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imidapril

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Description

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

imidapril : A member of the class of imidazolidines that is (4S)-1-methyl-2-oxoimidazolidine-4-carboxylic acid in which the hydrogen of the imidazolidine nitrogen has been substituted by (1S)-1-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}ethyl group. It is the prodrug for imidaprilat, an ACE inhibitor used for the treatment of chronic heart failure. [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]

Cross-References

ID SourceID
PubMed CID5485193
CHEMBL ID3183293
CHEBI ID31691
SCHEMBL ID136722
MeSH IDM0179259
PubMed CID5464343
CHEMBL ID317094
CHEBI ID135654
SCHEMBL ID34098
MeSH IDM0179259

Synonyms (98)

Synonym
AC-526
imidapril hydrochloride
novarok
ta-6366
tanatril
sh-6366
imidapril hydrochloride [jan]
imidapril monohydrochloride
imidapril (hydrochloride)
4-imidazolidinecarboxylic acid, 3-(2-((1-(ethoxycarbonyl)-3-phenylpropyl)amino)-1-oxopropyl)-1-methyl-2-oxo-, monohydrochloride, (4s-(3(r*(r*)),4r*))-
4-imidazolidinecarboxylic acid, 3-((2s)-2-(((1s)-1-(ethoxycarbonyl)-3-phenylpropyl)amino)-1-oxopropyl)-1-methyl-2-oxo-, monohydrochloride, (4s)-
ta 6366
NCGC00181342-01
imidapril hcl
89396-94-1
D01549
tanatril (tn)
imidapril hydrochloride (jp17)
(4s)-3-[(2s)-2-[[(1s)-1-(ethoxycarbonyl)-3-phenylpropyl]amino]-1-oxopropyl]-1-methyl-2-oxo-4-imidazolidinecarboxylic acid hydrochloride
dtxsid7046912 ,
dtxcid5026912
tox21_112801
cas-89396-94-1
smr003475023
MLS004712066
AKOS015994537
7nsf9gg1nu ,
unii-7nsf9gg1nu
S2109
SCHEMBL136722
tox21_112801_1
NCGC00181342-02
BS-1005
imidapril hydrochloride [mart.]
3-((2s)-2-((1s)-n-(1-ethoxycarbonyl-3-phenylpropyl)amino)-propionyl)-1-methyl-2-oxoimidazolidine-4-carboxylic acid, hydrochloride-, 4s-
imidapril monohydrochloride [mi]
4-imidazolidinecarboxylic acid, 3-((2s)-2-(((1s)-1-(ethoxycarbonyl)-3-phenylpropyl)amino)-1-oxopropyl)-1-methyl-2-oxo-, hydrochloride (1:1), (4s)-
imidapril hydrochloride [who-dd]
CS-5010
HY-B1451
CHEMBL3183293
I0901
tanapril
novaloc
mfcd00923828
imidapril hydrochloride, >=98% (hplc)
CHEBI:31691
(s)-3-((s)-2-(((s)-1-ethoxy-1-oxo-4-phenylbutan-2-yl)amino)propanoyl)-1-methyl-2-oxoimidazolidine-4-carboxylic acid hydrochloride
(4s)-3-[(2s)-2-[[(2s)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]propanoyl]-1-methyl-2-oxoimidazolidine-4-carboxylic acid;hydrochloride
(s)-3-((s)-2-((s)-1-ethoxy-1-oxo-4-phenylbutan-2-ylamino)propanoyl)-1-methyl-2-oxoimidazolidine-4-carboxylic acid hydrochloride
imidapril hydrochloride,(s)
(4s)-3-[(2s)-2-[[(2s)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]propanoyl]-1-methyl-2-oxoimidazolidine-4-carboxylic acid,hydrochloride
CCG-269148
C77009
Q27268625
A917212
(s)-3-[(s)-2-((s)-1-ethoxycarbonyl-3-phenyl-propylamino)-propionyl]-1-methyl-2-oxo-imidazolidine-4-carboxylic acid
(s)-3-((s)-2-(((s)-1-ethoxy-1-oxo-4-phenylbutan-2-yl)amino)propanoyl)-1-methyl-2-oxoimidazolidine-4-carboxylicacidhydrochloride
89371-37-9
imidapril
(s)-3-(n-((s)-1-ethoxycarbonyl-3-phenylpropyl)-l-alanyl)-1-methyl-2-oxoimidazoline-4-carboxylic acid
imidaprilum [inn-latin]
imidaprilum
(4s)-3-{n-[(2s)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]-l-alanyl}-1-methyl-2-oxoimidazolidine-4-carboxylic acid
CHEBI:135654
(4s)-1-methyl-3-[(2s)-2-[n-((1s)-1-ethoxycarbonyl-3-phenylpropyl)amino]propionyl]-2-oxo-imidazolidine-4-carboxylic acid
CHEMBL317094 ,
hipertene
hipertene (tn)
imidapril (inn)
D08068
(4s)-3-[(2s)-2-[[(2s)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]propanoyl]-1-methyl-2-oxoimidazolidine-4-carboxylic acid
bdbm50020400
3-[2-(1-ethoxycarbonyl-3-phenyl-propylamino)-propionyl]-1-methyl-2-oxo-imidazolidine-4-carboxylic acid
AKOS015967028
bw7h1tjs22 ,
imidapril [inn:ban]
unii-bw7h1tjs22
1-((s)-2-((s)-1-ethoxy-1-oxo-4-phenylbutan-2-ylamino)propanoyl)-3-methyl-2-oxo-2,3-dihydro-1h-imidazole-5-carboxylic acid
gtpl6377
SCHEMBL34098
imidapril [who-dd]
imidapril [inn]
imidapril [mi]
DTXSID2048242
Q-102511
AC-25844
AB01565810_02
(4s)-3-[(2s)-2-{[(2s)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}propanoyl]-1-methyl-2-oxoimidazolidine-4-carboxylic acid
NCGC00181342-03
DB11783
(s)-3-((s)-2-((s)-1-ethoxy-1-oxo-4-phenylbutan-2-ylamino)propanoyl)-1-methyl-2-oxoimidazolidine-4-carboxylic acid
Q1041804
(s)-3-((s)-2-(((s)-1-ethoxy-1-oxo-4-phenylbutan-2-yl)amino)propanoyl)-1-methyl-2-oxoimidazolidine-4-carboxylic acid
A846430
(s)-3-(((s)-1-ethoxy-1-oxo-4-phenylbutan-2-yl)-l-alanyl)-1-methyl-2-oxoimidazolidine-4-carboxylic acid
CS-0137517
HY-B1451A

