Page last updated: 2024-12-11

sch 44342

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

SCH 44342: inhibits farnesyl protein transferase; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	9845545
CHEMBL ID	289404
SCHEMBL ID	2732013
MeSH ID	M0255806

Synonyms (10)

Synonym
bdbm14454
1-(4-{13-chloro-4-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3,5,7,12,14-hexaen-2-ylidene}piperidin-1-yl)-2-(pyridin-4-yl)ethan-1-one
sch 44342
chembl289404 ,
1-(4-pyridylacetyl)-4-(8-chloro-5,6-dihydro-11h-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)piperidine
sch-44342
SCHEMBL2732013
sch44342
1-[4-(13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene)piperidin-1-yl]-2-pyridin-4-ylethanone
Z2985386801

Research Excerpts

Pharmacokinetics

Excerpt	Reference	Relevance
" Information on serum/plasma concentration, bioavailability and half-life can often aid the discovery process by selecting those candidates with the desired pharmacokinetic parameters."	( Pharmacokinetic screening for the selection of new drug discovery candidates is greatly enhanced through the use of liquid chromatography-atmospheric pressure ionization tandem mass spectrometry. Bryant, MS; Korfmacher, WA; Lin, CC; Nardo, C; Nomeir, AA; Wang, S, 1997)	0.3

Bioavailability

Excerpt	Reference	Relevance
" Information on serum/plasma concentration, bioavailability and half-life can often aid the discovery process by selecting those candidates with the desired pharmacokinetic parameters."	( Pharmacokinetic screening for the selection of new drug discovery candidates is greatly enhanced through the use of liquid chromatography-atmospheric pressure ionization tandem mass spectrometry. Bryant, MS; Korfmacher, WA; Lin, CC; Nardo, C; Nomeir, AA; Wang, S, 1997)	0.3

Dosage Studied

Excerpt	Relevance	Reference
" We report here three structural classes of 8-chlorobenzocycloheptapyridines as novel, nonpeptidic, nonsulfhydryl FPT inhibitors having antitumor activity in mice when dosed orally."	( Antitumor 8-chlorobenzocycloheptapyridines: a new class of selective, nonpeptidic, nonsulfhydryl inhibitors of ras farnesylation. Alvarez, C; Bishop, WR; Bryant, MS; Carr, D; Catino, J; Doll, RJ; Ganguly, AK; James, L; Kaminski, JJ; King, I; Kirschmeier, P; Li, Z; Lin, CC; Liu, M; Mallams, AK; Nardo, C; Njoroge, FG; Petrin, J; Remiszewski, SW; Rossman, RR; Snow, ME; Taveras, AG; Vibulbhan, B; Wang, S; Wong, J, 1997)	0.3

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (5)

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)	IC50 (µMol)	19.5208	0.0005	0.4716	10.0000	AID1797226; AID46504; AID46671; AID71307; AID71310; AID71316; AID72823; AID73121; AID73123; AID73400; AID74645; AID74806
Protein farnesyltransferase subunit beta	Homo sapiens (human)	IC50 (µMol)	0.6250	0.0005	0.2177	2.5000	AID1797226; AID46504; AID46671; AID71307; AID71310; AID71316; AID72823; AID73121; AID73123; AID73400
Geranylgeranyl transferase type-1 subunit beta	Homo sapiens (human)	IC50 (µMol)	114.0000	0.0073	2.3642	10.0000	AID74645; AID74806
Protein farnesyltransferase subunit beta	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.2500	0.0019	0.6507	2.9860	AID73560
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.2500	0.0019	0.5451	2.9860	AID73560
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (9)

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]

Molecular Functions (10)

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]

Ceullar Components (6)

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 (20)

