lb42908 profile

LB42908: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

LB42908 : A member of the class of pyrrolecarboxamides that is 1H-pyrrole substituted by [1-(3a,7a-dihydro-1,3-benzodioxol-5-ylmethyl)-1H-imidazol-5-yl]methyl, (4-methylpiperazin-1-yl)carbonyl, and naphthalen-1-yl groups at positions 1, 3 and 4, respectively. It is a potent inhibitor of Ras farnesyltransferase (IC50= 0.9nM against H-Ras and 2.4nM against K-Ras) with potential anticancer activity. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

ID Source	ID
PubMed CID	397855
CHEMBL ID	105592
SCHEMBL ID	2287583
MeSH ID	M0416317

Synonym
226927-89-5
lb42908
(1-((1-(benzo[d][1,3]dioxol-5-ylmethyl)-1h-imidazol-5-yl)methyl)-4-(naphthalen-1-yl)-1h-pyrrol-3-yl)(4-methylpiperazin-1-yl)methanone
lb-42908
nsc712392
NCI60_037947
methanone,3- benzodioxol-5- yl)methyl]-1h-imidazol-5-yl]methyl]-4-91-naphthalenyl)-1h-pyrrol-3-yl-
nsc-712392
CHEMBL105592 ,
[1-(3-benzo[1,3]dioxol-5-ylmethyl-3h-imidazol-4-ylmethyl)-4-naphthalen-1-yl-1h-pyrrol-3-yl]-(4-methyl-piperazin-1-yl)-methanone
bdbm50106864
[1-[[3-(1,3-benzodioxol-5-ylmethyl)imidazol-4-yl]methyl]-4-naphthalen-1-ylpyrrol-3-yl]-(4-methylpiperazin-1-yl)methanone
SCHEMBL2287583
6hw5qf8xfd ,
methanone, (1-((1-(1,3-benzodioxol-5-ylmethyl)-1h-imidazol-5-yl)methyl)-4-(1-naphthalenyl)-1h-pyrrol-3-yl)(4-methyl-1-piperazinyl)-
unii-6hw5qf8xfd
piperazine, 1-((1-((1-(1,3-benzodioxol-5-ylmethyl)-1h-imidazol-5-yl)methyl)-4-(1-naphthalenyl)-1h-pyrrol-3-yl)carbonyl)-4-methyl
(1-((1-(1,3-benzodioxol-5-ylmethyl)-1h-imidazol-5-yl)methyl)-4-(1-naphthalenyl)-1h-pyrrol-3-yl)(4-methyl-1-piperazinyl)methanone

Excerpt	Reference	Relevance
" Moreover, the potent antitumor effects of IL-12N220L were further augmented by combination with chemotherapy using farnesyltransferase inhibitor (FTI), LB42908."	( Enhancement of interleukin-12 gene-based tumor immunotherapy by the reduced secretion of p40 subunit and the combination with farnesyltransferase inhibitor. Ha, SJ; Jin, HT; Kim, HJ; Koh, JS; Lee, JB; Sung, YC; Youn, JI, 2005)	0.53

Excerpt	Relevance	Reference
" Repeated dosing of LB42908 in rats did not significantly affect its own metabolism, indicating that long-term administration of LB42908 would not alter its pharmacokinetic profiles."	( Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities. Aeri, K; Chang, M; Kim, HJ; Koh, JS; Lee, SH, 2012)	1