Research Excerpts

Overview

Imidapril is an ACE inhibitor with one ofthe lowest incidences (less than 1% of patients) of dry irritant cough. It is a long-acting ACE inhibitor that is rapidly converted in the liver to its active metabolite, imidapilat.

ExcerptReferenceRelevance
"Imidapril is an angiotensin converting enzyme (ACE) inhibitor without a sulfhydril group which has been shown from previous study to have low incidence of ACE inhibitor induced cough."( Comparison of the incidence of imidapril and enalapril induced cough.
Boonyapisit, W; Tresukosol, D, 2010
)
2.09
"Imidapril is an ACE inhibitor with one ofthe lowest incidences (less than 1% of patients) of dry irritant cough. "( [Combination therapy of hypertension in general clinical practice. The results of the KOHYBA study].
Chroust, K; Krupicka, J; Soucek, M, 2010
)
1.8
"Imidapril is an angiotensin I converting enzyme inhibitor, a class of drugs with known cardioprotective activity. "( Impact of imidapril on cardiac mitochondrial function in an ex-vivo animal model of global myocardial ischemia.
Carreira, R; Gala, S; Gonçalves, LM; Monteiro, P; Nobre, S; Providência, LA, 2005
)
2.17
"Imidapril is an angiotensin-converting enzyme inhibitor that is widely used in treating hypertension, although the responses vary among individuals. "( A single nucleotide polymorphism in the carboxylesterase gene is associated with the responsiveness to imidapril medication and the promoter activity.
Geshi, E; Katagiri, T; Kimura, T; Koba, S; Koga, A; Muramatsu, M; Saito, T; Sakai, T; Suzuki, H; Yoshimura, M, 2005
)
1.99
"Imidapril is a long-acting ACE inhibitor that is rapidly converted in the liver to its active metabolite, imidaprilat."( Imidapril in heart failure.
Dolezal, T, 2006
)
2.5
"Imidapril is a new angiotensin-converting enzyme inhibitor and an oral prodrug of imidaprilat."( Radioimmunoassay for imidapril, a new angiotensin-converting enzyme inhibitor, and imidaprilat, its active metabolite, in human plasma and urine.
Banno, K; Ishibashi, K; Ito, M; Mizobe, M; Morikawa, S; Murata, K; Sato, T; Suzuki, T; Takai, T; Yamanaka, K, 1996
)
1.33
"Imidapril is a newly synthesized non-sulfhydryl-containing angiotensin I converting enzyme (ACE) inhibitor. "( [Studies on angiotensin I converting enzyme (ACE) inhibitory effect of imidapril. (I). Inhibition of various tissue ACEs in vitro].
Hashimoto, Y; Kubo, M; Minobe, S; Sugaya, T; Taniguchi, T; Watanabe, T, 1992
)
1.96

Treatment

Imidapril treatment of infarcted animals improved cardiac performance and attenuated alterations in SR Ca(2+) pump and Ca( 2+) release activities. Imidaprin treatment significantly decreased urinary albumin excretions and improved glomerulosclerosis of OLETF rats.