Assay ID	Title	Year	Journal	Article
AID73560	Activity against rat brain Farnesyltransferase	1997	Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19	Ras farnesyltransferase: a new therapeutic target.
AID71316	Inhibitory activity against recombinant human farnesyltransferase	1997	Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25	Identification of novel farnesyl protein transferase inhibitors using three-dimensional database searching methods.
AID73121	Compound ability to inhibit the transfer of [3H]- farnesyl from Farnesyltransferase to H-Ras-CVLS, a process that is mediated by FPT	1998	Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24	(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent.
AID72823	Inhibition of [3H]farnesyl pyrophosphate binding to human farnesyltransferase	2003	Bioorganic & medicinal chemistry letters, May-05, Volume: 13, Issue:9	A novel metal-chelating inhibitor of protein farnesyltransferase.
AID74645	Activity against Geranylgeranyl transferase type I	1997	Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19	Ras farnesyltransferase: a new therapeutic target.
AID46504	In vitro inhibition of Ras processing in COS cells	1998	Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18	Inhibitors of farnesyl protein transferase. Synthesis and biological activity of amide and cyanoguanidine derivatives containing a 5,11-dihydro[1]benzthiepin, benzoxepin, and benzazepin [4,3-b]pyridine ring system.
AID13685	Compound was evaluated for maximum plasma concentration by administering orally at 25 mg/kg in mice	1997	Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26	Structure-activity relationship of 3-substituted N-(pyridinylacetyl)-4- (8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene )- piperidine inhibitors of farnesyl-protein transferase: design and synthesis of in vivo active antitumor comp
AID71310	In vitro FPT potency by measuring the ability to inhibit the transfer of [3H]farnesyl from farnesyl pyrophosphate to H-Ras-CLVS.	1998	Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18	Inhibitors of farnesyl protein transferase. Synthesis and biological activity of amide and cyanoguanidine derivatives containing a 5,11-dihydro[1]benzthiepin, benzoxepin, and benzazepin [4,3-b]pyridine ring system.
AID74806	Compound was tested for the inhibition of Geranylgeranyl transferase type I	1997	Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26	Structure-activity relationship of 3-substituted N-(pyridinylacetyl)-4- (8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene )- piperidine inhibitors of farnesyl-protein transferase: design and synthesis of in vivo active antitumor comp
AID71307	Compound was tested for the inhibition of Farnesyltransferase	1997	Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26	Structure-activity relationship of 3-substituted N-(pyridinylacetyl)-4- (8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene )- piperidine inhibitors of farnesyl-protein transferase: design and synthesis of in vivo active antitumor comp
AID73123	Inhibition of Farnesyltransferase	1999	Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12	Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships.
AID11141	Compound was evaluated for the area under the concentration - time curve by administering intravenously at 25 mg/kg in mice	1997	Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26	Structure-activity relationship of 3-substituted N-(pyridinylacetyl)-4- (8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene )- piperidine inhibitors of farnesyl-protein transferase: design and synthesis of in vivo active antitumor comp
AID73400	Inhibitory concentration against farnesyltransferase was determined	2004	Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8	Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy?
AID24329	half life period is evaluated by administering intravenously at 25 mg/kg in mice	1997	Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26	Structure-activity relationship of 3-substituted N-(pyridinylacetyl)-4- (8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene )- piperidine inhibitors of farnesyl-protein transferase: design and synthesis of in vivo active antitumor comp
AID46494	Compound was tested for the inhibition of COS cells in monkey.	1997	Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26	Structure-activity relationship of 3-substituted N-(pyridinylacetyl)-4- (8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene )- piperidine inhibitors of farnesyl-protein transferase: design and synthesis of in vivo active antitumor comp
AID46671	Inhibiting the farnesylation of H-ras proteins in COS-7 monkey cells transiently expressing H-ras[Val12]-CVLS in the whole cell assay.	1998	Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24	(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent.
AID14764	Pharmacokinetic parameter area under the curve (0-24 hr) for the compound was evaluated in nude mice after oral administration.	1998	Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24	(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent.
AID11142	Compound was evaluated for the area under the concentration - time curve by administering orally at 25 mg/kg in mice	1997	Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26	Structure-activity relationship of 3-substituted N-(pyridinylacetyl)-4- (8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene )- piperidine inhibitors of farnesyl-protein transferase: design and synthesis of in vivo active antitumor comp
AID493017	Wombat Data for BeliefDocking	1997	Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26	Structure-activity relationship of 3-substituted N-(pyridinylacetyl)-4- (8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene )- piperidine inhibitors of farnesyl-protein transferase: design and synthesis of in vivo active antitumor comp
AID1797226	In Vitro Enzyme Assay of FPT from Article 10.1021/jm980462b: \\(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl prote	1998	Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24	(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	10 (83.33)	18.2507
2000's	2 (16.67)	29.6817
2010's	0 (0.00)	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]

Market Indicators

Research Demand Index: 11.62

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

Metric	This Compound (vs All)
Research Demand Index	11.62 (24.57)
Research Supply Index	2.56 (2.92)
Research Growth Index	4.18 (4.65)
Search Engine Demand Index	0.00 (26.88)
Search Engine Supply Index	0.00 (0.95)