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)	IC50 (µMol)	5.3344	0.0005	0.4716	10.0000	AID73403; AID73406; AID74788
Protein farnesyltransferase subunit beta	Homo sapiens (human)	IC50 (µMol)	0.0017	0.0005	0.2177	2.5000	AID73403; AID73406
Geranylgeranyl transferase type-1 subunit beta	Homo sapiens (human)	IC50 (µMol)	16.0000	0.0073	2.3642	10.0000	AID74788
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
transforming growth factor beta receptor signaling pathway	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
protein farnesylation	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
protein geranylgeranylation	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
positive regulation of Rac protein signal transduction	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
skeletal muscle acetylcholine-gated channel clustering	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
positive regulation of tubulin deacetylation	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
positive regulation of deacetylase activity	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
positive regulation of skeletal muscle acetylcholine-gated channel clustering	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
lipid metabolic process	Protein farnesyltransferase subunit beta	Homo sapiens (human)
protein farnesylation	Protein farnesyltransferase subunit beta	Homo sapiens (human)
protein geranylgeranylation	Geranylgeranyl transferase type-1 subunit beta	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
protein farnesyltransferase activity	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
protein farnesyltransferase activity	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
protein geranylgeranyltransferase activity	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
Rab geranylgeranyltransferase activity	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
protein binding	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
microtubule binding	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
receptor tyrosine kinase binding	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
alpha-tubulin binding	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
molecular adaptor activity	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
CAAX-protein geranylgeranyltransferase activity	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
protein farnesyltransferase activity	Protein farnesyltransferase subunit beta	Homo sapiens (human)
protein farnesyltransferase activity	Protein farnesyltransferase subunit beta	Homo sapiens (human)
protein binding	Protein farnesyltransferase subunit beta	Homo sapiens (human)
zinc ion binding	Protein farnesyltransferase subunit beta	Homo sapiens (human)
protein geranylgeranyltransferase activity	Geranylgeranyl transferase type-1 subunit beta	Homo sapiens (human)
CAAX-protein geranylgeranyltransferase activity	Geranylgeranyl transferase type-1 subunit beta	Homo sapiens (human)
protein binding	Geranylgeranyl transferase type-1 subunit beta	Homo sapiens (human)
zinc ion binding	Geranylgeranyl transferase type-1 subunit beta	Homo sapiens (human)
CAAX-protein geranylgeranyltransferase activity	Geranylgeranyl transferase type-1 subunit beta	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
cytosol	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
plasma membrane	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
CAAX-protein geranylgeranyltransferase complex	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
microtubule associated complex	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
protein farnesyltransferase complex	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
cytoplasm	Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)
cytosol	Protein farnesyltransferase subunit beta	Homo sapiens (human)
microtubule associated complex	Protein farnesyltransferase subunit beta	Homo sapiens (human)
protein farnesyltransferase complex	Protein farnesyltransferase subunit beta	Homo sapiens (human)
CAAX-protein geranylgeranyltransferase complex	Geranylgeranyl transferase type-1 subunit beta	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (116)

