torcetrapib profile

ID Source	ID
PubMed CID	159325
CHEMBL ID	479527
CHEBI ID	49203
SCHEMBL ID	49081
MeSH ID	M0464865

Synonym
torcetrapib ,
cp-529414
D06195
torcetrapib (usan/inn)
262352-17-0
cp-529,414
cp 529414
1(2h)-quinolinecarboxylic acid, 4-(((3,5-bis(trifluoromethyl)phenyl)methyl) (methoxycarbonyl)amino)-2-ethyl-3,4-dihydro-6-(trifluoromethyl)-, ethyl ester, (2r,4s)-
ethyl (2r,4s)-4-((3,5-bis(trifluoromethyl)benzyl)(methoxycarbonyl)amino)-2-ethyl-6-(trifluoromethyl)-3,4-dihydroquinoline-1(2h)-carboxylate
torcetrapib [usan]
(2r,4s)-4-((3,5-bis-trifluoromethylbenzyl)methoxycarbonylamino)-2-ethyl-6-trifluoromethyl-3,4-dihydro-2h-quinoline-1-carboxylic acid ethyl ester
ethyl (2r,4s)-4-{[3,5-bis(trifluoromethyl)benzyl](methoxycarbonyl)amino}-2-ethyl-6-(trifluoromethyl)-3,4-dihydroquinoline-1(2h)-carboxylate
CHEBI:49203 ,
bdbm50312718
CHEMBL479527 ,
ethyl (2r,4s)-4-[[3,5-bis(trifluoromethyl)phenyl]methyl-methoxycarbonylamino]-2-ethyl-6-(trifluoromethyl)-3,4-dihydro-2h-quinoline-1-carboxylate
A818334
ethyl (2r,4s)-4-[[3,5-bis(trifluoromethyl)phenyl]methyl-methoxycarbonyl-amino]-2-ethyl-6-(trifluoromethyl)-3,4-dihydro-2h-quinoline-1-carboxylate
0rp ,
ethyl (2r,4s)-4-{[3,5-bis(trifluoromethyl)benzyl](methoxycarbonyl)amino}-2-ethyl-6-(trifluoromethyl)-3,4-dihydroquinoline-1(2h )-carboxylate
unii-4n4457mv2u
4n4457mv2u ,
1(2h)-quinolinecarboxylic acid, 4-(((3,5-bis(trifluoromethyl)phenyl)methyl) (methoxycarbonyl)amino)-2-ethyl-3,4-dihydro-6-(trifluoromethyl)-, ethyl ester, (2r,4s)-
torcetrapib [usan:inn]
NCGC00346703-01
S2792
c26h25f9n2o4
ethyl (2r,4s)-4-[[3,5-bis(trifluoromethyl)benzyl](methoxycarbonyl)amino]-2-ethyl-6-(trifluoromethyl)-3,4-dihydroquinoline-1(2h)-carboxylate
torcetrapib [mi]
torcetrapib [inn]
torcetrapib [mart.]
torcetrapib [who-dd]
SCHEMBL49081
MLS006010664
smr004701649
CS-3497
(2r, 4s)-4-[(3,5-bis-trifluoromethyl-benzyl)-methoxycarbonyl-amino]-2-ethyl-6-trifluoromethyl-3,4-dihydro-2h-quinoline-1-carboxylic acid ethyl ester
W-202112
(2r,4s)-4-[[[3,5-bis(trifluoromethyl)phenyl]methyl](methoxycarbonyl)amino]-2-ethyl-6-(trifluoromethyl)-1,2,3,4-tetrahydroquinoline-1-carboxylic acid ethyl ester
(2r,4s)-ethyl 4-((3,5-bis(trifluoromethyl)benzyl)(methoxycarbonyl)amino)-2-ethyl-6-(trifluoromethyl)-3,4-dihydroquinoline-1(2h)-carboxylate
AC-35371
HB0879
(2r,4s)-4-[[[3,5-bis(trifluoromethyl)phenyl]methyl](methoxycarbonyl)amino]-2-ethyl-6- (trifluoromethyl)-1,2,3,4-tetrahydroquinoline-1-carboxylic acid ethyl ester
HY-12089
AKOS024458018
DTXSID20180873
mfcd09260777
EX-A081
sr-01000944945
SR-01000944945-1
torcetrapib, >=98% (hplc)
(2r,4s)-4-{[3,5-bis(trifluoromethyl)benzyl](methoxycarbonyl)amino}-2-ethyl-6-(trifluoromethyl)-3,4-dihydroquinoline-1(2h
)-carboxylate
torcetrapib (cp-529414)
DB06281
AS-16356
Q7825530
AMY24146
BRD-K55675242-001-03-0
CCG-270197
1(2h)-quinolinecarboxylic acid, 4-[[[3,5-bis(trifluoromethyl)phenyl]methyl](methoxycarbonyl)amino]-2-ethyl-3,4-dihydro-6-(trifluoromethyl)-, ethyl ester, (2r,4s)-
262350-59-4
(2r,4s)-rel-ethyl 4-((3,5-bis(trifluoromethyl)benzyl)(methoxycarbonyl)amino)-2-ethyl-6-(trifluoromethyl)-3,4-dihydroquinoline-1(2h)-carboxylate
NCGC00346703-03

Research Excerpts

Overview

Torcetrapib is a highly lipophilic (Clog P=7.45) and water insoluble cholesteryl ester transfer protein (CETP) inhibitor developed for the treatment of atherosclerosis. It primarily raises high-density lipoprotein cholesterol levels, and has generally been shown to reduce Atherosclerosis in rabbits.

Excerpt	Reference	Relevance
"Torcetrapib is a cholesteryl ester transfer protein inhibitor with an undesired response of increasing arterial pressure in humans. "	( Cardiovascular effects of torcetrapib in conscious and pentobarbital-anesthetized dogs. Campbell, TJ; Cox, BF; Gintant, GA; Kempf-Grote, AJ; King, AJ; Marsh, KC; Mittelstadt, SW; Nelson, RA; Polakowski, JS; Preusser, LC, 2009)	2.1
"Torcetrapib is a cholesteryl ester transfer protein inhibitor that primarily raises high-density lipoprotein cholesterol levels, and cholesteryl ester transfer protein inhibition has generally been shown to reduce atherosclerosis in rabbits."	( Torcetrapib/atorvastatin combination therapy. Bays, H; Davidson, M; McKenney, J, 2005)	2.49
"Torcetrapib is a highly lipophilic (Clog P=7.45) and water insoluble cholesteryl ester transfer protein (CETP) inhibitor developed for the treatment of atherosclerosis. "	( Development of a self-emulsifying formulation that reduces the food effect for torcetrapib. Erhart, LC; Freel, D; Gumkowski, MJ; Murdande, SB; Perlman, ME; Rodricks, CM; Shah, TS; Thornton-Manning, J, 2008)	2.02
"Torcetrapib is an inhibitor of cholesteryl ester-transfer protein (CETP) that increases high-density lipoprotein (HDL) cholesterol levels."	( New approaches to atherosclerotic cardiovascular disease. the potentialities of torcetrapib. Dueñas-Laita, A; Pérez-Castrillon, JL, 2006)	1.28

Effects

Torcetrapib has been shown to decrease the fractional catabolic rate (FCR) of HDL apolipoproteins (apo) A-I and A-II, enhance the FCR of TRL apoB-100 and apoE. It has no significant effects on fecal cholesterol excretion in humans.

Excerpt	Reference	Relevance
"Torcetrapib has been shown to decrease the fractional catabolic rate (FCR) of HDL apolipoproteins (apo) A-I and A-II, enhance the FCR of TRL apoB-100 and apoE, and decrease TRL apoB-48 production, but has no significant effects on fecal cholesterol excretion in humans."	( Effects of cholesteryl ester transfer protein inhibitors on human lipoprotein metabolism: why have they failed in lowering coronary heart disease risk? Schaefer, EJ, 2013)	1.11
"Torcetrapib has some compound-specific and off-target effects, such as raising blood pressure and aldosterone, which could affect an increase in cardiovascular events and mortality."	( Cholesteryl ester transfer protein inhibitors as high-density lipoprotein raising agents. Shinkai, H, 2009)	1.07
"Torcetrapib has been shown to increase HDL cholesterol levels by 46% when given alone and by 61% when given in combination with atorvastatin, as well as to decrease LDL cholesterol levels by more than that achieved by atorvastatin alone."	( Torcetrapib and atorvastatin: a novel combination therapy for dyslipidemia. Zareba, G, 2006)	2.5

Treatment

Treatment with Torcetrapib did not affect appearance of macrophage cholesterol in plasma and liver, but inhibited its excretion into feces. An inverse relationship was observed between changes in HDL-C and percentage atheroma volume (r=-0.17, P<0.001)

Excerpt	Reference	Relevance
"In torcetrapib-treated patients, an inverse relationship was observed between changes in HDL-C and percentage atheroma volume (r=-0.17, P<0.001)."	( Cholesteryl ester transfer protein inhibition, high-density lipoprotein raising, and progression of coronary atherosclerosis: insights from ILLUSTRATE (Investigation of Lipid Level Management Using Coronary Ultrasound to Assess Reduction of Atherosclerosi Brennan, DM; Nicholls, SJ; Nissen, SE; Tardif, JC; Tuzcu, EM, 2008)	0.86
"Treatment with torcetrapib was associated with an increase in plasma levels of aldosterone and corticosterone and, in vitro, was shown to release aldosterone from adrenocortical cells."	( Torcetrapib-induced blood pressure elevation is independent of CETP inhibition and is accompanied by increased circulating levels of aldosterone. Bloomfield, D; Briscoe, RJ; Brown, PN; Cumiskey, AM; Ehrhart, J; Forrest, MJ; Hershey, JC; Keller, WJ; Ma, X; McPherson, HE; Messina, E; Peterson, LB; Sharif-Rodriguez, W; Siegl, PK; Sinclair, PJ; Sparrow, CP; Stevenson, AS; Sun, SY; Tsai, C; Vargas, H; Walker, M; West, SH; White, V; Woltmann, RF, 2008)	2.13
"Treatment with torcetrapib improves glycemic control in atorvastatin-treated patients with type 2 diabetes mellitus. "	( Effect of torcetrapib on glucose, insulin, and hemoglobin A1c in subjects in the Investigation of Lipid Level Management to Understand its Impact in Atherosclerotic Events (ILLUMINATE) trial. Barter, PJ; Boekholdt, SM; Breazna, A; Kastelein, JJ; Rye, KA; Tardif, JC; Waters, DD, 2011)	1.12
"Treatment with Torcetrapib did not affect appearance of macrophage cholesterol in plasma and liver, but inhibited its excretion into feces."	( The effect of cholesteryl ester transfer protein overexpression and inhibition on reverse cholesterol transport. Blum, D; D'Souza, W; Maugeais, C; Mizrahi, J; Mukhamedova, N; Niesor, E; Sviridov, D; Tchoua, U, 2008)	0.69

Toxicity

This study tested whether genetic variation in the CETP gene is consistent with a protective effect of cholesteryl ester transfer protein (CETP) inhibition on risk of ischemic events and on total mortality.

