 |
| E3 ubiquitin-protein ligase RNF31 | Homo sapiens (human) | IC50 | 0.5100 | 1 | 1 |
| Geranylgeranyl transferase type-1 subunit beta | Bos taurus (cattle) | IC50 | 4.9143 | 5 | 7 |
| Geranylgeranyl transferase type-1 subunit beta | Homo sapiens (human) | IC50 | 19.9912 | 10 | 12 |
| Geranylgeranyl transferase type-1 subunit beta | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 1 | 1 |
| GTPase HRas | Homo sapiens (human) | IC50 | 0.0242 | 3 | 3 |
| GTPase HRas | Homo sapiens (human) | Ki | 0.0016 | 1 | 1 |
| GTPase KRas | Homo sapiens (human) | IC50 | 1.4742 | 4 | 4 |
| GTPase NRas | Homo sapiens (human) | Ki | 0.0003 | 1 | 1 |
| Histone-lysine N-methyltransferase EHMT2 | Homo sapiens (human) | IC50 | 3.4650 | 2 | 2 |
| Histone-lysine N-methyltransferase SUV39H1 | Homo sapiens (human) | IC50 | 0.2600 | 1 | 1 |
| Mycothiol S-conjugate amidase | Mycobacterium tuberculosis H37Rv | IC50 | 50.0000 | 1 | 1 |
| Protein farnesyltransferase alpha subunit | Plasmodium falciparum (malaria parasite P. falciparum) | IC50 | 0.1335 | 1 | 2 |
| Protein farnesyltransferase subunit beta | Bos taurus (cattle) | IC50 | 0.0145 | 7 | 10 |
| Protein farnesyltransferase subunit beta | Homo sapiens (human) | IC50 | 15.0930 | 35 | 43 |
| Protein farnesyltransferase subunit beta | Rattus norvegicus (Norway rat) | IC50 | 0.0028 | 2 | 2 |
| Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Bos taurus (cattle) | IC50 | 2.0321 | 12 | 17 |
| Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Homo sapiens (human) | IC50 | 16.1617 | 45 | 55 |
| Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Rattus norvegicus (Norway rat) | IC50 | 0.3139 | 4 | 4 |
| Pyruvate kinase PKM | Homo sapiens (human) | IC50 | 22.6400 | 1 | 1 |
| RanBP-type and C3HC4-type zinc finger-containing protein 1 | Homo sapiens (human) | IC50 | 0.5100 | 1 | 1 |
| Sharpin | Homo sapiens (human) | IC50 | 0.5100 | 1 | 1 |
| Squalene synthase | Homo sapiens (human) | IC50 | 0.3000 | 1 | 1 |
| Squalene synthase | Bos taurus (cattle) | IC50 | 0.0210 | 1 | 1 |
| Thioredoxin reductase 1, cytoplasmic | Rattus norvegicus (Norway rat) | IC50 | 0.8100 | 3 | 3 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Geranylgeranyl transferase type-1 subunit beta | Homo sapiens (human) | EC50 | 3.4460 | 2 | 2 |
| Protein farnesyltransferase subunit beta | Homo sapiens (human) | EC50 | 0.0920 | 1 | 1 |
| Protein farnesyltransferase subunit beta | Mus musculus (house mouse) | EC50 | 0.0410 | 4 | 5 |
| Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Homo sapiens (human) | EC50 | 3.4460 | 2 | 2 |
| Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Mus musculus (house mouse) | EC50 | 0.0410 | 4 | 5 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Geranylgeranyl transferase type-1 subunit beta | Homo sapiens (human) | Inhibition | 0.0980 | 1 | 1 |
| Geranylgeranyl transferase type-1 subunit beta | Homo sapiens (human) | MIC | 1.0000 | 2 | 2 |
| GTPase HRas | Homo sapiens (human) | IC90 | 0.0180 | 1 | 1 |
| GTPase KRas | Homo sapiens (human) | IC90 | 0.1080 | 1 | 1 |
| Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Homo sapiens (human) | Inhibition | 0.0980 | 1 | 1 |
| Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Homo sapiens (human) | MIC | 1.0000 | 2 | 2 |