Assay ID	Title	Year	Journal	Article
AID667843	Metabolic stability in Sprague-Dawley rat liver microsomal fraction assessed as recovery of N-Deethylated derivative at piperazine moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667846	Metabolic stability in beagle dog liver S9 fraction assessed as recovery of N-Dealkylated derivative at imidazole moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667860	Metabolic stability in Sprague-Dawley rat liver microsomal fraction assessed as recovery of Oxidative derivative at imidazole, pyrrole, or naphthalene moieties at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667698	Metabolic stability in human liver S9 fraction assessed as recovery of N-Demethylated derivative at piperazine moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667990	Inhibition of human CYP2C8-mediated taxol 6alpha-hydroxylation in liver microsomes at 10 uM preincubated for 15 mins prior substrate addition	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID668021	Metabolic stability in Sprague-Dawley rat liver microsomes assessed as rate of formation of N-Oxide derivative at piperazine moiety for 10 mins per mg of protein at 100 mg/kg, po bid for 2 weeks (Rvb = 0.047 +/- 0.007 nmol/min/mg)	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667973	Half life in rhesus monkey liver microsomal fraction at 20 uM by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667864	Metabolic stability in Sprague-Dawley rat liver microsomal fraction assessed as recovery of N-Hydroxylated derivative at piperazine moiety of M1 at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID668024	Metabolic stability in Sprague-Dawley rat liver microsomes assessed as rate of formation of N-Demethylated derivative at piperazine moiety of M5 for 10 mins per mg of protein at 100 mg/kg, po bid for 2 weeks (Rvb = 0.003 +/- 0.002 nmol/min/mg)	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID668022	Metabolic stability in Sprague-Dawley rat liver microsomes assessed as rate of formation of N-Dealkylated derivative at imidazole moiety for 10 mins per mg of protein at 100 mg/kg, po bid for 2 weeks (Rvb = 0.016 +/- 0.005 nmol/min/mg)	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667850	Metabolic stability in human liver microsomal fraction assessed as recovery of N-Dealkylated derivative at imidazole moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667871	Metabolic stability in rhesus monkey liver microsomal fraction assessed as recovery of N-Demethylated derivative at piperazine moiety of M5 at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667975	Half life in human liver microsomal fraction at 20 uM by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667874	Metabolic stability in Sprague-Dawley rat liver microsomal fraction assessed as recovery of N-Dealkylated derivative at piperazine moiety of M4 at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667863	Metabolic stability in Sprague-Dawley rat liver S9 fraction assessed as recovery of N-Hydroxylated derivative at piperazine moiety of M1 at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID668023	Metabolic stability in Sprague-Dawley rat liver microsomes assessed as rate of formation of Catechol derivative by ring opening and O-demethylation at piperonyl moiety for 10 mins per mg of protein at 100 mg/kg, po bid for 2 weeks (Rvb = 0.006 +/- 0.001 n	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667853	Metabolic stability in beagle dog liver S9 fraction assessed as recovery of Catechol derivative by ring opening and O-demethylation at piperonyl moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667691	Metabolic stability in human liver microsomal fraction at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667977	Metabolic stability in Sprague-Dawley rat kidney S9 fraction at 10 ug/mL after 60 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667694	Metabolic stability in beagle dog liver S9 fraction assessed as recovery of N-Demethylated derivative at piperazine moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667865	Metabolic stability in rhesus monkey liver S9 fraction assessed as recovery of N-Hydroxylated derivative at piperazine moiety of M1 at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667834	Metabolic stability in Sprague-Dawley rat liver S9 fraction assessed as recovery of N-Oxide derivative at piperazine moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667873	Metabolic stability in Sprague-Dawley rat liver S9 fraction assessed as recovery of N-Dealkylated derivative at piperazine moiety of M4 at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667848	Metabolic stability in rhesus monkey liver S9 fraction assessed as recovery of N-Dealkylated derivative at imidazole moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667685	Metabolic stability in Sprague-Dawley rat liver microsomal fraction at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667687	Metabolic stability in beagle dog liver microsomal fraction at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667841	Metabolic stability in human liver microsomal fraction assessed as recovery of N-Oxide derivative at piperazine moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID668017	Ex vivo induction of CYP2C9-mediated diclofenac 4-hydroxylation in Sprague-Dawley rat liver microsomes at 100 mg/kg, po bid for 2 weeks relative to control	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID668018	Ex vivo induction of CYP3A4-mediated Nifedipine oxidation in Sprague-Dawley rat liver microsomes at 100 mg/kg, po bid for 2 weeks relative to control	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID668002	Inhibition of human CYP2E1-mediated p-Nitrophenol hydroxylation in liver microsomes at 10 uM preincubated for 15 mins prior substrate addition	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667837	Metabolic stability in beagle dog liver microsomal fraction assessed as recovery