Excerpt	Reference	Relevance
" There were no dose-related increases in the frequency of adverse events."	( Efficacy and safety of torcetrapib, a novel cholesteryl ester transfer protein inhibitor, in individuals with below-average high-density lipoprotein cholesterol levels. Davidson, MH; McKenney, JM; Revkin, JH; Shear, CL, 2006)	0.64
" The incidence of all-causality and treatment-related adverse events was similar across placebo and torcetrapib treatment groups with no evidence of a dose-related response."	( Efficacy and safety of torcetrapib, a novel cholesteryl ester transfer protein inhibitor, in individuals with below-average high-density lipoprotein cholesterol levels on a background of atorvastatin. Davidson, MH; McKenney, JM; Revkin, JH; Shear, CL, 2006)	0.86
" Using data from the Rating Atherosclerotic Disease Change by Imaging with a New CETP Inhibitor [corrected] (RADIANCE) trials, which assessed the impact of torcetrapib on carotid intima-media thickness (cIMT), we sought to explore potential mechanisms underlying this adverse outcome."	( Cholesteryl ester transfer protein inhibitor torcetrapib and off-target toxicity: a pooled analysis of the rating atherosclerotic disease change by imaging with a new CETP inhibitor (RADIANCE) trials. Basart, DC; Bots, ML; Evans, GW; Grobbee, DE; Kastelein, JJ; Sijbrands, EJ; Stalenhoef, AF; Stroes, ES; van Leuven, SI; Vergeer, M; Visseren, FL, 2008)	0.8
"These analyses support mineralocorticoid-mediated off-target toxicity in patients receiving torcetrapib as a contributing factor to an adverse outcome."	( Cholesteryl ester transfer protein inhibitor torcetrapib and off-target toxicity: a pooled analysis of the rating atherosclerotic disease change by imaging with a new CETP inhibitor (RADIANCE) trials. Basart, DC; Bots, ML; Evans, GW; Grobbee, DE; Kastelein, JJ; Sijbrands, EJ; Stalenhoef, AF; Stroes, ES; van Leuven, SI; Vergeer, M; Visseren, FL, 2008)	0.83
"Efficacy and safety data for dalcetrapib (RO4607381/JTT-705) are presented, following a report of increased mortality and cardiac events with another cholesteryl ester transfer protein inhibitor, torcetrapib, associated with off-target adverse effects (hypertension and the activation of the renin-angiotensin-aldosterone system)."	( Safety and tolerability of dalcetrapib. Buckley, BM; Burgess, T; Capponi, AM; Kallend, D; Kastelein, JJ; Niesor, EJ; Stein, EA; Steiner, G; Stroes, ES, 2009)	0.54
"This study tested whether genetic variation in the CETP gene is consistent with a protective effect of cholesteryl ester transfer protein (CETP) inhibition on risk of ischemic events and on total mortality, without the adverse effects reported for torcetrapib."	( Genetic inhibition of CETP, ischemic vascular disease and mortality, and possible adverse effects. Frikke-Schmidt, R; Johannsen, TH; Nordestgaard, BG; Schou, J; Tybjærg-Hansen, A, 2012)	0.56
"Genetic CETP inhibition associates with reductions in risk of ischemic heart disease, myocardial infarction, ischemic cerebrovascular disease, and ischemic stroke, with a corresponding antiatherogenic lipid profile, and with increased longevity, without adverse effects."	( Genetic inhibition of CETP, ischemic vascular disease and mortality, and possible adverse effects. Frikke-Schmidt, R; Johannsen, TH; Nordestgaard, BG; Schou, J; Tybjærg-Hansen, A, 2012)	0.38
"Early detection of adverse effects of novel therapies and understanding of their mechanisms could improve the safety and efficiency of drug development."	( Improving Assessment of Drug Safety Through Proteomics: Early Detection and Mechanistic Characterization of the Unforeseen Harmful Effects of Torcetrapib. DeLisle, RK; Ganz, P; Hyde, C; Malarstig, A; Murthy, AC; Ostroff, R; Segal, MR; Weiss, SJ; Williams, SA, 2018)	0.68

Pharmacokinetics

The area under the concentration versus time curve from zero to infinity of torcetrapib accounted for approximately 7.5% of the total radioactivity. This review covers the development and validation of assay methods that were used to obtain preclinical and clinical pharmacokinetic parameters.

Excerpt	Reference	Relevance
" The application of the assay to a pharmacokinetic study of (-)-TTB in hamsters is described."	( Development and validation of an enantioselective HPLC-UV method using Chiralpak AD-H to quantify (+)- and (-)-torcetrapib enantiomers in hamster plasma--application to a pharmacokinetic study. Dubey, PK; Mullangi, R; Srinivas, NR; Trivedi, RK, 2007)	0.55
" The availability of pharmacokinetic parameters (clearance: CL/F, volume of distribution: Vd/F, elimination rate constant: K(el) and elimination half-life: t(l/2)) in mice, rats and monkeys, enabled the prediction of human parameter values using the well accepted tool of allometry."	( Use of bile correction factors for allometric prediction of human pharmacokinetic parameters of torcetrapib, a facile cholesteryl ester transfer protein inhibitor. Ahlawat, P; Mullangi, R; Srinivas, NR; Trivedi, RK, )	0.35
" This review covers the development and validation of assay methods that were used to obtain preclinical and clinical pharmacokinetic parameters of torcetrapib."	( Torcetrapib for animal and human pharmacokinetic studies: applicability of chiral and achiral methodologies. Ramesh, M; Srinivas, NR; Trivedi, RK, 2009)	2

Compound-Compound Interactions

Excerpt	Reference	Relevance
" As apoE is a potent ligand for the LDL receptor, we next evaluated the effects of TOR in combination with the LDL-lowering drug berberine, which upregulates LDL receptor expression in dyslipidemic hamsters."	( Upregulating reverse cholesterol transport with cholesteryl ester transfer protein inhibition requires combination with the LDL-lowering drug berberine in dyslipidemic hamsters. Briand, F; Muzotte, E; Sulpice, T; Thieblemont, Q, 2013)	0.39

Bioavailability

Excerpt	Reference	Relevance
"The present study investigated the use of lipid based drug delivery systems to enhance the oral bioavailability of the CETP inhibitors CP-532,623 and torcetrapib."	( In vitro-in vivo evaluation of lipid based formulations of the CETP inhibitors CP-529,414 (torcetrapib) and CP-532,623. Ambler, CM; Brockhurst, B; Edwards, GA; Mack, MC; McEvoy, CL; Perlman, ME; Porter, CJ; Trevaskis, NL, 2014)	0.82
" In addition, in vivo pharmacokinetic studies revealed a significant increase (∼6 to 11-fold) in oral bioavailability in rats dosed with the SLMs and SLNs compared to conventional drug powders."	( Modulating Drug Release and Enhancing the Oral Bioavailability of Torcetrapib with Solid Lipid Dispersion Formulations. Bak, A; Lee, KJ; Leung, DH; Liu, Y; Salituro, GM, 2015)	0.65
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51

Dosage Studied

When the dosage of torcetrapib was doubled (at maximum tolerated dose), HDL increased by over 100%. Male beagles (n = 6) received single oral doses of vehicle or torcetsarib at 10 or 30 mg/kg; BP were acquired simultaneously by HDO and telemetry.

Excerpt	Relevance	Reference
" When the dosage of torcetrapib was doubled (at maximum tolerated dose), HDL increased by over 100%."	( Torcetrapib and atorvastatin: a novel combination therapy for dyslipidemia. Zareba, G, 2006)	2.1
" Torcetrapib was dosed orally (3, 30 mg/kg) and intravenously (0."	( Cardiovascular effects of torcetrapib in conscious and pentobarbital-anesthetized dogs. Campbell, TJ; Cox, BF; Gintant, GA; Kempf-Grote, AJ; King, AJ; Marsh, KC; Mittelstadt, SW; Nelson, RA; Polakowski, JS; Preusser, LC, 2009)	1.56
" Male beagles (n = 6) received single oral doses of vehicle or torcetrapib at 10 or 30 mg/kg; BP were acquired simultaneously by HDO and telemetry from 2 h before dosage until 7 h afterward."	( Comparison of telemetry and high-definition oscillometry for blood pressure measurements in conscious dogs: effects of torcetrapib. Breidenbach, A; Greiter-Wilke, A; Holzgrefe, HH; Jenni, R; Meyer, O, 2010)	0.81
" Dalcetrapib did not change plasma (3)H-cholesterol level but increased (3)H-cholesterol in plasma HDL vs non-HDL, after oral dosing of labeled cholesterol."	( Effect of dalcetrapib, a CETP modulator, on non-cholesterol sterol markers of cholesterol homeostasis in healthy subjects. Blum, D; Chaput, E; Derks, M; Kallend, D; Niesor, EJ; Staempfli, A, 2011)	0.37
" The in vitro drug release and the in vivo absorption of the solid lipid micro- and nanoparticles after oral dosing in rats were evaluated against conventional crystalline drug powders as well as a spray dried amorphous polymer dispersion formulation."	( Modulating Drug Release and Enhancing the Oral Bioavailability of Torcetrapib with Solid Lipid Dispersion Formulations. Bak, A; Lee, KJ; Leung, DH; Liu, Y; Salituro, GM, 2015)	0.65

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

Role	Description
anticholesteremic drug	A substance used to lower plasma cholesterol levels.
CETP inhibitor	Any inhibitor of cholesterylester transfer protein (CETP), which transfers cholesterol from high density lipoproteins (HDL, the 'good' cholesterol-containing particles) to low or very low density lipoproteins (LDL or VLDL, the 'bad' cholesterol-containing particles). Inhibition of this process results in higher HDL levels and lower LDL levels. CETP inhibitors are under investigation as potential drugs to reduce the risk of arteriosclerotic vascular disease (atherosclerosis).
[role information is derived from 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]