This Compound (11.62)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	2 (16.67%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	10 (83.33%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
1,10-phenanthroline 1,10-phenanthroline: RN given refers to parent cpd; inhibits Zn-dependent metalloproteinases	2.01	1	phenanthroline	EC 2.7.1.1 (hexokinase) inhibitor; EC 3.4.19.3 (pyroglutamyl-peptidase I) inhibitor
2,2'-dipyridyl 2,2'-Dipyridyl: A reagent used for the determination of iron.. 2,2'-bipyridine : A bipyridine in which the two pyridine moieties are linked by a bond between positions C-2 and C-2'.	2.01	1	bipyridine	chelator; ferroptosis inhibitor
ethylenediamine ethylenediamine: RN given refers to parent cpd; edamine is the recommended contraction for the ethylenediamine radical. ethylenediamine : An alkane-alpha,omega-diamine in which the alkane is ethane.	2.01	1	alkane-alpha,omega-diamine	GABA agonist
methionine Methionine: A sulfur-containing essential L-amino acid that is important in many body functions.. methionine : A sulfur-containing amino acid that is butyric acid bearing an amino substituent at position 2 and a methylthio substituent at position 4.	1.99	1	aspartate family amino acid; L-alpha-amino acid; methionine zwitterion; methionine; proteinogenic amino acid	antidote to paracetamol poisoning; human metabolite; micronutrient; mouse metabolite; nutraceutical
gliotoxin Gliotoxin: A fungal toxin produced by various species of Trichoderma, Gladiocladium fimbriatum, Aspergillus fumigatus, and Penicillium. It is used as an immunosuppressive agent.. gliotoxin : A pyrazinoindole with a disulfide bridge spanning a dioxo-substituted pyrazine ring; mycotoxin produced by several species of fungi.	3.09	1	dipeptide; organic disulfide; organic heterotetracyclic compound; pyrazinoindole	antifungal agent; EC 2.5.1.58 (protein farnesyltransferase) inhibitor; immunosuppressive agent; mycotoxin; proteasome inhibitor
sch 37370 N-acetyldesloratadine: dual antagonist of platelet-activating factor and histamine	3.12	1
b 581 B 581: blocks farnesylated but not geranylgeranylated or myristylated, oncogenic Ras signaling & transformation. 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.	3.09	1	dipeptide	EC 2.5.1.58 (protein farnesyltransferase) inhibitor; peptidomimetic
lonafarnib lonafarnib: inhibitor of farnesyl protein transferase. 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.	3.79	3	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	antineoplastic agent; EC 2.5.1.58 (protein farnesyltransferase) inhibitor
tipifarnib [no description available]	3.12	1	imidazoles; monochlorobenzenes; primary amino compound; quinolone	antineoplastic agent; apoptosis inducer; EC 2.5.1.58 (protein farnesyltransferase) inhibitor
l 778,123 L-778,123 (free base) : 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.	3.12	1	imidazoles; monochlorobenzenes; nitrile; piperazinone; tertiary amino compound	antineoplastic agent; EC 2.5.1.58 (protein farnesyltransferase) inhibitor; EC 2.5.1.59 (protein geranylgeranyltransferase type I) inhibitor
fti 276 FTI 276: a ras CAAX (C - Cys; A - aliphatic amino acid; X - Ser or Met) peptidomimetic; inhibits farnesyltransferase; FTI-277 is the methyl ester derivative of FTI-276	3.12	1	methionine derivative
bms 214662 7-cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine: a farnesyltransferase inhibitor; structure in first source. 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.	3.12	1	benzenes; benzodiazepine; imidazoles; nitrile; sulfonamide; thiophenes	antineoplastic agent; apoptosis inducer; EC 2.5.1.58 (protein farnesyltransferase) inhibitor
chaetomellic acid a chaetomellic acid A: structure given in first source; an inhibitor of farnesyl-protein transferase	3.09	1
manumycin manumycin: an NSAID; RN given for (1S-(1alpha,3(2E,4E,6S*),5alpha,5(1E,3E,5E),6alpha))-isomer; a farnesyl protein transferase inhibitor; from Streptomyces parvulus; MF C31-H38-N2-O7; structure given in first source. manumycin A : 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.	2.01	1	enamide; epoxide; organic heterobicyclic compound; polyketide; secondary carboxamide; tertiary alcohol	antiatherosclerotic agent; antimicrobial agent; antineoplastic agent; apoptosis inducer; bacterial metabolite; EC 1.8.1.9 (thioredoxin reductase) inhibitor; EC 2.5.1.58 (protein farnesyltransferase) inhibitor; marine metabolite
ggti 298 GGTI 298: inhibits geranylgeranyltransferase-I; structure in first source	3.12	1	leucine derivative
lonafarnib 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 : A benzocycloheptapyridine that is benzo[5,6]cyclohepta[1,2-b]pyridine which is substituted at positions 3 and 10 by bromines, at position 8 by chlorine, and at position 11 by an N-acetylpiperidin-4-yl group in which one of the hydrogens of the acetyl moiety has been replaced by a 1-carbamoylpiperidin-4-yl group.	1.99	1	benzocycloheptapyridine; heteroarylpiperidine; N-acylpiperidine; organobromine compound; organochlorine compound; ureas
actinoplanic acid a actinoplanic acid A: isolated from Actinoplanes; inhibits farnesyl-protein transferase; structure in first source	3.09	1
piperidines Piperidines: A family of hexahydropyridines.	2.9	4

Condition	Relationship Strength	Studies
Benign Neoplasms [description not available]	3.79	2
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.	3.79	2
Experimental Neoplasms [description not available]	1.99	1

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