ExcerptReferenceRelevance
"Imidapril treatment of infarcted animals improved cardiac performance and attenuated alterations in SR Ca(2+) pump and Ca(2+) release activities."( Sarcoplasmic reticulum Ca2+ transport and gene expression in congestive heart failure are modified by imidapril treatment.
Dhalla, NS; Netticadan, T; Ren, B; Saini, HK; Shao, Q; Takeda, N, 2005
)
1.27
"Imidapril treatment improved cardiac performance, attenuated cardiac remodeling, and reduced morphological changes in the heart and lung."( Influence of long-term treatment of imidapril on mortality, cardiac function, and gene expression in congestive heart failure due to myocardial infarction.
Dhalla, NS; Ganguly, PK; Ren, B; Shao, Q; Takeda, N; Tappia, PS, 2004
)
1.32
"The imidapril treatment significantly inhibited serum ACE activity and increased plasma bradykinin concentration."( Long-term treatment with imidapril but not with nifedipine enhances plasma NOx concentration in patients with essential hypertension.
Horiuchi, M; Kouzuma, R; Mizuki, T; Morishita, T; Nakashima, Y; Nakata, S; Okazaki, M; Suda, O; Sumiyama-Fujinishi, A; Tasaki, H; Tsutsui, M; Yanagihara, N, 2006
)
1.12
"Imidapril-treated animals showed improved cardiac function under urethane anesthesia."( Prolonging action of imidapril on the lifespan expectancy of cardiomyopathic hamsters.
Doi, H; Kaburaki, M; Kurosawa, H; Narita, H; Ogiku, N; Ohmachi, Y; Yabana, H, 1996
)
1.33
"Imidapril treatment significantly attenuated the blood pressure elevation and reduced the increases in cardiac and aortic weight."( Serum N-acetyl-beta-D-glucosaminidase activity in a genetic rat model of non-insulin-dependent diabetes mellitus.
Gomi, T; Goto, A; Hirawa, N; Ikeda, T; Kawabata, Y; Nagoshi, H; Numabe, A; Omata, M; Toyo-oka, T; Uehara, Y, 1997
)
1.02
"Imidapril treatment significantly decreased urinary albumin excretions and improved glomerulosclerosis of OLETF rats, while amlodipine failed to improve nephropathy of OLETF rats despite lowering of blood pressure."( Role of intrarenal angiotensin-converting enzyme in nephropathy of type II diabetic rats.
Iwao, H; Kim, S; Taniguchi, M; Zhan, Y, 2002
)
1.04
"Imidapril treatment partially prevented the changes due to MI in LV function (rate of pressure development, 24+/-2.3% reduction and rate of pressure decay, 14+/-1.8% reduction), myofibrillar Ca(2+) ATPase activity (8.2+/-0.7 micromol Pi/mg/hr), MHC protein content (alpha-MHC, 24% reduction and beta-MHC, 525% increase) and MHC gene expression (alpha-MHC, 18% reduction and beta-MHC, 15% increase)."( Modification of myosin gene expression by imidapril in failing heart due to myocardial infarction.
Dhalla, NS; Liu, X; Ren, B; Rupp, H; Takeda, N; Wang, J, 2002
)
1.3
"Treatment with imidapril reduced renal angiotensin II and NAD(P)H oxidase expression and the oxidative products (kidney lipid peroxidation product: 0.16+/-0.02, P<0.001; urinary hydrogen peroxide: 3.1+/-0.2, P<0.01 versus DSHF rats)."( Angiotensin II and oxidative stress in Dahl Salt-sensitive rat with heart failure.
Fujita, T; Goto, A; Kobayashi, N; Matsuoka, H; Onozato, ML; Tojo, A, 2002
)
0.65
"Treatment with imidapril did not change AT2 receptor and ACE expression detected by RT-PCR in the injured artery."( Important role of nitric oxide in the effect of angiotensin-converting enzyme inhibitor imidapril on vascular injury.
Chen, R; Cui, TX; Horiuchi, M; Iwai, M; Liu, HW; Min, LJ; Shiuchi, T; Sugaya, T; Suzuki, J; Wu, L, 2003
)
0.88
"The treatment of imidapril and Caweidiluo could restrain the development of left ventricle hypertrophy after operation, and imidapril decreased the contents of TNF-alpha, Ang II and ET-1 in myocardium compared with overload group (all P<0.01)."( [Study of effects of drugs on myocardial hypertrophy due to overload].
Cao, RH; Chen, SL; Du, YG; Lü, JY; Qiao, ZD; Wang, GP; Zhang, ZY, 2005
)
0.66
"Oral treatment with imidapril (10 mg/kg/d), an ACE inhibitor, 1 h before each ISO treatment and on the following 6 d, improved ventricular hypertrophy, the elevation of the left ventricular end diastolic pressure, the reduction in contractility, and the prolongation of the time constant."( Induction of cardiac angiotensinogen mRNA and angiotensin converting enzyme (ACE) activity in isoproterenol-induced heart injury.
Ishida, R; Ogiku, N; Saeki, K; Sugiura, M, 1996
)
0.61
"Treatment with imidapril for 10 weeks significantly reduced the enhanced glomerular expression of TGF-beta1 and collagen IV mRNA in nephrectomized rats, and prevented the associated proteinuria and glomerulosclerosis."( Imidapril inhibits increased transforming growth factor-beta1 expression in remnant kidney model.
Hamaguchi, A; Iwao, H; Kim, S; Wanibuchi, H, 1997
)
2.08
"Treatment with imidapril significantly prevented the L-NAME-induced increase in the gene expression and immunoreactivity of PAI-1, but candesartan cilexetil showed no such effect."( Differential effects of imidapril and candesartan cilexetil on plasminogen activator inhibitor-1 expression induced by prolonged inhibition of nitric oxide synthesis in rat hearts.
Egashira, K; Katoh, M; Mitsui, T; Narita, H; Takeshita, A, 2000
)
0.95
"Pretreatment with imidapril (ACE inhibitor) and candesartan cilexitil (AT1 receptor antagonist) significantly prevented the increase in the phosphorylation of JAK1 at 120 min and STAT3 at 30 and 120 min."( Myocardial ischemia activates the JAK-STAT pathway through angiotensin II signaling in in vivo myocardium of rats.
Beppu, S; Ishikura, F; Kobayashi, H; Omura, T; Takeuchi, K; Yoshikawa, J; Yoshiyama, M, 2001
)
0.63
"Treatment with Imidapril 5-20 mg once daily caused a decrease in BP by 21 +/- 17/11 +/- 10 mmHg (p < 0.01/0.01)."( [Efficiency and safety of ACE-inhibiting imidapril in patients with essential hypertension].
Klein, W; Maier, R; Stoschitzky, K; Zweiker, R, 2002
)
0.92

Toxicity

ExcerptReferenceRelevance
" Adverse drug reactions were observed in 20."( Efficacy and safety of imidapril in patients with essential hypertension: a double-blind comparison with captopril.
Chen, MF; Chiang, FT; Chien, KL; Huang, PJ; Lai, LP, 2001
)
0.62
" ACE-inhibitor related adverse effects (cough, vertigo, headache, pruritus, tachycardia, orthostatic dysregulation or nausea) were observed in 38 patients (< 2%)."( [Efficiency and safety of ACE-inhibiting imidapril in patients with essential hypertension].
Klein, W; Maier, R; Stoschitzky, K; Zweiker, R, 2002
)
0.58

Pharmacokinetics

The combination of imidapril with a diuretic, beta-adrenoceptor antagonist or calcium-channel blocker seems a reasonable and safe treatment option when striving for additive pharmacodynamic effects. However, the slower biotransformation did not result in statistically significant differences in Cmax and AUC for either imidAPril or its active metabolite following repeated administration.