Class	Description
quinolines	A class of aromatic heterocyclic compounds each of which contains a benzene ring ortho fused to carbons 2 and 3 of a pyridine ring.
carbamate ester	Any ester of carbamic acid or its N-substituted derivatives.
(trifluoromethyl)benzenes	An organofluorine compound that is (trifluoromethyl)benzene and derivatives arising from substitution of one or more of the phenyl hydrogens.
[compound class information is derived from 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]

Pathway	Proteins	Compounds
Transport of small molecules	392	95
Lipoprotein metabolism	53	9
Plasma lipoprotein remodeling	25	6
HDL remodeling	9	6

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	1.6933	0.0123	7.9835	43.2770	AID1645841
EWS/FLI fusion protein	Homo sapiens (human)	Potency	27.8008	0.0013	10.1577	42.8575	AID1259252; AID1259253; AID1259255; AID1259256
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Cholesteryl ester transfer protein	Homo sapiens (human)	IC50 (µMol)	0.0152	0.0030	0.2169	4.1000	AID1476688; AID1568147; AID464757; AID645306
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
triglyceride metabolic process	Cholesteryl ester transfer protein	Homo sapiens (human)
lipid transport	Cholesteryl ester transfer protein	Homo sapiens (human)
cholesterol metabolic process	Cholesteryl ester transfer protein	Homo sapiens (human)
negative regulation of macrophage derived foam cell differentiation	Cholesteryl ester transfer protein	Homo sapiens (human)
regulation of cholesterol efflux	Cholesteryl ester transfer protein	Homo sapiens (human)
phospholipid transport	Cholesteryl ester transfer protein	Homo sapiens (human)
cholesterol transport	Cholesteryl ester transfer protein	Homo sapiens (human)
positive regulation of cholesterol transport	Cholesteryl ester transfer protein	Homo sapiens (human)
triglyceride transport	Cholesteryl ester transfer protein	Homo sapiens (human)
very-low-density lipoprotein particle remodeling	Cholesteryl ester transfer protein	Homo sapiens (human)
low-density lipoprotein particle remodeling	Cholesteryl ester transfer protein	Homo sapiens (human)
high-density lipoprotein particle remodeling	Cholesteryl ester transfer protein	Homo sapiens (human)
cholesterol homeostasis	Cholesteryl ester transfer protein	Homo sapiens (human)
reverse cholesterol transport	Cholesteryl ester transfer protein	Homo sapiens (human)
phosphatidylcholine metabolic process	Cholesteryl ester transfer protein	Homo sapiens (human)
lipid homeostasis	Cholesteryl ester transfer protein	Homo sapiens (human)
phospholipid homeostasis	Cholesteryl ester transfer protein	Homo sapiens (human)
triglyceride homeostasis	Cholesteryl ester transfer protein	Homo sapiens (human)
positive regulation of phospholipid transport	Cholesteryl ester transfer protein	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
phospholipid transporter activity	Cholesteryl ester transfer protein	Homo sapiens (human)
lipid binding	Cholesteryl ester transfer protein	Homo sapiens (human)
cholesterol binding	Cholesteryl ester transfer protein	Homo sapiens (human)
triglyceride binding	Cholesteryl ester transfer protein	Homo sapiens (human)
phosphatidylcholine binding	Cholesteryl ester transfer protein	Homo sapiens (human)
cholesterol transfer activity	Cholesteryl ester transfer protein	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
extracellular region	Cholesteryl ester transfer protein	Homo sapiens (human)
extracellular space	Cholesteryl ester transfer protein	Homo sapiens (human)
vesicle	Cholesteryl ester transfer protein	Homo sapiens (human)
extracellular exosome	Cholesteryl ester transfer protein	Homo sapiens (human)
high-density lipoprotein particle	Cholesteryl ester transfer protein	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (75)