of N-Oxide derivative at piperazine moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667872	Metabolic stability in human liver microsomal fraction assessed as recovery of N-Demethylated derivative at piperazine moiety of M5 at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667869	Metabolic stability in beagle dog liver microsomal fraction assessed as recovery of N-Demethylated derivative at piperazine moiety of M5 at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667688	Metabolic stability in rhesus monkey liver S9 fraction at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667880	Half life in Sprague-Dawley rat liver microsomal fraction at 20 uM by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667844	Metabolic stability in Sprague-Dawley rat liver S9 fraction assessed as recovery of N-Dealkylated derivative at imidazole moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667982	Metabolic stability in Sprague-Dawley rat mesentery S9 fraction at 10 ug/mL after 60 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID668004	Inhibition of human CYP3A4-mediated Nifedipine oxidation in liver microsomes at 10 uM preincubated for 15 mins prior substrate addition	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667842	Metabolic stability in Sprague-Dawley rat liver S9 fraction assessed as recovery of N-Deethylated derivative at piperazine moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667868	Metabolic stability in beagle dog liver S9 fraction assessed as recovery of N-Demethylated derivative at piperazine moiety of M5 at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667985	Inhibition of human CYP1A2-mediated phenacetin O-deethylation in liver microsomes at 10 uM coincubated with substrate	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667870	Metabolic stability in rhesus monkey liver S9 fraction assessed as recovery of N-Demethylated derivative at piperazine moiety of M5 at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667859	Metabolic stability in Sprague-Dawley rat liver S9 fraction assessed as recovery of Oxidative derivative at imidazole, pyrrole, or naphthalene moieties at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667840	Metabolic stability in human liver S9 fraction assessed as recovery of N-Oxide derivative at piperazine moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667857	Metabolic stability in human liver S9 fraction assessed as recovery of Catechol derivative by ring opening and O-demethylation at piperonyl moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667861	Metabolic stability in rhesus monkey liver S9 fraction assessed as recovery of Oxidative derivative at imidazole, pyrrole, or naphthalene moieties at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID668020	Metabolic stability in Sprague-Dawley rat liver microsomes assessed as rate of formation of N-Demethylated derivative at piperazine moiety for 10 mins per mg of protein at 100 mg/kg, po bid for 2 weeks (Rvb = 0.141 +/- 0.008 nmol/min/mg)	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667856	Metabolic stability in rhesus monkey liver microsomal fraction assessed as recovery of Catechol derivative by ring opening and O-demethylation at piperonyl moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID668019	Metabolic stability in Sprague-Dawley rat liver microsomes assessed as rate of disappearance for 10 mins per mg of protein at 100 mg/kg, po bid for 2 weeks (Rvb = 0.393 +/- 0.053 nmol/min/mg)	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667991	Inhibition of human CYP2C9-mediated diclofenac 4-hydroxylation in liver microsomes at 10 uM coincubated with substrate	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667835	Metabolic stability in Sprague-Dawley rat liver microsomal fraction assessed as recovery of N-Oxide derivative at piperazine moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667995	Inhibition of human CYP2C19-mediated S-Mephenytoin 4'-hydroxylation in liver microsomes at 10 uM coincubated with substrate	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667881	Half life in beagle dog liver S9 fraction at 20 uM by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667981	Metabolic stability in Sprague-Dawley rat muscle S9 fraction at 10 ug/mL after 60 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667971	Half life in beagle dog liver microsomal fraction at 20 uM by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667993	Inhibition of human CYP2C9-mediated tolbutamide 6-hydroxylation in liver microsomes at 10 uM coincubated with substrate	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID668007	Ex vivo induction of CYP-isozymes in Sprague-Dawley rat liver microsomes at 100 mg/kg, po bid for 2 weeks relative to control	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID668005	Inhibition of human CYP3A4 in liver microsomes	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667876	Metabolic stability in rhesus monkey liver microsomal fraction assessed as recovery of N-Dealkylated derivative at piperazine moiety of M4 at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667697	Metabolic stability in rhesus monkey liver microsomal fraction assessed as recovery of N-Demethylated derivative at piperazine moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667984	Metabolic stability in Sprague-Dawley rat plasma at 10 ug/mL after 60 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667879	Half life in Sprague-Dawley rat liver S9 fraction at 20 uM by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667976	Metabolic stability in Sprague-Dawley rat liver S9 fraction at 10 ug/mL after 60 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667987	Inhibition of human CYP2A6-mediated coumarin 7-hydroxylation in liver microsomes at 10 uM coincubated with substrate	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667974	Half life in human liver S9 fraction at 20 uM by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667684	Metabolic stability in Sprague-Dawley rat liver S9 fraction at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667983	Metabolic stability in Sprague-Dawley rat lung S9 fraction at 10 ug/mL after 60 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667847	Metabolic stability in beagle dog liver microsomal fraction assessed as recovery of N-Dealkylated derivative at imidazole moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID73403	Inhibition of farnesyltransferase activity against H-Ras	2001	Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23	A novel class of highly potent, selective, and non-peptidic inhibitor of Ras farnesyltransferase (FTase).