ExcerptReferenceRelevance
"In order to obtain a rational explanation and analytical method of the unique pharmacokinetic behaviors of imidapril and imidaprilat in human, a new pharmacokinetic model was designed by introducing a saturable-reversible angiotensin I converting enzyme (ACE)-imidaprilat binding process and a linear imidapril-imidaprilat conversion process."( A saturable tissue-angiotensin I converting enzyme (ACE) binding model for the pharmacokinetic analysis of imidapril, a new ACE inhibitor, and its active metabolite in human.
Mizobe, M; Noda, K; Tagawa, K, 1995
)
0.72
"The possible influence of impaired liver function on the pharmacokinetic disposition of imidapril, a novel prodrug type angiotensin-converting enzyme (ACE) inhibitor, and its active metabolite, imidaprilat, was investigated."( Pharmacokinetics of imidapril and its active metabolite imidaprilat following single dose and during steady state in patients with impaired liver function.
Hoogkamer, JF; Kirch, W; Kleinbloesem, CH; Lankhaar, G; Nokhodian, A; Ouwerkerk, MJ; Ungethüm, W, 1997
)
0.84
" However, the slower biotransformation did not result in statistically significant differences in Cmax and AUC for either imidapril or its active metabolite following repeated administration."( Pharmacokinetics of imidapril and its active metabolite imidaprilat following single dose and during steady state in patients with impaired liver function.
Hoogkamer, JF; Kirch, W; Kleinbloesem, CH; Lankhaar, G; Nokhodian, A; Ouwerkerk, MJ; Ungethüm, W, 1997
)
0.83
"Imidapril is regarded as an ACE inhibitor of which the pharmacokinetic disposition is only slightly affected in patients with impaired liver function."( Pharmacokinetics of imidapril and its active metabolite imidaprilat following single dose and during steady state in patients with impaired liver function.
Hoogkamer, JF; Kirch, W; Kleinbloesem, CH; Lankhaar, G; Nokhodian, A; Ouwerkerk, MJ; Ungethüm, W, 1997
)
2.06
"To investigate the potential pharmacokinetic and pharmacodynamic interaction between imidapril and digoxin."( Pharmacokinetic and pharmacodynamic interaction trial after repeated oral doses of imidapril and digoxin in healthy volunteers.
Harder, S; Thürmann, PA, 1997
)
0.75
" Cmax was 19."( Pharmacokinetic and pharmacodynamic interaction trial after repeated oral doses of imidapril and digoxin in healthy volunteers.
Harder, S; Thürmann, PA, 1997
)
0.52
"To investigate the pharmacokinetic profile of the ACE-inhibitor imidapril in 10 hypertensive patients after a first single dose (10 mg) and after 28 days therapy with imidapril 10 mg once daily."( Single dose and steady state pharmacokinetics and pharmacodynamics of the ACE-inhibitor imidapril in hypertensive patients.
Harder, S; Thürmann, PA; Ungethüm, W, 1998
)
0.76
"In this group of hypertensive patients, the pharmacokinetic profile and the drop in ACE-activity as well as in blood pressure seen after a single dose of imidapril and at steady state were similar."( Single dose and steady state pharmacokinetics and pharmacodynamics of the ACE-inhibitor imidapril in hypertensive patients.
Harder, S; Thürmann, PA; Ungethüm, W, 1998
)
0.72
" However, Cmax and AUC for both imidapril and imidaprilat were significantly higher in patients with severe renal impairment than in healthy volunteers."( Pharmacokinetics of imidapril and its active metabolite imidaprilat following single dose and during steady state in patients with chronic renal failure.
Hoogkamer, JF; Kirch, W; Kleinbloesem, CH; Lankhaar, G; Nokhodian, A; Ouwerkerk, MJ; Ungethüm, W, 1998
)
0.91
"The pharmacokinetic and dynamic interactions of the angiotensin-converting enzyme (ACE) inhibitor imidapril with other therapeutic principles used in hypertension and heart failure were evaluated."( Pharmacokinetic and dynamic interactions of the angiotensin-converting enzyme inhibitor imidapril with hydrochlorothiazide, bisoprolol and nilvadipine.
Belz, GG; Breithaupt-Grögler, K; Meurer-Witt, B; Ungethüm, W, 2001
)
0.75
" Plasma concentrations of imidaprilat and H were followed up to 48 h, those of B and N up to 24 h and area under the concentration time curve (AUC), maximum plasma concentration (Cmax) and time to Cmax (tmax) were determined."( Pharmacokinetic and dynamic interactions of the angiotensin-converting enzyme inhibitor imidapril with hydrochlorothiazide, bisoprolol and nilvadipine.
Belz, GG; Breithaupt-Grögler, K; Meurer-Witt, B; Ungethüm, W, 2001
)
0.83
"The combination of imidapril with a diuretic, beta-adrenoceptor antagonist or calcium-channel blocker seems a reasonable and safe treatment option when striving for additive pharmacodynamic effects not accompanied by relevant pharmacokinetic interactions."( Pharmacokinetic and dynamic interactions of the angiotensin-converting enzyme inhibitor imidapril with hydrochlorothiazide, bisoprolol and nilvadipine.
Belz, GG; Breithaupt-Grögler, K; Meurer-Witt, B; Ungethüm, W, 2001
)
0.86