Assay ID	Title	Year	Journal	Article
AID1347089	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347092	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347106	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347082	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347154	Primary screen GU AMC qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347104	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347098	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID1347108	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347101	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347100	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1568167	In vivo inhibition of CETP in hCETP/apoB-100 dual transgenic mouse assessed as reduction in [3H]-CE transfer at 10 mg/kg, po administered via gavage measured after 2 to 8 hrs by radioactivity based assay	2019	ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6	Discovery of a Lead Triphenylethanamine Cholesterol Ester Transfer Protein (CETP) Inhibitor.
AID394647	Increase in HDLC level in normal chow diet-fed cynomolgus monkey at 30 mg/kg, po for 5 days measured after 10 hrs of last dose	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein i
AID394653	Plasma concentration in normal chow diet-fed cynomolgus monkey at 10 mg/kg, po for 5 days	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein i
AID1476716	Toxicity in cannulated Sprague-Dawley rat assessed as increase in mean arterial pressure at 5 mg/kg, iv by blood pressure transducer based method	2017	Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20	Discovery of a Novel Piperidine-Based Inhibitor of Cholesteryl Ester Transfer Protein (CETP) That Retains Activity in Hypertriglyceridemic Plasma.
AID394649	Ex vivo inhibition of CETP in normal chow diet-fed cynomolgus monkey at 3 mg/kg, po for 5 days by Roar assay	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein i
AID394625	Inhibition of microsomal triglyceride transfer protein by cell based assay	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein i
AID1476715	Toxicty in human NCI-H295R cells assessed as increase in aldosterone levels at 0.1 to 10000 nM after 24 hrs by scintillation proximity assay	2017	Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20	Discovery of a Novel Piperidine-Based Inhibitor of Cholesteryl Ester Transfer Protein (CETP) That Retains Activity in Hypertriglyceridemic Plasma.
AID645306	Inhibition of CETP-mediated BODIPY-labeled cholesteryl ester transfer after 45 mins by FRET analysis	2011	ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6	Discovery of substituted biphenyl oxazolidinone inhibitors of cholesteryl ester transfer protein.
AID394643	Increase in HDLC level in normal chow diet-fed human CETP transgenic mouse model at 30 mg/kg, po for 5 days measured after 2 hrs of last dose	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein i
AID394646	Increase in HDLC level in normal chow diet-fed cynomolgus monkey at 10 mg/kg, po for 5 days measured after 10 hrs of last dose	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein i
AID1783849	Induction of aldosterone elevation in C57BL/6 mouse plasma at 30 mg/kg, po by mass-spectrometry (MS)-based assay	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
AID464756	Inhibition of human plasma CETP assessed as [3H]cholesterol ester transfer after 18 hrs by scintillation proximity assay	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	Novel tetrahydrochinoline derived CETP inhibitors.
AID1568169	Upregulation of CYP11B1 gene expression in human NCI-H295R cells at 0.002 to 0.006 uM measured after 24 hrs relative to control	2019	ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6	Discovery of a Lead Triphenylethanamine Cholesterol Ester Transfer Protein (CETP) Inhibitor.
AID661658	Inhibition of CETP in human plasma assessed as transfer of fluorescently labelled cholesteryl ester to VLDL by fluorimetry	2012	Bioorganic & medicinal chemistry letters, Jun-01, Volume: 22, Issue:11	Design and synthesis of new tetrahydroquinolines derivatives as CETP inhibitors.
AID1292100	In vivo inhibition of CETP in human whole plasma at 120 mg for 14 days	2016	Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8	Design, synthesis and biological evaluation of N,N-3-phenyl-3-benzylaminopropanamide derivatives as novel cholesteryl ester transfer protein inhibitor.
AID699948	Inhibition of [3H]cholesteryl ester transfer from HDL to LDL in human CETP expressed transgenic mouse coexpressing apoB-100 at 30 mg/kg, po measured at 8 hrs relative to predose condition	2012	Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13	Diphenylpyridylethanamine (DPPE) derivatives as cholesteryl ester transfer protein (CETP) inhibitors.
AID394626	Inhibition of endothelial lipase by cell based assay	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein i
AID699954	Inhibition of CETP-mediated [3H]cholesteryl ester transfer activity in human plasma after 2.5 hrs by scintillation counter	2012	Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13	Diphenylpyridylethanamine (DPPE) derivatives as cholesteryl ester transfer protein (CETP) inhibitors.
AID699953	Inhibition of [3H]cholesteryl ester transfer from HDL to LDL in human CETP expressed transgenic mouse coexpressing apoB-100 at 30 mg/kg, po	2012	Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13	Diphenylpyridylethanamine (DPPE) derivatives as cholesteryl ester transfer protein (CETP) inhibitors.
AID464758	Inhibition of human plasma CETP assessed as cholesterol ester transfer after 24 hrs by fluorescence assay	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	Novel tetrahydrochinoline derived CETP inhibitors.
AID1568148	Inhibition of CETP in human whole plasma assessed as reduction in [3H]-CE/HDL transfer incubated for 2.5 hrs by topcount scintillation counting assay	2019	ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6	Discovery of a Lead Triphenylethanamine Cholesterol Ester Transfer Protein (CETP) Inhibitor.
AID394651	Ex vivo inhibition of CETP in normal chow diet-fed cynomolgus monkey at 30 mg/kg, po for 5 days by Roar assay	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein i
AID394650	Ex vivo inhibition of CETP in normal chow diet-fed cynomolgus monkey at 10 mg/kg, po for 5 days by Roar assay	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein i
AID1476690	1-Octanol-phosphate buffered saline partition coefficient, log D of compound at pH 7.6 by tandem mass spectrometry method	2017	Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20	Discovery of a Novel Piperidine-Based Inhibitor of Cholesteryl Ester Transfer Protein (CETP) That Retains Activity in Hypertriglyceridemic Plasma.
AID699952	AUC (0 to 8 hrs) in transgenic mouse expressing human CETP and apoB-100 at 30 mg/kg, po	2012	Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13	Diphenylpyridylethanamine (DPPE) derivatives as cholesteryl ester transfer protein (CETP) inhibitors.
AID394621	Inhibition of PLTP activity assessed as phosphatidylcholine transferred from [3H]phosphatidylcholine (dipalmitoyl)-labeled liposomes to HDL by cell based liquid scintillation counter	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein i
AID699949	Inhibition of [3H]cholesteryl ester transfer from HDL to LDL in human CETP expressed transgenic mouse coexpressing apoB-100 at 30 mg/kg, po measured at 4 hrs relative to predose condition	2012	Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13	Diphenylpyridylethanamine (DPPE) derivatives as cholesteryl ester transfer protein (CETP) inhibitors.
AID394622	Inhibition of LCAT activity in human plasma assessed as change in cholesteryl ester/free cholesterol ratio by cell based assay	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein i
AID1568147	Inhibition of human recombinant CETP assessed as reduction in [3H]CE/HDL transfer incubated for 4 hrs by scintillation proximity assay	2019	ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6	Discovery of a Lead Triphenylethanamine Cholesterol Ester Transfer Protein (CETP) Inhibitor.
AID1500886	Octanol-water partition coefficient, log P of the compound at pH 7.4 by HPLC based shake flask method	2017	European journal of medicinal chemistry, Oct-20, Volume: 139	Discovery of pentacyclic triterpene 3β-ester derivatives as a new class of cholesterol ester transfer protein inhibitors.
AID657499	Inhibition of CETP in human plasma assessed as reduction in fluorescent intensity by fluorescence analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Design, synthesis and structure-activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors.
AID394623	Inhibition of hepatic lipase activity assessed as release of free fatty acid from hydrolysis of VLDL by cell based assay	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein i
AID1476717	Toxicity in cannulated Sprague-Dawley rat assessed as increase in plasma aldosterone levels at 5 mg/kg, iv by radioimmunoassay	2017	Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20	Discovery of a Novel Piperidine-Based Inhibitor of Cholesteryl Ester Transfer Protein (CETP) That Retains Activity in Hypertriglyceridemic Plasma.
AID1568170	Upregulation of CYP11B2 gene expression in human NCI-H295R cells at 0.002 to 0.006 uM measured after 24 hrs relative to control	2019	ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6	Discovery of a Lead Triphenylethanamine Cholesterol Ester Transfer Protein (CETP) Inhibitor.
AID1166825	Terminal elimination half life in healthy human administered as single oral dose	2014	Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21	Potent cholesteryl ester transfer protein inhibitors of reduced lipophilicity: 1,1'-spiro-substituted hexahydrofuroquinoline derivatives.
AID394652	Plasma concentration in normal chow diet-fed cynomolgus monkey at 3 mg/kg, po for 5 days	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein i
AID394638	Increase in HDLC level in high-fat fed hamster model at 30 mg/kg, po for 5 days measured after 2 hrs of last dose	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein i
AID657506	Induction of cortisol synthase mRNA level in human NCI-H295 cells by in vitro branched DNA method	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Design, synthesis and structure-activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors.
AID699951	Inhibition of [3H]cholesteryl ester transfer from HDL to LDL in human CETP expressed transgenic mouse plasma coexpressing apoB-100 at 30 mg/kg, po measured at 2 hrs relative to predose condition	2012	Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13	Diphenylpyridylethanamine (DPPE) derivatives as cholesteryl ester transfer protein (CETP) inhibitors.
AID657507	Induction of aldosterone synthase mRNA level in human NCI-H295 cells by in vitro branched DNA method	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Design, synthesis and structure-activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors.