AID667695	Metabolic stability in beagle dog liver microsomal fraction assessed as recovery of N-Demethylated derivative at piperazine moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID668003	Inhibition of human CYP3A4-mediated Nifedipine oxidation in liver microsomes at 10 uM coincubated with substrate	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667994	Inhibition of human CYP2C9-mediated tolbutamide 6-hydroxylation in liver microsomes at 10 uM preincubated for 15 mins prior substrate addition	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID668001	Inhibition of human CYP2E1-mediated p-Nitrophenol hydroxylation in liver microsomes at 10 uM coincubated with substrate	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667686	Metabolic stability in beagle dog liver S9 fraction at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667972	Half life in rhesus monkey liver S9 fraction at 20 uM by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667875	Metabolic stability in rhesus monkey liver S9 fraction assessed as recovery of N-Dealkylated derivative at piperazine moiety of M4 at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667839	Metabolic stability in rhesus monkey liver microsomal fraction assessed as recovery of N-Oxide derivative at piperazine moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667878	Metabolic stability in human liver microsomal fraction assessed as recovery of N-Dealkylated derivative at piperazine moiety of M4 at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667851	Metabolic stability in Sprague-Dawley rat liver S9 fraction assessed as recovery of Catechol derivative by ring opening and O-demethylation at piperonyl moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667690	Metabolic stability in human liver S9 fraction at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID668000	Inhibition of human CYP2E1-mediated chlorzoxazone 6-hydroxylation in liver microsomes at 10 uM preincubated for 15 mins prior substrate addition	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667699	Metabolic stability in human liver microsomal fraction assessed as recovery of N-Demethylated derivative at piperazine moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667696	Metabolic stability in rhesus monkey liver S9 fraction assessed as recovery of N-Demethylated derivative at piperazine moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667996	Inhibition of human CYP2C19-mediated S-Mephenytoin 4'-hydroxylation in liver microsomes at 10 uM preincubated for 15 mins prior substrate addition	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667867	Metabolic stability in Sprague-Dawley rat liver microsomal fraction assessed as recovery of N-Demethylated derivative at piperazine moiety of M5 at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667980	Metabolic stability in Sprague-Dawley rat large intestine S9 fraction at 10 ug/mL after 60 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667992	Inhibition of human CYP2C9-mediated diclofenac 4-hydroxylation in liver microsomes at 10 uM preincubated for 15 mins prior substrate addition	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667845	Metabolic stability in Sprague-Dawley rat liver microsomal fraction assessed as recovery of N-Dealkylated derivative at imidazole moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667866	Metabolic stability in Sprague-Dawley rat liver S9 fraction assessed as recovery of N-Demethylated derivative at piperazine moiety of M5 at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667862	Metabolic stability in rhesus monkey liver microsomal fraction assessed as recovery of Oxidative derivative at imidazole, pyrrole, or naphthalene moieties at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667693	Metabolic stability in Sprague-Dawley rat liver microsomal fraction assessed as recovery of N-Demethylated derivative at piperazine moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667998	Inhibition of human CYP2D6-mediated dextromethorphan O-demethylation in liver microsomes at 10 uM preincubated for 15 mins prior substrate addition	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667877	Metabolic stability in human liver S9 fraction assessed as recovery of N-Dealkylated derivative at piperazine moiety of M4 at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667988	Inhibition of human CYP2A6-mediated coumarin 7-hydroxylation in liver microsomes at 10 uM preincubated for 15 mins prior substrate addition	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667854	Metabolic stability in beagle dog liver microsomal fraction assessed as recovery of Catechol derivative by ring opening and O-demethylation at piperonyl moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID668016	Ex vivo induction of CYP1A2-mediated phenacetin O-deethylation in Sprague-Dawley rat liver microsomes at 100 mg/kg, po bid for 2 weeks relative to control	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667979	Metabolic stability in Sprague-Dawley rat small intestine S9 fraction at 10 ug/mL after 60 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID668006	Reversible inhibition of human CYP3A4 in liver microsomes by Dixon and Cornish-Bowden