Bioavailability

ExcerptReferenceRelevance
"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
" This method was very useful for use in pharmacokinetic and bioavailability studies of the three metabolites of imidapril in humans."( Determination of three metabolites of a new angiotensin-converting enzyme inhibitor, imidapril, in plasma and urine by gas chromatography-mass spectrometry using multiple ion detection.
Banno, K; Horimoto, S; Mabuchi, M; Matsuoka, M, 1992
)
0.72
" Bioavailability of TA-606 was 11 times higher than that of 606A in Sprague-Dawley rats, with consistent hypotensive potencies in spontaneously hypertensive rats (SHRs)."( Pharmacologic profile of TA-606, a novel angiotensin II-receptor antagonist in the rat.
Hashimoto, Y; Hayashida, K; Kaji, H; Kurosawa, Y; Minami, K; Murata, S; Narita, H; Ohashi, R, 1998
)
0.3
" Thus, the knowledge about the characteristic and site-specific expression of CES1 and CES2 in rat intestine will help to predict the oral bioavailability of ester prodrugs."( Identification of carboxylesterases expressed in rat intestine and effects of their hydrolyzing activity in predicting first-pass metabolism of ester prodrugs.
Gao, J; Liu, D; Liu, Y; Ren, X; Xu, Y; Zhang, C, 2011
)
0.37
"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

Imidapril in once-daily doses of up to 20mg was shown to be at least as effective as candesartan cilexetil in reducing BP. Using the same dosing regimen, only perindopril inhibited the brain ACE activities by more than 50%.

ExcerptRelevanceReference
" Following oral administration of 14C-labeled imidapril and 6366 A to rats, plasma concentrations of radioactivity were much higher after [N-methyl-14C]-imidapril dosing than after [N-methyl-14C]-6366 A dosing at all time points."( Metabolic fate of the new angiotensin-converting enzyme inhibitor imidapril in animals. 1st communication: absorption, pharmacokinetics and excretion in rats and dogs.
Endo, M; Kohno, M; Otsuka, M; Takaiti, O; Yamada, Y, 1992
)
0.78
" Examination of the time course of plasma radioactivity after the single and multiple (7 and 14 times) oral administration revealed that the Cmax and AUCO-24 h values slightly, but significantly, increased according to repeated dosing and the beta-phase of the t1/2 of disappearance became longer after consecutive dosing."( Metabolic fate of the new angiotensin-converting enzyme inhibitor imidapril in animals. 3rd communication: tissue accumulation after consecutive oral administration of [N-methyl-14C]-imidapril in rats.
Endo, M; Kohno, M; Otsuka, M; Suzuki, T; Takaiti, O; Yamada, Y, 1992
)
0.52
" Various pharmacokinetic parameters were estimated by the simultaneous curve fitting method using the plasma concentration data and the urinary excretion data of imidapril and imidaprilat in a multiple dosing study of healthy human volunteers."( A saturable tissue-angiotensin I converting enzyme (ACE) binding model for the pharmacokinetic analysis of imidapril, a new ACE inhibitor, and its active metabolite in human.
Mizobe, M; Noda, K; Tagawa, K, 1995
)
0.7
"Plasma imidapril concentrations after single and, although less pronounced, after repeated dosing were higher in the liver disease patients, whereas imidaprilat concentrations were lower."( Pharmacokinetics of imidapril and its active metabolite imidaprilat following single dose and during steady state in patients with impaired liver function.
Hoogkamer, JF; Kirch, W; Kleinbloesem, CH; Lankhaar, G; Nokhodian, A; Ouwerkerk, MJ; Ungethüm, W, 1997
)
1.08
"Twenty-four-hour ambulatory blood pressure monitoring (ABPM) provides the most accurate efficacy assessment of an antihypertensive agent throughout a 24-hour dosing interval."( A multicentre, 12-week study of imidapril and candesartan cilexetil in patients with mild to moderate hypertension using ambulatory blood pressure monitoring.
Alegría, E; Gonzalez-Juanatey, JR; Marquez, E; Olivan, J; Palma-Gamiz, JL; Pêgo, M; Pujol, M; Sagastagoitia-Gorostiza, JD, 2007
)
0.62
"Imidapril in once-daily doses of up to 20mg was shown to be at least as effective as candesartan cilexetil given in once-daily doses of up to 16 mg in reducing BP throughout the entire 24-hour dosing interval."( A multicentre, 12-week study of imidapril and candesartan cilexetil in patients with mild to moderate hypertension using ambulatory blood pressure monitoring.
Alegría, E; Gonzalez-Juanatey, JR; Marquez, E; Olivan, J; Palma-Gamiz, JL; Pêgo, M; Pujol, M; Sagastagoitia-Gorostiza, JD, 2007
)
2.07
" Using the same dosing regimen, only perindopril inhibited the brain ACE activities by more than 50%, whereas imidapril and enalapril showed much less potent effects."( Effect of a centrally active angiotensin-converting enzyme inhibitor, perindopril, on cognitive performance in a mouse model of Alzheimer's disease.
Kanda, T; Nagata, Y; Shirakura, S; Suzuki, N; Takahashi, S; Takayama, M; Uchida, S; Yamada, K, 2010
)
0.57
" The proposed methods were successfully applied to the pharmaceutical dosage form containing the investigated compound without any interference from the excipients."( UV derivative spectrophotometric and RP-HPLC methods for determination of imidapril hydrochloride in tablets and for its stability assessment in solid state.
Kolasa, K; Regulska, K; Stanisz, B,
)
0.36
" Imidapril had a superior effect for preventing ventricular remodeling characterized by fibrosis and collagen accumulation in left ventricle compared with ramipril in the moderate and large MI groups, even though the dosage used in this study was too small to reduce systemic blood pressure."( A comparison between imidapril and ramipril on attenuation of ventricular remodeling after myocardial infarction.
Hirata, Y; Isobe, M; Nagai, R; Ogawa, M; Suzuki, J; Watanabe, R, 2012
)
1.61
" No mutagenic effect was observed confirming that the presence of DKP in IMD final dosage form has no impact on cancer initiation."( Is there any association between imidapril hydrochloride stability profile under dry air conditions and cancer initiation?
Murias, M; Regulska, K; Regulski, M; Stanisz, B, 2013
)
0.67
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
antihypertensive agentAny drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitorAn EC 3.4.15.* (peptidyl-dipeptidase) inhibitor that interferes with the action of peptidyl-dipeptidase A (EC 3.4.15.1).
prodrugA compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.
[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]