AID394645	Increase in HDLC level in normal chow diet-fed cynomolgus monkey at 3 mg/kg, po for 5 days measured after 10 hrs of last dose	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein i
AID394654	Plasma concentration in normal chow diet-fed cynomolgus monkey at 30 mg/kg, po for 5 days	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein i
AID1476688	Inhibition of CETP in human plasma measured every 30 mins for 120 mins by fluorescence method	2017	Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20	Discovery of a Novel Piperidine-Based Inhibitor of Cholesteryl Ester Transfer Protein (CETP) That Retains Activity in Hypertriglyceridemic Plasma.
AID394624	Inhibition of lipoprotein lipase activity assessed as release of free fatty acid from hydrolysis of VLDL by cell based assay	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein i
AID464757	Inhibition of CETP assessed as cholesterol ester transfer after 4 hrs by microemulsion based fluorescence assay	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	Novel tetrahydrochinoline derived CETP inhibitors.
AID1347411	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[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	148 (56.70)	29.6817
2010's	105 (40.23)	24.3611
2020's	8 (3.07)	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	28 (10.26%)	5.53%
Reviews	68 (24.91%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	177 (64.84%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (14)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
Phase 3, Multi-Center, Double-Blind, Randomized, Crossover Study Of The Efficacy, Safety, And Tolerability Of Fixed Combination Torcetrapib (Cp-529,414)/Atorvastatin, Compared With Atorvastatin Therapy Alone, And Fenofibrate Alone, In Subjects With Fredri [NCT00145431]	Phase 3	41 participants (Actual)	Interventional	2005-03-31	Terminated
Phase 3 Multi Center, Double Blind, Randomized, Parallel Group Evaluation Of The Fixed Combination Torcetrapib/Atorvastatin, Administered Orally, Once Daily (Qd), Compared With Atorvastatin Alone, On The Occurrence Of Major Cardiovascular Events In Subjec [NCT00134264]	Phase 3	15,067 participants (Actual)	Interventional	2004-07-31	Terminated
A Phase 3, Double Blind, Placebo-Controlled, Randomized, Parallel Group, Multicenter Study of the Efficacy, Safety and Tolerability of Fixed Combination Torcetrapib/Atorvastatin Administered Orally Once Daily for 6 Months, Compared to Atorvastatin Alone o [NCT00138762]	Phase 3	3,800 participants	Interventional	2004-07-31	Completed
Phase 3 Multi-Center, Double-Blind, Randomized, Parallel Group, Carotid B-mode Ultrasound Evaluation of the Anti-Atherosclerotic Efficacy, Safety, and Tolerability of Fixed Combination CP-529,414/Atorvastatin, Administered Orally, Once Daily (QD) for 24 M [NCT00134238]	Phase 3	755 participants (Actual)	Interventional	2003-11-30	Terminated
A Phase 3, Open-Label, Multisite, Randomized, Parallel Group Study of the Efficacy and Safety of Fixed Combination Torcetrapib/Atorvastatin Administered Once Daily (QD) Compared to Simvastatin for 6 Weeks in Subjects With Hypercholesterolemia (A5091031) [NCT00267280]	Phase 3	640 participants	Interventional	2006-01-31	Terminated
Phase 3 Multi-Center, Open Label, Forced Titration Study To Evaluate The Efficacy, Safety, And Tolerability Of Torcetrapib/Atorvastatin Combination Administered Orally, Once Daily (Qd) In Patients With Homozygous Familial Hypercholesterolaemia [NCT00134511]	Phase 3	30 participants	Interventional	2005-03-31	Completed
Phase 3, Multi-Site, Double-Blind, Randomized, Forced Titration, Parallel Group Evaluation Of The Efficacy, Safety, And Tolerability Of Fixed Combination Torcetrapib (CP 529,414)/Atorvastatin Administered Orally, Once Daily (Qd) For Eighteen Weeks, Compar [NCT00134498]	Phase 3	160 participants	Interventional	2005-02-28	Completed
A Phase 3, Double-Blind, Randomized, Multisite Trial Of The Efficacy, Safety, And Tolerability Of The Fixed Combination Torcetrapib/Atorvastatin Administered Orally, Once Daily For 12 Months, Compared To Atorvastatin Alone, Titrated Based On NCEP ATP-III [NCT00137462]	Phase 3	900 participants	Interventional	2004-11-30	Completed
Phase 3 Multi-Center, Double-Blind, Randomized, Parallel Group, Forced Titration Study Of The Efficacy, Safety, And Tolerability Of Torcetrapib/Atorvastatin Compared To Fenofibrate In Subjects With Fredrickson Type IIB Dyslipidemia (Mixed Hyperlipidemia [NCT00139061]	Phase 3	128 participants	Interventional	2005-03-31	Completed
Phase 3 Multi-Center, Double-Blind, Randomized, Parallel Group, Carotid B-Mode Ultrasound Evaluation of the Anti-Atherosclerotic Efficacy, Safety and Tolerability of Fixed Combination CP-529,414/Atorvastatin, Administered Orally, Once Daily (QD) for 24 Mo [NCT00136981]	Phase 3	800 participants	Interventional	2003-12-31	Completed
Phase 3, Multi-Center, Double-Blind, Randomized, Parallel Group, Coronary Artery Intravascular Ultrasound Evaluation of the Anti-Atherosclerotic Efficacy, Safety, and Tolerability of Fixed Combination CP-529,414/Atorvastatin, Administered Orally, Once Dai [NCT00134173]	Phase 3	1,100 participants	Interventional	2003-10-31	Completed
Phase 3, Multi-Center, Double-Blind, Randomized, Parallel Group, Study of the Efficacy, Safety, and Tolerability of Fixed Combination Torcetrapib (CP-529,414) / Atorvastatin Administered Orally, Once Daily (QD) for Six Months, Compared With Maximally Tole [NCT00134485]	Phase 3	400 participants	Interventional	2005-03-31	Completed
Phase 3, Open-Label, Multi-Center, Double-Blind, Randomized, Parallel Group Study Efficacy and Safety of Fixed Combination Torcetrapib/Atorvastatin, Administered Once Daily (QD) Compared to Fixed Combination Ezetimibe/Simvastatin for 6 Weeks in Subjects W [NCT00267267]	Phase 3	1,784 participants	Interventional	2006-01-31	Terminated
A Phase 3, Open-Label, Multisite, Randomized, Parallel Group Study of the Efficacy and Safety of Fixed Combination Torcetrapib/Atorvastatin Administered Once Daily (QD) Compared to Simvastatin for 6 Weeks in Subjects With Hypercholesterolemia (A5091030) [NCT00267254]	Phase 3	640 participants	Interventional	2006-01-31	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
carbamates [no description available]	2.03	1	0	amino-acid anion
niacin Niacin: A water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has PELLAGRA-curative, vasodilating, and antilipemic properties.. vitamin B3 : Any member of a group of vitamers that belong to the chemical structural class called pyridines that exhibit biological activity against vitamin B3 deficiency. Vitamin B3 deficiency causes a condition known as pellagra whose symptoms include depression, dermatitis and diarrhea. The vitamers include nicotinic acid and nicotinamide (and their ionized and salt forms).. nicotinic acid : A pyridinemonocarboxylic acid that is pyridine in which the hydrogen at position 3 is replaced by a carboxy group.	7.48	13	0	pyridine alkaloid; pyridinemonocarboxylic acid; vitamin B3	antidote; antilipemic drug; EC 3.5.1.19 (nicotinamidase) inhibitor; Escherichia coli metabolite; human urinary metabolite; metabolite; mouse metabolite; plant metabolite; vasodilator agent
phosphoric acid phosphoric acid: concise etchant is 37% H3PO4. phosphoric acid : A phosphorus oxoacid that consists of one oxo and three hydroxy groups joined covalently to a central phosphorus atom.	2.05	1	0	phosphoric acids	algal metabolite; fertilizer; human metabolite; NMR chemical shift reference compound; solvent
1-anilino-8-naphthalenesulfonate 1-anilino-8-naphthalenesulfonate: RN given refers to parent cpd. 8-anilinonaphthalene-1-sulfonic acid : A naphthalenesulfonic acid that is naphthalene-1-sulfonic acid substituted by a phenylamino group at position 8.	3.56	2	0	aminonaphthalene; naphthalenesulfonic acid	fluorescent probe
berberine [no description available]	2.08	1	0	alkaloid antibiotic; berberine alkaloid; botanical anti-fungal agent; organic heteropentacyclic compound	antilipemic drug; antineoplastic agent; antioxidant; EC 1.1.1.141 [15-hydroxyprostaglandin dehydrogenase (NAD(+))] inhibitor; EC 1.1.1.21 (aldehyde reductase) inhibitor; EC 1.13.11.52 (indoleamine 2,3-dioxygenase) inhibitor; EC 1.21.3.3 (reticuline oxidase) inhibitor; EC 2.1.1.116 [3'-hydroxy-N-methyl-(S)-coclaurine 4'-O-methyltransferase] inhibitor; EC 2.1.1.122 [(S)-tetrahydroprotoberberine N-methyltransferase] inhibitor; EC 2.7.11.10 (IkappaB kinase) inhibitor; EC 3.1.1.4 (phospholipase A2) inhibitor; EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor; EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; geroprotector; hypoglycemic agent; metabolite; potassium channel blocker
clofibric acid Clofibric Acid: An antilipemic agent that is the biologically active metabolite of CLOFIBRATE.. clofibric acid : A monocarboxylic acid that is isobutyric acid substituted at position 2 by a p-chlorophenoxy group. It is a metabolite of the drug clofibrate.	5.58	3	0	aromatic ether; monocarboxylic acid; monochlorobenzenes	anticholesteremic drug; antilipemic drug; antineoplastic agent; herbicide; marine xenobiotic metabolite; PPARalpha agonist
valproic acid Valproic Acid: A fatty acid with anticonvulsant and anti-manic properties that is used in the treatment of EPILEPSY and BIPOLAR DISORDER. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of VOLTAGE-GATED SODIUM CHANNELS.. valproic acid : A branched-chain saturated fatty acid that comprises of a propyl substituent on a pentanoic acid stem.	2.05	1	0	branched-chain fatty acid; branched-chain saturated fatty acid	anticonvulsant; antimanic drug; EC 3.5.1.98 (histone deacetylase) inhibitor; GABA agent; neuroprotective agent; psychotropic drug; teratogenic agent
fenofibrate Pharmavit: a polyvitamin product, comprising vitamins A, D2, B1, B2, B6, C, E, nicotinamide, & calcium pantothene; may be a promising agent for application to human populations exposed to carcinogenic and genetic hazards of ionizing radiation; RN from CHEMLINE	2.45	2	0	aromatic ether; chlorobenzophenone; isopropyl ester; monochlorobenzenes	antilipemic drug; environmental contaminant; geroprotector; xenobiotic
gemfibrozil [no description available]	2.02	1	0	aromatic ether	antilipemic drug
2-propanol 2-Propanol: An isomer of 1-PROPANOL. It is a colorless liquid having disinfectant properties. It is used in the manufacture of acetone and its derivatives and as a solvent. Topically, it is used as an antiseptic.. propan-2-ol : A secondary alcohol that is propane in which one of the hydrogens attached to the central carbon is substituted by a hydroxy group.	2.03	1	0	secondary alcohol; secondary fatty alcohol	protic solvent
metoprolol Metoprolol: A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.. metoprolol : A propanolamine that is 1-(propan-2-ylamino)propan-2-ol substituted by a 4-(2-methoxyethyl)phenoxy group at position 1.	2.04	1	0	aromatic ether; propanolamine; secondary alcohol; secondary amino compound	antihypertensive agent; beta-adrenergic antagonist; environmental contaminant; geroprotector; xenobiotic