plot analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID668013	Toxicity in Sprague-Dawley rat assessed as changes in microsomal protein level at 100 mg/kg, po bid for 2 weeks relative to control	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667858	Metabolic stability in human liver microsomal fraction assessed as recovery of Catechol derivative by ring opening and O-demethylation at piperonyl moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667999	Inhibition of human CYP2E1-mediated chlorzoxazone 6-hydroxylation in liver microsomes at 10 uM coincubated with substrate	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID668010	Toxicity in Sprague-Dawley rat assessed as changes in liver weight at 100 mg/kg, po bid for 2 weeks relative to control	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667838	Metabolic stability in rhesus monkey liver S9 fraction assessed as recovery of N-Oxide derivative at piperazine moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667692	Metabolic stability in Sprague-Dawley rat liver S9 fraction assessed as recovery of N-Demethylated derivative at piperazine moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID74788	Inhibition of Geranylgeranyl transferase type I	2001	Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23	A novel class of highly potent, selective, and non-peptidic inhibitor of Ras farnesyltransferase (FTase).
AID667986	Inhibition of human CYP1A2-mediated phenacetin O-deethylation in liver microsomes at 10 uM preincubated for 15 mins prior substrate addition	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667997	Inhibition of human CYP2D6-mediated dextromethorphan O-demethylation in liver microsomes at 10 uM coincubated with substrate	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667855	Metabolic stability in rhesus monkey liver S9 fraction assessed as recovery of Catechol derivative by ring opening and O-demethylation at piperonyl moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667849	Metabolic stability in rhesus monkey liver microsomal fraction assessed as recovery of N-Dealkylated derivative at imidazole moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667689	Metabolic stability in rhesus monkey liver microsomal fraction at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID73406	Inhibition of farnesyltransferase activity against K-Ras	2001	Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23	A novel class of highly potent, selective, and non-peptidic inhibitor of Ras farnesyltransferase (FTase).
AID667978	Metabolic stability in Sprague-Dawley rat stomach S9 fraction at 10 ug/mL after 60 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667989	Inhibition of human CYP2C8-mediated taxol 6alpha-hydroxylation in liver microsomes at 10 uM coincubated with substrate	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID667836	Metabolic stability in beagle dog liver S9 fraction assessed as recovery of N-Oxide derivative at piperazine moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
AID310774	Inhibition of FTase	2007	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1	Farnesyltransferase pharmacophore model derived from diverse classes of inhibitors.
AID667852	Metabolic stability in Sprague-Dawley rat liver microsomal fraction assessed as recovery of Catechol derivative by ring opening and O-demethylation at piperonyl moiety at 20 uM after 30 mins by LC-MS/MS analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	4 (66.67)	29.6817
2010's	2 (33.33)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	6 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
beta-naphthoflavone beta-Naphthoflavone: A polyaromatic hydrocarbon inducer of P4501A1 and P4501A2 cytochromes. (Proc Soc Exp Biol Med 1994 Dec:207(3):302-308). beta-naphthoflavone : An extended flavonoid resulting from the formal fusion of a benzene ring with the f side of flavone.	2.07	1	extended flavonoid; naphtho-gamma-pyrone; organic heterotricyclic compound	aryl hydrocarbon receptor agonist
ketoconazole 1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.	2.07	1	dichlorobenzene; dioxolane; ether; imidazoles; N-acylpiperazine; N-arylpiperazine
pyrroles 1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.	2.03	1	pyrrole; secondary amine
tipifarnib [no description available]	2.07	1	imidazoles; monochlorobenzenes; primary amino compound; quinolone	antineoplastic agent; apoptosis inducer; EC 2.5.1.58 (protein farnesyltransferase) inhibitor
ritonavir Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.	2.07	1	1,3-thiazoles; carbamate ester; carboxamide; L-valine derivative; ureas	antiviral drug; environmental contaminant; HIV protease inhibitor; xenobiotic
lb42708 LB42708: farnesyltransferase inhibitor; structure in first source	2.03	1

Condition	Relationship Strength	Studies
Cancer of Lung [description not available]	2.07	1
Colorectal Cancer [description not available]	2.07	1
Invasiveness, Neoplasm [description not available]	2.07	1
Lung Neoplasms Tumors or cancer of the LUNG.	2.07	1
Colorectal Neoplasms Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.	2.07	1
Benign Neoplasms [description not available]	2.02	1
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	2.02	1

lb42908

Description

Cross-References

Synonyms (18)

Research Excerpts

Compound-Compound Interactions

Dosage Studied

Protein Targets (3)

Inhibition Measurements

Biological Processes (9)

Molecular Functions (10)

Ceullar Components (6)

Bioassays (116)

Research

Studies (6)

Market Indicators

Research Demand Index: 12.43

Study Types

lb42908

Description

Cross-References

Synonyms (18)

Research Excerpts

Compound-Compound Interactions

Dosage Studied

Protein Targets (3)

Inhibition Measurements

Biological Processes (9)

Molecular Functions (10)

Ceullar Components (6)

Bioassays (116)

Research

Studies (6)

Market Indicators

Research Demand Index: 12.43

Study Types

Related Drugs (6)

Related Conditions (7)