Drug Classes (6)

ClassDescription
dipeptideAny molecule that contains two amino-acid residues connected by peptide linkages.
dipeptideAny molecule that contains two amino-acid residues connected by peptide linkages.
imidazolidines
dicarboxylic acid monoesterA monoester of a dicarboxylic acid.
secondary amino compoundA compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
ethyl esterAny carboxylic ester resulting from the formal condensation of the carboxy group of a carboxylic acid with ethanol.
N-acylureaA member of the class of ureas that has the general formula R-CO-NH-CO-NH2 or R-CO-NH-CO-NH-CO-R', formally derived by the acylation of one or both of the nitrogens of a urea moiety.
[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]

Protein Targets (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AR proteinHomo sapiens (human)Potency33.49150.000221.22318,912.5098AID1259243
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency4.77240.01237.983543.2770AID1645841
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency3.54810.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Angiotensin-converting enzyme Homo sapiens (human)IC50 (µMol)9.90000.00010.533610.0000AID37638
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (72)

Processvia Protein(s)Taxonomy
response to hypoxiaAngiotensin-converting enzyme Homo sapiens (human)
kidney developmentAngiotensin-converting enzyme Homo sapiens (human)
blood vessel remodelingAngiotensin-converting enzyme Homo sapiens (human)
angiotensin maturationAngiotensin-converting enzyme Homo sapiens (human)
regulation of renal output by angiotensinAngiotensin-converting enzyme Homo sapiens (human)
neutrophil mediated immunityAngiotensin-converting enzyme Homo sapiens (human)
antigen processing and presentation of peptide antigen via MHC class IAngiotensin-converting enzyme Homo sapiens (human)
regulation of systemic arterial blood pressure by renin-angiotensinAngiotensin-converting enzyme Homo sapiens (human)
proteolysisAngiotensin-converting enzyme Homo sapiens (human)
spermatogenesisAngiotensin-converting enzyme Homo sapiens (human)
female pregnancyAngiotensin-converting enzyme Homo sapiens (human)
regulation of blood pressureAngiotensin-converting enzyme Homo sapiens (human)
male gonad developmentAngiotensin-converting enzyme Homo sapiens (human)
response to xenobiotic stimulusAngiotensin-converting enzyme Homo sapiens (human)
embryo development ending in birth or egg hatchingAngiotensin-converting enzyme Homo sapiens (human)
post-transcriptional regulation of gene expressionAngiotensin-converting enzyme Homo sapiens (human)
negative regulation of gene expressionAngiotensin-converting enzyme Homo sapiens (human)
substance P catabolic processAngiotensin-converting enzyme Homo sapiens (human)
bradykinin catabolic processAngiotensin-converting enzyme Homo sapiens (human)
regulation of smooth muscle cell migrationAngiotensin-converting enzyme Homo sapiens (human)
regulation of vasoconstrictionAngiotensin-converting enzyme Homo sapiens (human)
animal organ regenerationAngiotensin-converting enzyme Homo sapiens (human)
response to nutrient levelsAngiotensin-converting enzyme Homo sapiens (human)
response to lipopolysaccharideAngiotensin-converting enzyme Homo sapiens (human)
mononuclear cell proliferationAngiotensin-converting enzyme Homo sapiens (human)
response to laminar fluid shear stressAngiotensin-converting enzyme Homo sapiens (human)
angiotensin-activated signaling pathwayAngiotensin-converting enzyme Homo sapiens (human)
vasoconstrictionAngiotensin-converting enzyme Homo sapiens (human)
hormone metabolic processAngiotensin-converting enzyme Homo sapiens (human)
hormone catabolic processAngiotensin-converting enzyme Homo sapiens (human)
eating behaviorAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of apoptotic processAngiotensin-converting enzyme Homo sapiens (human)
peptide catabolic processAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of vasoconstrictionAngiotensin-converting enzyme Homo sapiens (human)
negative regulation of glucose importAngiotensin-converting enzyme Homo sapiens (human)
regulation of synaptic plasticityAngiotensin-converting enzyme Homo sapiens (human)
lung alveolus developmentAngiotensin-converting enzyme Homo sapiens (human)
amyloid-beta metabolic processAngiotensin-converting enzyme Homo sapiens (human)
arachidonic acid secretionAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of neurogenesisAngiotensin-converting enzyme Homo sapiens (human)
heart contractionAngiotensin-converting enzyme Homo sapiens (human)
regulation of angiotensin metabolic processAngiotensin-converting enzyme Homo sapiens (human)
hematopoietic stem cell differentiationAngiotensin-converting enzyme Homo sapiens (human)
angiogenesis involved in coronary vascular morphogenesisAngiotensin-converting enzyme Homo sapiens (human)
cellular response to glucose stimulusAngiotensin-converting enzyme Homo sapiens (human)
response to dexamethasoneAngiotensin-converting enzyme Homo sapiens (human)
cell proliferation in bone marrowAngiotensin-converting enzyme Homo sapiens (human)
regulation of heart rate by cardiac conductionAngiotensin-converting enzyme Homo sapiens (human)
negative regulation of calcium ion importAngiotensin-converting enzyme Homo sapiens (human)
response to thyroid hormoneAngiotensin-converting enzyme Homo sapiens (human)
blood vessel diameter maintenanceAngiotensin-converting enzyme Homo sapiens (human)
regulation of hematopoietic stem cell proliferationAngiotensin-converting enzyme Homo sapiens (human)
negative regulation of gap junction assemblyAngiotensin-converting enzyme Homo sapiens (human)
cellular response to aldosteroneAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of peptidyl-cysteine S-nitrosylationAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of systemic arterial blood pressureAngiotensin-converting enzyme Homo sapiens (human)
cholesterol biosynthetic processLiver carboxylesterase 1Homo sapiens (human)
cholesterol metabolic processLiver carboxylesterase 1Homo sapiens (human)
response to toxic substanceLiver carboxylesterase 1Homo sapiens (human)
positive regulation of cholesterol effluxLiver carboxylesterase 1Homo sapiens (human)
negative regulation of cholesterol storageLiver carboxylesterase 1Homo sapiens (human)
epithelial cell differentiationLiver carboxylesterase 1Homo sapiens (human)
cholesterol homeostasisLiver carboxylesterase 1Homo sapiens (human)
reverse cholesterol transportLiver carboxylesterase 1Homo sapiens (human)
medium-chain fatty acid metabolic processLiver carboxylesterase 1Homo sapiens (human)
regulation of bile acid biosynthetic processLiver carboxylesterase 1Homo sapiens (human)
cellular response to cholesterolLiver carboxylesterase 1Homo sapiens (human)
cellular response to low-density lipoprotein particle stimulusLiver carboxylesterase 1Homo sapiens (human)
cholesterol ester hydrolysis involved in cholesterol transportLiver carboxylesterase 1Homo sapiens (human)
positive regulation of cholesterol metabolic processLiver carboxylesterase 1Homo sapiens (human)
regulation of bile acid secretionLiver carboxylesterase 1Homo sapiens (human)
lipid catabolic processLiver carboxylesterase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (20)