pentobarbital Pentobarbital: A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236). pentobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and sec-pentyl groups.	7.05	1	0	barbiturates	GABAA receptor agonist
probucol Probucol: A drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. (From Martindale, The Extra Pharmacopoeia, 30th ed, p993).. probucol : A dithioketal that is propane-2,2-dithiol in which the hydrogens attached to both sulfur atoms are replaced by 3,5-di-tert-butyl-4-hydroxyphenyl groups. An anticholesteremic drug with antioxidant and anti-inflammatory properties, it is used to treat high levels of cholesterol in blood.	3.27	1	0	dithioketal; polyphenol	anti-inflammatory drug; anticholesteremic drug; antilipemic drug; antioxidant; cardiovascular drug
rofecoxib [no description available]	2.03	1	0	butenolide; sulfone	analgesic; cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug
thalidomide Thalidomide: A piperidinyl isoindole originally introduced as a non-barbiturate hypnotic, but withdrawn from the market due to teratogenic effects. It has been reintroduced and used for a number of immunological and inflammatory disorders. Thalidomide displays immunosuppressive and anti-angiogenic activity. It inhibits release of TUMOR NECROSIS FACTOR-ALPHA from monocytes, and modulates other cytokine action.. thalidomide : A racemate comprising equimolar amounts of R- and S-thalidomide.. 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione : A dicarboximide that is isoindole-1,3(2H)-dione in which the hydrogen attached to the nitrogen is substituted by a 2,6-dioxopiperidin-3-yl group.	2.15	1	0	phthalimides; piperidones
triacetin Triacetin: A triglyceride that is used as an antifungal agent.. triacetin : A triglyceride obtained by acetylation of the three hydroxy groups of glycerol. It has fungistatic properties (based on release of acetic acid) and has been used in the topical treatment of minor dermatophyte infections.	2.04	1	0	triglyceride	adjuvant; antifungal drug; food additive carrier; food emulsifier; food humectant; fuel additive; plant metabolite; solvent
urethane [no description available]	2.05	1	0	carbamate ester	fungal metabolite; mutagen
corticosterone [no description available]	3.55	2	0	11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone	human metabolite; mouse metabolite
spironolactone Spironolactone: A potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p827). spironolactone : A steroid lactone that is 17alpha-pregn-4-ene-21,17-carbolactone substituted by an oxo group at position 3 and an alpha-acetylsulfanyl group at position 7.	3.15	1	0	3-oxo-Delta(4) steroid; oxaspiro compound; steroid lactone; thioester	aldosterone antagonist; antihypertensive agent; diuretic; environmental contaminant; xenobiotic
aldosterone [no description available]	10.55	15	3	11beta-hydroxy steroid; 18-oxo steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid hormone; mineralocorticoid; primary alpha-hydroxy ketone; steroid aldehyde	human metabolite; mouse metabolite
alanine Alanine: A non-essential amino acid that occurs in high levels in its free state in plasma. It is produced from pyruvate by transamination. It is involved in sugar and acid metabolism, increases IMMUNITY, and provides energy for muscle tissue, BRAIN, and the CENTRAL NERVOUS SYSTEM.. alanine : An alpha-amino acid that consists of propionic acid bearing an amino substituent at position 2.	2.15	1	0	alanine zwitterion; alanine; L-alpha-amino acid; proteinogenic amino acid; pyruvate family amino acid	EC 4.3.1.15 (diaminopropionate ammonia-lyase) inhibitor; fundamental metabolite
glutamine Glutamine: A non-essential amino acid present abundantly throughout the body and is involved in many metabolic processes. It is synthesized from GLUTAMIC ACID and AMMONIA. It is the principal carrier of NITROGEN in the body and is an important energy source for many cells.. L-glutamine : An optically active form of glutamine having L-configuration.. glutamine : An alpha-amino acid that consists of butyric acid bearing an amino substituent at position 2 and a carbamoyl substituent at position 4.	3.41	1	1	amino acid zwitterion; glutamine family amino acid; glutamine; L-alpha-amino acid; polar amino acid zwitterion; proteinogenic amino acid	EC 1.14.13.39 (nitric oxide synthase) inhibitor; Escherichia coli metabolite; human metabolite; metabolite; micronutrient; mouse metabolite; nutraceutical; Saccharomyces cerevisiae metabolite
dithionitrobenzoic acid Dithionitrobenzoic Acid: A standard reagent for the determination of reactive sulfhydryl groups by absorbance measurements. It is used primarily for the determination of sulfhydryl and disulfide groups in proteins. The color produced is due to the formation of a thio anion, 3-carboxyl-4-nitrothiophenolate.. dithionitrobenzoic acid : An organic disulfide that results from the formal oxidative dimerisation of 2-nitro-5-thiobenzoic acid. An indicator used to quantify the number or concentration of thiol groups.	2.1	1	0	nitrobenzoic acid; organic disulfide	indicator
2-acetyltributylcitrate [no description available]	2.58	2	0	organooxygen compound
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.	14.48	46	23	pyrrole; secondary amine
thiazoles [no description available]	2.05	1	0	1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
linuron Linuron: A selective pre- and post-emergence herbicide. (From Merck Index, 11th ed). linuron : A member of the class of phenylureas that is N-methyl urea substituted by a methoxy group at position 1 and a 3,4-dichlorophenyl group at position 3.	2.21	1	0	dichlorobenzene; phenylureas	agrochemical; environmental contaminant; herbicide; xenobiotic
fluorobenzenes Fluorobenzenes: Derivatives of BENZENE that contain FLUORINE.. monofluorobenzene : The simplest member of the class of monofluorobenzenes that is benzene carrying a single fluoro substituent.. fluorobenzenes : Any fluoroarene that is a benzene or a substituted benzene carrying at least one fluoro group.	3.55	2	0	monofluorobenzenes	NMR chemical shift reference compound
oleanolic acid [no description available]	2.15	1	0	hydroxy monocarboxylic acid; pentacyclic triterpenoid	plant metabolite
dihydrotestosterone Dihydrotestosterone: A potent androgenic metabolite of TESTOSTERONE. It is produced by the action of the enzyme 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE.. 17beta-hydroxyandrostan-3-one : A 17beta-hydroxy steroid that is testosterone in which the 4-5 double bond has been reduced to a single bond with unspecified configuration at position 5.. 17beta-hydroxy-5alpha-androstan-3-one : A 17beta-hydroxy steroid that is testosterone in which the 4,5 double bond has been reduced to a single bond with alpha-configuration at position 5.	3.15	1	0	17beta-hydroxy steroid; 17beta-hydroxyandrostan-3-one; 3-oxo-5alpha-steroid	androgen; Daphnia magna metabolite; human metabolite; mouse metabolite
d-alpha tocopherol Vitamin E: A generic descriptor for all TOCOPHEROLS and TOCOTRIENOLS that exhibit ALPHA-TOCOPHEROL activity. By virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus, these compounds exhibit varying degree of antioxidant activity, depending on the site and number of methyl groups and the type of ISOPRENOIDS.. tocopherol : A collective name for a group of closely related lipids that contain a chroman-6-ol nucleus substituted at position 2 by a methyl group and by a saturated hydrocarbon chain consisting of three isoprenoid units. They are designated as alpha-, beta-, gamma-, and delta-tocopherol depending on the number and position of additional methyl substituents on the aromatic ring. Tocopherols occur in vegetable oils and vegetable oil products, almost exclusively with R,R,R configuration. Tocotrienols differ from tocopherols only in having three double bonds in the hydrocarbon chain.. vitamin E : Any member of a group of fat-soluble chromanols that exhibit biological activity against vitamin E deficiency. The vitamers in this class consists of a chroman-6-ol core which is substituted at position 2 by a methyl group and (also at position 2) either a saturated or a triply-unsaturated hydrocarbon chain consisting of three isoprenoid units. The major function of vitamin E is to act as a natural antioxidant by scavenging free radicals and molecular oxygen.. (R,R,R)-alpha-tocopherol : An alpha-tocopherol that has R,R,R configuration. The naturally occurring stereoisomer of alpha-tocopherol, it is found particularly in sunflower and olive oils.	2.05	1	0	alpha-tocopherol	algal metabolite; antiatherogenic agent; anticoagulant; antioxidant; antiviral agent; EC 2.7.11.13 (protein kinase C) inhibitor; immunomodulator; micronutrient; nutraceutical; plant metabolite
octylmethoxycinnamate octylmethoxycinnamate: a sunscreen used for prevention of DNA photodamage	2.58	2	0	cinnamate ester
octocrylene [no description available]	2.21	1	0	diarylmethane
vinyl carbamate vinyl carbamate: promutagen & more carcinogenic analog of ethyl carbamate (urethane); structure	2.05	1	0	carbamate ester
phenyl acetate phenyl acetate: The ester formed between phenol and acetic acid. Don't confuse with phenylacetic acid derivatives listed under PHENYLACETATES.. phenyl acetate : An acetate ester obtained by the formal condensation of phenol with acetic acid.	3.19	1	0	benzenes; phenyl acetates
colforsin Colforsin: Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.	2.58	2	0	acetate ester; cyclic ketone; labdane diterpenoid; organic heterotricyclic compound; tertiary alpha-hydroxy ketone; triol	adenylate cyclase agonist; anti-HIV agent; antihypertensive agent; plant metabolite; platelet aggregation inhibitor; protein kinase A agonist
simvastatin Simvastatin: A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.. simvastatin : A member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug.	2.02	1	0	delta-lactone; fatty acid ester; hexahydronaphthalenes; statin (semi-synthetic)	EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor; EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor; ferroptosis inducer; geroprotector; prodrug
pravastatin Pravastatin: An antilipemic fungal metabolite isolated from cultures of Nocardia autotrophica. It acts as a competitive inhibitor of HMG CoA reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES).. pravastatin : A carboxylic ester resulting from the formal condensation of (S)-2-methylbutyric acid with the hydroxy group adjacent to the ring junction of (3R,5R)-7-[(1S,2S,6S,8S,8aR)-6,8-dihydroxy-2-methyl-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]-3,5-dihydroxyheptanoic acid. Derived from microbial transformation of mevastatin, pravastatin is a reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA). The sodium salt is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but has the advantage of fewer side effects compared with lovastatin and simvastatin.	2.44	2	0	3-hydroxy carboxylic acid; carbobicyclic compound; carboxylic ester; hydroxy monocarboxylic acid; secondary alcohol; statin (semi-synthetic)	anticholesteremic drug; environmental contaminant; metabolite; xenobiotic