Processvia Protein(s)Taxonomy
endopeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
carboxypeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
metalloendopeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
calmodulin bindingAngiotensin-converting enzyme Homo sapiens (human)
peptidase activityAngiotensin-converting enzyme Homo sapiens (human)
metallopeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
exopeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
tripeptidyl-peptidase activityAngiotensin-converting enzyme Homo sapiens (human)
peptidyl-dipeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
zinc ion bindingAngiotensin-converting enzyme Homo sapiens (human)
chloride ion bindingAngiotensin-converting enzyme Homo sapiens (human)
mitogen-activated protein kinase kinase bindingAngiotensin-converting enzyme Homo sapiens (human)
bradykinin receptor bindingAngiotensin-converting enzyme Homo sapiens (human)
mitogen-activated protein kinase bindingAngiotensin-converting enzyme Homo sapiens (human)
metallodipeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
heterocyclic compound bindingAngiotensin-converting enzyme Homo sapiens (human)
sterol esterase activityLiver carboxylesterase 1Homo sapiens (human)
methylumbelliferyl-acetate deacetylase activityLiver carboxylesterase 1Homo sapiens (human)
carboxylesterase activityLiver carboxylesterase 1Homo sapiens (human)
carboxylic ester hydrolase activityLiver carboxylesterase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (16)

Processvia Protein(s)Taxonomy
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
extracellular spaceAngiotensin-converting enzyme Homo sapiens (human)
extracellular regionAngiotensin-converting enzyme Homo sapiens (human)
extracellular spaceAngiotensin-converting enzyme Homo sapiens (human)
lysosomeAngiotensin-converting enzyme Homo sapiens (human)
endosomeAngiotensin-converting enzyme Homo sapiens (human)
plasma membraneAngiotensin-converting enzyme Homo sapiens (human)
external side of plasma membraneAngiotensin-converting enzyme Homo sapiens (human)
basal plasma membraneAngiotensin-converting enzyme Homo sapiens (human)
brush border membraneAngiotensin-converting enzyme Homo sapiens (human)
extracellular exosomeAngiotensin-converting enzyme Homo sapiens (human)
sperm midpieceAngiotensin-converting enzyme Homo sapiens (human)
plasma membraneAngiotensin-converting enzyme Homo sapiens (human)
cytoplasmLiver carboxylesterase 1Homo sapiens (human)
endoplasmic reticulumLiver carboxylesterase 1Homo sapiens (human)
endoplasmic reticulum lumenLiver carboxylesterase 1Homo sapiens (human)
lipid dropletLiver carboxylesterase 1Homo sapiens (human)
cytosolLiver carboxylesterase 1Homo sapiens (human)
lipid dropletLiver carboxylesterase 1Homo sapiens (human)
endoplasmic reticulumLiver carboxylesterase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (55)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS 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.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID171890Change in systolic blood pressure1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Studies on angiotensin converting enzyme inhibitors. 4. Synthesis and angiotensin converting enzyme inhibitory activities of 3-acyl-1-alkyl-2-oxoimidazolidine-4-carboxylic acid derivatives.
AID192447Initial systolic blood pressure in spontaneously hypertensive rats after administration of 10 mg/kg of compound perorally1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Studies on angiotensin converting enzyme inhibitors. 4. Synthesis and angiotensin converting enzyme inhibitory activities of 3-acyl-1-alkyl-2-oxoimidazolidine-4-carboxylic acid derivatives.
AID456232Activity at human recombinant CES1 expressed in baculovirus-infected Spodoptera frugiperda Sf21 cells assessed as substrate hydrolysis by fluorescence assay2010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
In silico prediction of human carboxylesterase-1 (hCES1) metabolism combining docking analyses and MD simulations.
AID192450Initial systolic blood pressure in spontaneously hypertensive rats after administration of 5 mg/kg of compound perorally1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Studies on angiotensin converting enzyme inhibitors. 4. Synthesis and angiotensin converting enzyme inhibitory activities of 3-acyl-1-alkyl-2-oxoimidazolidine-4-carboxylic acid derivatives.
AID192448Initial systolic blood pressure in spontaneously hypertensive rats after administration of 1 mg/kg of compound perorally1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Studies on angiotensin converting enzyme inhibitors. 4. Synthesis and angiotensin converting enzyme inhibitory activities of 3-acyl-1-alkyl-2-oxoimidazolidine-4-carboxylic acid derivatives.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID183134Inhibitory effect of on Angiotensin I induced pressor responses in normotensive rats when given perorally1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Studies on angiotensin converting enzyme inhibitors. 4. Synthesis and angiotensin converting enzyme inhibitory activities of 3-acyl-1-alkyl-2-oxoimidazolidine-4-carboxylic acid derivatives.
AID37638Inhibitory activity on Angiotensin I converting enzyme (ACE) obtained from pig renal cortex and hippuryl-histidyl-leucine as substrate1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Studies on angiotensin converting enzyme inhibitors. 4. Synthesis and angiotensin converting enzyme inhibitory activities of 3-acyl-1-alkyl-2-oxoimidazolidine-4-carboxylic acid derivatives.
AID184237Maximum inhibitory effect of on Angiotensin I induced pressor responses in anesthetized normotensive rats with 0.5 mg/Kg dose of compound given perorally1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Studies on angiotensin converting enzyme inhibitors. 4. Synthesis and angiotensin converting enzyme inhibitory activities of 3-acyl-1-alkyl-2-oxoimidazolidine-4-carboxylic acid derivatives.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID192449Initial systolic blood pressure in spontaneously hypertensive rats after administration of 2 mg/kg of compound perorally1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Studies on angiotensin converting enzyme inhibitors. 4. Synthesis and angiotensin converting enzyme inhibitory activities of 3-acyl-1-alkyl-2-oxoimidazolidine-4-carboxylic acid derivatives.
AID184236Maximum inhibitory effect of on Angiotensin I induced pressor responses in anesthetized normotensive rats with 0.2 mg/Kg dose of compound given perorally1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Studies on angiotensin converting enzyme inhibitors. 4. Synthesis and angiotensin converting enzyme inhibitory activities of 3-acyl-1-alkyl-2-oxoimidazolidine-4-carboxylic acid derivatives.
AID190638The time required for the maximal fall in blood pressure after administration of the compound1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Studies on angiotensin converting enzyme inhibitors. 4. Synthesis and angiotensin converting enzyme inhibitory activities of 3-acyl-1-alkyl-2-oxoimidazolidine-4-carboxylic acid derivatives.
AID192455Maximum inhibitory effect of on Angiotensin I induced pressor responses in anesthetized normotensive rats with 1.0 mg/Kg dose of compound given perorally1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Studies on angiotensin converting enzyme inhibitors. 4. Synthesis and angiotensin converting enzyme inhibitory activities of 3-acyl-1-alkyl-2-oxoimidazolidine-4-carboxylic acid derivatives.
AID174936The duration time of the hypotensive effect showing statistically significant difference from initial value was determined1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Studies on angiotensin converting enzyme inhibitors. 4. Synthesis and angiotensin converting enzyme inhibitory activities of 3-acyl-1-alkyl-2-oxoimidazolidine-4-carboxylic acid derivatives.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (235)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (0.43)18.7374
1990's76 (32.34)18.2507
2000's103 (43.83)29.6817
2010's49 (20.85)24.3611
2020's6 (2.55)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 54.48

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

MetricThis Compound (vs All)
Research Demand Index54.48 (24.57)
Research Supply Index5.71 (2.92)
Research Growth Index6.91 (4.65)
Search Engine Demand Index84.24 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (54.48)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials62 (26.05%)5.53%
Reviews0 (0.00%)6.00%
Reviews6 (2.52%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies9 (3.78%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other9 (100.00%)84.16%
Other161 (67.65%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (3)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Randomized, Controlled, Parallel Arm, PROBE Study to Evaluate Different Effects of Imidapril and Candesartan on Fibrinolysis and Insulin-Sensitivity in Patients With Mild to Moderate Hypertension [NCT00644475]Phase 360 participants (Anticipated)Interventional2008-03-31Recruiting
Randomized, Controlled, PROBE Trial, Evaluating the Antiproteinuric Effect of Imidapril Versus Ramipril in Type 2 Diabetic Patients and Mild to Moderate Hypertension With Microalbuminuria [NCT01230034]Phase 3206 participants (Anticipated)Interventional2010-10-31Recruiting
Phase II Study for the Second-Line Treatment of Hypertension in Patients With Autosomal Dominant Polycystic Kidney Disease; ACEI vs. CCB [NCT00890279]Phase 2160 participants (Anticipated)Interventional2009-07-31Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]