atorvastatin [no description available]	14.57	47	23	aromatic amide; dihydroxy monocarboxylic acid; monofluorobenzenes; pyrroles; statin (synthetic)	environmental contaminant; xenobiotic
ursolic acid [no description available]	2.15	1	0	hydroxy monocarboxylic acid; pentacyclic triterpenoid	geroprotector; plant metabolite
betulinic acid [no description available]	2.15	1	0	hydroxy monocarboxylic acid; pentacyclic triterpenoid	anti-HIV agent; anti-inflammatory agent; antimalarial; antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; plant metabolite
lathosterol lathosterol: RN given refers to (3beta,5alpha)-isomer. 5alpha-cholest-7-en-3beta-ol : A cholestanoid that is (5alpha)-cholest-7-ene substituted by a beta-hydroxy group at position 3.	3.45	1	1	3beta-sterol; C27-steroid; cholestanoid; Delta(7)-sterol	human metabolite; mouse metabolite
sultosilic acid sultosilic acid: RN given refers to parent cpd; structure given in first source	4.04	1	0	benzenesulfonate ester
suplatast tosilate [no description available]	2.05	1	0
oxazolidin-2-one Oxazolidinones: Derivatives of oxazolidin-2-one. They represent an important class of synthetic antibiotic agents.. oxazolidin-2-one : An oxazolidinone that is 1,3-oxazolidine with an oxo substituent at position 2.. oxazolidinone : An oxazolidine containing one or more oxo groups.	9.55	37	0	carbamate ester; oxazolidinone	metabolite
rosiglitazone [no description available]	3.54	2	0	aminopyridine; thiazolidinediones	EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; insulin-sensitizing drug
diosgenin [no description available]	2.05	1	0	3beta-sterol; hexacyclic triterpenoid; sapogenin; spiroketal	antineoplastic agent; antiviral agent; apoptosis inducer; metabolite
bosentan anhydrous Bosentan: A sulfonamide and pyrimidine derivative that acts as a dual endothelin receptor antagonist used to manage PULMONARY HYPERTENSION and SYSTEMIC SCLEROSIS.	2.07	1	0	primary alcohol; pyrimidines; sulfonamide	antihypertensive agent; endothelin receptor antagonist
deoxyglucose Deoxyglucose: 2-Deoxy-D-arabino-hexose. An antimetabolite of glucose with antiviral activity.. deoxyglucose : A deoxyhexose comprising glucose having at least one hydroxy group replaced by hydrogen.	2.1	1	0
caprylates Caprylates: Derivatives of caprylic acid. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain a carboxy terminated eight carbon aliphatic structure.. octanoate : A straight-chain saturated fatty acid anion that is the conjugate base of octanoic acid (caprylic acid); believed to block adipogenesis.	2.04	1	0	fatty acid anion 8:0; straight-chain saturated fatty acid anion	human metabolite; Saccharomyces cerevisiae metabolite
proline Proline: A non-essential amino acid that is synthesized from GLUTAMIC ACID. It is an essential component of COLLAGEN and is important for proper functioning of joints and tendons.. proline : An alpha-amino acid that is pyrrolidine bearing a carboxy substituent at position 2.	3.41	1	1	amino acid zwitterion; glutamine family amino acid; L-alpha-amino acid; proline; proteinogenic amino acid	algal metabolite; compatible osmolytes; Escherichia coli metabolite; micronutrient; mouse metabolite; nutraceutical; Saccharomyces cerevisiae metabolite
ezetimibe Ezetimibe: An azetidine derivative and ANTICHOLESTEREMIC AGENT that inhibits intestinal STEROL absorption. It is used to reduce total CHOLESTEROL; LDL CHOLESTEROL, and APOLIPOPROTEINS B in the treatment of HYPERLIPIDEMIAS.. ezetimibe : A beta-lactam that is azetidin-2-one which is substituted at 1, 3, and 4 by p-fluorophenyl, 3-(p-fluorophenyl)-3-hydroxypropyl, and 4-hydroxyphenyl groups, respectively (the 3R,3'S,4S enantiomer).	6.7	6	1	azetidines; beta-lactam; organofluorine compound	anticholesteremic drug; antilipemic drug; antimetabolite
oleanolic acid 3-acetate oleanolic acid 3-acetate: from Gardenia jasminoides; RN given for (3beta)-isomer	2.15	1	0
avasimibe [no description available]	3.19	1	0	monoterpenoid
methyl protodioscin methyl protodioscin: structure in first source	2.05	1	0
biotin vitamin B7 : Any member of a group of vitamers that belong to the chemical structural class called biotins that exhibit biological activity against vitamin B7 deficiency. Vitamin B7 deficiency is very rare in individuals who take a normal balanced diet. Foods rich in biotin are egg yolk, liver, cereals, vegetables (spinach, mushrooms) and rice. Symptoms associated with vitamin B7 deficiency include thinning hair, scaly skin rashes around eyes, nose and mouth, and brittle nails. The vitamers include biotin and its ionized and salt forms.	2.04	1	0	biotins; vitamin B7	coenzyme; cofactor; Escherichia coli metabolite; fundamental metabolite; human metabolite; mouse metabolite; nutraceutical; prosthetic group; Saccharomyces cerevisiae metabolite
angiotensin ii Giapreza: injectable form of angiotensin II used to increase blood pressure in adult patients with septic or other distributive shock. Ile(5)-angiotensin II : An angiotensin II that acts on the central nervous system (PDB entry: 1N9V).	2.51	2	0	amino acid zwitterion; angiotensin II	human metabolite
campesterol campesterol: RN refers to (3beta,24R)-isomer; structure	3.45	1	1	3beta-hydroxy-Delta(5)-steroid; 3beta-sterol; C28-steroid; phytosterols	mouse metabolite
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.	2.02	1	0	1,3-thiazoles; carbamate ester; carboxamide; L-valine derivative; ureas	antiviral drug; environmental contaminant; HIV protease inhibitor; xenobiotic
ouabain Ouabain: A cardioactive glycoside consisting of rhamnose and ouabagenin, obtained from the seeds of Strophanthus gratus and other plants of the Apocynaceae; used like DIGITALIS. It is commonly used in cell biological studies as an inhibitor of the NA(+)-K(+)-EXCHANGING ATPASE.. cardiac glycoside : Steroid lactones containing sugar residues that act on the contractile force of the cardiac muscles.. ouabain : A steroid hormone that is a multi-hydroxylated alpha-L-rhamnosyl cardenoloide. It binds to and inhibits the plasma membrane Na(+)/K(+)-ATPase (sodium pump). It has been isolated naturally from Strophanthus gratus.	3.15	1	0	11alpha-hydroxy steroid; 14beta-hydroxy steroid; 5beta-hydroxy steroid; alpha-L-rhamnoside; cardenolide glycoside; steroid hormone	anti-arrhythmia drug; cardiotonic drug; EC 2.3.3.1 [citrate (Si)-synthase] inhibitor; EC 3.1.3.41 (4-nitrophenylphosphatase) inhibitor; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor; EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor; ion transport inhibitor; plant metabolite
desmosterol Desmosterol: An intermediate in the synthesis of cholesterol.. desmosterol : A cholestanoid that is cholesta-5,24-diene substituted by a beta-hydroxy group at position 3. It is an intermediate metabolite obtained during the synthesis of cholesterol.	3.45	1	1	3beta-hydroxy-Delta(5)-steroid; 3beta-sterol; C27-steroid; cholestanoid	human metabolite; mouse metabolite
lignans Lignans: A class of dibenzylbutane derivatives which occurs in higher plants and in fluids (bile, serum, urine, etc.) in man and other animals. These compounds, which have a potential anti-cancer role, can be synthesized in vitro by human fecal flora. (From Singleton & Sainsbury, Dictionary of Microbiology and Molecular Biology, 2d ed)	3.27	1	0
drf 2725 ragaglitazar: a phenoxazine analogue of phenyl propanoic acid; Ragaglitazar is a coligand of PPARalpha and PPARgamma	3.13	1	0
gw 3965 GW 3965: a liver X receptor ligand	3.13	1	0	diarylmethane
gamma-sitosterol clionasterol : A member of the class of phytosterols that is poriferast-5-ene carrying a beta-hydroxy substituent at position 3.	3.45	1	1	3beta-hydroxy-Delta(5)-steroid; 3beta-sterol; phytosterols	marine metabolite; plant metabolite
trilostane trilostane: inhibits conversion of pregnenolone to progesterone; adrenal blocking agent used in treatment of Cushing's syndrome. trilostane : An epoxy steroid that is 3,17beta-dihydroxy-5alpha-androst-2-ene-2-carbonitrile in which the oxygen of the epoxy group is joined to the 4alpha and 5 alpha positions.	3.15	1	0	17beta-hydroxy steroid; 3-hydroxy steroid; androstanoid; epoxy steroid; nitrile	abortifacient; antineoplastic agent; EC 1.1.1.210 [3beta(or 20alpha)-hydroxysteroid dehydrogenase] inhibitor
monooctanoin monooctanoin: dissolution agent for retained cholesterol bile duct stones; RN in Chemline for octanoic acid, ester with 1,2,3-propanetriol, MF unknown: 11140-04-8; RN for octanoic acid, 2,3-dihydroxypropyl ester (1-monooctanoin): 502-54-5; RN in 9th CI Form Index for (+-)-1-monooctanoin: 19670-49-6. rac-1-monooctanoylglycerol : A rac-1-monoacylglycerol comprising equal amounts of 1-octanoyl-sn-glycerol and 3-octanoyl-sn-glycerol.. 1-monooctanoylglycerol : A 1-monoglyceride that has octanoyl as the acyl group.	2.04	1	0	1-monoglyceride; octanoate ester; rac-1-monoacylglycerol
cytellin cytellin: a phytosterol preparation of mainly B-sitosterol, that was marketed by Eli Lilly to lower cholesterol 1957 to 1982	3.45	1	1
cholesteryl oleate cholesteryl oleate: RN given refers to ((Z)-isomer). cholesteryl oleate : The (Z)-stereoisomer of cholesteryl octadec-9-enoate.	2.08	1	0	CE(18:1); cholesteryl octadec-9-enoate	mouse metabolite
cholestanol Cholestanol: A cholesterol derivative found in human feces, gallstones, eggs, and other biological matter.	3.45	1	1	cholestanoid
beta-escin [no description available]	2.05	1	0
dalcetrapib dalcetrapib: inhibits cholesteryl ester transfer protein (CETP)	12.74	53	2	anilide
3-((3-(4-chloro-3-ethylphenoxy)phenyl)(3-(1,1,2,2-tetrafluoroethoxy)benzyl)amino)-1,1,1-trifluoropropan-2-ol 3-((3-(4-chloro-3-ethylphenoxy)phenyl)(3-(1,1,2,2-tetrafluoroethoxy)benzyl)amino)-1,1,1-trifluoropropan-2-ol: inhibits cholesteryl ester transfer protein; structure in first source	2.5	2	0
gw 590735 2-methyl-2-(4-(((4-methyl-2-(4-trifluoromethylphenyl)-thiazol-5-ylcarbonyl)amino)methyl)phenoxy)propionic acid: an HDLc raising agent; structure in first source	2.05	1	0
ta-8995 TA-8995: inhibits cholesteryl ester transfer protein	4.44	3	0
anacetrapib [no description available]	9.68	42	0
phytosterols Phytosterols: A class of organic compounds known as sterols or STEROIDS derived from plants.. phytosterols : Sterols similar to cholesterol which occur in plants and vary only in carbon side chains and/or presence or absence of a double bond.	3.45	1	1
rifamycins [no description available]	2.04	1	0
endothelin-1 Endothelin-1: A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)	2.07	1	0
evacetrapib [no description available]	7.6	20	0	benzazepine
calca protein, human CALCA protein, human: RefSeq NM_001741	2.02	1	0
3'-hydroxy-5'-(4-isobutylpiperazinyl)benzoxazinorifamycin KRM 1648: structure in first source	2.04	1	0	phenoxazine
leoligin leoligin: inhibits intimal hyperplasia of venous bypass grafts; isolated from Edelweiss; structure in first source	3.27	1	0

Condition	Indicated	Relationship Strength	Studies	Trials
Coronary Heart Disease [description not available]	0	14.18	16	1
Coronary Disease An imbalance between myocardial functional requirements and the capacity of the CORONARY VESSELS to supply sufficient blood flow. It is a form of MYOCARDIAL ISCHEMIA (insufficient blood supply to the heart muscle) caused by a decreased capacity of the coronary vessels.	1	11.18	16	1
Hypertriglyceridemia A condition of elevated levels of TRIGLYCERIDES in the blood.	1	5.39	2	0
Congenital Zika Syndrome [description not available]	0	2.25	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	4.87	7	0
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	0	2.25	1	0
Cardiovascular Diseases Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.	0	13.44	56	4
Atherogenesis [description not available]	0	16.11	57	16
Atherosclerosis A thickening and loss of elasticity of the walls of ARTERIES that occurs with formation of ATHEROSCLEROTIC PLAQUES within the ARTERIAL INTIMA.	0	16.11	57	16
Dyslipidemia [description not available]	0	18.58	29	12
Dyslipidemias Abnormalities in the serum levels of LIPIDS, including overproduction or deficiency. Abnormal serum lipid profiles may include high total CHOLESTEROL, high TRIGLYCERIDES, low HIGH DENSITY LIPOPROTEIN CHOLESTEROL, and elevated LOW DENSITY LIPOPROTEIN CHOLESTEROL.	0	13.58	29	12
Apoplexy [description not available]	0	8.68	5	4
Adverse Drug Event [description not available]	0	8.92	7	4
Cardiac Failure [description not available]	0	8.66	5	4
Cardiovascular Stroke [description not available]	0	9.39	7	4
Heart Failure A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.	0	8.66	5	4
Myocardial Infarction NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION).	0	9.39	7	4
Stroke A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)	0	8.68	5	4
Drug-Related Side Effects and Adverse Reactions Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.	0	8.92	7	4
Chronic Kidney Diseases [description not available]	0	3.01	1	0
Uremia A clinical syndrome associated with the retention of renal waste products or uremic toxins in the blood. It is usually the result of RENAL INSUFFICIENCY. Most uremic toxins are end products of protein or nitrogen CATABOLISM, such as UREA or CREATININE. Severe uremia can lead to multiple organ dysfunctions with a constellation of symptoms.	0	3.01	1	0
Renal Insufficiency, Chronic Conditions in which the KIDNEYS perform below the normal level for more than three months. Chronic kidney insufficiency is classified by five stages according to the decline in GLOMERULAR FILTRATION RATE and the degree of kidney damage (as measured by the level of PROTEINURIA). The most severe form is the end-stage renal disease (CHRONIC KIDNEY FAILURE). (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002)	0	3.01	1	0
Arteriosclerosis, Coronary [description not available]	0	10.49	16	3
Coronary Artery Disease Pathological processes of CORONARY ARTERIES that may derive from a congenital abnormality, atherosclerotic, or non-atherosclerotic cause.	0	10.49	16	3
Hyperglycemia, Postprandial Abnormally high BLOOD GLUCOSE level after a meal.	0	6.2	4	1
Insulin Sensitivity [description not available]	0	5.28	4	1
Hyperglycemia Abnormally high BLOOD GLUCOSE level.	0	6.2	4	1
Insulin Resistance Diminished effectiveness of INSULIN in lowering blood sugar levels: requiring the use of 200 units or more of insulin per day to prevent HYPERGLYCEMIA or KETOSIS.	0	5.28	4	1
Cardiac Diseases [description not available]	0	6.2	7	1
Hyperlipoproteinemia [description not available]	0	3.01	1	0
Heart Diseases Pathological conditions involving the HEART including its structural and functional abnormalities.	0	6.2	7	1
Hyperlipoproteinemias Conditions with abnormally elevated levels of LIPOPROTEINS in the blood. They may be inherited, acquired, primary, or secondary. Hyperlipoproteinemias are classified according to the pattern of lipoproteins on electrophoresis or ultracentrifugation.	0	3.01	1	0
Kidney Diseases Pathological processes of the KIDNEY or its component tissues.	0	5.06	3	0
Lipid Metabolism, Inborn Error [description not available]	0	2.52	2	0
Elevated Cholesterol [description not available]	0	6.06	12	0
Hypercholesterolemia A condition with abnormally high levels of CHOLESTEROL in the blood. It is defined as a cholesterol value exceeding the 95th percentile for the population.	1	8.06	12	0
Gargoylism, Hunter Syndrome [description not available]	0	2.15	1	0
Mucopolysaccharidosis II Systemic lysosomal storage disease marked by progressive physical deterioration and caused by a deficiency of L-sulfoiduronate sulfatase. This disease differs from MUCOPOLYSACCHARIDOSIS I by slower progression, lack of corneal clouding, and X-linked rather than autosomal recessive inheritance. The mild form produces near-normal intelligence and life span. The severe form usually causes death by age 15.	0	2.15	1	0
Aldosteronism [description not available]	0	4.57	3	0
Hyperaldosteronism A condition caused by the overproduction of ALDOSTERONE. It is characterized by sodium retention and potassium excretion with resultant HYPERTENSION and HYPOKALEMIA.	0	4.57	3	0
Diabetes Mellitus, Adult-Onset [description not available]	0	6.65	4	1
Diabetes Mellitus, Type 2 A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.	0	6.65	4	1
Disease Exacerbation [description not available]	0	10	8	7
Apolipoprotein B-100, Familial Defective [description not available]	0	11.03	12	11
Hyperlipoproteinemia Type II A group of familial disorders characterized by elevated circulating cholesterol contained in either LOW-DENSITY LIPOPROTEINS alone or also in VERY-LOW-DENSITY LIPOPROTEINS (pre-beta lipoproteins).	1	13.03	12	11
Blood Pressure, High [description not available]	0	6.06	12	0
Hypertension Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.	0	6.06	12	0
Adrenal Cancer [description not available]	0	2.46	2	0
Carcinoma, Anaplastic [description not available]	0	2.05	1	0
Carcinoma A malignant neoplasm made up of epithelial cells tending to infiltrate the surrounding tissues and give rise to metastases. It is a histological type of neoplasm and not a synonym for cancer.	0	2.05	1	0
Water-Electrolyte Imbalance Disturbances in the body's WATER-ELECTROLYTE BALANCE.	0	2.05	1	0
Anesthesia A state characterized by loss of feeling or sensation. This depression of nerve function is usually the result of pharmacologic action and is induced to allow performance of surgery or other painful procedures.	0	2.46	2	0
Cardiometabolic Syndrome A cluster of symptoms that are risk factors for CARDIOVASCULAR DISEASES and TYPE 2 DIABETES MELLITUS. The major components not only include metabolic dysfunctions of METABOLIC SYNDROME but also HYPERTENSION, and ABDOMINAL OBESITY.	0	3.88	1	0
Obesity A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).	0	4.29	2	0
Metabolic Syndrome A cluster of symptoms that are risk factors for CARDIOVASCULAR DISEASES and TYPE 2 DIABETES MELLITUS. The major components of metabolic syndrome include ABDOMINAL OBESITY; atherogenic DYSLIPIDEMIA; HYPERTENSION; HYPERGLYCEMIA; INSULIN RESISTANCE; a proinflammatory state; and a prothrombotic (THROMBOSIS) state.	0	3.88	1	0
Genetic Predisposition [description not available]	0	2.74	3	0
Infection [description not available]	0	2.05	1	0
Infections Invasion of the host organism by microorganisms or their toxins or by parasites that can cause pathological conditions or diseases.	0	2.05	1	0
Electrolytes Substances that dissociate into two or more ions, to some extent, in water. Solutions of electrolytes thus conduct an electric current and can be decomposed by it (ELECTROLYSIS). (Grant & Hackh's Chemical Dictionary, 5th ed)	0	2.05	1	0
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	0	3.65	3	0
Diseases, Metabolic [description not available]	0	2.05	1	0
Aging The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time.	0	2.05	1	0
Metabolic Diseases Generic term for diseases caused by an abnormal metabolic process. It can be congenital due to inherited enzyme abnormality (METABOLISM, INBORN ERRORS) or acquired due to disease of an endocrine organ or failure of a metabolically important organ such as the liver. (Stedman, 26th ed)	0	2.05	1	0
Hypolipoproteinemia [description not available]	0	2.97	1	0
Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	0	2.07	1	0
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	0	2.06	1	0
Hyperlipemia [description not available]	0	5.91	6	0
Hyperlipidemias Conditions with excess LIPIDS in the blood.	1	7.91	6	0
Acute Coronary Syndrome An episode of MYOCARDIAL ISCHEMIA that generally lasts longer than a transient anginal episode that ultimately may lead to MYOCARDIAL INFARCTION.	0	2.99	1	0
Heart Disease, Ischemic [description not available]	0	2.75	3	0
Myocardial Ischemia A disorder of cardiac function caused by insufficient blood flow to the muscle tissue of the heart. The decreased blood flow may be due to narrowing of the coronary arteries (CORONARY ARTERY DISEASE), to obstruction by a thrombus (CORONARY THROMBOSIS), or less commonly, to diffuse narrowing of arterioles and other small vessels within the heart. Severe interruption of the blood supply to the myocardial tissue may result in necrosis of cardiac muscle (MYOCARDIAL INFARCTION).	0	2.75	3	0
Arteriosclerosis Thickening and loss of elasticity of the walls of ARTERIES of all sizes. There are many forms classified by the types of lesions and arteries involved, such as ATHEROSCLEROSIS with fatty lesions in the ARTERIAL INTIMA of medium and large muscular arteries.	0	5.24	4	0
Bacterial Endocarditides [description not available]	0	2.02	1	0
Endocarditis, Bacterial Inflammation of the ENDOCARDIUM caused by BACTERIA that entered the bloodstream. The strains of bacteria vary with predisposing factors, such as CONGENITAL HEART DEFECTS; HEART VALVE DISEASES; HEART VALVE PROSTHESIS IMPLANTATION; or intravenous drug use.	0	2.02	1	0
Innate Inflammatory Response [description not available]	0	3.35	2	0
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	0	3.35	2	0
Angor Pectoris [description not available]	0	2.03	1	0
Cardiac Output, Low A state of subnormal or depressed cardiac output at rest or during stress. It is a characteristic of CARDIOVASCULAR DISEASES, including congenital, valvular, rheumatic, hypertensive, coronary, and cardiomyopathic. The serious form of low cardiac output is characterized by marked reduction in STROKE VOLUME, and systemic vasoconstriction resulting in cold, pale, and sometimes cyanotic extremities.	0	2.03	1	0
Angina Pectoris The symptom of paroxysmal pain consequent to MYOCARDIAL ISCHEMIA usually of distinctive character, location and radiation. It is thought to be provoked by a transient stressful situation during which the oxygen requirements of the MYOCARDIUM exceed that supplied by the CORONARY CIRCULATION.	0	2.03	1	0
Diathesis [description not available]	0	2.03	1	0
Arterial Diseases, Carotid [description not available]	0	4.34	1	1
Carotid Artery Diseases Pathological conditions involving the CAROTID ARTERIES, including the common, internal, and external carotid arteries. ATHEROSCLEROSIS and TRAUMA are relatively frequent causes of carotid artery pathology.	0	4.34	1	1
Flushing A transient reddening of the face that may be due to fever, certain drugs, exertion, or stress.	0	2.03	1	0
Familial Combined Hyperlipidemia [description not available]	0	7.46	4	4
Hyperlipidemia, Familial Combined A type of familial lipid metabolism disorder characterized by a variable pattern of elevated plasma CHOLESTEROL and/or TRIGLYCERIDES. Multiple genes on different chromosomes may be involved, such as the major late transcription factor (UPSTREAM STIMULATORY FACTORS) on CHROMOSOME 1.	1	9.46	4	4
Weight Reduction [description not available]	0	2.03	1	0
Urinary Tract Diseases [description not available]	0	2.03	1	0
Weight Loss Decrease in existing BODY WEIGHT.	0	2.03	1	0
Smoking Cessation Discontinuing the habit of SMOKING.	0	2.03	1	0
Diabetes Mellitus A heterogeneous group of disorders characterized by HYPERGLYCEMIA and GLUCOSE INTOLERANCE.	0	2.03	1	0
Diseases, Peripheral Vascular [description not available]	0	2.04	1	0
Peripheral Vascular Diseases Pathological processes involving any one of the BLOOD VESSELS in the vasculature outside the HEART.	0	2.04	1	0
Amentia [description not available]	0	2.95	1	0
Cancer of Lung [description not available]	0	2.95	1	0
Dementia An acquired organic mental disorder with loss of intellectual abilities of sufficient severity to interfere with social or occupational functioning. The dysfunction is multifaceted and involves memory, behavior, personality, judgment, attention, spatial relations, language, abstract thought, and other executive functions. The intellectual decline is usually progressive, and initially spares the level of consciousness.	0	2.95	1	0
Lung Neoplasms Tumors or cancer of the LUNG.	0	2.95	1	0
Hyperhomocysteinemia Condition in which the plasma levels of homocysteine and related metabolites are elevated (	0	2.04	1	0

torcetrapib

Cross-References

Synonyms (64)

Research Excerpts

Overview

Effects

Treatment

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Roles (2)

Drug Classes (3)

Pathways (4)

Protein Targets (3)

Potency Measurements

Inhibition Measurements

Biological Processes (19)

Molecular Functions (6)

Ceullar Components (5)

Bioassays (75)

Research

Studies (261)

Market Indicators

Research Demand Index: 37.40

Study Types

Clinical Trials (14)

Trial Overview

torcetrapib

Cross-References

Synonyms (64)

Research Excerpts

Overview

Effects

Treatment

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Roles (2)

Drug Classes (3)

Pathways (4)

Protein Targets (3)

Potency Measurements

Inhibition Measurements

Biological Processes (19)

Molecular Functions (6)

Ceullar Components (5)

Bioassays (75)

Research

Studies (261)

Market Indicators

Research Demand Index: 37.40

Study Types

Clinical Trials (14)

Trial Overview

Related Drugs (83)

Related Conditions (97)